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Assay Detail

CHEMBL3783006

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

Binding
Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Betti C, Starnowska J, Mika J, Dyniewicz J, Frankiewicz L, Novoa A, Bochynska M, Keresztes A, Kosson P, Makuch W, Van Duppen J, Chung NN, Vanden Broeck J, Lipkowski AW, Schiller PW, Janssens F, Ceusters M, Sommen F, Meert T, Przewlocka B, Tourwé D, Ballet S.
ACS Med Chem Lett (2015) 6 : 1209 -1214
PubMed 26713106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.59 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181202 1 8.85
CHEMBL3408519 1 8.73
CHEMBL3781680 1 8.23
CHEMBL1782141 1 8.07
CHEMBL3781336 1 7.89
CHEMBL3781519 1 7.69
CHEMBL3780686 1 7.52
CHEMBL3780820 1 7.15
CHEMBL3780776 1 6.86
CHEMBL3780818 1 6.27
CHEMBL3780408 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181202 IC50 = 1.41 nM 8.85
CHEMBL3408519 IC50 = 1.86 nM 8.73
CHEMBL3781680 IC50 = 5.9 nM 8.23
CHEMBL1782141 IC50 = 8.51 nM 8.07
CHEMBL3781336 IC50 = 13.0 nM 7.89
CHEMBL3781519 IC50 = 20.3 nM 7.69
CHEMBL3780686 IC50 = 30.1 nM 7.52
CHEMBL3780820 IC50 = 70.2 nM 7.15
CHEMBL3780776 IC50 = 137.0 nM 6.86
CHEMBL3780818 IC50 = 538.0 nM 6.27
CHEMBL3780408 IC50 = 658.0 nM 6.18