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

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ChEMBL ligand: CHEMBL4439321
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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: O60563P50750]
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]
GtoPdb Inhibition of CDK9/CycT1 in vitro, at low ATP concentration - 7.89 pIC50 13 nM IC50 ChemMedChem (2017) 12: 1776-1793 [PMID:28961375]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]