1-azakenpaullone [Ligand Id: 8018] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL336961 (Azakenpaullone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Inhibition of human cyclin-dependent kinase 1-cyclin B | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
| ChEMBL | Inhibition of CDK1/cyclinB | B | 5.7 | pIC50 | 2000 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| GtoPdb | CDK1/cyclin B complex in assay | - | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
| 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 GST-tagged CDK1/cyclin B (unknown origin) expressed in Escherichia coli | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2017) 142: 244-265 [PMID:28803677] |
| GtoPdb | CDK1/cyclin B complex in assay | - | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
| 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 human Cyclin-dependent kinase 5-p35nck5a | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
| ChEMBL | Inhibition of recombinant CDK5/p25 expressed in Escherichia coli | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2008) 51: 2196-2207 [PMID:18345612] |
| GtoPdb | CDK5/p25 complex in assay | - | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| GtoPdb | - | - | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-6 [PMID:14698171] |
| ChEMBL | Inhibition of human glycogen synthase kinase-3 beta | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 413-416 [PMID:14698171] |
| ChEMBL | Inhibition of GSK3-beta | B | 7.74 | pIC50 | 18 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266] | ||||||||
| ChEMBL | Inhibition of rat GSK3beta expressed in Sf9 cells incubated for 30 mins using GS-1 peptide substrate and [gamma-32P]ATP by scintillation counting method | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2017) 142: 244-265 [PMID:28803677] |
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]
