BS-194 [Ligand Id: 8176] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1234833 |
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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: P24385, Q00534] | ||||||||
| 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: O60563, P50750] | ||||||||
| 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: P06493, P14635] | ||||||||
| 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] |
| ChEMBL | Inhibition of human CDK2 expressed in baculovirus infected Sf9 cells using Histone H1 as substrate incubated for 10 mins by scintillation counting method | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2021) 218: 113389-113389 [PMID:33784602] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| 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: P11802, P24385] | ||||||||
| 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: P50613, P51946] | ||||||||
| 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: O60563, Q00535] | ||||||||
| 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 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]
