PP1 [Ligand Id: 8836] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL306380 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Inhibition of tie-2 at 5 uM ATP | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Inhibition of CK1delta in the presence of 20uM ATP | B | 6.77 | pIC50 | 170 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR | B | 6.7 | pKi | 199.53 | nM | Ki | ACS Med Chem Lett (2012) 3: 383-386 [PMID:24900482] |
| GtoPdb | - | - | 6.6 | pIC50 | 250 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| 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 human KIT using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | B | 5.88 | pIC50 | 1318 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2010) 53: 357-367 [PMID:19928858] |
| ChEMBL | Displacement of N,N'-(2,2'-(3,3'-disulfanediylbis(2,5-dioxopyrrolidine-3,1-diyl))bis(ethane-2,1-diyl))bis(2-(3-(3-tert-butyl-5-(3-naphthalen-1-ylureido)-1H-pyrazol-1-yl)phenylamino)acetamide) from inactive form of p38alpha expressed in Escherichia coli BL21(DE3) cells by enzyme fragment complementation assay | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2010) 53: 357-367 [PMID:19928858] |
| GtoPdb | - | - | 6.19 | pIC50 | 640 | nM | IC50 | Biochem J (2003) 371: 199-204 [PMID:12534346] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | B | 6.18 | pIC50 | 657 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| LCK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| LCK proto-oncogene, Src family tyrosine kinase/Proto-oncogene tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240] | ||||||||
| ChEMBL | Inhibition of Lck in the presence of 50uM ATP | B | 7.4 | pIC50 | 40 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Measurement of Inhibitory Activity Against RET (V804L, V804M): Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mutation) kinase activity, the website of AnaSpec states that Srctide (GEEPLYWSFPAKKK) corresponds to the substrate peptide for reaction to measure RET kinase activity. Thus, the amino acid sequence was partly modified and biotinylated to prepare biotinylated peptides (biotin-EEPLYWSFPAKKK). The purified recombinant human RET (V804L or V804M) protein used in the test was purchased from Eurofins.To measure the inhibitory activity, first, the test compounds were individually diluted with dimethyl sulfoxide (DMSO) stepwise. Subsequently, RET (V804L or V804M) protein, the substrate peptides (the final concentration: 250 nM), magnesium chloride (the final concentration: 10 mM), ATP (the final concentration: 10 μM), and a solution of a test compound in DMSO (the final concentration of DMSO: 5%) were added to a buffer for kinase reaction (13.5 mM Tris, pH of 7.5, 2 mM dithiothreitol, 0.009% Tween-20). Each of the mixtures was incubated at 25° C. for 120 minutes to perform a kinase reaction. EDTA was then added thereto to give a final concentration of 40 mM so that the reaction was terminated. A detection solution containing Eu-labeled antiphosphotyrosine antibody PT66 (PerkinElmer) and SureLight APC-SA (PerkinElmer) was added thereto, and each mixture was allowed to stand at room temperature for 2 hours or more. Finally, the intensity of fluorescence under excitation light with a wavelength of 337 nm was measured with a PHERAstar FS (BMG Labtech) at the two wavelengths of 620 nm and 665 nm. The phosphorylation level was calculated from the ratio of the fluorescence intensity at the two wavelengths, and the compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM). | B | 5.46 | pIC50 | 3434 | nM | IC50 | US-10807986-B2. Fused pyrimidine compound or salt thereof (2020) |
| ChEMBL | Measurement of Inhibitory Activity Against RET (In Vitro): Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET kinase activity, the website of AnaSpec states that Srctide (GEEPLYWSFPAKKK) corresponds to the substrate peptide for reaction to measure RET kinase activity. Thus, the amino acid sequence was partly modified and biotinylated to prepare biotinylated peptides (biotin-EEPLYWSFPAKKK). The purified recombinant human RET protein used in the test was purchased from Carna Biosciences, Inc.To measure the inhibitory activity, first, the compounds of the present invention were individually diluted with dimethyl sulfoxide (DMSO) stepwise. Subsequently, RET protein, the substrate peptide (the final concentration: 250 nM), magnesium chloride (the final concentration: 10 mM), ATP (the final concentration: 10 μM), and a solution of the compound of the present invention in DMSO (the final concentration of DMSO: 2.5%) were added to a buffer for kinase reaction (13.5 mM Tris, pH of 7.5, 2 mM dithiothreitol, 0.009% Tween-20). Each of the mixtures was incubated at 25° C. for 100 minutes to perform a kinase reaction. EDTA was then added thereto to give a final concentration of 24 mM so that the reaction was terminated. A detection solution containing Eu-labeled antiphosphotyrosine antibody PT66 (PerkinElmer) and SureLight APC-SA (PerkinElmer) was added thereto, and each mixture was allowed to stand at room temperature for 2 hours or more. Finally, the intensity of fluorescence under the excitation light with a wavelength of 337 nm was measured with a PHERAstar FS (BMG Labtech) at the two wavelengths of 620 nm and 665 nm. The phosphorylation level was calculated from the ratio of the fluorescence intensity at the two wavelengths, and the compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM). | B | 5.46 | pIC50 | 3434 | nM | IC50 | US-11046696-B2. Fused pyrimidine compound or salt thereof (2021) |
| ChEMBL | Measurement of Inhibitory Activity Against RET (V804L, V804M): Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET (V804L or V804M) (i.e., RET with V804L or V804M mutation) kinase activity, the website of AnaSpec states that Srctide (GEEPLYWSFPAKKK) corresponds to the substrate peptide for reaction to measure RET kinase activity. Thus, the amino acid sequence was partly modified and biotinylated to prepare biotinylated peptides (biotin-EEPLYWSFPAKKK). The purified recombinant human RET (V804L or V804M) protein used in the test was purchased from Eurofins.To measure the inhibitory activity, first, the test compounds were individually diluted with dimethyl sulfoxide (DMSO) stepwise. Subsequently, RET (V804L or V804M) protein, the substrate peptides (the final concentration: 250 nM), magnesium chloride (the final concentration: 10 mM), ATP (the final concentration: 10 μM), and a solution of a test compound in DMSO (the final concentration of DMSO: 5%) were added to a buffer for kinase reaction (13.5 mM Tris, pH of 7.5, 2 mM dithiothreitol, 0.009% Tween-20). Each of the mixtures was incubated at 25° C. for 120 minutes to perform a kinase reaction. EDTA was then added thereto to give a final concentration of 40 mM so that the reaction was terminated. A detection solution containing Eu-labeled antiphosphotyrosine antibody PT66 (PerkinElmer) and SureLight APC-SA (PerkinElmer) was added thereto, and each mixture was allowed to stand at room temperature for 2 hours or more. Finally, the intensity of fluorescence under excitation light with a wavelength of 337 nm was measured with a PHERAstar FS (BMG Labtech) at the two wavelengths of 620 nm and 665 nm. The phosphorylation level was calculated from the ratio of the fluorescence intensity at the two wavelengths, and the compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM). | B | 5.48 | pIC50 | 3288 | nM | IC50 | US-10807986-B2. Fused pyrimidine compound or salt thereof (2020) |
| ChEMBL | Measurement of Inhibitory Activity Against RET (In Vitro): Regarding the conditions for measurement of in vitro inhibitory activity of compounds against RET kinase activity, the website of AnaSpec states that Srctide (GEEPLYWSFPAKKK) corresponds to the substrate peptide for reaction to measure RET kinase activity. Thus, the amino acid sequence was partly modified and biotinylated to prepare biotinylated peptides (biotin-EEPLYWSFPAKKK). The purified recombinant human RET protein used in the test was purchased from Carna Biosciences, Inc.To measure the inhibitory activity, first, the compounds of the present invention were individually diluted with dimethyl sulfoxide (DMSO) stepwise. Subsequently, RET protein, the substrate peptide (the final concentration: 250 nM), magnesium chloride (the final concentration: 10 mM), ATP (the final concentration: 10 μM), and a solution of the compound of the present invention in DMSO (the final concentration of DMSO: 2.5%) were added to a buffer for kinase reaction (13.5 mM Tris, pH of 7.5, 2 mM dithiothreitol, 0.009% Tween-20). Each of the mixtures was incubated at 25° C. for 100 minutes to perform a kinase reaction. EDTA was then added thereto to give a final concentration of 24 mM so that the reaction was terminated. A detection solution containing Eu-labeled antiphosphotyrosine antibody PT66 (PerkinElmer) and SureLight APC-SA (PerkinElmer) was added thereto, and each mixture was allowed to stand at room temperature for 2 hours or more. Finally, the intensity of fluorescence under the excitation light with a wavelength of 337 nm was measured with a PHERAstar FS (BMG Labtech) at the two wavelengths of 620 nm and 665 nm. The phosphorylation level was calculated from the ratio of the fluorescence intensity at the two wavelengths, and the compound concentration at which phosphorylation was inhibited by 50% was defined as the IC50 value (nM). | B | 5.48 | pIC50 | 3288 | nM | IC50 | US-11046696-B2. Fused pyrimidine compound or salt thereof (2021) |
| ChEMBL | Inhibition of human RET using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| Proto-oncogene tyrosine-protein kinase Src in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523] | ||||||||
| ChEMBL | Inhibition of Src in the presence of 50uM ATP | B | 7.28 | pIC50 | 53 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| 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 | Inhibition of src at 5 mM ATP | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibition of src (unknown origin) | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2021) 64: 10581-10605 [PMID:34313432] |
| ChEMBL | Inhibition of C-terminal His-tagged full length human SRC expressed in insect cells preincubated for 20 mins using poly[Glu,Tyr]4:1 as substrate measured after 5 to 120 mins in presence of [gamma-33P]ATP by Kinome assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| ChEMBL | Inhibition of Src (unknown origin) | B | 8 | pIC50 | <10 | nM | IC50 | Bioorg Med Chem (2024) 98: 117561-117561 [PMID:38157838] |
| ChEMBL | Inhibition of GST-tagged human recombinant c-src using biotinylated peptide as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by microplate reader analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | Medchemcomm (2015) 6: 1518-1534 |
| 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 | Inhibition of RIP2 in the presence of 100uM ATP | B | 7.59 | pIC50 | 26 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of human mTOR using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | B | 5.03 | pIC50 | 9318 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| 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 | Inhibition of human ABL using EAIYAAPFAKKK as substrate in presence of [gamma-33P]ATP | B | 6.83 | pIC50 | 147 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of N-terminal GST tagged BLK (1 to 505 end residues) (unknown origin) expressed in Sf21insect cells by time resolved fluorescence based assay | B | 6.84 | pIC50 | 144 | nM | IC50 | Eur J Med Chem (2023) 256: 115460-115460 [PMID:37163946] |
| ChEMBL | Induction of ubiquitin proteasomal system dependent BLK degradation in human Ramos cells measured after 12 hrs by Western blot analysis | B | 7.52 | pEC50 | >30 | nM | EC50 | Eur J Med Chem (2023) 256: 115460-115460 [PMID:37163946] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of CSK in the presence of 20uM ATP | B | 6.19 | pIC50 | 640 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| GtoPdb | - | - | 6.28 | pIC50 | 520 | nM | IC50 | Biochem J (2003) 371: 199-204 [PMID:12534346] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of human FYN using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| ChEMBL | Inhibition of FYN (unknown origin) by cell culture based assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 142: 229-243 [PMID:28814374] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| ChEMBL | Inhibition of FYN (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
| ChEMBL | ADP-Glo Kinase Assay: The assay procedure determines the IC50 of each potential FYN kinase inhibitor by measuring the enzyme catalyzed ATP-dependent phosphorylation of the FYN substrate peptide. The ADP-Glo™ Kinase Assay is specifically designed to quantify kinase activity by measuring the ADP produced in the reaction The reaction buffer comprises 40 mM Tris.HCl (pH 7.5), 20 mM MgCl2, 0.1 mg/ml BSA and 5 microM DTT. Individual compounds within the chemical library were dissolved in DMSO at known concentrations. Briefly, 2.5 microliters of reaction buffer containing 3 picograms of FYN kinase and serial dilutions of each potential FYN kinase inhibitor (9 3-fold dilutions of a 10 micromolar top sample) are placed into each well of a 384 well microtiter plate and incubated at room temperature for 30 minutes. An additional 2.5 microliters of reaction buffer containing 100 picograms of the FYN substrate and 12.5 picomoles of ATP are then added to each well and the reaction carried out for 90 minutes at room temperature. | B | 8.22 | pIC50 | 6 | nM | IC50 | US-10688093-B2. Methods, compositions, and uses of novel Fyn kinase inhibitors (2020) |
| ChEMBL | ADP-Glo™ Kinase Assay: The ADP-Glo™ Kinase Assay is specifically designed to quantify kinase activity by measuring the ADP produced in the reaction The reaction buffer comprises 40 mM Tris·HCl (pH 7.5), 20 mM MgCl2, 0.1 mg/ml BSA and 5 microM DTT. Individual compounds within the chemical library were dissolved in DMSO at known concentrations. Briefly, 2.5 microliters of reaction buffer containing 3 picograms of FYN kinase and serial dilutions of each potential FYN kinase inhibitor (9 3-fold dilutions of a 10 micromolar top sample) are placed into each well of a 384 well microtiter plate and incubated at room temperature for 30 minutes. An additional 2.5 microliters of reaction buffer containing 100 picograms of the FYN substrate and 12.5 picomoles of ATP are then added to each well and the reaction carried out for 90 minutes at room temperature. The reactions are terminated by addition of 5 microliters of the ADP-Glo™ Reagent component of the ADP-Glo™ Kinase Assay kit to each well. The ADP-Glo™ Reagent comprises an ATP-dependent adenylate cyclase, an inorganic pyrophosphatase and an excess of staurosporine. The adenylate cyclase converts the remaining ATP to cAMP and pyrophospahte, the pyrophosphatase converts the pyrophosphate to phosphate and the staurosporine inhibits the activity of the FYN kinase, the net effect is to remove all residual ATP while preserving the ADP produced by FYN kinase. The terminated reactions are incubated for 40 minutes at room temperature, prior to addition of the Kinase Detection Reagent component of the ADP-Glo Kinase Assay kit to each well. The Kinase Detection Reagent comprises pyruvate kinase, phosphoenol pyruvate (PEP), luciferin and luciferase. The pyruvate kinase converts PEP to pyruvate and in the process generates ATP from the residual ADP present in the terminated reaction. The ATP is then consumed by the luciferase catalyzed, light emitting conversion of luciferin to oxyluciferin producing AMP, pyrophosphate and CO2. The emitted light was measured on an Envion Luminometer to determine the relative activity of the FYN kinase in each well. A 10 point dose-response curve for each potential FYN kinase inhibitor dilution series was used to determine the IC50, of each compound. Details of the analysis, including assay procedures and representative dilution schema for measuring kinase inhibitors are presented in the Technical Manual accompanying the ADP-Glo™ Kinase Assay kit (Doc. TM313, Promega Corp.) as well as U.S. Pat. Nos. 8,183,007 and 8,802,411, the contents of which are incorporated herein, in their entirety. | B | 8.22 | pIC50 | 6 | nM | IC50 | US-11701353-B2. Methods, compositions, and uses of novel FYN kinase inhibitors (2023) |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of LCK | B | 7.2 | pKi | 63.1 | nM | Ki | ACS Med Chem Lett (2012) 3: 383-386 [PMID:24900482] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase catalytic domain at 5 uM ATP | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase at 5 uM ATP | B | 6.82 | pIC50 | 151 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | J Biol Chem (1996) 271: 695-701 [PMID:8557675] |
| ChEMBL | Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited. | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 417-420 |
| ChEMBL | Inhibition of LCK (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498] |
| 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 | Inhibition of human YES using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P] ATP | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2016) 59: 4697-4710 [PMID:27115835] |
| 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 Vascular endothelial growth factor receptor 2 at 5 uM ATP | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2167-2170 [PMID:11012021] |
| WNK lysine deficient protein kinase 1 in Human [GtoPdb: 2280] [UniProtKB: Q9H4A3] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | 12700 | nM | Ki | Biochemistry (2009) 48: 10255-66 [PMID:19739668] |
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]
