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Assay Detail

CHEMBL1063782

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Binding
Inhibitory constant against ROCK1
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.
Jacobs M, Hayakawa K, Swenson L, Bellon S, Fleming M, Taslimi P, Doran J.
J Biol Chem (2006) 281 : 260 -268
PubMed 16249185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.04 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406821 1 8.22
CHEMBL559147 Y-27632 1 6.82
CHEMBL1233300 HYDROXYFASUDIL 1 6.82
CHEMBL38380 FASUDIL 3.0 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406821 Ki = 6.0 nM 8.22
CHEMBL559147 Y-27632 Ki = 150.0 nM 6.82
CHEMBL1233300 HYDROXYFASUDIL Ki = 150.0 nM 6.82
CHEMBL38380 FASUDIL Ki = 530.0 nM 6.28