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Assay Detail

CHEMBL895354

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Binding
Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Albizu L, Teppaz G, Seyer R, Bazin H, Ansanay H, Manning M, Mouillac B, Durroux T.
J Med Chem (2007) 50 : 4976 -4985
PubMed 17850055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.16 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394602 1 9.55
CHEMBL419667 RELCOVAPTAN 2.0 1 9.07
CHEMBL373742 VASOPRESSIN 4.0 1 8.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394602 Ki = 0.28 nM 9.55
CHEMBL419667 RELCOVAPTAN Ki = 0.85 nM 9.07
CHEMBL373742 VASOPRESSIN Ki = 1.35 nM 8.87