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Assay Detail

CHEMBL5148375

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

Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V2 receptor (CHEMBL1790)
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
IC50 2 7.84 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208751 1 8.04
CHEMBL5207885 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208751 IC50 = 9.2 nM 8.04
CHEMBL5207885 IC50 = 23.0 nM 7.64