Cdk4 inhibitor III [Ligand Id: 5952] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL290904 |
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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 A2 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | CDK2/cyclin A complex | - | 6.7 | pIC50 | >200 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 461-4 [PMID:10743948] |
| 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 | 4.7 | pIC50 | >20000 | 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| 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 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | CDK2/cyclin A complex | - | 6.7 | pIC50 | >200 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 461-4 [PMID:10743948] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Inhibition of Cyclin-dependent kinase 4 (CDK4/cyclin Dl) | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 461-464 [PMID:10743948] |
| GtoPdb | CDK4/cyclin D1 complex | - | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 461-4 [PMID:10743948] |
| 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 | 5.02 | pIC50 | 9500 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of CDK4/cyclin D1 (unknown origin) | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | CDK4/cyclin D1 complex | - | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 461-4 [PMID:10743948] |
| 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 | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1] | ||||||||
| GtoPdb | - | - | 6.3 | pIC50 | 500 | nM | IC50 | ACS Chem Biol (2014) 9: 2471-8 [PMID:25137013] |
| ChEMBL | Inhibition of SETD8 (unknown origin) | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr | B | 6.43 | pIC50 | 370 | nM | IC50 | Eur J Med Chem (2022) 237: 114410-114410 [PMID:35525212] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of N-terminal 3xFlag-His6-tagged SARS-CoV-2 papain-like protease nsp3 (1564 to 1878 residues) expressed in baculovirus infected Sf9 insect cells using Pro3 as substrate by fluorescence based assay | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (2022) 65: 7561-7580 [PMID:35620927] |
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]
