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Assay Detail

CHEMBL4426326

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

Binding
Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Boss C, Bolli MH, Gatfield J.
Bioorg Med Chem Lett (2016) 26 : 3381 -3394
PubMed 27321813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.85 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24461 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24461 Ki = 1.4 nM 8.85