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Assay Detail

CHEMBL3074522

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

Binding
Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Myocardium
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin-1 receptor (CHEMBL4566)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and biological evaluation of benzofuran derivatives as ET receptor antagonists
Cai J, Chen J, Cao M, Wang P, Feng C, Ji M
Med Chem Res (2013) 22 : 5472 -5480
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.53 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2296899 1 7.64
CHEMBL314691 BQ-123 2.0 1 7.55
CHEMBL2296900 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2296899 IC50 = 23.0 nM 7.64
CHEMBL314691 BQ-123 IC50 = 28.0 nM 7.55
CHEMBL2296900 IC50 = 39.0 nM 7.41