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Assay Detail

CHEMBL2175262

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

Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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
Ki 15 8.00 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603708 1 9.24
CHEMBL373742 VASOPRESSIN 4.0 1 8.83
CHEMBL119793 1 8.57
CHEMBL2172295 1 8.40
CHEMBL2172289 1 8.24
CHEMBL2172391 1 8.12
CHEMBL2172290 1 8.04
CHEMBL2172392 1 7.90
CHEMBL2172291 1 7.85
CHEMBL2172294 1 7.85
CHEMBL2172393 1 7.78
CHEMBL2172390 1 7.60
CHEMBL2172288 1 7.58
CHEMBL2172293 1 7.26
CHEMBL2172292 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603708 Ki = 0.57 nM 9.24
CHEMBL373742 VASOPRESSIN Ki = 1.48 nM 8.83
CHEMBL119793 Ki = 2.68 nM 8.57
CHEMBL2172295 Ki = 4.0 nM 8.40
CHEMBL2172289 Ki = 5.69 nM 8.24
CHEMBL2172391 Ki = 7.6 nM 8.12
CHEMBL2172290 Ki = 9.02 nM 8.04
CHEMBL2172392 Ki = 12.7 nM 7.90
CHEMBL2172291 Ki = 14.22 nM 7.85
CHEMBL2172294 Ki = 14.05 nM 7.85
CHEMBL2172393 Ki = 16.8 nM 7.78
CHEMBL2172390 Ki = 25.3 nM 7.60
CHEMBL2172288 Ki = 26.1 nM 7.58
CHEMBL2172293 Ki = 54.3 nM 7.26
CHEMBL2172292 Ki = 187.7 nM 6.73