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Assay Detail

CHEMBL1175729

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Functional
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 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

Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
Lee YS, Fernandes S, Kulkarani V, Mayorov A, Davis P, Ma SW, Brown K, Gillies RJ, Lai J, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2010) 20 : 4080 -4084
PubMed 20547453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.83 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1172253 1 7.96
CHEMBL1172251 1 7.40
CHEMBL1172252 1 7.22
CHEMBL1172428 1 6.96
CHEMBL235743 1 6.92
CHEMBL1172249 1 6.89
CHEMBL1172245 1 6.62
CHEMBL1172429 1 6.43
CHEMBL1172247 1 6.39
CHEMBL1172248 1 6.21
CHEMBL1172244 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1172253 IC50 = 11.0 nM 7.96
CHEMBL1172251 IC50 = 40.0 nM 7.40
CHEMBL1172252 IC50 = 60.0 nM 7.22
CHEMBL1172428 IC50 = 110.0 nM 6.96
CHEMBL235743 IC50 = 120.0 nM 6.92
CHEMBL1172249 IC50 = 130.0 nM 6.89
CHEMBL1172245 IC50 = 240.0 nM 6.62
CHEMBL1172429 IC50 = 370.0 nM 6.43
CHEMBL1172247 IC50 = 410.0 nM 6.39
CHEMBL1172248 IC50 = 610.0 nM 6.21
CHEMBL1172244 IC50 = 730.0 nM 6.14