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Assay Detail

CHEMBL863361

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

Binding
Displacement of [125I]OVTA antagonist from rat oxytocin receptor expressed in HEK293-EBNA cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Expert

Target

Oxytocin receptor (CHEMBL3996)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 13 7.87 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445816 1 9.17
CHEMBL2113189 1 8.57
CHEMBL2113201 1 8.34
CHEMBL2113185 1 8.10
CHEMBL2113208 1 7.92
CHEMBL2113203 1 7.82
CHEMBL1254117 1 7.60
CHEMBL2113177 1 7.60
CHEMBL2113211 1 7.48
CHEMBL382301 ATOSIBAN 4.0 1 7.12
CHEMBL2113200 1 6.85
CHEMBL2113181 1 -
CHEMBL2113179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445816 Ki = 0.67 nM 9.17
CHEMBL2113189 Ki = 2.7 nM 8.57
CHEMBL2113201 Ki = 4.6 nM 8.34
CHEMBL2113185 Ki = 8.0 nM 8.10
CHEMBL2113208 Ki = 12.0 nM 7.92
CHEMBL2113203 Ki = 15.0 nM 7.82
CHEMBL1254117 Ki = 25.0 nM 7.60
CHEMBL2113177 Ki = 25.0 nM 7.60
CHEMBL2113211 Ki = 33.0 nM 7.48
CHEMBL382301 ATOSIBAN Ki = 76.0 nM 7.12
CHEMBL2113200 Ki = 140.0 nM 6.85
CHEMBL2113181 Ki - -
CHEMBL2113179 Ki - -