BMS-265246 [Ligand Id: 8051] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL310840
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
There should be some charts here, you may need to enable JavaScript!
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: P20248P24941]
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: P50613P51946P51948]
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: O60563P50750]
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: O95067P06493P14635Q8WWL7]
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: P06493P14635]
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: O96020P24864P24941]
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: P24864P24941]
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: P11802P24385P30279P30281]
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: P11802P24385]
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: Q00535Q15078]
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 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]