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Assay Detail

CHEMBL761405

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

Binding
Binding affinity against cloned human oxytocin receptor from human embryonic kidney cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type kidney
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.
Kuo MS, Bock MG, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Williams PD, Woyden CJ.
Bioorg Med Chem Lett (1998) 8 : 3081 -3086
PubMed 9873680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104237 1 8.70
CHEMBL322187 1 8.41
CHEMBL105406 1 8.27
CHEMBL105514 1 8.13
CHEMBL102994 1 8.10
CHEMBL24781 1 8.03
CHEMBL104530 1 7.82
CHEMBL105039 1 7.77
CHEMBL318174 1 7.27
CHEMBL102762 1 7.24
CHEMBL105960 1 7.14
CHEMBL319646 1 7.14
CHEMBL27157 1 7.06
CHEMBL105673 1 6.80
CHEMBL105733 1 6.58
CHEMBL322162 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104237 Ki = 2.0 nM 8.70
CHEMBL322187 Ki = 3.9 nM 8.41
CHEMBL105406 Ki = 5.4 nM 8.27
CHEMBL105514 Ki = 7.34 nM 8.13
CHEMBL102994 Ki = 7.9 nM 8.10
CHEMBL24781 Ki = 9.3 nM 8.03
CHEMBL104530 Ki = 15.0 nM 7.82
CHEMBL105039 Ki = 17.0 nM 7.77
CHEMBL318174 Ki = 54.0 nM 7.27
CHEMBL102762 Ki = 58.0 nM 7.24
CHEMBL105960 Ki = 73.0 nM 7.14
CHEMBL319646 Ki = 73.0 nM 7.14
CHEMBL27157 Ki = 87.0 nM 7.06
CHEMBL105673 Ki = 160.0 nM 6.80
CHEMBL105733 Ki = 260.0 nM 6.58
CHEMBL322162 Ki = 1800.0 nM 5.75