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Assay Detail

CHEMBL682971

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

Binding
Inhibitory effect against Human Endothelin A receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.
Fukami T, Nagase T, Fujita K, Hayama T, Niiyama K, Mase T, Nakajima S, Fukuroda T, Saeki T, Nishikibe M.
J Med Chem (1995) 38 : 4309 -4324
PubMed 7473559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.28 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336033 1 8.08
CHEMBL342615 1 7.52
CHEMBL343379 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336033 IC50 = 8.3 nM 8.08
CHEMBL342615 IC50 = 30.0 nM 7.52
CHEMBL343379 IC50 = 590.0 nM 6.23