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Assay Detail

CHEMBL870966

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

Functional
Reduction in oxytocin-induced uterine contraction in iv dosed anaesthetized rat
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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
Activity 3 - -
IC50 2 6.69 6.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382301 ATOSIBAN 4.0 2 6.73
CHEMBL377414 2 6.64
CHEMBL208787 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382301 ATOSIBAN IC50 = 186.0 nM 6.73
CHEMBL377414 IC50 = 227.0 nM 6.64
CHEMBL382301 ATOSIBAN Activity = 0.63 mg kg-1 -
CHEMBL208787 Activity = 5.4 mg kg-1 -
CHEMBL377414 Activity = 0.22 mg kg-1 -