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Assay Detail

CHEMBL673229

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

Binding
Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from CHO cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Riechers H, Albrecht HP, Amberg W, Baumann E, Bernard H, Böhm HJ, Klinge D, Kling A, Müller S, Raschack M, Unger L, Walker N, Wernet W.
J Med Chem (1996) 39 : 2123 -2128
PubMed 8667356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.24 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302564 1 7.69
CHEMBL305980 1 7.61
CHEMBL25344 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302564 Ki = 20.4 nM 7.69
CHEMBL305980 Ki = 24.5 nM 7.61
CHEMBL25344 Ki = 371.0 nM 6.43