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Assay Detail

CHEMBL5653650

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Functional
Antagonist activity at ETA receptor in rat MMQ cells assessed as inhibition of phosphatidylinositol hydrolysis by myo-[3H]inositol radioactivity based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type MMQ
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin-1 receptor (CHEMBL4566)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 3 9.77 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111277 1 10.30
CHEMBL111612 ABT-546 1 9.23
CHEMBL332794 A-192621 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111277 IC50 = 0.05 nM 10.30
CHEMBL111612 ABT-546 IC50 = 0.59 nM 9.23
CHEMBL332794 A-192621 IC50 >= 700.0 nM -