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Assay Detail

CHEMBL4201601

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

Binding
Displacement of [3H]-AVP from human OXR receptor expressed in CHO cell membranes by radioligand binding assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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
Ki 24 6.80 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4210854 1 7.98
CHEMBL601931 1 7.77
CHEMBL4218211 1 7.43
CHEMBL4206233 1 7.08
CHEMBL4206482 1 6.98
CHEMBL603708 1 6.96
CHEMBL4205970 1 6.82
CHEMBL363910 1 6.70
CHEMBL4205046 1 6.49
CHEMBL4209952 1 6.47
CHEMBL4213812 1 6.40
CHEMBL4215696 1 6.16
CHEMBL4204008 1 6.10
CHEMBL4216926 1 5.88
CHEMBL4210158 1 -
CHEMBL4209266 1 -
CHEMBL4207120 1 -
CHEMBL4215258 1 -
CHEMBL4216873 1 -
CHEMBL4207413 1 -
CHEMBL4202525 1 -
CHEMBL344848 1 -
CHEMBL4218739 1 -
CHEMBL4209421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4210854 Ki = 10.4 nM 7.98
CHEMBL601931 Ki = 17.0 nM 7.77
CHEMBL4218211 Ki = 37.4 nM 7.43
CHEMBL4206233 Ki = 84.0 nM 7.08
CHEMBL4206482 Ki = 104.0 nM 6.98
CHEMBL603708 Ki = 109.0 nM 6.96
CHEMBL4205970 Ki = 150.0 nM 6.82
CHEMBL363910 Ki = 199.0 nM 6.70
CHEMBL4205046 Ki = 325.0 nM 6.49
CHEMBL4209952 Ki = 340.0 nM 6.47
CHEMBL4213812 Ki = 396.0 nM 6.40
CHEMBL4215696 Ki = 686.0 nM 6.16
CHEMBL4204008 Ki = 800.0 nM 6.10
CHEMBL4216926 Ki = 1333.0 nM 5.88
CHEMBL4210158 Ki > 1000.0 nM -
CHEMBL4209266 Ki < 10.0 nM -
CHEMBL4207120 Ki > 1000.0 nM -
CHEMBL4215258 Ki < 10.0 nM -
CHEMBL4216873 Ki < 10.0 nM -
CHEMBL4207413 Ki < 10.0 nM -
CHEMBL4202525 Ki > 1000.0 nM -
CHEMBL344848 Ki < 10.0 nM -
CHEMBL4218739 Ki < 10.0 nM -
CHEMBL4209421 Ki < 10.0 nM -