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ChEMBL ligand: CHEMBL3301610 (Verzenio, Abemaciclib, LY-2835219, Verzenios) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385, Q00534] | ||||||||
ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation counting analysis | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] | ||||||||
ChEMBL | Competitive inhibition of CDK6/cyclin D3 (unknown origin) assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | B | 8.09 | pKi | 8.2 | nM | Ki | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of human CDK6/Cyclin-D3 | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
ChEMBL | Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2018) 144: 1-28 [PMID:29247857] |
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 recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide | B | 5.41 | pKi | 3910 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 5.51 | pIC50 | 3112 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 T (unknown origin) | B | 7.24 | pKi | 57 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | B | 7 | pIC50 | 101 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
ChEMBL | Inhibition of human CDK9/Cyclin-T1 | B | 7.24 | pIC50 | 57 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
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) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 5.82 | pIC50 | 1523 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
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) | B | 5.79 | pKi | 1627 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Inhibition of human CDK1/cyclin B1 (unknown origin) | B | 5.79 | pIC50 | 1627 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
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 | 6.43 | pIC50 | 371 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
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 human CDK2/cyclin E | B | 6.3 | pKi | 504 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
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 | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2017) 142: 424-458 [PMID:28911822] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of CDK4 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
ChEMBL | Inhibition of CDK4 (unknown origin) after 90 mins by ADP-Glo assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
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 recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation counting analysis | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
ChEMBL | Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
ChEMBL | Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur. J. Med. Chem. (2016) 108: 701-719 [PMID:26741853] |
ChEMBL | Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4/G1/S-specific cyclin-E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885554] [GtoPdb: 1976] [UniProtKB: P11802, P24864] | ||||||||
ChEMBL | Inhibition of human CDK4/cyclin D1 using ULight-substrate after 1 hr by LANCE assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2018) 148: 140-153 [PMID:29459274] |
GtoPdb | CDK4/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8.7 | pIC50 | 2 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
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 | 6.39 | pIC50 | 405 | 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] | ||||||||
GtoPdb | CDK6/cyclin D1 complex expressed in and purified from insect cells. Assays used the methanesulfonate salt of the compound. | - | 8 | pIC50 | 10 | nM | IC50 | Invest New Drugs (2014) 32: 825-37 [PMID:24919854] |
ChEMBL | Inhibition of CDK6 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 142: 424-458 [PMID:28911822] |
ChEMBL | Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
ChEMBL | Inhibition of CDK6 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5332-5336 [PMID:29074254] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 4.96 | pIC50 | 10900 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 974-978 [PMID:29429832] |
ChEMBL data shown on this page come from version 27:
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]