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Assay Detail

CHEMBL1009212

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of ROCK2 assessed as myosin light chain phosphorylation by cell-based assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Rho-associated protein kinase 2 (CHEMBL2973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
Sessions EH, Yin Y, Bannister TD, Weiser A, Griffin E, Pocas J, Cameron MD, Ruiz C, Lin L, Schürer SC, Schröter T, LoGrasso P, Feng Y.
Bioorg Med Chem Lett (2008) 18 : 6390 -6393
PubMed 18996009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.03 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL455446 1 7.64
CHEMBL455658 1 7.60
CHEMBL517561 1 7.55
CHEMBL461338 1 7.34
CHEMBL454654 1 7.18
CHEMBL455659 1 7.07
CHEMBL454638 1 7.00
CHEMBL454639 1 6.67
CHEMBL462194 1 6.57
CHEMBL509011 1 6.48
CHEMBL508975 1 6.27
CHEMBL452598 1 -
CHEMBL518665 1 -
CHEMBL462193 1 -
CHEMBL518825 1 -
CHEMBL517891 1 -
CHEMBL461339 1 -
CHEMBL454624 1 -
CHEMBL452734 1 -
CHEMBL453635 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL455446 IC50 = 23.0 nM 7.64
CHEMBL455658 IC50 = 25.0 nM 7.60
CHEMBL517561 IC50 = 28.0 nM 7.55
CHEMBL461338 IC50 = 46.0 nM 7.34
CHEMBL454654 IC50 = 66.0 nM 7.18
CHEMBL455659 IC50 = 86.0 nM 7.07
CHEMBL454638 IC50 = 99.0 nM 7.00
CHEMBL454639 IC50 = 212.0 nM 6.67
CHEMBL462194 IC50 = 271.0 nM 6.57
CHEMBL509011 IC50 = 330.0 nM 6.48
CHEMBL508975 IC50 = 533.0 nM 6.27
CHEMBL452598 IC50 < 6.0 nM -
CHEMBL518665 IC50 - -
CHEMBL462193 IC50 - -
CHEMBL518825 IC50 - -
CHEMBL517891 IC50 - -
CHEMBL461339 IC50 - -
CHEMBL454624 IC50 - -
CHEMBL452734 IC50 < 6.0 nM -
CHEMBL453635 IC50 - -