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Assay Detail

CHEMBL5535231

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

Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
Baska F, Bozó É, Szeleczky Z, Szántó G, Vukics K, Szakács Z, Domány-Kovács K, Kurkó D, Vass E, Thán M, Vastag M, Temesvári K, Lévai S, Halász AS, Szondiné Kordás K, Román V, Greiner I, Bata I.
J Med Chem (2024) 67 : 643 -673
PubMed 38165765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.80 5.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5574495 1 5.93
CHEMBL4297183 BALOVAPTAN 3.0 1 5.80
CHEMBL5579703 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5574495 Ki = 1170.0 nM 5.93
CHEMBL4297183 BALOVAPTAN Ki = 1600.0 nM 5.80
CHEMBL5579703 Ki = 2190.0 nM 5.66