atuveciclib [Ligand Id: 11687] activity data from GtoPdb and ChEMBL

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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
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]