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Assay Detail

CHEMBL873602

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

Binding
Inhibitory concentration towards Endothelin A receptor in human
1
Total Activities
1
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

Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
Wu C, Decker ER, Blok N, Bui H, You TJ, Wang J, Bourgoyne AR, Knowles V, Berens KL, Holland GW, Brock TA, Dixon RA.
J Med Chem (2004) 47 : 1969 -1986
PubMed 15055997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.85 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282724 SITAXENTAN 4.0 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282724 SITAXENTAN IC50 = 1.4 nM 8.85