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Assay Detail

CHEMBL677273

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

Binding
Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS 7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Ming Fai Chan, Raju B, Kois A, Castillo RS, Verner EJ, Chengde Wu, Emily Hwang, Okun I, Stavros F, Balaji V
Bioorg Med Chem Lett (1996) 6 : 2393 -2398
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.07 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76623 1 6.85
CHEMBL311258 1 6.21
CHEMBL80782 1 5.48
CHEMBL267458 BMS-182874 1 4.85
CHEMBL80980 1 4.80
CHEMBL76860 1 4.57
CHEMBL77962 1 4.34
CHEMBL27065 1 4.31
CHEMBL310427 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76623 IC50 = 140.0 nM 6.85
CHEMBL311258 IC50 = 610.0 nM 6.21
CHEMBL80782 IC50 = 3300.0 nM 5.48
CHEMBL267458 BMS-182874 IC50 = 14000.0 nM 4.85
CHEMBL80980 IC50 = 16000.0 nM 4.80
CHEMBL76860 IC50 = 27000.0 nM 4.57
CHEMBL77962 IC50 = 46000.0 nM 4.34
CHEMBL27065 IC50 = 49000.0 nM 4.31
CHEMBL310427 IC50 = 55000.0 nM 4.26