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Assay Detail

CHEMBL4426320

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

Binding
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
2
Total Activities
2
Compounds Tested
1
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 receptor type B (CHEMBL1785)
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 2 6.59 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1628620 1 7.16
CHEMBL2103873 MACITENTAN 4.0 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1628620 IC50 = 69.0 nM 7.16
CHEMBL2103873 MACITENTAN IC50 = 987.0 nM 6.01