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Assay Detail

CHEMBL751120

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

Binding
Binding affinity for Opioid receptor delta 1 determined by displacing [3H]-DSLET from rat brain membrane binding sites
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The opioid mu agonist/delta antagonist DIPP-NH(2)[Psi] produces a potent analgesic effect, no physical dependence, and less tolerance than morphine in rats.
Schiller PW, Fundytus ME, Merovitz L, Weltrowska G, Nguyen TM, Lemieux C, Chung NN, Coderre TJ.
J Med Chem (1999) 42 : 3520 -3526
PubMed 10479285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.84 9.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538700 1 9.93
CHEMBL2370502 1 9.41
CHEMBL119590 1 9.35
CHEMBL8234 ENKEPHALIN 1 8.60
CHEMBL332803 1 8.52
CHEMBL119535 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538700 Ki = 0.118 nM 9.93
CHEMBL2370502 Ki = 0.393 nM 9.41
CHEMBL119590 Ki = 0.447 nM 9.35
CHEMBL8234 ENKEPHALIN Ki = 2.53 nM 8.60
CHEMBL332803 Ki = 3.0 nM 8.52
CHEMBL119535 Ki = 61.0 nM 7.21