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Assay Detail

CHEMBL5653652

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human ETB receptor transfected in CHO cell membrane assessed as inhibition constant incubated for 3 hrs by 125I-labelled ET-1 saturation binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endothelin receptor type B (CHEMBL1785)
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
Ki 2 8.49 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111277 1 8.91
CHEMBL332794 A-192621 1 8.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111277 Ki = 1.23 nM 8.91
CHEMBL332794 A-192621 Ki = 8.8 nM 8.06