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Assay Detail

CHEMBL822187

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

Binding
Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.
Mitch CH, Leander JD, Mendelsohn LG, Shaw WN, Wong DT, Cantrell BE, Johnson BG, Reel JK, Snoddy JD, Takemori AE.
J Med Chem (1993) 36 : 2842 -2850
PubMed 8410999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.06 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL982 NALMEFENE 4.0 1 8.47
CHEMBL300662 1 8.28
CHEMBL98507 1 7.99
CHEMBL80 NALOXONE 4.0 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL982 NALMEFENE Ki = 3.4 nM 8.47
CHEMBL300662 Ki = 5.2 nM 8.28
CHEMBL98507 Ki = 10.27 nM 7.99
CHEMBL80 NALOXONE Ki = 32.0 nM 7.50