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Assay Detail

CHEMBL5373404

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

Binding
Agonist activity at RLucII/GFP10-tagged beta-arrestin-1 (unknown origin) recruitment expressed in HEK293 cells co-expressing human UT assessed as beta-arrestin recruitment by BRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-arrestin-1 (CHEMBL1795088)
Type SINGLE PROTEIN
Organism Homo sapiens

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 11 6.86 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5417669 1 9.31
CHEMBL5414487 1 8.03
CHEMBL593662 UROTENSIN-II 1 7.69
CHEMBL5421473 1 7.02
CHEMBL5401911 1 6.93
CHEMBL5421352 1 6.76
CHEMBL5422077 1 6.07
CHEMBL5416714 1 6.03
CHEMBL5396036 1 5.92
CHEMBL5423896 1 5.91
CHEMBL5406651 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5417669 EC50 = 0.4898 nM 9.31
CHEMBL5414487 EC50 = 9.333 nM 8.03
CHEMBL593662 UROTENSIN-II EC50 = 20.42 nM 7.69
CHEMBL5421473 EC50 = 95.5 nM 7.02
CHEMBL5401911 EC50 = 117.49 nM 6.93
CHEMBL5421352 EC50 = 173.78 nM 6.76
CHEMBL5422077 EC50 = 851.14 nM 6.07
CHEMBL5416714 EC50 = 933.25 nM 6.03
CHEMBL5396036 EC50 = 1202.26 nM 5.92
CHEMBL5423896 EC50 = 1230.27 nM 5.91
CHEMBL5406651 EC50 = 1778.28 nM 5.75