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Assay Detail

CHEMBL1046460

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Functional
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated contraction
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Yamamoto T, Nair P, Ma SW, Davis P, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
Bioorg Med Chem (2009) 17 : 7337 -7343
PubMed 19762245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.67 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.57
CHEMBL611925 1 8.08
CHEMBL592969 1 7.72
CHEMBL595972 1 7.44
CHEMBL611924 1 7.14
CHEMBL611926 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN IC50 = 2.7 nM 8.57
CHEMBL611925 IC50 = 8.3 nM 8.08
CHEMBL592969 IC50 = 19.0 nM 7.72
CHEMBL595972 IC50 = 36.0 nM 7.44
CHEMBL611924 IC50 = 73.0 nM 7.14
CHEMBL611926 IC50 = 85.0 nM 7.07