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Assay Detail

CHEMBL5616069

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

Binding
Inhibition of ROCK1 (unknown origin) incubated for 10 mins in presence of ATP by mobility shift assay
10
Total Activities
10
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

Development of Nitric Oxide-Donating Netarsudil Derivatives as a Synergistic Therapy for Glaucoma with Reduced Ocular Irritation.
Li C, Zhu M, Liu S, Zhang J, Ye H, Zhang C, Ji D, Tang H, Zhang Y, Wu J, Huang Z.
J Med Chem (2024) 67 : 16311 -16327
PubMed 39163586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.05 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5619410 1 8.90
CHEMBL5618424 1 8.83
CHEMBL5618715 1 8.60
CHEMBL5619145 1 8.31
CHEMBL4594250 NETARSUDIL 4.0 1 7.88
CHEMBL3426621 RIPASUDIL 3.0 1 7.76
CHEMBL5619199 1 7.65
CHEMBL5619370 1 7.54
CHEMBL5619614 1 7.54
CHEMBL5619023 1 7.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5619410 IC50 = 1.26 nM 8.90
CHEMBL5618424 IC50 = 1.48 nM 8.83
CHEMBL5618715 IC50 = 2.54 nM 8.60
CHEMBL5619145 IC50 = 4.94 nM 8.31
CHEMBL4594250 NETARSUDIL IC50 = 13.18 nM 7.88
CHEMBL3426621 RIPASUDIL IC50 = 17.4 nM 7.76
CHEMBL5619199 IC50 = 22.47 nM 7.65
CHEMBL5619370 IC50 = 28.98 nM 7.54
CHEMBL5619614 IC50 = 28.61 nM 7.54
CHEMBL5619023 IC50 = 35.41 nM 7.45