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Assay Detail

CHEMBL3240142

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

Binding
Inhibition of truncated ROCK-2 (unknown origin) after 60 mins by IMAP assay
8
Total Activities
8
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 2 (CHEMBL2973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.
Chen HH, Namil A, Severns B, Ward J, Kelly C, Drace C, McLaughlin MA, Yacoub S, Li B, Patil R, Sharif N, Hellberg MR, Rusinko A, Pang IH, Combrink KD.
Bioorg Med Chem Lett (2014) 24 : 1875 -1879
PubMed 24684843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.29 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3238167 1 7.62
CHEMBL3238168 1 7.44
CHEMBL599163 1 7.41
CHEMBL571948 Y-39983 1.0 1 7.24
CHEMBL3238166 1 7.19
CHEMBL3238164 1 7.17
CHEMBL3238163 1 7.12
CHEMBL3238165 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3238167 IC50 = 24.0 nM 7.62
CHEMBL3238168 IC50 = 36.0 nM 7.44
CHEMBL599163 IC50 = 39.0 nM 7.41
CHEMBL571948 Y-39983 IC50 = 58.0 nM 7.24
CHEMBL3238166 IC50 = 65.0 nM 7.19
CHEMBL3238164 IC50 = 68.0 nM 7.17
CHEMBL3238163 IC50 = 76.0 nM 7.12
CHEMBL3238165 IC50 = 75.0 nM 7.12