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Assay Detail

CHEMBL862402

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

Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LV2
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.
Failli AA, Shumsky JS, Steffan RJ, Caggiano TJ, Williams DK, Trybulski EJ, Ning X, Lock Y, Tanikella T, Hartmann D, Chan PS, Park CH.
Bioorg Med Chem Lett (2006) 16 : 954 -959
PubMed 16297621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.54 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363910 1 7.10
CHEMBL202447 1 7.04
CHEMBL203513 1 6.74
CHEMBL203739 1 6.53
CHEMBL381763 1 6.41
CHEMBL380733 1 6.38
CHEMBL205013 1 6.32
CHEMBL201889 1 6.31
CHEMBL202106 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363910 IC50 = 80.0 nM 7.10
CHEMBL202447 IC50 = 91.5 nM 7.04
CHEMBL203513 IC50 = 183.0 nM 6.74
CHEMBL203739 IC50 = 296.0 nM 6.53
CHEMBL381763 IC50 = 390.0 nM 6.41
CHEMBL380733 IC50 = 413.0 nM 6.38
CHEMBL205013 IC50 = 475.0 nM 6.32
CHEMBL201889 IC50 = 493.0 nM 6.31
CHEMBL202106 IC50 = 933.0 nM 6.03