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Assay Detail

CHEMBL735758

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Functional
Tested for inhibition of amplification of electrically induced twitch in mouse vas deferens (MVD)
8
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 Expert

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Phe3-substituted analogues of deltorphin C. Spatial conformation and topography of the aromatic ring in peptide recognition by delta opioid receptors.
Salvadori S, Bryant SD, Bianchi C, Balboni G, Scaranari V, Attila M, Lazarus LH.
J Med Chem (1993) 36 : 3748 -3756
PubMed 8254604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.14 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317956 DELTORPHIN C 1 9.47
CHEMBL124941 2 9.42
CHEMBL124435 1 9.39
CHEMBL330991 1 6.81
CHEMBL121946 2 6.30
CHEMBL122159 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317956 DELTORPHIN C IC50 = 0.34 nM 9.47
CHEMBL124941 IC50 = 0.38 nM 9.42
CHEMBL124435 IC50 = 0.41 nM 9.39
CHEMBL124941 IC50 = 0.46 nM 9.34
CHEMBL330991 IC50 = 156.0 nM 6.81
CHEMBL121946 IC50 = 498.0 nM 6.30
CHEMBL121946 IC50 = 554.0 nM 6.26
CHEMBL122159 IC50 > 10000.0 nM -