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Assay Detail

CHEMBL1003111

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Functional
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
13
Total Activities
13
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

Further studies on lead compounds containing the opioid pharmacophore Dmt-Tic.
Balboni G, Fiorini S, Baldisserotto A, Trapella C, Sasaki Y, Ambo A, Marczak ED, Lazarus LH, Salvadori S.
J Med Chem (2008) 51 : 5109 -5117
PubMed 18680274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.75 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL501451 1 8.59
CHEMBL458631 1 8.57
CHEMBL109390 1 7.57
CHEMBL444197 1 6.75
CHEMBL501202 1 6.58
CHEMBL500937 1 5.83
CHEMBL442577 1 5.76
CHEMBL498799 1 5.58
CHEMBL450263 1 5.54
CHEMBL450566 1 -
CHEMBL499099 1 -
CHEMBL502302 1 -
CHEMBL448360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL501451 IC50 = 2.57 nM 8.59
CHEMBL458631 IC50 = 2.69 nM 8.57
CHEMBL109390 IC50 = 26.92 nM 7.57
CHEMBL444197 IC50 = 179.0 nM 6.75
CHEMBL501202 IC50 = 265.0 nM 6.58
CHEMBL500937 IC50 = 1466.0 nM 5.83
CHEMBL442577 IC50 = 1724.0 nM 5.76
CHEMBL498799 IC50 = 2655.0 nM 5.58
CHEMBL450263 IC50 = 2886.0 nM 5.54
CHEMBL450566 IC50 > 10000.0 nM -
CHEMBL499099 IC50 > 10000.0 nM -
CHEMBL502302 IC50 > 10000.0 nM -
CHEMBL448360 IC50 > 10000.0 nM -