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Assay Detail

CHEMBL5228481

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

Binding
Inhibition of ROCK1 (unknown origin)
7
Total Activities
7
Compounds Tested
1
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

Emerging targets in drug discovery against neurodegenerative diseases: Control of synapsis disfunction by the RhoA/ROCK pathway.
Martín-Cámara O, Cores Á, López-Alvarado P, Menéndez JC.
Eur J Med Chem (2021) 225 : 113742 -113742
PubMed 34388381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.86 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1971943 BAY-549 1 9.22
CHEMBL5287991 1 8.91
CHEMBL220241 GSK-269962A 1 8.80
CHEMBL571948 Y-39983 1.0 1 8.44
CHEMBL5266198 1 7.72
CHEMBL1233300 HYDROXYFASUDIL 1 6.14
CHEMBL5278924 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1971943 BAY-549 IC50 = 0.6 nM 9.22
CHEMBL5287991 IC50 = 1.22 nM 8.91
CHEMBL220241 GSK-269962A IC50 = 1.6 nM 8.80
CHEMBL571948 Y-39983 IC50 = 3.6 nM 8.44
CHEMBL5266198 IC50 = 19.0 nM 7.72
CHEMBL1233300 HYDROXYFASUDIL IC50 = 720.0 nM 6.14
CHEMBL5278924 IC50 = 1590.0 nM 5.80