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Assay Detail

CHEMBL678229

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

Binding
Inhibitory concentration against 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

Selective optimization of side activities: another way for drug discovery.
Wermuth CG.
J Med Chem (2004) 47 : 1303 -1314
PubMed 14998318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.70 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267458 BMS-182874 1 6.82
CHEMBL453 SULFISOXAZOLE 4.0 1 6.11
CHEMBL437 SULFATHIAZOLE 4.0 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267458 BMS-182874 IC50 = 150.0 nM 6.82
CHEMBL453 SULFISOXAZOLE IC50 = 780.0 nM 6.11
CHEMBL437 SULFATHIAZOLE IC50 = 69000.0 nM 4.16