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Assay Detail

CHEMBL4426319

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

Binding
Displacement of 125I-ET1 from pig ETB receptor transfected in grivet COS7 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin receptor type B (CHEMBL3949)
Type SINGLE PROTEIN
Organism Sus scrofa

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 3 8.39 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451582 1 9.07
CHEMBL54057 1 8.70
CHEMBL112624 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451582 IC50 = 0.86 nM 9.07
CHEMBL54057 IC50 = 2.0 nM 8.70
CHEMBL112624 IC50 = 41.0 nM 7.39