Assay Detail

CHEMBL4426325

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Binding

Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1

ChEMBL ↗

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Target

Endothelin-1 receptor (CHEMBL252) ↗

Open DB target context

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Endothelin-1 receptor (CHEMBL252) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Endothelin-1 receptor

CHEMBL252

Anchored from Assay target.

Protein identity Endothelin-1 receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

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	8.47	8.47

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2103873	MACITENTAN	4.0	1	8.47

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2103873	MACITENTAN	IC50	=	3.4	nM	8.47