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Assay Detail

CHEMBL682958

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

Binding
Binding affinity towards ET1 receptor was determined in A10 cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Cell Type A10
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
Ki 1 7.26 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267458 BMS-182874 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267458 BMS-182874 Ki = 55.0 nM 7.26