Compound name
CCT251545
Protein family
Protein Kinase
Target name
CDK8
Affinity biochemical (nM)
7.2
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001300a
SMILES
Cn1cc(-c2ccc(-c3cncc(Cl)c3N3CCC4(CCNC4=O)CC3)cc2)cn1
InChIKey
LBFYQISQYCGDDW-UHFFFAOYSA-N
NCBI gene ID
1024
UniProt ID
P49336
Synonyms
K35
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Reporter displacement assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26796641/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Millipore)
Selectivity platform number of targets
291
Selectivity remarks
Screened at 1 µM, closest targets as % of control: GSK3A (>80%), GSK3B (>80%), LCK (>80%), PKG1B (>80%), full screening data available as supporting information, In-vitro potency (enzymatic assay): IC50(TNKS1) >10 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(GSK3A) = 0.462 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(GSK3B) = 0.690 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(LCK) >10 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(PKG1B) >10 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
Screened at 10 µM against a panel of 55 receptors, ion channels, and enzymes (CEREP panel), closest targets as % of control: KOP (72%), 5HT Transporter (70%), full screening data available as supporting information, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(GSK3A) = 0.462 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(GSK3B) = 0.690 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(LCK) >10 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
In-vitro potency (enzymatic assay, Millipore): IC50(PKG1B) >10 µM, https://pubs.acs.org/doi/10.1021/jm501436m;
Screened at 10 µM against a panel of 55 receptors, ion channels, and enzymes (CEREP panel), closest targets as % of control: KOP (72%), 5HT Transporter (70%), full screening data available as supporting information, https://pubs.acs.org/doi/10.1021/jm501436m;
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/jm501436m
Selectivity Number of Off-targets
2