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Assay Detail

CHEMBL4121240

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

Binding
Displacement of [3H]OT from human mammary gland oxytocin receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
6
Total Activities
6
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

Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.
Beard R, Stucki A, Schmitt M, Py G, Grundschober C, Gee AD, Tate EW.
Bioorg Med Chem (2018) 26 : 3039 -3045
PubMed 29602673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.46 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395429 OXYTOCIN 4.0 1 8.92
CHEMBL373742 VASOPRESSIN 4.0 1 8.22
CHEMBL4129142 1 7.30
CHEMBL4128839 1 6.85
CHEMBL4126100 1 6.78
CHEMBL4127791 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395429 OXYTOCIN Ki = 1.2 nM 8.92
CHEMBL373742 VASOPRESSIN Ki = 6.0 nM 8.22
CHEMBL4129142 Ki = 50.0 nM 7.30
CHEMBL4128839 Ki = 142.0 nM 6.85
CHEMBL4126100 Ki = 166.0 nM 6.78
CHEMBL4127791 Ki = 220.0 nM 6.66