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Assay Detail

CHEMBL682961

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

Functional
Antagonism of ET1 induced increase in intracellular Ca+2 in rabbit carotid artery rings
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Artery
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
Stein PD, Hunt JT, Floyd DM, Moreland S, Dickinson KE, Mitchell C, Liu EC, Webb ML, Murugesan N, Dickey J.
J Med Chem (1994) 37 : 329 -331
PubMed 8308857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.11 5.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30228 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30228 IC50 = 7800.0 nM 5.11