Assay Detail

CHEMBL5653638

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Functional

Antagonist activity at ETA receptor (unknown origin)

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	Functional
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Endothelin-1 receptor (CHEMBL252) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies.

Wu-Wong JR, Dixon DB, Chiou WJ, Sorensen BK, Liu G, Jae HS, Tasker A, von Geldern TW, Winn M, Opgenorth TJ.
Clin Sci (Lond) (2002) 103 Suppl 48 : 107 -111
PubMed 12193066 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	10.26	10.26

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL9194	ATRASENTAN	3.0	1	10.26

Activity Data

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