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Assay Detail

CHEMBL770197

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

Functional
Antagonism of sarafotoxin S6c-induced vasoconstriction in rabbit pulmonary artery at both ETA and ETB receptors
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Endothelin receptor, ET-A/ET-B (CHEMBL2096678)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
Kikuchi T, Kubo K, Ohtaki T, Suzuki N, Asami T, Shimamoto N, Wakimasu M, Fujino M.
J Med Chem (1993) 36 : 4087 -4093
PubMed 8258832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373292 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373292 Kd = 3.981 nM 8.40