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Assay Detail

CHEMBL1776941

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Functional
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists.
Napier S, Wishart G, Arbuckle W, Baker J, Barn D, Bingham M, Brown A, Byford A, Claxton C, Craighead M, Buchanan K, Fielding L, Gibson L, Goodwin R, Goutcher S, Irving N, MacSweeney C, Milne R, Mort C, Presland J, Sloan H, Thomson F, Turnbull Z, Young T.
Bioorg Med Chem Lett (2011) 21 : 3163 -3167
PubMed 21458261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.35 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774024 1 7.43
CHEMBL1774023 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774024 IC50 = 37.15 nM 7.43
CHEMBL1774023 IC50 = 54.95 nM 7.26