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Assay Detail

CHEMBL2175253

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

Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
4
Total Activities
4
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

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective fluorescent nonpeptidic antagonists for vasopressin V₂ GPCR: application to ligand screening and oligomerization assays.
Loison S, Cottet M, Orcel H, Adihou H, Rahmeh R, Lamarque L, Trinquet E, Kellenberger E, Hibert M, Durroux T, Mouillac B, Bonnet D.
J Med Chem (2012) 55 : 8588 -8602
PubMed 22984902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.51 8.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172289 1 8.86
CHEMBL2172290 1 8.63
CHEMBL2172291 1 8.60
CHEMBL2172288 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172289 Kd = 1.38 nM 8.86
CHEMBL2172290 Kd = 2.33 nM 8.63
CHEMBL2172291 Kd = 2.53 nM 8.60
CHEMBL2172288 Kd = 11.1 nM 7.96