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Assay Detail

CHEMBL4201296

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

Binding
Displacement of [Na125I]-synthetic URP from human UT receptor expressed in HEK293 cell membranes incubated for 2 hrs by gamma-counting
9
Total Activities
9
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

Urotensin-2 receptor (CHEMBL3764)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of New Allosteric Modulators of the Urotensinergic System through Substitution of the Urotensin II-Related Peptide (URP) Phenylalanine Residue.
Billard E, Hébert TE, Chatenet D.
J Med Chem (2018) 61 : 8707 -8716
PubMed 30183282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.04 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205274 1 8.40
CHEMBL4208184 1 8.27
CHEMBL4217514 1 8.25
CHEMBL3104471 1 7.71
CHEMBL4213101 1 7.57
CHEMBL4213538 1 -
CHEMBL4216988 1 -
CHEMBL4209654 1 -
CHEMBL4204786 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205274 IC50 = 3.981 nM 8.40
CHEMBL4208184 IC50 = 5.37 nM 8.27
CHEMBL4217514 IC50 = 5.623 nM 8.25
CHEMBL3104471 IC50 = 19.5 nM 7.71
CHEMBL4213101 IC50 = 26.92 nM 7.57
CHEMBL4213538 IC50 > 1000.0 nM -
CHEMBL4216988 IC50 > 1000.0 nM -
CHEMBL4209654 IC50 > 1000.0 nM -
CHEMBL4204786 IC50 > 1000.0 nM -