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Assay Detail

CHEMBL861292

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Functional
Agonist activity at delta opioid receptor by inhibition of muscle contraction in electrically stimulated isolated mouse vas deferens
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Lee YS, Agnes RS, Badghisi H, Davis P, Ma SW, Lai J, Porreca F, Hruby VJ.
J Med Chem (2006) 49 : 1773 -1780
PubMed 16509592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.56 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.57
CHEMBL408889 1 8.29
CHEMBL413644 1 7.62
CHEMBL412331 1 7.58
CHEMBL375412 1 7.58
CHEMBL407057 1 7.54
CHEMBL442483 1 7.44
CHEMBL408832 1 7.42
CHEMBL374325 1 7.38
CHEMBL438739 1 7.08
CHEMBL405192 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN IC50 = 2.7 nM 8.57
CHEMBL408889 IC50 = 5.1 nM 8.29
CHEMBL413644 IC50 = 24.0 nM 7.62
CHEMBL412331 IC50 = 26.0 nM 7.58
CHEMBL375412 IC50 = 26.0 nM 7.58
CHEMBL407057 IC50 = 29.0 nM 7.54
CHEMBL442483 IC50 = 36.0 nM 7.44
CHEMBL408832 IC50 = 38.0 nM 7.42
CHEMBL374325 IC50 = 42.0 nM 7.38
CHEMBL438739 IC50 = 84.0 nM 7.08
CHEMBL405192 IC50 = 230.0 nM 6.64