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 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]
