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Assay Detail

CHEMBL673235

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

Binding
Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cells
6
Total Activities
6
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

2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Winn M, von Geldern TW, Opgenorth TJ, Jae HS, Tasker AS, Boyd SA, Kester JA, Mantei RA, Bal R, Sorensen BK, Wu-Wong JR, Chiou WJ, Dixon DB, Novosad EI, Hernandez L, Marsh KC.
J Med Chem (1996) 39 : 1039 -1048
PubMed 8676339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.26 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8978 L-754142 1 8.27
CHEMBL8823 SB-209670 1 7.83
CHEMBL8981 PD-156707 1 6.86
CHEMBL8923 1 6.86
CHEMBL428661 1 6.46
CHEMBL267458 BMS-182874 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8978 L-754142 Ki = 5.4 nM 8.27
CHEMBL8823 SB-209670 Ki = 14.7 nM 7.83
CHEMBL8981 PD-156707 Ki = 139.0 nM 6.86
CHEMBL8923 Ki = 139.0 nM 6.86
CHEMBL428661 Ki = 343.0 nM 6.46
CHEMBL267458 BMS-182874 Ki > 50000.0 nM -