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Assay Detail

CHEMBL3419319

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

Binding
Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
2
Total Activities
2
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

Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach.
Ratni H, Rogers-Evans M, Bissantz C, Grundschober C, Moreau JL, Schuler F, Fischer H, Alvarez Sanchez R, Schnider P.
J Med Chem (2015) 58 : 2275 -2289
PubMed 25654260 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.03 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416860 1 5.03
CHEMBL3416861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416860 Ki = 9308.0 nM 5.03
CHEMBL3416861 Ki > 27000.0 nM -