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Assay Detail

CHEMBL819372

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

Binding
Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
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 Expert

Target

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

Publication

Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.
Dyatkin AB, Hoekstra WJ, Hlasta DJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Gunnet JW, Hageman W, Look R, Maryanoff BE.
Bioorg Med Chem Lett (2002) 12 : 3081 -3084
PubMed 12372506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.85 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430841 1 7.64
CHEMBL106229 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430841 Ki = 23.0 nM 7.64
CHEMBL106229 Ki = 890.0 nM 6.05