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Assay Detail

CHEMBL817837

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

Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
13
Total Activities
13
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 V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.
Matthews JM, Greco MN, Hecker LR, Hoekstra WJ, Andrade-Gordon P, de Garavilla L, Demarest KT, Ericson E, Gunnet JW, Hageman W, Look R, Moore JB, Maryanoff BE.
Bioorg Med Chem Lett (2003) 13 : 753 -756
PubMed 12639574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.33 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350576 1 8.10
CHEMBL424183 1 7.96
CHEMBL166135 1 7.92
CHEMBL165554 1 7.89
CHEMBL165076 1 7.82
CHEMBL165670 1 7.70
CHEMBL351453 1 7.36
CHEMBL166261 1 7.30
CHEMBL349965 1 6.77
CHEMBL349062 1 6.75
CHEMBL166265 1 6.72
CHEMBL165183 1 6.68
CHEMBL350792 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350576 IC50 = 8.0 nM 8.10
CHEMBL424183 IC50 = 11.0 nM 7.96
CHEMBL166135 IC50 = 12.0 nM 7.92
CHEMBL165554 IC50 = 13.0 nM 7.89
CHEMBL165076 IC50 = 15.0 nM 7.82
CHEMBL165670 IC50 = 20.0 nM 7.70
CHEMBL351453 IC50 = 44.0 nM 7.36
CHEMBL166261 IC50 = 50.0 nM 7.30
CHEMBL349965 IC50 = 170.0 nM 6.77
CHEMBL349062 IC50 = 180.0 nM 6.75
CHEMBL166265 IC50 = 190.0 nM 6.72
CHEMBL165183 IC50 = 210.0 nM 6.68
CHEMBL350792 IC50 = 550.0 nM 6.26