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Assay Detail

CHEMBL870949

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Functional
Antagonist activity against human OTR expressed in CHO cells measured as calcium influx by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

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 2 8.60 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377414 1 8.80
CHEMBL208787 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377414 Ki = 1.585 nM 8.80
CHEMBL208787 Ki = 3.981 nM 8.40