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Assay Detail

CHEMBL905189

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Functional
Agonist activity at delta opioid receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
10
Total Activities
10
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, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Yamamoto T, Nair P, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Vanderah TW, Yamamura HI, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 2779 -2786
PubMed 17516639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.40 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340032 DADLE 1 9.57
CHEMBL200199 BIPHALIN 1 8.57
CHEMBL439019 1 7.77
CHEMBL389652 1 7.66
CHEMBL229280 1 7.48
CHEMBL389651 1 7.00
CHEMBL426363 1 6.77
CHEMBL387670 1 6.72
CHEMBL2371978 1 6.39
CHEMBL2371977 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340032 DADLE IC50 = 0.27 nM 9.57
CHEMBL200199 BIPHALIN IC50 = 2.7 nM 8.57
CHEMBL439019 IC50 = 17.0 nM 7.77
CHEMBL389652 IC50 = 22.0 nM 7.66
CHEMBL229280 IC50 = 33.0 nM 7.48
CHEMBL389651 IC50 = 100.0 nM 7.00
CHEMBL426363 IC50 = 170.0 nM 6.77
CHEMBL387670 IC50 = 190.0 nM 6.72
CHEMBL2371978 IC50 = 410.0 nM 6.39
CHEMBL2371977 IC50 = 910.0 nM 6.04