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Assay Detail

CHEMBL870967

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

Binding
Displacement of [3H]oxytocin from rat OTR
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxytocin receptor (CHEMBL3996)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.
Borthwick AD, Davies DE, Exall AM, Hatley RJ, Hughes JA, Irving WR, Livermore DG, Sollis SL, Nerozzi F, Valko KL, Allen MJ, Perren M, Shabbir SS, Woollard PM, Price MA.
J Med Chem (2006) 49 : 4159 -4170
PubMed 16821776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.53 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377414 1 8.00
CHEMBL382301 ATOSIBAN 4.0 1 7.40
CHEMBL208787 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377414 Ki = 10.0 nM 8.00
CHEMBL382301 ATOSIBAN Ki = 39.81 nM 7.40
CHEMBL208787 Ki = 63.1 nM 7.20