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Assay Detail

CHEMBL846736

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

Binding
In vitro for its binding affinity to rat V2 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V2 receptor (CHEMBL3766)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.
Albright JD, Delos Santos EG, Dusza JP, Chan PS, Coupet J, Ru X, Mazandarani H.
Bioorg Med Chem Lett (2000) 10 : 695 -698
PubMed 10782666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.24 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162748 1 8.22
CHEMBL351970 1 7.44
CHEMBL350090 1 7.16
CHEMBL350383 1 6.92
CHEMBL162588 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162748 IC50 = 6.0 nM 8.22
CHEMBL351970 IC50 = 36.0 nM 7.44
CHEMBL350090 IC50 = 69.0 nM 7.16
CHEMBL350383 IC50 = 120.0 nM 6.92
CHEMBL162588 IC50 = 340.0 nM 6.47