Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL679116

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

Binding
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A10
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin-1 receptor (CHEMBL4566)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Morimoto H, Shimadzu H, Kushiyama E, Kawanishi H, Hosaka T, Kawase Y, Yasuda K, Kikkawa K, Yamauchi-Kohno R, Yamada K.
J Med Chem (2001) 44 : 3355 -3368
PubMed 11585441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.75 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175616 BOSENTAN SODIUM 1 8.85
CHEMBL115951 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175616 BOSENTAN SODIUM IC50 = 1.4 nM 8.85
CHEMBL115951 IC50 = 230.0 nM 6.64