Compound name
CGP60474
Protein family
Protein Kinase
Target name
CDK9
Affinity biochemical (nM)
13
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001067a
SMILES
C1=CC(=CC(=C1)Cl)NC2=NC=CC(=N2)C3=CC(=NC=C3)NCCCO
InChIKey
IYNDTACKOAXKBJ-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
Radiometric kinase assay (conc. ATP = Km)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00049
Affinity biochemical relation
=
Selectivity platform
Ambit KINOMEscan
Selectivity platform number of targets
402
Selectivity remarks
Screened at 10 µM (KINOMEscan, DiscoverX), off-target with >90% PoC; IC50(CDK4/7) = 220/200 nM (Radiometric kinase assay,https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00049);
In-vitro potency (radiometric kinase assay, using ATP = Km): IC50(CDK1/cyclinB) = 26 nM, IC50(CDK2/cyclinE) = 3 nM, IC50(CDK2/cyclinA) = 4 nM, IC50(CDK4/cyclinD) = 216 nM, IC50(CDK5/p25) = 10 nM, IC50(CDK7/cyclinH) = 200 nM, IC50(CDK9/cyclinT)= 13 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00049;
In-vitro potency (radiometric kinase assay, using ATP = Km): IC50(CDK1/cyclinB) = 26 nM, IC50(CDK2/cyclinE) = 3 nM, IC50(CDK2/cyclinA) = 4 nM, IC50(CDK4/cyclinD) = 216 nM, IC50(CDK5/p25) = 10 nM, IC50(CDK7/cyclinH) = 200 nM, IC50(CDK9/cyclinT)= 13 nM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00049;
Selectivity Source Knowledge
https://lincs.hms.harvard.edu/db/datasets/20054/results
Selectivity Number of Off-targets
12