BS-181 [Ligand Id: 9405] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1801932 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948] | ||||||||
| ChEMBL | Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 6.87 | pIC50 | 134 | nM | IC50 | Eur J Med Chem (2016) 108: 701-719 [PMID:26741853] |
| GtoPdb | Evaluated using purified recombinant CDK7/CycH/MAT1 complex and measuring free ATP remaining in the reaction using a luciferase assay. | - | 7.68 | pIC50 | 21 | nM | IC50 | Cancer Res (2009) 69: 6208-15 [PMID:19638587] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 5.75 | pIC50 | 1790 | nM | IC50 | Eur J Med Chem (2016) 108: 701-719 [PMID:26741853] |
| 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 | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 5.09 | pIC50 | 8100 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2016) 108: 701-719 [PMID:26741853] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Competitive reversible inhibition of CDK2 (unknown origin) | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK2 (unknown origin) | B | 6.06 | pIC50 | 880 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| GtoPdb | Evaluated using purified recombinant CDK2/cycE complex and measuring free ATP remaining in the reaction using a luciferase assay. | - | 6.06 | pIC50 | 880 | nM | IC50 | Cancer Res (2009) 69: 6208-15 [PMID:19638587] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP | B | 5.74 | pIC50 | 1800 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| GtoPdb | Evaluated using purified recombinant CDK2/cycE complex and measuring free ATP remaining in the reaction using a luciferase assay. | - | 6.06 | pIC50 | 880 | nM | IC50 | Cancer Res (2009) 69: 6208-15 [PMID:19638587] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Inhibition of CDK4 (unknown origin) | B | 4.35 | pIC50 | 44700 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| ChEMBL | Competitive reversible inhibition of CDK4 (unknown origin) | B | 4.48 | pIC50 | 33000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK4 (unknown origin) | B | 4.48 | pIC50 | 33000 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| 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/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP | B | 4.35 | pIC50 | 44700 | nM | IC50 | Eur J Med Chem (2016) 108: 701-719 [PMID:26741853] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP | B | 5.43 | pIC50 | 3700 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| ChEMBL | Competitive reversible inhibition of CDK5 (unknown origin) | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK5 (unknown origin) | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP | B | 5.43 | pIC50 | 3700 | nM | IC50 | Eur J Med Chem (2016) 108: 701-719 [PMID:26741853] |
| 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 | 4.33 | pIC50 | 47000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK6 (unknown origin) | B | 4.33 | pIC50 | 47000 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Inhibition of CDK7 (unknown origin) | B | 6.87 | pIC50 | 134 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
| ChEMBL | Competitive reversible inhibition of CDK7 (unknown origin) | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
| ChEMBL | Inhibition of CDK7 (unknown origin) | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| GtoPdb | Evaluated using purified recombinant CDK7/CycH/MAT1 complex and measuring free ATP remaining in the reaction using a luciferase assay. | - | 7.68 | pIC50 | 21 | nM | IC50 | Cancer Res (2009) 69: 6208-15 [PMID:19638587] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613, P51946] | ||||||||
| ChEMBL | Inhibition of CDK7/cyclinH/MAT1 assessed as amount of ATP released by luciferase activity based PKLight assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2010) 53: 8508-8522 [PMID:21080703] |
| GtoPdb | Evaluated using purified recombinant CDK7/CycH/MAT1 complex and measuring free ATP remaining in the reaction using a luciferase assay. | - | 7.68 | pIC50 | 21 | nM | IC50 | Cancer Res (2009) 69: 6208-15 [PMID:19638587] |
| cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2020) 63: 7458-7474 [PMID:32150405] |
| ChEMBL | Inhibition of CDK9 (unknown origin) | B | 5.66 | pIC50 | 2180 | nM | IC50 | Eur J Med Chem (2016) 110: 291-301 [PMID:26851505] |
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]
