fadraciclib [Ligand Id: 10461] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3655762 |
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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 | 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: O60563, 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 | 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: P06493, P14635] | ||||||||
| 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: P24864, P24941] | ||||||||
| 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: P11802, P24864] | ||||||||
| 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: Q00535, Q15078] | ||||||||
| 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: P50613, P51946] | ||||||||
| 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 33:
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]
