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 34:

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]