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Assay Detail

CHEMBL862398

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

Binding
Displacement of [3H]AVP from human V1a receptor expressed in CHO cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V1a receptor (CHEMBL1889)
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 10 5.69 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363910 1 6.11
CHEMBL203513 1 5.75
CHEMBL201889 1 5.22
CHEMBL373199 1 -
CHEMBL381458 1 -
CHEMBL381763 1 -
CHEMBL378143 1 -
CHEMBL202106 1 -
CHEMBL202105 1 -
CHEMBL201890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363910 IC50 = 778.0 nM 6.11
CHEMBL203513 IC50 = 1783.0 nM 5.75
CHEMBL201889 IC50 = 5954.0 nM 5.22
CHEMBL373199 IC50 - -
CHEMBL381458 IC50 - -
CHEMBL381763 IC50 - -
CHEMBL378143 IC50 - -
CHEMBL202106 IC50 - -
CHEMBL202105 IC50 - -
CHEMBL201890 IC50 - -