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Assay Detail

CHEMBL1065233

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

Binding
Displacement of [3H]AVP from human vasopressin V1a 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

Vasopressin V1a receptor (CHEMBL1889)
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 7.11 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603708 1 8.56
CHEMBL605373 1 7.75
CHEMBL601931 1 7.57
CHEMBL602872 1 7.43
CHEMBL602871 1 6.78
CHEMBL603075 1 6.77
CHEMBL360648 1 6.48
CHEMBL363910 1 6.46
CHEMBL602671 1 6.20
CHEMBL601930 1 -
CHEMBL601929 1 -
CHEMBL590175 1 -
CHEMBL24781 1 -
CHEMBL603076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603708 Ki = 2.74 nM 8.56
CHEMBL605373 Ki = 18.0 nM 7.75
CHEMBL601931 Ki = 27.0 nM 7.57
CHEMBL602872 Ki = 37.0 nM 7.43
CHEMBL602871 Ki = 167.0 nM 6.78
CHEMBL603075 Ki = 170.0 nM 6.77
CHEMBL360648 Ki = 330.0 nM 6.48
CHEMBL363910 Ki = 344.0 nM 6.46
CHEMBL602671 Ki = 633.0 nM 6.20
CHEMBL601930 Ki > 5000.0 nM -
CHEMBL601929 Ki > 5000.0 nM -
CHEMBL590175 Ki > 1000.0 nM -
CHEMBL24781 Ki - -
CHEMBL603076 Ki > 5000.0 nM -