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 A2 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) |
| ChEMBL | Inhibition of CDK2 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| 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] |
| ChEMBL | Inhibition of CDK5 (unknown origin) | B | 7.68 | pIC50 | 21 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| 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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] | ||||||||
| ChEMBL | Inhibition of CDK7 (unknown origin) | B | 6.71 | pIC50 | 193 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
| 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 | Inhibition of CDK9 (unknown origin) | B | 7.59 | pIC50 | 26 | nM | IC50 | RSC Med Chem (2022) 13: 688-710 [PMID:35814933] |
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]
