Compound name
Atuveciclib
Protein family
Protein Kinase
Target name
CDK9
Affinity biochemical (nM)
13
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001631a
SMILES
COc1cc(F)ccc1-c1ncnc(Nc2cccc(CS(C)(=N)=O)c2)n1
InChIKey
ACWKGTGIJRCOOM-UHFFFAOYSA-N
NCBI gene ID
1025
UniProt ID
P50750
Synonyms
PITALRE, C-2k, TAK
Mode of action
inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (inhibition of CDK9/cyclinT1 phosphorylation using 10 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28961375/
Affinity biochemical relation
=
Selectivity platform
KinaseProfilerTM (Merck Millipore)
Selectivity platform number of targets
230
Selectivity remarks
Screened at 10 µM, closest targets as % of contr.: GSK3B (3%), GSK3A (4%), KIT (6%), CDK3 (cyclinE, 10%), EPHB1 (11%), CAMK2B (13%), CDK2 (cyclinE, 13%), CDK1 (cyclinE, 14%), YES (14%), ARG (16%), CDK5(p35, 20%), EPHA1 (20%), NTRK1(20%), CAMK2G (21%), CAMK2D (22%), LYN(23%), FYN(24%), MLK1(24%), IRAK1(27%), SRC(28%), FGR(29%), FLT4(30%); In-vitro potency of closest targets (Merck Millipore kinase assay using 10 µM ATP): IC50(ARG) = 2843 nM, IC50(CAMK2B) = 1650 nM, IC50(CAMK2G) = 2081 nM, IC50(CAMK2D) = 3340 nM, IC50(SRC) = 5293 nM, IC50(EPHA1) = 1737 nM, IC50(EPHB1) = 2032 nM, IC50(FGR) = 7754 nM, IC50(GSK3A) = 45 nM, IC50(GSK3B) = 87 nM, IC50(IRAK1) = 5454 nM, IC50(LYN) = 3514 nM, IC50(MLK1) = 3010 nM, IC50(YES) = 1495 nM;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/28961375/