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Assay Detail

CHEMBL4201620

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

Functional
Agonist activity at human OTR expressed in HEK cells assessed as increase in intracellular calcium flux incubated for 45 mins by Indo1-AM dye based fluorescence 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

Oxytocin receptor (CHEMBL2049)
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 7.46 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763342 1 8.52
CHEMBL360648 1 7.55
CHEMBL4204210 1 7.26
CHEMBL4216174 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763342 EC50 = 3.0 nM 8.52
CHEMBL360648 EC50 = 28.0 nM 7.55
CHEMBL4204210 EC50 = 55.0 nM 7.26
CHEMBL4216174 EC50 = 300.0 nM 6.52