dasatinib [Ligand Id: 5678] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1421 (BMS-354825, Dasatinib accord, Dasatinib accordpharma, Dasatinib (anhydrous), Dasatinib anhydrous) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Crk-like protein in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6066237] [UniProtKB: P47941] | ||||||||
| ChEMBL | Inhibition of CrkL in mouse BaF3 cells harbouring BCR-ABL1 T315I mutant measured after 6 hrs by immunoblotting analysis | B | 5.3 | pIC50 | >5000 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Binding affinity to human DDR2 incubated for 45 mins by Kinobead based pull down assay | B | 7.15 | pKd | 70.79 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human DDR2 incubated for 45 mins by Kinobead based pull down assay | B | 7.15 | pKd | 70 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of DDR2 (unknown origin) | B | 7.27 | pIC50 | 54 | nM | IC50 | Eur J Med Chem (2024) 265: 116100-116100 [PMID:38171149] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Binding affinity to human EPHA1 incubated for 45 mins by Kinobead based pull down assay | B | 7.82 | pKd | 15 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHA1 incubated for 45 mins by Kinobead based pull down assay | B | 7.83 | pKd | 14.79 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA1 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 7.51 | pIC50 | 30.6 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Binding affinity to human EPHA2 incubated for 45 mins by Kinobead based pull down assay | B | 8.23 | pKd | 5.93 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHA2 incubated for 45 mins by Kinobead based pull down assay | B | 8.23 | pKd | 5.9 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to recombinant human EPHA2 (D596 to G900 residues) expressed in insect cells incubated for 30 mins by MST assay | B | 8.49 | pKd | 3.26 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA2 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.35 | pIC50 | 4.5 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] | ||||||||
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Binding affinity to human EPHA4 incubated for 45 mins by Kinobead based pull down assay | B | 8.14 | pKd | 7.31 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHA4 incubated for 45 mins by Kinobead based pull down assay | B | 8.14 | pKd | 7.3 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA4 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Binding affinity to human EPHA5 incubated for 45 mins by Kinobead based pull down assay | B | 8.43 | pKd | 3.7 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHA5 incubated for 45 mins by Kinobead based pull down assay | B | 8.44 | pKd | 3.66 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA5 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A6/Ephrin type-A receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33] | ||||||||
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA6 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA7 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322] | ||||||||
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHA8 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Binding affinity to human EPHB2 incubated for 45 mins by Kinobead based pull down assay | B | 8.4 | pKd | 3.94 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHB2 incubated for 45 mins by Kinobead based pull down assay | B | 8.41 | pKd | 3.9 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHB2 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Binding affinity to human EPHB3 incubated for 45 mins by Kinobead based pull down assay | B | 7.54 | pKd | 29 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHB3 incubated for 45 mins by Kinobead based pull down assay | B | 7.54 | pKd | 28.84 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHB3 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 7.76 | pIC50 | 17.4 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Binding affinity to human EPHB4 incubated for 45 mins by Kinobead based pull down assay | B | 8.43 | pKd | 3.7 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHB4 incubated for 45 mins by Kinobead based pull down assay | B | 8.43 | pKd | 3.68 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHB4 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 8.68 | pIC50 | 2.07 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] | ||||||||
| ChEMBL | Binding affinity to human EPHB6 incubated for 45 mins by Kinobead based pull down assay | B | 7.46 | pKd | 34.36 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human EPHB6 incubated for 45 mins by Kinobead based pull down assay | B | 7.47 | pKd | 34 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Nano Luc-fused full length C-terminal EPHB6 (unknown origin) expressed in HEK293T cells using NanoGlo as substrate incubated for 2 hrs in presence of tracer by NanoBRET assay | B | 6.83 | pIC50 | 147.2 | nM | IC50 | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell survival | B | 6.17 | pIC50 | 678 | nM | IC50 | Bioorg Med Chem Lett (2024) 100: 129612-129612 [PMID:38199330] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell survival | B | 6.23 | pIC50 | 584 | nM | IC50 | Bioorg Med Chem Lett (2024) 100: 129612-129612 [PMID:38199330] |
| 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 | Binding affinity to human DDR1 incubated for 45 mins by Kinobead based pull down assay | B | 7.37 | pKd | 43 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human DDR1 incubated for 45 mins by Kinobead based pull down assay | B | 7.37 | pKd | 42.66 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of DDR1 (unknown origin) | B | 7.59 | pIC50 | 26 | nM | IC50 | Eur J Med Chem (2024) 265: 116100-116100 [PMID:38171149] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Inhibition of NanoLuc-fused FMS (unknown origin) transfected in HEK293 cells by NanoBRET assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2024) 274: 116557-116557 [PMID:38850857] |
| ChEMBL | Inhibition of recombinant His-tagged human CSF1R catalytic domain expressed in baculovirus expression system using TAMRA-KKKSPGEYVNIEFG as substrate preincubated for 30 mins followed by substrate addition and measured after 120 mins in presence of ATP by fluorescence polarization assay | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2024) 15: 722-730 [PMID:38746878] |
| 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 in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of KIT in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of c-KIT in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of KIT in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of KIT in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of KIT in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Binding affinity to human MAPK14 incubated for 45 mins by Kinobead based pull down assay | B | 6.02 | pKd | 954.99 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human MAPK14 incubated for 45 mins by Kinobead based pull down assay | B | 6.02 | pKd | 945 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| 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 | Binding affinity to human ZAK incubated for 45 mins by Kinobead based pull down assay | B | 6.66 | pKd | 218.78 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human ZAK incubated for 45 mins by Kinobead based pull down assay | B | 6.66 | pKd | 217 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| Myelin transcription factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331044] [UniProtKB: Q01538] | ||||||||
| ChEMBL | Inhibition of MYT1 (unknown origin) | B | 6.65 | pIC50 | 226 | nM | IC50 | J Med Chem (2024) 67: 420-432 [PMID:38146659] |
| 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 | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 7.26 | pIC50 | 55 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 6.26 | pIC50 | 550 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| 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 | Binding affinity to human SRC incubated for 45 mins by Kinobead based pull down assay | B | 8.52 | pKd | 3 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human SRC incubated for 45 mins by Kinobead based pull down assay | B | 8.56 | pKd | 2.75 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Inhibition of Src in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Src in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of SRC in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Src in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Src in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Inhibition of Src in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | B | 6 | pIC50 | 1000 | nM | IC50 | Oncotarget (2015) 6: 18921-18932 [PMID:26254279] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Inhibition of GST tagged Src (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.22 | pIC50 | 6 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Src (unknown origin) assessed as inhibition of phosphorylation using PTK biotinylated peptide substrate 2 as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2005) 65: 4500-5 [PMID:15930265] |
| 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 | Binding affinity to human BRAF incubated for 45 mins by Kinobead based pull down assay | B | 5.49 | pKd | 3235.94 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human BRAF incubated for 45 mins by Kinobead based pull down assay | B | 5.49 | pKd | 3231 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 6 | pIC50 | >1000 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| 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 | Binding affinity to human ABL1 incubated for 45 mins by Kinobead based pull down assay | B | 8.3 | pKd | 5 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human ABL1 incubated for 45 mins by Kinobead based pull down assay | B | 8.33 | pKd | 4.68 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| GtoPdb | Binding affinity for the unphosphorylated kinase domain of the human ABL protein. | - | 10.49 | pKd | 0.03 | nM | Kd | J Med Chem (2019) 62: 9281-9298 [PMID:31539241] |
| ChEMBL | Inhibition of GST tagged Abl T315l mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 5 | pIC50 | >10000 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of human ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by 0.5 mM ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of human unphosphorylated ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of human phosphorylated ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of GST tagged Abl T315l mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 6 | pIC50 | >1000 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Inhibition of GST tagged Abl L387M mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl Y253F mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl H396P mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.52 | pIC50 | 3 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl V379I mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.65 | pIC50 | 2.25 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl G250E mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.7 | pIC50 | 2 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl H396R mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.7 | pIC50 | 2 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl Y253H mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl F359V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl E255V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl E255K mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl Y253H mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl F317L mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.94 | pIC50 | 1.15 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by 0.5 mM ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of human N-terminal his tagged unphosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by 5 mM ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 9 | pIC50 | 1 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of GST tagged Abl F317L mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl F311L mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl M244V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl M244V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl H396R mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of human N-terminal his tagged phosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of GST tagged Abl V379I mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl E255V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl L387M mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of human ABL1 H396P mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Cancer Cell (2011) 19: 556-568 [PMID:21481795] |
| ChEMBL | Inhibition of GST tagged Abl F359V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl F311L mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl H396P mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl Y253F mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl G250E mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| GtoPdb | - | - | 9.6 | pIC50 | 0.27 | nM | IC50 | Genes Cells (2013) 18: 110-22 [PMID:23279183] |
| ChEMBL | Inhibition of GST tagged Abl E255K mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 10 | pIC50 | 0.1 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| 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 | Binding affinity to human ABL2 incubated for 45 mins by Kinobead based pull down assay | B | 8.4 | pKd | 4 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human ABL2 incubated for 45 mins by Kinobead based pull down assay | B | 8.44 | pKd | 3.63 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Binding affinity to human FRK incubated for 45 mins by Kinobead based pull down assay | B | 8.3 | pKd | 5 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human FRK incubated for 45 mins by Kinobead based pull down assay | B | 8.34 | pKd | 4.57 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Binding affinity to human FYN incubated for 45 mins by Kinobead based pull down assay | B | 8.4 | pKd | 4 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human FYN incubated for 45 mins by Kinobead based pull down assay | B | 8.43 | pKd | 3.71 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Binding affinity to human HCK incubated for 45 mins by Kinobead based pull down assay | B | 7.54 | pKd | 29 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human HCK incubated for 45 mins by Kinobead based pull down assay | B | 7.54 | pKd | 28.84 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Binding affinity to human LCK incubated for 45 mins by Kinobead based pull down assay | B | 8.13 | pKd | 7.41 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human LCK incubated for 45 mins by Kinobead based pull down assay | B | 8.15 | pKd | 7 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Binding affinity to human LYN incubated for 45 mins by Kinobead based pull down assay | B | 8.09 | pKd | 8.13 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human LYN incubated for 45 mins by Kinobead based pull down assay | B | 8.1 | pKd | 8 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| ChEMBL | Inhibition of GST tagged Lyn (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| ChEMBL | Inhibition of GST tagged Lyn (unknown origin) assessed as inhibition of phosphorylation using PTK biotinylated peptide substrate 2 as substrate preincubated for 5 mins followed by [gamma-32P]ATP addition | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Cancer Res (2005) 65: 4500-4505 [PMID:15930265] |
| 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 | Binding affinity to human YES1 incubated for 45 mins by Kinobead based pull down assay | B | 8.4 | pKd | 4 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Binding affinity to human YES1 incubated for 45 mins by Kinobead based pull down assay | B | 8.43 | pKd | 3.71 | nM | Kd | ChemMedChem (2018) 13: 1629-1633 [PMID:29928781] |
| ChEMBL | Kinase Screening Assay: Compound IC50 values were determined from 10-point, 1:3 dilution curves starting at either 100 μM or 10 μM with 10 μM ATP, by Reaction Biology Corp. For the whole kinome screen compounds were screened against 340 wild type kinases at a single dose of 1 μM, in duplicate, with 10 μM of ATP by Reaction Biology Corp. The data was averaged and plotted as percentage enzyme activity relative to DMSO, as negative control, using DiscoverRX TREEspot software. | B | 8 | pIC50 | <10 | nM | IC50 | US-10294227-B2. Compounds (2019) |
| salt inducible kinase 1 in Human [GtoPdb: 2197] [UniProtKB: P57059] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | <3 | nM | IC50 | Biochem J (2015) 465: 271-9 [PMID:25351958] |
| salt inducible kinase 2 in Human [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | <3 | nM | IC50 | Biochem J (2015) 465: 271-9 [PMID:25351958] |
| SIK family kinase 3 in Human [GtoPdb: 2199] [UniProtKB: Q9Y2K2] | ||||||||
| GtoPdb | - | - | 8 | pIC50 | 10 | nM | IC50 | Biochem J (2015) 465: 271-9 [PMID:25351958] |
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]
