Cdk4 inhibitor [Ligand Id: 5950] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL64758
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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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]
GtoPdb CDK2/cyclin E complex - 6.28 pIC50 520 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
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 6.73 pIC50 185 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
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 5.4 pIC50 4000 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]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 1-cyclin B using histone as substrate B 5.68 pIC50 2100 nM IC50 J Med Chem (2003) 46: 2027-2030 [PMID:12747775]
GtoPdb CDK1/cyclin B complex - 5.68 pIC50 2100 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
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/cyclinB (unknown origin) B 5.68 pIC50 2100 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK1/cyclin B complex - 5.68 pIC50 2100 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
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 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941]
GtoPdb CDK2/cyclin E complex - 6.28 pIC50 520 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 2-cyclin E using Rb21 as substrate B 6.28 pIC50 520 nM IC50 J Med Chem (2003) 46: 2027-2030 [PMID:12747775]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
GtoPdb CDK2/cyclin E complex - 6.28 pIC50 520 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
ChEMBL Inhibition of CDK2/cyclinE (unknown origin) B 6.28 pIC50 520 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
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 6.64 pIC50 229 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
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 7.04 pIC50 91 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 4-cyclin D1 using Rb21 as substrate B 7.12 pIC50 76 nM IC50 J Med Chem (2003) 46: 2027-2030 [PMID:12747775]
ChEMBL Inhibition of CDK4/cyclinD1 (unknown origin) B 7.12 pIC50 76 nM IC50 J Med Chem (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK4/cyclin D1 complex - 7.12 pIC50 76 nM IC50 J Med Chem (2003) 46: 2027-30 [PMID:12747775]
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 6.81 pIC50 154 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 5.22 pIC50 6000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]

ChEMBL data shown on this page come from version 32:

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]