compound 46 [PMID: 16451062] [Ligand Id: 8355] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL201307
  • mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • C-terminal Src kinase/Tyrosine-protein kinase CSK in Human [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL Inhibitory activity against JNK1alpha B 4 pIC50 >100000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibitory activity against CDK2 B 4.21 pIC50 62000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibitory activity against EGFR B 6.1 pIC50 800 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
ChEMBL Inhibition of EGFR kinase B 6.1 pIC50 800 nM IC50 Nat Chem Biol (2006) 2: 358-364 [PMID:16783341]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibitory activity against FAK B 5.4 pIC50 4000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory activity against human hERG receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibitory activity against IGFR B 4.89 pIC50 13000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibitory activity against p38-alpha MAPK B 4 pIC50 >100000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
GtoPdb - - 9 pIC50 <1 nM IC50 J Med Chem (2006) 49: 955-70 [PMID:16451062]
ChEMBL Inhibition of Aurora A kinase activity B 9 pIC50 <1 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
ChEMBL Inhibition of aurora A kinase B 9 pIC50 <1 nM IC50 J Med Chem (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibition of Aurora A kinase B 9 pIC50 <1 nM IC50 Nat Chem Biol (2006) 2: 358-364 [PMID:16783341]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
GtoPdb - - 8.15 pIC50 <7 nM IC50 J Med Chem (2006) 49: 955-70 [PMID:16451062]
ChEMBL Inhibition of aurora B kinase B 8.15 pIC50 7 nM IC50 J Med Chem (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibition of Aurora B kinase B 8.15 pIC50 7 nM IC50 Nat Chem Biol (2006) 2: 358-364 [PMID:16783341]
C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240]
ChEMBL Inhibitory activity against CSK B 4.68 pIC50 21000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibitory activity against JAK3 B 4.6 pIC50 25000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibitory activity against SRC B 5.52 pIC50 3000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibitory activity against KDR B 6 pIC50 1000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]