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Assay Detail

CHEMBL1031376

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Binding
Inhibition of ROCK2
7
Total Activities
7
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

Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
Feng Y, Yin Y, Weiser A, Griffin E, Cameron MD, Lin L, Ruiz C, Schürer SC, Inoue T, Rao PV, Schröter T, Lograsso P.
J Med Chem (2008) 51 : 6642 -6645
PubMed 18834107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.63 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485214 1 8.82
CHEMBL521179 SR-3677 1 8.49
CHEMBL485215 1 8.48
CHEMBL510515 1 8.14
CHEMBL485213 1 7.34
CHEMBL485568 1 6.12
CHEMBL485567 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485214 IC50 = 1.5 nM 8.82
CHEMBL521179 SR-3677 IC50 = 3.2 nM 8.49
CHEMBL485215 IC50 = 3.3 nM 8.48
CHEMBL510515 IC50 = 7.2 nM 8.14
CHEMBL485213 IC50 = 46.0 nM 7.34
CHEMBL485568 IC50 = 760.0 nM 6.12
CHEMBL485567 IC50 = 920.0 nM 6.04