Compound name
GSK270822A
Protein family
Protein Kinase
Target name
ROCK1
Affinity biochemical (nM)
9
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001238a
SMILES
CC1=C(C(=O)Nc2ccc3[nH]ncc3c2)C(c2ccc3ccccc3c2)CC(=O)N1
InChIKey
ODLNBFNBEPOFNC-UHFFFAOYSA-N
NCBI gene ID
6093
UniProt ID
Q13464
Synonyms
p160ROCK
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation Proximity Assay (SPA)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/jm0609014
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Nanosyn)
Selectivity platform number of targets
232
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: ROCK1 (90.09%), ROCK2 (84.2%), PRKC (75.32%), AURKA (70.59%), RON (67.51%), RET (65.79%), full screening data available at Chembl, screened also at 100 nM, https://pubmed.ncbi.nlm.nih.gov/26501955/;
In-vitro potency (Scintillation Proximity Assay, SPA): IC50(RSK1) = 1100 nM, https://pubs.acs.org/doi/10.1021/jm0609014;
In-vitro potency (Scintillation Proximity Assay, SPA): IC50(RPS6KB1) = 1550 nM, https://pubs.acs.org/doi/10.1021/jm0609014;
In-vitro potency (Scintillation Proximity Assay, SPA): IC50(RSK1) = 1100 nM, https://pubs.acs.org/doi/10.1021/jm0609014;
In-vitro potency (Scintillation Proximity Assay, SPA): IC50(RPS6KB1) = 1550 nM, https://pubs.acs.org/doi/10.1021/jm0609014;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26501955/
Selectivity Number of Off-targets
0