Cdk2 inhibitor IV [Ligand Id: 5949] 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: CHEMBL1802728
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 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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: Q00535, Q15078]
There should be some charts here, you may need to enable JavaScript!
  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
There should be some charts here, you may need to enable JavaScript!
  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
There should be some charts here, you may need to enable JavaScript!
  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948]
GtoPdb CDK7/cyclin H complex used in assay - 5.41 pIC50 3900 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
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 5.64 pIC50 2300 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 5.29 pIC50 5100 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]
GtoPdb CDK1/cyclin B complex used in assay - 5.18 pIC50 6600 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
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 5.24 pIC50 5800 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
GtoPdb CDK2/cyclin A complex used in assay - 6.39 pIC50 410 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
ChEMBL Inhibition of CDK2 (unknown origin) B 6.4 pIC50 400 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb - - 6.4 pIC50 400 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 5.96 pIC50 1100 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK2/cyclin A complex used in assay - 6.39 pIC50 410 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
GtoPdb - - 6.4 pIC50 400 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]
GtoPdb CDK4/cyclin D complex used in assay - 5.26 pIC50 5500 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
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 6.03 pIC50 940 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
GtoPdb CDK5/p25 complex used in assay - 4.82 pIC50 15000 nM IC50 Mol Cancer Ther (2005) 4: 1328-37 [PMID:16170024]
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 5.06 pIC50 8800 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 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]
GtoPdb - - 5.7 pIC50 2000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-14 [PMID:21632247]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
GtoPdb - - 7.17 pIC50 67 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate B 7.17 pIC50 67 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate B 7.46 pIC50 35 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb - - 7.46 pIC50 35 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]

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]