BMS-265246 [Ligand Id: 8051] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL310840 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Mol Cancer Ther (2011) 10: 242-54 [PMID:21216932] |
| 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 GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Mol Cancer Ther (2011) 10: 242-54 [PMID:21216932] |
| ChEMBL | Inhibition of Cyclin-dependent kinase 1-cyclin B | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2405-2408 [PMID:12824044] |
| 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 His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Mol Cancer Ther (2011) 10: 242-54 [PMID:21216932] |
| ChEMBL | Inhibition of GST-tagged CDK1/cyclin B1 (unknown origin) expressed in baculovirus expression system using histone H1 as substrate measured after 45 mins in presence of [gamma33P]ATP by liquid scintillation counting method | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
| ChEMBL | Inhibitory activity against Cyclin-dependent kinase 2-cyclin E | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2405-2408 [PMID:12824044] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Mol Cancer Ther (2011) 10: 242-54 [PMID:21216932] |
| 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 GST-tagged CDK2/Cyclin E (unknown origin) expressed in baculovirus expression system using GST-pRb (776 to 928 residues) as substrate measured after 45 mins in presence of [gamma33P]-ATP by liquid scintillation counting method | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Mol Cancer Ther (2011) 10: 242-54 [PMID:21216932] |
| ChEMBL | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095942] [GtoPdb: 1976] [UniProtKB: P11802, P24385, P30279, P30281] | ||||||||
| ChEMBL | Inhibition of CDK4-Cyclin D | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2405-2408 [PMID:12824044] |
| 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 GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 6.65 | pIC50 | 222 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of GST-tagged CDK4/Cyclin D1 (unknown origin) expressed in baculovirus expression system using GST-pRb (776 to 928 residues) as substrate measured after 1 hr in presence of [gamma33P]-ATP by liquid scintillation counting method | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
| 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 GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | B | 6.59 | pIC50 | 258 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
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]
