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Assay Detail

CHEMBL676578

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

Functional
Compound was evaluated for in vitro functional inhibitory potency for prevention of ET-1 induced constriction of rat aortic rings (ETA receptors)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
Neidhart W, Breu V, Burri K, Clozel M, Hirth G, Klinkhammer U, Giller T, Ramuz H
Bioorg Med Chem Lett (1997) 7 : 2223 -2228
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.30 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72037 1 9.30
CHEMBL957 BOSENTAN 4.0 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72037 Kd = 0.5012 nM 9.30
CHEMBL957 BOSENTAN Kd = 50.12 nM 7.30