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Assay Detail

CHEMBL4121250

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

Functional
Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assay
4
Total Activities
4
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

Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.
Beard R, Stucki A, Schmitt M, Py G, Grundschober C, Gee AD, Tate EW.
Bioorg Med Chem (2018) 26 : 3039 -3045
PubMed 29602673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.44 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126100 1 7.85
CHEMBL4127791 1 7.46
CHEMBL4129142 1 5.36
CHEMBL4128839 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126100 IC50 = 14.0 nM 7.85
CHEMBL4127791 IC50 = 35.0 nM 7.46
CHEMBL4129142 IC50 = 4400.0 nM 5.36
CHEMBL4128839 IC50 = 7862.0 nM 5.10