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Assay Detail

CHEMBL891367

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of deltorphin 2-induced effect on muscle contractions
7
Total Activities
7
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

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Li T, Jinsmaa Y, Nedachi M, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Bryant SD, Marczak E, Li Q, Swartzwelder HS, Lazarus LH, Okada Y.
Bioorg Med Chem (2007) 15 : 1237 -1251
PubMed 17142049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.96 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412923 1 8.60
CHEMBL412924 1 7.32
CHEMBL397177 1 7.15
CHEMBL232303 1 6.83
CHEMBL396506 1 6.38
CHEMBL412922 1 6.32
CHEMBL397176 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412923 Kd = 2.512 nM 8.60
CHEMBL412924 Kd = 47.86 nM 7.32
CHEMBL397177 Kd = 70.79 nM 7.15
CHEMBL232303 Kd = 147.91 nM 6.83
CHEMBL396506 Kd = 416.87 nM 6.38
CHEMBL412922 Kd = 478.63 nM 6.32
CHEMBL397176 Kd = 741.31 nM 6.13