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Assay Detail

CHEMBL5042989

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

Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321N1
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Characterization of New V<sub>1A</sub> Antagonist Compounds: The Separation of Four Atropisomeric Stereoisomers.
Szeleczky Z, Szakács Z, Bozó É, Baska F, Vukics K, Lévai S, Temesvári K, Vass E, Béni Z, Krámos B, Magdó I, Szántay C, Kóti J, Domány-Kovács K, Greiner I, Bata I.
J Med Chem (2021) 64 : 10445 -10468
PubMed 34255509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.60 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344159 TOLVAPTAN 4.0 1 9.00
CHEMBL5070075 1 6.70
CHEMBL5070261 1 6.33
CHEMBL4799793 1 6.25
CHEMBL5074709 1 6.05
CHEMBL5081323 1 5.97
CHEMBL4297183 BALOVAPTAN 3.0 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344159 TOLVAPTAN Ki = 1.0 nM 9.00
CHEMBL5070075 Ki = 200.0 nM 6.70
CHEMBL5070261 Ki = 470.0 nM 6.33
CHEMBL4799793 Ki = 560.0 nM 6.25
CHEMBL5074709 Ki = 900.0 nM 6.05
CHEMBL5081323 Ki = 1070.0 nM 5.97
CHEMBL4297183 BALOVAPTAN Ki = 1200.0 nM 5.92