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Assay Detail

CHEMBL4431775

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

Binding
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis.
Aubert JD, Juillerat-Jeanneret L.
J Med Chem (2016) 59 : 8168 -8188
PubMed 27266371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 10.47 10.47
IC50 1 10.26 10.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9194 ATRASENTAN 3.0 2 10.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9194 ATRASENTAN Ki = 0.034 nM 10.47
CHEMBL9194 ATRASENTAN IC50 = 0.055 nM 10.26