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Assay Detail

CHEMBL4392280

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

Binding
Displacement of [3H]OT from recombinant human OTR expressed in HEK293 cell membranes measured after 1 hr
9
Total Activities
9
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

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors.
Ichinose W, Cherepanov SM, Shabalova AA, Yokoyama S, Yuhi T, Yamaguchi H, Watanabe A, Yamamoto Y, Okamoto H, Horike S, Terakawa J, Daikoku T, Watanabe M, Mano N, Higashida H, Shuto S.
J Med Chem (2019) 62 : 3297 -3310
PubMed 30896946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.91 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4474284 1 9.29
CHEMBL395429 OXYTOCIN 4.0 1 9.24
CHEMBL4458988 1 9.05
CHEMBL3354594 1 8.96
CHEMBL3354579 1 8.85
CHEMBL4583231 1 8.85
CHEMBL3301668 CARBETOCIN 3.0 1 8.74
CHEMBL373742 VASOPRESSIN 4.0 1 8.70
CHEMBL4467042 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4474284 Ki = 0.51 nM 9.29
CHEMBL395429 OXYTOCIN Ki = 0.58 nM 9.24
CHEMBL4458988 Ki = 0.9 nM 9.05
CHEMBL3354594 Ki = 1.1 nM 8.96
CHEMBL3354579 Ki = 1.4 nM 8.85
CHEMBL4583231 Ki = 1.4 nM 8.85
CHEMBL3301668 CARBETOCIN Ki = 1.8 nM 8.74
CHEMBL373742 VASOPRESSIN Ki = 2.0 nM 8.70
CHEMBL4467042 Ki = 3.0 nM 8.52