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Assay Detail

CHEMBL905190

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Functional
Agonist activity at mu opioid receptor in Hartley guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 7 6.89 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.06
CHEMBL340032 DADLE 1 7.62
CHEMBL229280 1 6.82
CHEMBL389651 1 6.47
CHEMBL389652 1 6.44
CHEMBL439019 1 6.43
CHEMBL426363 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN IC50 = 8.8 nM 8.06
CHEMBL340032 DADLE IC50 = 24.0 nM 7.62
CHEMBL229280 IC50 = 150.0 nM 6.82
CHEMBL389651 IC50 = 340.0 nM 6.47
CHEMBL389652 IC50 = 360.0 nM 6.44
CHEMBL439019 IC50 = 370.0 nM 6.43
CHEMBL426363 IC50 = 380.0 nM 6.42