BS-194 [Ligand Id: 8176] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1234833
  • calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
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  • casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • cyclin dependent kinase 8/Cell division protein kinase 8 in Human [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
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  • cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
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  • cyclin dependent kinase 5/Cyclin-T1/Cyclin-dependent-like kinase 5 in Human [ChEMBL: CHEMBL3885549] [GtoPdb: 1977] [UniProtKB: O60563Q00535]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
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  • Insulin receptor-related receptor/Insulin receptor-related protein in Human [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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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 15/Mitogen-activated protein kinase 15 in Human [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
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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 kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
ChEMBL Inhibition of CAMKKbeta B 5.61 pIC50 2450 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CK1 B 5.98 pIC50 1040 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385Q00534]
ChEMBL Inhibition of CDK6/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay B 4.45 pIC50 35500 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of CDK9/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay B 7.05 pIC50 90 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
GtoPdb - - 7.05 pIC50 90 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
cyclin dependent kinase 8/Cell division protein kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336]
ChEMBL Competitive reversible inhibition of CDK8 (unknown origin) B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
GtoPdb - - 7.48 pIC50 33 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Inhibition of CDK1/cyclinB1 assessed as amount of ATP released by luciferase activity based PKLight assay B 7.48 pIC50 33 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
GtoPdb - - 8.52 pIC50 3 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Competitive reversible inhibition of CDK2 (unknown origin) B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
GtoPdb - - 8.52 pIC50 3 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Inhibition of CDK2/cyclinE assessed as amount of ATP released by luciferase activity based PKLight assay B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Competitive reversible inhibition of CDK4 (unknown origin) B 4.7 pIC50 20000 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
GtoPdb - - 7.52 pIC50 30 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Competitive reversible inhibition of CDK5 (unknown origin) B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
ChEMBL Competitive reversible inhibition of CDK6 (unknown origin) B 4.45 pIC50 35500 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
GtoPdb - - 6.6 pIC50 250 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Competitive reversible inhibition of CDK7 (unknown origin) B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613P51946]
GtoPdb - - 6.6 pIC50 250 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assay B 6.6 pIC50 250 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
cyclin dependent kinase 5/Cyclin-T1/Cyclin-dependent-like kinase 5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885549] [GtoPdb: 1977] [UniProtKB: O60563Q00535]
GtoPdb - - 7.52 pIC50 30 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Inhibition of CDK5/cyclinT assessed as amount of ATP released by luciferase activity based PKLight assay B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Inhibition of DYRK1A B 5.68 pIC50 2100 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
Insulin receptor-related receptor/Insulin receptor-related protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616]
ChEMBL Inhibition of IRR B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL Inhibition of ERK1 B 5.43 pIC50 3730 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
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 5.51 pIC50 3110 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
GtoPdb - - 6.48 pIC50 330 nM IC50 J Med Chem (2010) 53: 8508-22 [PMID:21080703]
ChEMBL Inhibition of ERK8 B 6.48 pIC50 330 nM IC50 J. Med. Chem. (2010) 53: 8508-8522 [PMID:21080703]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]