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Assay Detail

CHEMBL5150292

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

Binding
Inhibition of ROCK1 (unknown origin)
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 1 (CHEMBL3231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.
Xie Z, Yang X, Duan Y, Han J, Liao C.
J Med Chem (2021) 64 : 1283 -1345
PubMed 33481605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.08 9.00
IC50 3 7.56 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4594250 NETARSUDIL 4.0 1 9.00
CHEMBL3545065 VEROSUDIL 2.0 1 8.70
CHEMBL5182402 1 8.30
CHEMBL4438748 1 7.82
CHEMBL571948 Y-39983 1.0 1 7.55
CHEMBL3426621 RIPASUDIL 3.0 1 7.29
CHEMBL559147 Y-27632 1 6.85
CHEMBL2005186 BELUMOSUDIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4594250 NETARSUDIL Ki = 1.0 nM 9.00
CHEMBL3545065 VEROSUDIL Ki = 2.0 nM 8.70
CHEMBL5182402 Ki = 5.0 nM 8.30
CHEMBL4438748 IC50 = 15.0 nM 7.82
CHEMBL571948 Y-39983 Ki = 28.0 nM 7.55
CHEMBL3426621 RIPASUDIL IC50 = 51.0 nM 7.29
CHEMBL559147 Y-27632 Ki = 140.0 nM 6.85
CHEMBL2005186 BELUMOSUDIL IC50 > 10000.0 nM -