Compound name
GSK429286A
Protein family
Protein Kinase
Target name
ROCK2
Affinity biochemical (nM)
63
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000134b
SMILES
CC1=C(C(=O)Nc2cc3cn[nH]c3cc2F)C(c2ccc(C(F)(F)F)cc2)CC(=O)N1
InChIKey
OLIIUAHHAZEXEX-UHFFFAOYSA-N
NCBI gene ID
9475
UniProt ID
O75116
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay (100 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm0609014
https://doi.org/10.1042/BJ20091035
Affinity biochemical relation
=
Selectivity platform
KinomeScan
Selectivity platform number of targets
317
Selectivity remarks
Screened at 10 µM, closest targets as % contr.: JAK3(JH1 catalytic domain) (3.2%), PRKACA (4.2%), PRKACB (6.4%); Additionally screened against 85 kinase targets at 1 µM, closest target as % of contr.: RPS6KA2 (20%), PMID: 19740074;
Selectivity Source Knowledge
https://lincs.hms.harvard.edu/db/sm/10012-101/
Selectivity Number of Off-targets
3