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Assay Detail

CHEMBL677269

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

Binding
Ability to inhibit specific binding of [125I]- -ET-1 to human GH cells which express endothelin B receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.24 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175616 BOSENTAN SODIUM 1 6.51
CHEMBL115951 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175616 BOSENTAN SODIUM IC50 = 310.0 nM 6.51
CHEMBL115951 IC50 = 1100.0 nM 5.96