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Assay Detail

CHEMBL3611626

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
9
Total Activities
9
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

Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Nair P, Yamamoto T, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2015) 25 : 3716 -3720
PubMed 26212775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.34 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3608938 1 8.22
CHEMBL3608939 1 8.02
CHEMBL3608937 1 7.89
CHEMBL3609615 1 7.48
CHEMBL3609621 1 7.39
CHEMBL3609616 1 7.37
CHEMBL3609618 1 6.75
CHEMBL3609617 1 6.52
CHEMBL3609620 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3608938 IC50 = 6.0 nM 8.22
CHEMBL3608939 IC50 = 9.5 nM 8.02
CHEMBL3608937 IC50 = 13.0 nM 7.89
CHEMBL3609615 IC50 = 33.0 nM 7.48
CHEMBL3609621 IC50 = 41.0 nM 7.39
CHEMBL3609616 IC50 = 43.0 nM 7.37
CHEMBL3609618 IC50 = 180.0 nM 6.75
CHEMBL3609617 IC50 = 300.0 nM 6.52
CHEMBL3609620 IC50 = 400.0 nM 6.40