Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL863363

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

Functional
Inhibitory activity against human Oxytocin induced intracellular Calcium mobilization in human Oxytocin receptor transfected HEK293-EBNA cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Expert

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.
Quattropani A, Dorbais J, Covini D, Pittet PA, Colovray V, Thomas RJ, Coxhead R, Halazy S, Scheer A, Missotten M, Ayala G, Bradshaw C, De Raemy-Schenk AM, Nichols A, Cirillo R, Tos EG, Giachetti C, Golzio L, Marinelli P, Church DJ, Barberis C, Chollet A, Schwarz MK.
J Med Chem (2005) 48 : 7882 -7905
PubMed 16302826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.57 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113185 1 8.15
CHEMBL2113208 1 8.15
CHEMBL2113211 1 8.10
CHEMBL445816 1 7.85
CHEMBL2113201 1 7.85
CHEMBL2113189 1 7.82
CHEMBL1254117 1 7.52
CHEMBL2113179 1 7.50
CHEMBL2113177 1 7.31
CHEMBL382301 ATOSIBAN 4.0 1 7.23
CHEMBL2113203 1 7.23
CHEMBL2113200 1 6.08
CHEMBL2113181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113185 IC50 = 7.0 nM 8.15
CHEMBL2113208 IC50 = 7.0 nM 8.15
CHEMBL2113211 IC50 = 8.0 nM 8.10
CHEMBL445816 IC50 = 14.0 nM 7.85
CHEMBL2113201 IC50 = 14.0 nM 7.85
CHEMBL2113189 IC50 = 15.0 nM 7.82
CHEMBL1254117 IC50 = 30.0 nM 7.52
CHEMBL2113179 IC50 = 32.0 nM 7.50
CHEMBL2113177 IC50 = 49.0 nM 7.31
CHEMBL382301 ATOSIBAN IC50 = 59.0 nM 7.23
CHEMBL2113203 IC50 = 59.0 nM 7.23
CHEMBL2113200 IC50 = 840.0 nM 6.08
CHEMBL2113181 IC50 - -