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Assay Detail

CHEMBL5373418

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

Binding
Antagonist activity at URP-activated RLucII-tagged Galpha-i (unknown origin) expressed in HEK293 cells co-expressing human UT/GFP10-tagged G-gamma by BRET assay (Rvb = 7.10 +/- 0.19 No_unit)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Urotensin II Receptor Modulation with 1,3,4-Benzotriazepin-2-one Tetrapeptide Mimics.
Wei X, Diarra S, Douchez A, Cunico Dallagnol JC, Hébert TE, Chatenet D, Lubell WD.
J Med Chem (2023) 66 : 14241 -14262
PubMed 37800680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.86 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421473 1 6.99
CHEMBL5414487 1 6.83
CHEMBL5416714 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421473 EC50 = 102.33 nM 6.99
CHEMBL5414487 EC50 = 147.91 nM 6.83
CHEMBL5416714 EC50 = 177.83 nM 6.75