Assay Detail

CHEMBL677093

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Binding

binding affinity against human Endothelin A receptor

ChEMBL ↗

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Target

Endothelin-1 receptor (CHEMBL4566) ↗

Open DB target context

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Endothelin-1 receptor (CHEMBL4566) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Endothelin-1 receptor

CHEMBL4566

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
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Endothelin-1 receptor (CHEMBL4566) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.

Jae HS, Winn M, von Geldern TW, Sorensen BK, Chiou WJ, Nguyen B, Marsh KC, Opgenorth TJ.
J Med Chem (2001) 44 : 3978 -3984
PubMed 11689084 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	10.33	10.33

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL9194	ATRASENTAN	3.0	1	10.33

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL9194	ATRASENTAN	Ki	=	0.047	nM	10.33