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Assay Detail

CHEMBL2423360

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
8
Total Activities
8
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

Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities.
Nair P, Yamamoto T, Largent-Milnes TM, Cowell S, Kulkarni V, Moye S, Navratilova E, Davis P, Ma SW, Vanderah TW, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2013) 23 : 4975 -4978
PubMed 23899615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.85 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419538 1 8.29
CHEMBL2419539 1 8.16
CHEMBL2419540 1 8.07
CHEMBL2419542 1 8.04
CHEMBL2419537 1 7.92
CHEMBL2419544 1 7.68
CHEMBL2419541 1 7.58
CHEMBL2419543 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419538 IC50 = 5.1 nM 8.29
CHEMBL2419539 IC50 = 6.9 nM 8.16
CHEMBL2419540 IC50 = 8.5 nM 8.07
CHEMBL2419542 IC50 = 9.1 nM 8.04
CHEMBL2419537 IC50 = 12.0 nM 7.92
CHEMBL2419544 IC50 = 21.0 nM 7.68
CHEMBL2419541 IC50 = 26.0 nM 7.58
CHEMBL2419543 IC50 = 85.0 nM 7.07