Assay Detail

CHEMBL679707

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Binding

Inhibition of endothelin (ET-A) binding to porcine heart membranes

ChEMBL ↗

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Target

Endothelin-1 receptor (CHEMBL4130) ↗

Open DB target context

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Endothelin-1 receptor (CHEMBL4130) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Endothelin-1 receptor

CHEMBL4130

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
Tissue	Heart
Subcellular	Membrane
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Endothelin-1 receptor (CHEMBL4130) ↗

Type	SINGLE PROTEIN
Organism	Sus scrofa

Publication

A case study of combinatorial libraries: Endothelin receptor antagonist hexapeptides

Neustadt B, Wu A, Smith E, Nechuta T, Fawzi A, Zhang H, Ganguly A
Bioorg Med Chem Lett (1995) 5 : 2041 -2044
· DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.46	8.10

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL262993	—	—	1	8.10
CHEMBL424227	—	—	1	6.82

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL262993	—	IC50	=	8.0	nM	8.10
CHEMBL424227	—	IC50	=	150.0	nM	6.82