EUB0000716a_ROCK2

Chemical structure of compound EUB0000716a
Compound name
BAY-549
Protein family
Protein Kinase
Target name
ROCK2
Affinity biochemical (nM)
1.1
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000716a
SMILES
Cc1c[nH]c2c1c(ccn2)Oc1c(cc(cc1F)Nc1cc(nc(N)n1)[Cl])F
InChIKey
NRSGWEVTVGZDFC-UHFFFAOYSA-N
NCBI gene ID
9475
UniProt ID
O75116
Mode of action
Inhibitor
Negative control
BAY-4900
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme activity assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-549
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 100 nM, closest targets as % of contr.: LATS2 (0.7%), PRKACA (28%), PRKACB (36%), LATS1 (42%), PRKG1 (49%); Screened in Upstate kinase panel against 114 kinases at 10 µM, >250 fold selective, closest targets: IC50(NTRK1) = 252 nM, IC50(FLT3) = 303 nM, IC50(PKA) = 734 nM; Screened against 45 GPCR targets (PDSP screen), closest targets: Ki(OPRK1) = 187.33 nM, Ki(SIGMAR1) = 6765.5 nM; Screened in Eurofins-Panlabs radioligand binding assay against 63 targets at 10 µM, closest targets: Ki(SLC6A3) = 0.039 µM, Ki(DAT2) = 0.027 µM;
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-549
Selectivity Number of Off-targets
1