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Assay Detail

CHEMBL4121246

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Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
5
Total Activities
5
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 V2 receptor (CHEMBL1790)
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
EC50 5 5.61 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395429 OXYTOCIN 4.0 1 7.54
CHEMBL4128839 1 5.43
CHEMBL4129142 1 5.41
CHEMBL4127791 1 4.97
CHEMBL4126100 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395429 OXYTOCIN EC50 = 29.0 nM 7.54
CHEMBL4128839 EC50 = 3669.0 nM 5.43
CHEMBL4129142 EC50 = 3900.0 nM 5.41
CHEMBL4127791 EC50 = 10764.0 nM 4.97
CHEMBL4126100 EC50 = 18919.0 nM 4.72