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Assay Detail

CHEMBL3783007

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

Binding
Agonist activity at delta opioid receptor in mouse vas deferens 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 Mus musculus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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 7.30 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408519 1 8.67
CHEMBL3781680 1 8.11
CHEMBL3780686 1 7.99
CHEMBL3781336 1 7.90
CHEMBL3781519 1 7.85
CHEMBL2181202 1 7.64
CHEMBL1782141 1 7.36
CHEMBL3780408 1 6.46
CHEMBL3780776 1 6.42
CHEMBL3780820 1 6.09
CHEMBL3780818 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408519 IC50 = 2.16 nM 8.67
CHEMBL3781680 IC50 = 7.7 nM 8.11
CHEMBL3780686 IC50 = 10.3 nM 7.99
CHEMBL3781336 IC50 = 12.6 nM 7.90
CHEMBL3781519 IC50 = 14.1 nM 7.85
CHEMBL2181202 IC50 = 23.1 nM 7.64
CHEMBL1782141 IC50 = 43.3 nM 7.36
CHEMBL3780408 IC50 = 349.0 nM 6.46
CHEMBL3780776 IC50 = 384.0 nM 6.42
CHEMBL3780820 IC50 = 814.0 nM 6.09
CHEMBL3780818 IC50 = 1660.0 nM 5.78