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Assay Detail

CHEMBL676576

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

Functional
Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated)
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 Expert

Target

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

Publication

Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.
Patt WC, Edmunds JJ, Repine JT, Berryman KA, Reisdorph BR, Lee C, Plummer MS, Shahripour A, Haleen SJ, Keiser JA, Flynn MA, Welch KM, Reynolds EE, Rubin R, Tobias B, Hallak H, Doherty AM.
J Med Chem (1997) 40 : 1063 -1074
PubMed 9089328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8981 PD-156707 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8981 PD-156707 Kd = 25.12 nM 7.60