compound 33 [PMID: 19364658] [Ligand Id: 8163] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL511410
  • casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
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  • component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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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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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • protein kinase C alpha/Protein kinase C alpha in Human [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
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  • ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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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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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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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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  • protein kinase A in Human [GtoPdb: 1694]
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  • checkpoint kinase 1 in Human [GtoPdb: 1987] [UniProtKB: O14757]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0]
ChEMBL Inhibition of CK1-gamma1 B 6.8 pIC50 160 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
GtoPdb - - 6.8 pIC50 160 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111]
ChEMBL Inhibition of IKKalpha B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Inhibition of human recombinant MK2 B 6.41 pIC50 390 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
GtoPdb - - 6.41 pIC50 390 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Inhibition of ERK2 B 5.38 pIC50 4200 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
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 PDGFRalpha B 4.95 pIC50 11100 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252]
ChEMBL Inhibition of PKCalpha B 4.47 pIC50 33600 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
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]
GtoPdb - - 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]
ChEMBL Inhibition of ROCK1 B 7.22 pIC50 60 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of RSK1 B 6.54 pIC50 290 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
GtoPdb - - 6.54 pIC50 290 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aurora B B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
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 FYN B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of SRC B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem (2009) 17: 3342-3351 [PMID:19364658]
protein kinase A in Human [GtoPdb: 1694]
GtoPdb - - 6.57 pIC50 270 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]
checkpoint kinase 1 in Human [GtoPdb: 1987] [UniProtKB: O14757]
GtoPdb - - 7.05 pIC50 90 nM IC50 Bioorg Med Chem (2009) 17: 3342-51 [PMID:19364658]

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]