Assay Detail

CHEMBL790901

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Functional

Inhibition of ET1 induced stimulation of phosphoinositide turnover

ChEMBL ↗

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Target

Rattus norvegicus (CHEMBL376) ↗

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Rattus norvegicus (CHEMBL376) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Rattus norvegicus

CHEMBL376

Anchored from Assay target.

Protein identity Rattus norvegicus

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	Rattus norvegicus
Confidence	1 — Organism
Curated By	Intermediate

Target

Rattus norvegicus (CHEMBL376) ↗

Type	ORGANISM
Organism	Rattus norvegicus

Publication

Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.

Wu C, Chan MF, Stavros F, Raju B, Okun I, Mong S, Keller KM, Brock T, Kogan TP, Dixon RA.
J Med Chem (1997) 40 : 1690 -1697
PubMed 9171878 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.16	9.16

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL282724	SITAXENTAN	4.0	1	9.16

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL282724	SITAXENTAN	Ki	=	0.686	nM	9.16