Assay Detail

CHEMBL682363

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Binding

Inhibitory activity against human endothelin A receptor

ChEMBL ↗

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Target

Endothelin-1 receptor (CHEMBL252) ↗

Open DB target context

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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
Confidence	9 — Direct single protein target
Curated By	Expert

Target

Endothelin-1 receptor (CHEMBL252) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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
IC50	1	9.31	9.31

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL111612	ABT-546	—	1	9.31

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL111612	ABT-546	IC50	=	0.49	nM	9.31