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Assay Detail

CHEMBL5163573

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Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
3
Total Activities
3
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

Long Residence Time at the Vasopressin V<sub>2</sub> Receptor Translates into Superior Inhibitory Effects in <i>Ex Vivo</i> and <i>In Vivo</i> Models of Autosomal Dominant Polycystic Kidney Disease.
Zhang H, Yan W, Sun Y, Yuan H, Su L, Cao X, Wang P, Xu Z, Hu Y, Wang Z, Wang Y, Fu K, Sun Y, Chen Y, Cheng J, Guo D.
J Med Chem (2022) 65 : 7717 -7728
PubMed 35363466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.25 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344159 TOLVAPTAN 4.0 1 7.95
CHEMBL5173331 1 7.03
CHEMBL5198918 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344159 TOLVAPTAN IC50 = 11.22 nM 7.95
CHEMBL5173331 IC50 = 93.33 nM 7.03
CHEMBL5198918 IC50 = 169.82 nM 6.77