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Assay Detail

CHEMBL4426312

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

Binding
Displacement of 125I-ET1 from human smooth muscle ETA receptor expressed in fall armyworm sf9 cell membranes
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 1 6.66 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115951 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115951 IC50 = 220.0 nM 6.66