compound 25 [PMID: 20855207] [Ligand Id: 8159] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1270399
  • calcium/calmodulin dependent protein kinase IV/CaM kinase IV in Human [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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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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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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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 2/Rho-associated protein kinase 2 in Human [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
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  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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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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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
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  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
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  • testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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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
calcium/calmodulin dependent protein kinase IV/CaM kinase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2494] [GtoPdb: 1955] [UniProtKB: Q16566]
ChEMBL Inhibition of Camk4 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CSNK1d B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of cMET B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKK-beta B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
interleukin 1 receptor associated kinase 4/Interleukin-1 receptor-associated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3778] [GtoPdb: 2045] [UniProtKB: Q9NWZ3]
ChEMBL Inhibition of IRK4 B 5.74 pIC50 1800 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
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 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
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 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116]
ChEMBL Inhibition of ROCK2 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Inhibition of RSK2 B 6.48 pIC50 330 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of AKT1 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of Aurora A B 8.4 pIC50 <=4 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
GtoPdb - - 8.4 pIC50 <4 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-43 [PMID:20855207]
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 7.89 pIC50 <=13 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
GtoPdb - - 7.89 pIC50 <13 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-43 [PMID:20855207]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
GtoPdb - - 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-43 [PMID:20855207]
ChEMBL Inhibition of CHK1 B 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
ChEMBL Inhibition of PLK3 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
ChEMBL Inhibition of TSSK2 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 B 8 pIC50 >10 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
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 6.29 pIC50 510 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]
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 VEGFR2 B 6.15 pIC50 710 nM IC50 Bioorg Med Chem Lett (2010) 20: 6739-6743 [PMID:20855207]

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]