Compound name
CCT244747
Protein family
Protein Kinase
Target name
CHEK1
Affinity biochemical (nM)
7.7
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001217a
SMILES
COc1cc(Nc2cnc(C#N)c(O[C@H](C)CN(C)C)n2)ncc1-c1cnn(C)c1
InChIKey
IENLGMOXAQMNEH-CYBMUJFWSA-N
NCBI gene ID
1111
UniProt ID
O14757
Synonyms
CHK1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Caliper microfluidic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23082860/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (radiometric assays, conc. ATP = Km, Dundee)
Selectivity platform number of targets
140
Selectivity remarks
Screened at 1 µM, closest targets >80% of inhibition: CHEK1 (17%), RSK1 (4%), RSK2 (9%), AMPK (5%), BRSK1 (11%), IRAK1 (17%), NTRK1 (13%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/23082860/;
Screened at 10 µM, against 121 kinases, closest targets as % of control: MAPK15 (11%), RSK1 (14%), STK33 (16%), AMPK (14%), BRSK2 (14%), NUAK1 (7%), PIM3 (17%), IRAK1 (9%), CHEK1 (6%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/23082860/;
Screened at 10 µM, against 121 kinases, closest targets as % of control: MAPK15 (11%), RSK1 (14%), STK33 (16%), AMPK (14%), BRSK2 (14%), NUAK1 (7%), PIM3 (17%), IRAK1 (9%), CHEK1 (6%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/23082860/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/23082860/
Selectivity Number of Off-targets
3