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Assay Detail

CHEMBL4201664

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

Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.
Frantz MC, Pellissier LP, Pflimlin E, Loison S, Gandía J, Marsol C, Durroux T, Mouillac B, Becker JAJ, Le Merrer J, Valencia C, Villa P, Bonnet D, Hibert M.
J Med Chem (2018) 61 : 8670 -8692
PubMed 30199637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.08 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204210 1 6.18
CHEMBL395429 OXYTOCIN 4.0 1 6.09
CHEMBL3301668 CARBETOCIN 3.0 1 5.96
CHEMBL3763342 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204210 EC50 = 660.0 nM 6.18
CHEMBL395429 OXYTOCIN EC50 = 810.0 nM 6.09
CHEMBL3301668 CARBETOCIN EC50 = 1100.0 nM 5.96
CHEMBL3763342 EC50 - -