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ChEMBL ligand: CHEMBL4439321 (Atuveciclib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
GtoPdb | Inhibition of CDK9/CycT1 in vitro, at physiological (high) ATP concentration | - | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2021) 64: 11651-11674 [PMID:34264057] |
ChEMBL | Competitive reversible inhibition of recombinant full-length His-tagged human CDK9/cyclin T expressed in baculovirus infected insect cells using biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed b substrate addition measured after 25 mins in presence of high ATP by TR-FRET analysis | B | 6.42 | pIC50 | 380 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
ChEMBL | Competitive reversible inhibition of recombinant full-length His-tagged human CDK9/cyclin T expressed in baculovirus infected insect cells using biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed b substrate addition measured after 25 mins in presence of low ATP by TR-FRET analysis | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350] |
ChEMBL | Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed in baculovirus expression system using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 mins by TR-FRET assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
GtoPdb | Inhibition of CDK9/CycT1 in vitro, at low ATP concentration | - | 7.89 | pIC50 | 13 | nM | IC50 | ChemMedChem (2017) 12: 1776-1793 [PMID:28961375] |
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 recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 mins by TR-FRET assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
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]