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Assay Detail

CHEMBL5464409

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Binding
Inhibition of Oxytocin at 1 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_260900)
8
Total Activities
2
Compounds Tested
3
Activity Types
10
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Profiling data from Eurofins-Panlabs
SGC Frankfurt
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 6 - -
IC50 1 7.81 7.81
Ki 1 8.30 8.30

Assay Parameters

Parameter Type Value Units Text
Detection method Detection method - Radioligand Binding
Incubation temperature Incubation temperature - 25°C
Incubation time Incubation time - 2 h
Ligand Ligand - [³H] Oxytocin
Ligand concentration Ligand concentration 0.8 nM
Ligand Kd Ligand Kd 0.39 nM
Non-specific ligand with concentration Non-specific ligand with concentration - 1 µM Oxytocin
Reference compound Reference compound - Oxytocin
reference compound IC50 reference compound IC50 950.0 nM
Source of protein Source of protein - Human recombinant Chem-1 (rat hematopoetic) cells

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4594444 PECAVAPTAN 2.0 7 8.30
CHEMBL5465173 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4594444 PECAVAPTAN Ki = 5.06 nM 8.30
CHEMBL4594444 PECAVAPTAN IC50 = 15.5 nM 7.81
CHEMBL4594444 PECAVAPTAN Inhibition = 95.0 % -
CHEMBL4594444 PECAVAPTAN Inhibition = 84.0 % -
CHEMBL4594444 PECAVAPTAN Inhibition = 41.0 % -
CHEMBL4594444 PECAVAPTAN Inhibition = 6.0 % -
CHEMBL4594444 PECAVAPTAN Inhibition = 3.0 % -
CHEMBL5465173 Inhibition = 12.0 % -