fadraciclib [Ligand Id: 10461] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3655762
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4/G1/S-specific cyclin-E1 in Human [ChEMBL: CHEMBL3885554] [GtoPdb: 1976] [UniProtKB: P11802P24864]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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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: P20248P24941]
GtoPdb Inhibition of CDK2/cyclin A - 7.05 pIC50 90 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
GtoPdb Inhibition of CDK2/cyclin E - 7.7 pIC50 20 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
ChEMBL Inhibition of CDK2/cyclin A (unknown origin) B 8.3 pIC50 5 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
GtoPdb Inhibition of CDK9/cyclin T1 - 7 pIC50 100 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
ChEMBL Inhibition of CDK9/cyclin T (unknown origin) B 7.59 pIC50 26 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Competitive reversible inhibition of CDK9/CyclinT (unknown origin) B 7.59 pIC50 26 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
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 CDK1/cyclin B (unknown origin) B 6.24 pIC50 578 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Kinase Assay: To evaluate the in-vitro kinase potency of the compounds, they were screened against CDK 2 and CDK9. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins generated at Cyclacel. Ltd Dundee, UK. B 7.05 pIC50 90 nM IC50 US-8592581-B2. Trisubstituted purine derivatives (2013)
GtoPdb Inhibition of CDK2/cyclin A - 7.05 pIC50 90 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
ChEMBL Kinase Assay: To evaluate the in-vitro kinase potency of the compounds, they were screened against CDK 2 and CDK9. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins generated at Cyclacel. Ltd Dundee, UK. B 7.7 pIC50 20 nM IC50 US-8592581-B2. Trisubstituted purine derivatives (2013)
GtoPdb Inhibition of CDK2/cyclin E - 7.7 pIC50 20 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
GtoPdb Inhibition of CDK2/cyclin A - 7.05 pIC50 90 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
GtoPdb Inhibition of CDK2/cyclin E - 7.7 pIC50 20 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
ChEMBL Competitive reversible inhibition of CDK2/cyclin E (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/G1/S-specific cyclin-E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885554] [GtoPdb: 1976] [UniProtKB: P11802P24864]
ChEMBL Inhibition of CDK4/cyclin E (unknown origin) B 6.63 pIC50 232 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Competitive reversible inhibition of CDK5 (unknown origin) B 7.64 pIC50 23 nM IC50 Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
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 CDK5/p25 (unknown origin) B 7.68 pIC50 21 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613P51946]
ChEMBL Inhibition of CDK7/cyclin H (unknown origin) B 6.71 pIC50 193 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
GtoPdb Inhibition of CDK9/cyclin T1 - 7 pIC50 100 nM IC50 WO2008122767A2. 2, 6, 9-substituted purine derivatives having anti proliferative properties (2008)
ChEMBL Kinase Assay: To evaluate the in-vitro kinase potency of the compounds, they were screened against CDK 2 and CDK9. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins generated at Cyclacel. Ltd Dundee, UK. B 7 pIC50 100 nM IC50 US-8592581-B2. Trisubstituted purine derivatives (2013)

ChEMBL data shown on this page come from version 31:

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]