entrectinib [Ligand Id: 8290] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1983268 (Entrectinib, NMS-E628, Rozlytrek, Rxdx-101, RXDX-101) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 26S proteasome regulatory subunit 6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831205] [UniProtKB: P43686] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Inhibition of PDK1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated non-catalytic subunit gamma 1/5`-AMP-activated protein kinase subunit gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2393] [GtoPdb: 1545] [UniProtKB: P54619] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase AMP-activated non-catalytic subunit gamma 2/5`-AMP-activated protein kinase subunit gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2453] [GtoPdb: 1546] [UniProtKB: Q9UGJ0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 1/AarF domain-containing protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105885] [GtoPdb: 1925] [UniProtKB: Q86TW2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6090] [UniProtKB: P61160] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Actin-related protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105857] [UniProtKB: P61158] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 2/Activated CDC42 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 6.38 | pKd | 420 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ACK1 (unknown origin) in presence of gamma33-ATP | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Acyl-CoA dehydrogenase family member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105816] [UniProtKB: Q6JQN1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Acyl-CoA dehydrogenase family member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105707] [UniProtKB: Q709F0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenine phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105819] [UniProtKB: P07741] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenosine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3589] [GtoPdb: 1231] [UniProtKB: P55263] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Adenylate kinase 2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4938] [UniProtKB: P54819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 2/ADP/ATP translocase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3709670] [GtoPdb: 1063] [UniProtKB: P05141] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Mitochondrial adenine nucleotide translocator 3/ADP/ATP translocase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105854] [GtoPdb: 1064] [UniProtKB: P12236] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Inhibition of recombinant ALK (unknown origin) | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.7 | pIC50 | >200 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 6.82 | pIC50 | 150 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Inhibition of human ALK secondary L1196M mutant assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assay | B | 6.91 | pIC50 | 124 | nM | IC50 | Bioorg Med Chem (2021) 47: 116396-116396 [PMID:34534734] |
| ChEMBL | Biochemical Assay: Kinase Buffer (KB) for ALKKinase buffer was composed of 50 mM HEPES pH 7.5 containing 1 mM MnCl2, mM MgCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA. 3×KB is buffer of the same composition and pH as KB, but with three times the concentration of each component.ii. Assay ConditionsThe kinase assay was run with a final enzyme concentration of 20 nM, in the presence of 8 microM ATP, 1 nM 33P-γ-ATP and 2 microM MBP. The MPB was purchased from Sigma-Aldrich, St. Louis, Mo., USA. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-9616059-B2. Substituted indazole derivatives active as kinase inhibitors (2017) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Biochemical Assay: ALK enzyme needs pre-activation in order to linearize reaction kinetics.Kinase Buffer (KB) for ALKKinase buffer was composed of 50 mM HEPES pH 7.5 containing 1 mM MnCl.sub.2, 5 mM MgCl.sub.2, 1 mM DTT, 3 microM Na.sub.3VO.sub.4, and 0.2 mg/mL BSA. 3.times.KB is buffer of the same composition and pH as KB, but with three times the concentration of each component.Assay ConditionsThe kinase assay was run with a final enzyme concentration of 20 nM, in the presence of 8 microM ATP, 1 nM .sup.33P-.gamma.-ATP and 2 microM MBP. The MPB was purchased from Sigma-Aldrich, St. Louis, Mo., USA. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-9029356-B2. Substituted indazole derivatives active as kinase inhibitors (2015) |
| ChEMBL | Biochemical Assay for Inhibitors of ALK Kinase Activity: ALK enzyme needs pre-activation in order to linearize reaction kinetics.i. Kinase Buffer (KB) for ALK.Kinase buffer was composed of 50 mM HEPES pH 7.5 containing 1 mM MnCl2, 5 mM. MgCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA. 3×KB is buffer of the same composition and pH as KB, but with three times the concentration of each component.ii. Assay ConditionsThe kinase assay was run with a final enzyme concentration of 20 nM, in the presence of 8 microM ATP, 1 nM 33P-γ-ATP and 2 microM MBP. The MPB was purchased from Sigma-Aldrich, St. Louis, Mo., USA. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-10081622-B2. Substituted indazole derivatives active as kinase inhibitors (2018) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | ALK Kinase Biochemical Assay: BioKinase buffer was composed of 50 mM HEPES pH 7.5 containing 1 mM MnCl2, 5 mM MgCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA. 3x KB is buffer of the same composition and pH as KB, but with three times the concentration of each component. The kinase assay was run with a final enzyme concentration of 20 nM, in the presence of 8 microM ATP, 1 nM 33P-γ-ATP and 2 microM MBP. The MPB was purchased from Sigma-Aldrich, St. Louis, Mo., USA. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-9255087-B2. Substituted indazole derivatives active as kinase inhibitors (2016) |
| ChEMBL | Inhibition of human ALK assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem (2021) 47: 116396-116396 [PMID:34534734] |
| ChEMBL | Inhibition of ALK (unknown origin) by radiometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2022) 230: 114096-114096 [PMID:35007864] |
| ChEMBL | Inhibition of recombinant ALK (unknown origin) in presence of gamma33-ATP | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of ALK (unknown origin) by TR-FRET assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2023) 258: 115618-115618 [PMID:37413881] |
| ChEMBL | Inhibition of ALK (unknown origin) by radiometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2018) 143: 182-199 [PMID:29174814] |
| ChEMBL | Inhibition of ALK (unknown origin) by radiometric assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2021) 64: 10286-10296 [PMID:34253025] |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Inhibition of ALK (unknown origin) by radiometric assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2021) 53: 128409-128409 [PMID:34628036] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Inhibition of ALK (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem (2022) 56: 116596-116596 [PMID:35033885] |
| AP2 associated kinase 1/AP2-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3830] [GtoPdb: 1921] [UniProtKB: Q2M2I8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent 6-phosphofructokinase, platelet type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2972] [UniProtKB: Q01813] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010634] [UniProtKB: Q92499] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX3X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5553] [UniProtKB: O00571] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DDX42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105782] [UniProtKB: Q86XP3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATP-dependent RNA helicase DHX30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105814] [UniProtKB: Q7L2E3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| coenzyme Q8A/Atypical kinase COQ8A, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5550] [GtoPdb: 1927] [UniProtKB: Q8NI60] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Aurora-2 Kinase Biochemical Assay: The kinase buffer was composed of 50 mM HEPES, pH 7.0, 10 mM MnCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA. The kinase assay was run with an enzyme concentration of 2.5 nM, 10 microM ATP, 1 nM 33P-γ-ATP, and 8 microM substrate, composed of 4 LRRWSLG repeats. | B | 6.47 | pIC50 | 338 | nM | IC50 | US-9255087-B2. Substituted indazole derivatives active as kinase inhibitors (2016) |
| ChEMBL | Biochemical Assay for Inhibitors of Aurora-2 Kinase Activity: The in vitro kinase inhibition assay was conducted in the same way as described for IGF-1R. At variance with IGF-1R, Aurora-2 enzyme does not need pre-activation.i. Kinase Buffer (KB) for Aurora-2The kinase buffer was composed of 50 mM HEPES, pH 7.0, 10 mM MnCl2, mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA.ii. Assay Conditions for Aurora-2 (Final Concentrations)The kinase assay was run with an enzyme concentration of 2.5 nM, 10 microM ATP, 1 nM 33P-γ-ATP, and 8 microM substrate, composed of 4 LRRWSLG repeats. | B | 6.47 | pIC50 | 338 | nM | IC50 | US-10081622-B2. Substituted indazole derivatives active as kinase inhibitors (2018) |
| ChEMBL | Biochemical Assay: i. Kinase Buffer (KB) for Aurora-2The kinase buffer was composed of 50 mM HEPES, pH 7.0, 10 mM MnCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA.ii. Assay Conditions for Aurora-2 (Final Concentrations)The kinase assay was run with an enzyme concentration of 2.5 nM, 10 microM ATP, 1 nM 33P-γ-ATP, and 8 microM substrate, composed of 4 LRRWSLG repeats. | B | 6.47 | pIC50 | 338 | nM | IC50 | US-9616059-B2. Substituted indazole derivatives active as kinase inhibitors (2017) |
| ChEMBL | Inhibition of AUR2 (unknown origin) in presence of gamma33-ATP | B | 6.67 | pIC50 | 215 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of AUR1 (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.A specific substrate was incubated with the kinase in appropriate buffer conditions in the presence of ATP traced with .sup.33P-.gamma.-ATP (gamma phosphate-labeled, Redivue.TM. Code Number AH9968, 1000-3000 Ci/mmole, Amersham Biosciences Piscataway, N.J., USA), optimal cofactors and test compound.At the end of the phosphorylation reaction, more than 98% cold and radioactive ATP were captured by an excess of Dowex ion exchange resin. The resin was allowed to settle to the bottom of reaction wells by gravity. Supernatant, containing substrate peptide, was subsequently withdrawn and transferred into a counting plate, and radioactivity (corresponding to phosphate incorporated into peptide) was evaluated by .beta.-counting. Assay Conditions:The kinase assay was run with a final enzyme concentration of 6 nM, in the presence of 6 microM ATP, 1 nM . | B | 6.47 | pIC50 | 338 | nM | IC50 | US-9029356-B2. Substituted indazole derivatives active as kinase inhibitors (2015) |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of TRKB (unknown origin) | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2019) 175: 129-148 [PMID:31077998] |
| ChEMBL | Inhibition of TRKB (unknown origin) by radiometric assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2022) 230: 114096-114096 [PMID:35007864] |
| ChEMBL | Inhibition of TRKB (unknown origin) by TR-FRET assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Inhibition of TRKB (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Inhibition of human TEL (336 residues) fused-TRKB (455 to 822 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of recombinant human TRKB incubated for 90 mins by selectscreen kinase assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of TRKB (unknown origin) by radiometric assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2021) 53: 128409-128409 [PMID:34628036] |
| ChEMBL | Inhibition of TrkB (unknown origin) by radiometric assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 10286-10296 [PMID:34253025] |
| ChEMBL | Inhibition of TRKB (unknown origin) incubated for 1 hr by mobility shift assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Inhibition of TrkB (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2022) 56: 116596-116596 [PMID:35033885] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| beta adrenergic receptor kinase 1/Beta-adrenergic receptor kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4079] [GtoPdb: 1466] [UniProtKB: P25098] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Bifunctional phosphoribosylaminoimidazole carboxylase/phosphoribosylaminoimidazole succinocarboxamide synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5922] [UniProtKB: P22234] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BMP2 inducible kinase/BMP-2-inducible protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4522] [GtoPdb: 1941] [UniProtKB: Q9NSY1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type IA/Bone morphogenetic protein receptor type-1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5275] [GtoPdb: 1786] [UniProtKB: P36894] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type IB/Bone morphogenetic protein receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5476] [GtoPdb: 1789] [UniProtKB: O00238] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BCR activator of RhoGEF and GTPase/Breakpoint cluster region protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5146] [GtoPdb: 2755] [UniProtKB: P11274] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| calcium/calmodulin dependent protein kinase IV/Calcium/calmodulin-dependent protein kinase type IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PKAalpha (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| protein kinase, cAMP-dependent, catalytic, beta subunit/cAMP-dependent protein kinase catalytic subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2918] [GtoPdb: 1477] [UniProtKB: P22694] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, catalytic, gamma subunit/cAMP-dependent protein kinase catalytic subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2743] [GtoPdb: 1478] [UniProtKB: P22612] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, cAMP-dependent, regulatory, type II, alpha subunit/cAMP-dependent protein kinase type II-alpha regulatory subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2221] [GtoPdb: 1474] [UniProtKB: P13861] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400] | ||||||||
| ChEMBL | Inhibition of CK2 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 1/Casein kinase I isoform gamma-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 2/Casein kinase I isoform gamma-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cell division cycle 7/CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111377] [GtoPdb: 1960] [UniProtKB: O00311, Q9UBU7] | ||||||||
| ChEMBL | Inhibition of CDC7/DBF4 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/CycA (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Chromodomain-helicase-DNA-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105742] [UniProtKB: Q14839] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| citron rho-interacting serine/threonine kinase/Citron Rho-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5579] [GtoPdb: 1509] [UniProtKB: O14578] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 10/Cyclin-dependent kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795191] [GtoPdb: 1962] [UniProtKB: Q15131] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 12/Cyclin-dependent kinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559692] [GtoPdb: 1965] [UniProtKB: Q9NYV4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 13/Cyclin-dependent kinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795192] [GtoPdb: 1966] [UniProtKB: Q14004] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 16/Cyclin-dependent kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4597] [GtoPdb: 1969] [UniProtKB: Q00536] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 17/Cyclin-dependent kinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5790] [GtoPdb: 1970] [UniProtKB: Q00537] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 3/Cyclin-dependent kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4442] [GtoPdb: 1975] [UniProtKB: Q00526] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin-dependent kinase like 5/Cyclin-dependent kinase-like 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163112] [GtoPdb: 1986] [UniProtKB: O76039] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| cyclin G associated kinase/Cyclin-G-associated kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4355] [GtoPdb: 2027] [UniProtKB: O14976] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Cysteine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105937] [UniProtKB: P49589] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Cytochrome c1, heme protein, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105975] [UniProtKB: P08574] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dCTP pyrophosphatase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769292] [UniProtKB: Q9H773] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Delta(24)-sterol reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331059] [UniProtKB: Q15392] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Deoxycytidine kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2447] [UniProtKB: P27707] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DnaJ homolog subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189122] [UniProtKB: P31689] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA replication licensing factor MCM4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105745] [UniProtKB: P33991] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase II alpha/DNA topoisomerase 2-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| DNA topoisomerase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 3/Dual specificity mitogen-activated protein kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2109] [GtoPdb: 2064] [UniProtKB: P46734] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 5/Dual specificity mitogen-activated protein kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4948] [GtoPdb: 2066] [UniProtKB: Q13163] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase 6/Dual specificity mitogen-activated protein kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2171] [GtoPdb: 2067] [UniProtKB: P52564] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MPS1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| testis associated actin remodelling kinase 2/Dual specificity testis-specific protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069163] [GtoPdb: 2240] [UniProtKB: Q96S53] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Dynamin-like GTPase OPA1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105705] [UniProtKB: O60313] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TP53 regulating kinase/EKC/KEOPS complex subunit TP53RK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938223] [GtoPdb: 2248] [UniProtKB: Q96S44] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Electron transfer flavoprotein subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105744] [UniProtKB: P38117] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Elongation factor Tu, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105970] [UniProtKB: P49411] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of EGFR1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic elongation factor 2 kinase/Eukaryotic elongation factor 2 kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418] | ||||||||
| ChEMBL | Inhibition of EEF2K (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| eukaryotic translation initiation factor 2 alpha kinase 1/Eukaryotic translation initiation factor 2-alpha kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6029] [GtoPdb: 2015] [UniProtKB: Q9BQI3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5] | ||||||||
| ChEMBL | Inhibition of PERK (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Exosome RNA helicase MTR4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105889] [UniProtKB: P42285] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ferrochelatase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879831] [UniProtKB: P22830] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of FGFR1 (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of FAK (unknown origin) in presence of gamma33-ATP | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| General transcription and DNA repair factor IIH helicase subunit XPD in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105743] [UniProtKB: P18074] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycine--tRNA ligase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105815] [UniProtKB: P41250] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, brain form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3856] [UniProtKB: P11216] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Glycogen phosphorylase, liver form in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2568] [UniProtKB: P06737] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| GTP-binding nuclear protein Ran in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741190] [UniProtKB: P62826] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| GTP-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105780] [UniProtKB: Q9BZE4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Guanine nucleotide-binding protein G(i) subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105887] [UniProtKB: P04899] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Haem oxygenase 2/Heme oxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2546] [GtoPdb: 1442] [UniProtKB: P30519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MET (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| neurotrophic receptor tyrosine kinase 1/High affinity nerve growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 8.7 | pKd | 2 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of N-terminal GST-tagged human recombinant TRKA G595R mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay | B | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2023) 253: 115291-115291 [PMID:37030091] |
| ChEMBL | Inhibition of N-terminal GST-tagged human recombinant TRKA G667C mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay | B | 7.07 | pIC50 | 86 | nM | IC50 | Eur J Med Chem (2023) 253: 115291-115291 [PMID:37030091] |
| ChEMBL | Inhibition of human TrkA G595R mutant expressed in mouse NIH/3T3 cells by HTRF assay | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| ChEMBL | Inhibition TRKA (unknown origin) | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2019) 175: 129-148 [PMID:31077998] |
| ChEMBL | Inhibition of human TEL (336 residues) fused-TRKA (440 to 796 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of human TrkA G667C mutant expressed in mouse NIH/3T3 cells by HTRF assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| ChEMBL | Inhibition of recombinant His-tagged human TRKA (441 to 796 residues) expressed in baculovirus expression system using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate preincubated for 1 hr followed by substrate addition in presence of ATP by mobility shift assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2021) 216: 113265-113265 [PMID:33652352] |
| ChEMBL | Inhibition of TRKA (unknown origin) incubated for 1 hr by mobility shift assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Inhibition of human TRKA assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem (2021) 47: 116396-116396 [PMID:34534734] |
| ChEMBL | Inhibition of TRKA (unknown origin) by radiometric assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2022) 230: 114096-114096 [PMID:35007864] |
| ChEMBL | Inhibition of wild type TRAK (unknown origin) incubated for 30 mins by caliper mobility shift assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2020) 28: 115811-115811 [PMID:33069129] |
| ChEMBL | Inhibition of TRKA (unknown origin) by TR-FRET assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Inhibition of TRKA (unknown origin) in presence of gamma33-ATP | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of TRKA (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Inhibition of TRKA (unknown origin) by radiometric assay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2021) 53: 128409-128409 [PMID:34628036] |
| ChEMBL | Inhibition of TrkA (unknown origin) by radiometric assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2021) 64: 10286-10296 [PMID:34253025] |
| ChEMBL | Inhibition of TrkA (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2022) 56: 116596-116596 [PMID:35033885] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Enzyme Assay: In each well of a 384-well plate, 1 nM-1.5 nM of wild type NTRK1 enzyme (BPS Bioscience; 40280) was incubated in a total of 12.5 μL of buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 10 mM MgCl2, 1 mM DTT) with 1-2 μM CSKtide (Tuft's University or Anaspec; FITC-AHA-KKKKD DIYFFFG-NH2) and 1 mM ATP at 25° C. for 60 minutes in the presence or absence of a dosed concentration series of compound (1% DMSO final concentration). The reaction was stopped by the addition of 70 μL of Stop buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 35 mM EDTA and 0.2% of Coating Reagent 3 (Caliper Lifesciences)). The plate was then read on a Caliper EZReader 2 (protocol settings: −1.7 psi, upstream voltage −500, downstream voltage −3000, post sample sip 35 s). Data was normalized to 0% and 100% inhibition controls and the IC50 calculated using a 4-parameter fit in the CORE LIMS. | B | 9.22 | pIC50 | 0.6 | nM | IC50 | US-10370379-B2. Compounds and compositions useful for treating disorders related to NTRK (2019) |
| ChEMBL | NTRK1 Wild Type Assay at 1 mM ATP: In each well of a 384-well plate, 1 nM-1.5 nM of wild type NTRK1 enzyme (BPS Bioscience; 40280) was incubated in a total of 12.5 μL of buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 10 mM MgCl2, 1 mM DTT) with 1-2 aM CSKtide (Tuft's University or Anaspec; FITC-AHA-KKKKD DIYFFFG-NH2) and 1 mM ATP at 25° C. for 60 minutes in the presence or absence of a dosed concentration series of compound (1% DMSO final concentration). The reaction was stopped by the addition of 70 μL of Stop buffer (100 mM HEPES pH 7.5, 0.015% Brij 35, 35 mM EDTA and 0.2% of Coating Reagent 3 (Caliper Lifesciences)). The plate was then read on a Caliper EZReader 2 (protocol settings: 1.7 psi, upstream voltage −500, downstream voltage −3000, post sample sip 35 s). Data was normalized to 0% and 100% inhibition controls and the IC50 calculated using a 4-parameter fit in the CORE LIMS. | B | 9.22 | pIC50 | 0.6 | nM | IC50 | US-11059827-B2. Compounds and compositions useful for treating disorders related to NTRK (2021) |
| ChEMBL | Inhibition of human wild type TrkA kinase domain expressed in mouse NIH/3T3 cells by HTRF assay | B | 9.66 | pIC50 | 0.22 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126624-126624 [PMID:31444087] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibition of IKK2 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa-B kinase subunit epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| inosine monophosphate dehydrogenase 2/Inosine-5`-monophosphate dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2002] [GtoPdb: 2625] [UniProtKB: P12268] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Biochemical Assay: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.A specific substrate was incubated with the kinase in appropriate buffer conditions in the presence of ATP traced with .sup.33P-.gamma.-ATP (gamma phosphate-labeled, Redivue.TM. Code Number AH9968, 1000-3000 Ci/mmole, Amersham Biosciences Piscataway, N.J., USA), optimal cofactors and test compound.At the end of the phosphorylation reaction, more than 98% cold and radioactive ATP were captured by an excess of Dowex ion exchange resin. The resin was allowed to settle to the bottom of reaction wells by gravity. Supernatant, containing substrate peptide, was subsequently withdrawn and transferred into a counting plate, and radioactivity (corresponding to phosphate incorporated into peptide) was evaluated by .beta.-counting. Assay Conditions:The kinase assay was run with a final enzyme concentration of 6 nM, in the presence of 6 microM ATP, 1 nM . | B | 6.58 | pIC50 | 263 | nM | IC50 | US-9029356-B2. Substituted indazole derivatives active as kinase inhibitors (2015) |
| ChEMBL | IGF-1R Kinase Biochemical Assay: Kinase buffer was composed of 50 mM HEPES pH 7.9 containing 3 mM MnCl2, 1 mM DTT, 3 microM Na3VO4, and 0.2 mg/mL BSA. 3x KB is buffer of the same composition and pH as KB, but with three times the concentration of each component. Prior to starting the kinase inhibition assay, IGF-1R was pre-phosphorylated in order to linearize reaction kinetics. To achieve this, the desired total quantity of enzyme was prepared at an enzyme concentration of 360 nM in KB containing 100 microM ATP, and this preparation was incubated for 30 min at 28° C. 3x Enzyme Mix was obtained by diluting this preactivated enzyme 20-fold in 3x KB. The kinase assay was run with a final enzyme concentration of 6 nM, in the presence of 6 microM ATP, 1 nM 33P-γ-ATP and 10 microM substrate, a carboxy-terminally biotinylated peptide of the following sequence: KKKSPGEYVNIEFGGGGGK-biotin (SEQ ID NO:5). The peptide was obtained in batches of >95% peptide purity from American Peptide Company, Inc. (Sunnyvale, Calif., USA). | B | 6.58 | pIC50 | 263 | nM | IC50 | US-9255087-B2. Substituted indazole derivatives active as kinase inhibitors (2016) |
| ChEMBL | Biochemical Assay for Inhibitors of IGF-1 R Kinase Activity: The inhibitory activity of putative kinase inhibitors and the potency of selected compounds were determined using a trans-phosphorylation assay.A specific substrate was incubated with the kinase in appropriate buffer conditions in the presence of ATP traced with 33P-γ-ATP (gamma phosphate-labeled, Redivue Code Number AH9968, 1000-3000 Ci/mmole, Amersham Biosciences Piscataway, N.J., USA), optimal cofactors and test compound.At the end of the phosphorylation reaction, more than 98% cold and radioactive ATP were captured by an excess of Dowex ion exchange resin. The resin was allowed to settle to the bottom of reaction wells by gravity. Supernatant, containing substrate peptide, was subsequently withdrawn and transferred into a counting plate, and radioactivity (corresponding to phosphate incorporated into peptide) was evaluated by β-counting. | B | 6.58 | pIC50 | 263 | nM | IC50 | US-10081622-B2. Substituted indazole derivatives active as kinase inhibitors (2018) |
| ChEMBL | Inhibition of IGF1R (unknown origin) in presence of gamma33-ATP | B | 6.91 | pIC50 | 122 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of IR (unknown origin) in presence of gamma33-ATP | B | 6.68 | pIC50 | 209 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| integrin linked kinase/Integrin-linked protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5247] [GtoPdb: 2041] [UniProtKB: Q13418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 3/Interleukin-1 receptor-associated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5081] [GtoPdb: 2044] [UniProtKB: Q9Y616] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Isoleucine--tRNA ligase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105821] [UniProtKB: Q9NSE4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Long-chain-fatty-acid--CoA ligase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105818] [UniProtKB: Q9ULC5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MAPKAPK2 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| microtubule affinity regulating kinase 4/MAP/microtubule affinity-regulating kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5754] [GtoPdb: 2100] [UniProtKB: Q96L34] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of KIT (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MELK (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Membrane-associated progesterone receptor component 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105706] [UniProtKB: O00264] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase, membrane associated tyrosine/threonine 1/Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Midasin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105779] [UniProtKB: Q9NU22] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| misshapen like kinase 1/Misshapen-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5518] [GtoPdb: 2103] [UniProtKB: Q8N4C8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ERK2 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| mitogen-activated protein kinase 10/Mitogen-activated protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 11/Mitogen-activated protein kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3961] [GtoPdb: 1500] [UniProtKB: Q15759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of P38alpha (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 8/Mitogen-activated protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mitogen-activated protein kinase kinase kinase 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4853] [GtoPdb: 2079] [UniProtKB: Q9Y6R4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase 6/Mitogen-activated protein kinase kinase kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163123] [GtoPdb: 2081] [UniProtKB: O95382] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5749] [GtoPdb: 2085] [UniProtKB: Q92918] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5330] [GtoPdb: 2086] [UniProtKB: Q12851] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5432] [GtoPdb: 2087] [UniProtKB: Q8IVH8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 4/Mitogen-activated protein kinase kinase kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6166] [GtoPdb: 2088] [UniProtKB: O95819] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| mitogen-activated protein kinase kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4852] [GtoPdb: 2089] [UniProtKB: Q9Y4K4] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105746] [UniProtKB: P35580] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Myosin-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105888] [UniProtKB: Q7Z406] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin light chain kinase 3/Myosin light chain kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4627] [GtoPdb: 2110] [UniProtKB: Q32MK0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105781] [UniProtKB: Q9P0J0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 5.83 | pKd | 1486 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288] | ||||||||
| ChEMBL | Inhibition of TRKC (unknown origin) | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2019) 175: 129-148 [PMID:31077998] |
| ChEMBL | Inhibition of TRKC (unknown origin) incubated for 1 hr by mobility shift assay | B | 8.19 | pIC50 | 6.5 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Inhibition of TRKC (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Inhibition of TRKC (unknown origin) by radiometric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2021) 53: 128409-128409 [PMID:34628036] |
| ChEMBL | Inhibition of TrkC (unknown origin) by radiometric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 10286-10296 [PMID:34253025] |
| ChEMBL | Inhibition of recombinant human TRKC incubated for 90 mins by selectscreen kinase assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of TRKC (unknown origin) by radiometric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2022) 230: 114096-114096 [PMID:35007864] |
| ChEMBL | Inhibition of TRKC (unknown origin) by TR-FRET assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2022) 72: 116995-116995 [PMID:36095945] |
| ChEMBL | Inhibition of human TEL (336 residues) fused-TRKC (454 to 825 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Inhibition of TrkC (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2022) 56: 116596-116596 [PMID:35033885] |
| ChEMBL | Inhibition of TRKC (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2023) 258: 115618-115618 [PMID:37413881] |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| ChEMBL | Kinase Inhibition Assay: Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of pre-diluted compounds in duplex, and allowed to stand at room temperature for 30 minutes. The corresponding substrate and ATP were added and reacted at room temperature for 60 minutes (in which negative and positive controls were set). After the reaction was completed, an antibody was added for detection. After incubation for 60 minutes at room temperature, detection was carried out with Evnvision and data were collected. The enzyme activity in the presence of each concentration of the compounds disclosed herein was determined by Evnvision microplate reader, and the inhibitory activity of the compounds at different concentrations on the enzyme activity was calculated. Then, according to the four-parameter equation, the inhibitory activity of the compounds at different concentrations on the enzyme activity was fitted using Graphpad 5.0 software, and the IC50 value was calculated. | B | 9 | pIC50 | <1 | nM | IC50 | US-11267806-B2. Indazole compound for use in inhibiting kinase activity, composition and application thereof (2022) |
| NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Nucleoside diphosphate kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2160] [UniProtKB: P22392] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Obg-like ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105704] [UniProtKB: Q9NTK5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105748] [UniProtKB: Q15067] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Peroxisomal acyl-coenzyme A oxidase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105817] [UniProtKB: O15254] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phenylalanine--tRNA ligase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105969] [UniProtKB: Q9NSD9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Phosphatidylethanolamine-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105856] [UniProtKB: P30086] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 alpha/Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795194] [GtoPdb: 2858] [UniProtKB: P48426] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PDGFRbeta (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Probable ATP-dependent RNA helicase DDX6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105783] [UniProtKB: P26196] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PKCbeta (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C iota/Protein kinase C iota type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of BRK (unknown origin) in presence of gamma33-ATP | B | 6.71 | pIC50 | 195 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of RET (unknown origin) in presence of gamma33-ATP | B | 6.41 | pIC50 | 393 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Inhibition of ROS1 (unknown origin) by radiometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2021) 64: 10286-10296 [PMID:34253025] |
| ChEMBL | Inhibition ROS1 (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2024) 275: 116540-116540 [PMID:38852338] |
| ChEMBL | Inhibition of ROS1 (unknown origin) by radiometric assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2021) 53: 128409-128409 [PMID:34628036] |
| ChEMBL | Inhibition of ROS1 (unknown origin) by radiometric assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2022) 230: 114096-114096 [PMID:35007864] |
| ChEMBL | Inhibition of ROS1 (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2023) 258: 115618-115618 [PMID:37413881] |
| ChEMBL | Inhibition of ROS1 (unknown origin) in presence of gamma33-ATP | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of ROS1 (unknown origin) by radiometric assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2018) 143: 182-199 [PMID:29174814] |
| ChEMBL | Inhibition of human TEL (336 residues) fused-ROS1 (1891 to 2347 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ChEMBL | Inhibition of ROS1 (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2022) 56: 116596-116596 [PMID:35033885] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Putative heat shock protein HSP 90-beta 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105858] [UniProtKB: Q58FF8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Putative nucleoside diphosphate kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105936] [UniProtKB: O60361] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Pyridoxal kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075181] [UniProtKB: O00764] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rab-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105853] [UniProtKB: Q5HYI8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of AKT1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| AKT serine/threonine kinase 2/RAC-beta serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| AKT serine/threonine kinase 3/RAC-gamma serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ras-related protein Rab-10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105971] [UniProtKB: P61026] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RAB27A, member RAS oncogene family/Ras-related protein Rab-27A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105702] [GtoPdb: 2916] [UniProtKB: P51159] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ras-related protein Rab-6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105703] [UniProtKB: P20340] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of FLT3 (unknown origin) in presence of gamma33-ATP | B | 6.79 | pIC50 | 164 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A4/Ribosomal protein S6 kinase alpha-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3125] [GtoPdb: 1524] [UniProtKB: O75676] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha-5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Ribosyldihydronicotinamide dehydrogenase [quinone] in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| RNA cytidine acetyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105935] [UniProtKB: Q9H0A0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| S-adenosylmethionine synthase isoform type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313835] [UniProtKB: P31153] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Septin-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105891] [UniProtKB: Q9UHD8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 16/Serine/threonine-protein kinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3938] [GtoPdb: 2213] [UniProtKB: O75716] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of MST4 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Serine/threonine kinase 38/Serine/threonine-protein kinase 38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075155] [GtoPdb: 1517] [UniProtKB: Q15208] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of CHK1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| endoplasmic reticulum to nucleus signaling 1/Serine/threonine-protein kinase/endoribonuclease IRE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163101] [GtoPdb: 2020] [UniProtKB: O75460] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| endoplasmic reticulum to nucleus signaling 2/Serine/threonine-protein kinase/endoribonuclease IRE2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105932] [GtoPdb: 2021] [UniProtKB: Q76MJ5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ciliogenesis associated kinase 1/Serine/threonine-protein kinase ICK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163126] [GtoPdb: 2038] [UniProtKB: Q9UPZ9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| lemur tyrosine kinase 3/Serine/threonine-protein kinase LMTK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523432] [GtoPdb: 2057] [UniProtKB: Q96Q04] | ||||||||
| ChEMBL | Inhibition of LMTK3 (unknown origin) | B | 5.33 | pIC50 | 4653 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127108-127108 [PMID:32192797] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase alpha/Serine/threonine-protein kinase MRCK alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4516] [GtoPdb: 1507] [UniProtKB: Q5VT25] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase beta/Serine/threonine-protein kinase MRCK beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5052] [GtoPdb: 1508] [UniProtKB: Q9Y5S2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| CDC42 binding protein kinase gamma/Serine/threonine-protein kinase MRCK gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5615] [GtoPdb: 1506] [UniProtKB: Q6DT37] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 1/Serine/threonine-protein kinase Nek1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5855] [GtoPdb: 2114] [UniProtKB: Q96PY6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 2/Serine/threonine-protein kinase Nek2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3835] [GtoPdb: 2117] [UniProtKB: P51955] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 3/Serine/threonine-protein kinase Nek3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5679] [GtoPdb: 2118] [UniProtKB: P51956] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 6/Serine/threonine-protein kinase Nek6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
| ChEMBL | Inhibition of NEK6 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| NIMA related kinase 7/Serine/threonine-protein kinase Nek7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4849] [GtoPdb: 2122] [UniProtKB: Q8TDX7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84] | ||||||||
| ChEMBL | Inhibition of NIM1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| nemo like kinase/Serine/threonine-protein kinase NLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5364] [GtoPdb: 2125] [UniProtKB: Q9UBE8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| p21 (RAC1) activated kinase 2/Serine/threonine-protein kinase PAK 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4487] [GtoPdb: 2134] [UniProtKB: Q13177] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PAK4 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PIM1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of PLK1 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| SIK family kinase 3/Serine/threonine-protein kinase SIK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6149] [GtoPdb: 2199] [UniProtKB: Q9Y2K2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| serine/threonine kinase 11/Serine/threonine-protein kinase STK11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5606] [GtoPdb: 2212] [UniProtKB: Q15831] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| unc-51 like kinase 3/Serine/threonine-protein kinase ULK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5047] [GtoPdb: 2273] [UniProtKB: Q6PHR2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Signal recognition particle receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105934] [UniProtKB: P08240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| STE20 related adaptor alpha/STE20-related kinase adapter protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795198] [GtoPdb: 2227] [UniProtKB: Q7RTN6] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Structural maintenance of chromosomes protein 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105747] [UniProtKB: Q14683] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Structural maintenance of chromosomes protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105890] [UniProtKB: O95347] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105973] [UniProtKB: Q9P2R7] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| transforming growth factor beta receptor 2/TGF-beta receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4267] [GtoPdb: 1795] [UniProtKB: P37173] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Thyroid hormone receptor-associated protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105820] [UniProtKB: Q9Y2W1] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| TRAF2 and NCK interacting kinase/TRAF2 and NCK-interacting protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of ABL (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| ABL proto-oncogene 2, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4014] [GtoPdb: 1924] [UniProtKB: P42684] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of JAK1 (unknown origin) in presence of gamma33-ATP | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 (unknown origin) in presence of gamma33-ATP | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of JAK3 (unknown origin) in presence of gamma33-ATP | B | 6.46 | pIC50 | 349 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of LCK (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| ChEMBL | Inhibition of SYK (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of ZAP70 (unknown origin) in presence of gamma33-ATP | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Tyrosine--tRNA ligase, cytoplasmic in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| U5 small nuclear ribonucleoprotein 200 kDa helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105972] [UniProtKB: O75643] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| aarF domain containing kinase 5/Uncharacterized aarF domain-containing protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105886] [GtoPdb: 1929] [UniProtKB: Q3MIX3] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| Uncharacterized protein FLJ45252 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105933] [UniProtKB: Q6ZSR9] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of VEGFR2 (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Inhibition of VEGFR3 (unknown origin) in presence of gamma33-ATP | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2016) 59: 3392-3408 [PMID:27003761] |
| Very long-chain specific acyl-CoA dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105892] [UniProtKB: P49748] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
| WEE1 G2 checkpoint kinase/Wee1-like protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291] | ||||||||
| ChEMBL | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | B | 4.52 | pKd | >30000 | nM | Kd | Science (2017) 358: null-null [PMID:29191878] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
