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Assay Detail

CHEMBL1065226

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

Binding
Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells
14
Total Activities
14
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

Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
Frantz MC, Rodrigo J, Boudier L, Durroux T, Mouillac B, Hibert M.
J Med Chem (2010) 53 : 1546 -1562
PubMed 20104850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.78 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL601931 1 7.77
CHEMBL605373 1 7.56
CHEMBL602872 1 6.96
CHEMBL603708 1 6.96
CHEMBL360648 1 6.83
CHEMBL363910 1 6.70
CHEMBL601930 1 6.61
CHEMBL602671 1 6.07
CHEMBL590175 1 5.60
CHEMBL601929 1 -
CHEMBL603076 1 -
CHEMBL603075 1 -
CHEMBL602871 1 -
CHEMBL24781 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601931 Ki = 17.0 nM 7.77
CHEMBL605373 Ki = 27.8 nM 7.56
CHEMBL602872 Ki = 111.0 nM 6.96
CHEMBL603708 Ki = 109.0 nM 6.96
CHEMBL360648 Ki = 147.0 nM 6.83
CHEMBL363910 Ki = 199.0 nM 6.70
CHEMBL601930 Ki = 245.0 nM 6.61
CHEMBL602671 Ki = 844.0 nM 6.07
CHEMBL590175 Ki = 2500.0 nM 5.60
CHEMBL601929 Ki > 5000.0 nM -
CHEMBL603076 Ki > 5000.0 nM -
CHEMBL603075 Ki > 5000.0 nM -
CHEMBL602871 Ki > 1000.0 nM -
CHEMBL24781 Ki - -