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Assay Detail

CHEMBL5653643

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Functional
Antagonist activity at ETA receptor (unknown origin) assessed as inhibition of arachidonic acid release by cell based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

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 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9194 ATRASENTAN 3.0 1 9.70
CHEMBL111277 1 -
CHEMBL332794 A-192621 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9194 ATRASENTAN IC50 = 0.2 nM 9.70
CHEMBL111277 IC50 - -
CHEMBL332794 A-192621 IC50 - -