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Assay Detail

CHEMBL4201613

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

Binding
Displacement of DY647 from SNAP-tagged V1A receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vasopressin V1a receptor (CHEMBL1889)
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
Ki 7 6.90 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763342 1 7.90
CHEMBL4217872 1 7.09
CHEMBL360648 1 6.71
CHEMBL4204210 1 5.90
CHEMBL4216174 1 -
CHEMBL4203314 1 -
CHEMBL4212928 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763342 Ki = 12.5 nM 7.90
CHEMBL4217872 Ki = 82.0 nM 7.09
CHEMBL360648 Ki = 196.0 nM 6.71
CHEMBL4204210 Ki = 1253.0 nM 5.90
CHEMBL4216174 Ki > 1000.0 nM -
CHEMBL4203314 Ki > 1000.0 nM -
CHEMBL4212928 Ki > 1000.0 nM -