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Assay Detail

CHEMBL5148374

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

Binding
Displacement of [3H]-vasopressin from human V1A receptor expressed in CHO cells membrane by microbeta scintillation counter analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzodiazepine Derivatives as Potent Vasopressin V<sub>2</sub> Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease.
Cao X, Wang P, Yuan H, Zhang H, He Y, Fu K, Fang Q, Liu H, Su L, Yin L, Xu P, Xie Y, Xiong X, Wang J, Zhu X, Guo D.
J Med Chem (2022) 65 : 9295 -9311
PubMed 35579344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.68 6.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208751 1 6.83
CHEMBL344159 TOLVAPTAN 4.0 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208751 Ki = 147.0 nM 6.83
CHEMBL344159 TOLVAPTAN Ki = 296.0 nM 6.53