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Assay Detail

CHEMBL3637632

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

Binding
Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Conformationally restricted κ-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.
Molenveld P, Bouzanne des Mazery R, Sterk GJ, Storcken RP, Autar R, van Oss B, van der Haas RN, Fröhlich R, Schepmann D, Wünsch B, Soeberdt M.
Bioorg Med Chem Lett (2015) 25 : 5326 -5330
PubMed 26411794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.28 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267495 NALFURAFINE 4.0 1 9.43
CHEMBL70 MORPHINE 4.0 1 8.70
CHEMBL80 NALOXONE 4.0 1 8.60
CHEMBL3634516 1 7.24
CHEMBL3634515 2 7.10
CHEMBL3634398 1 6.89
CHEMBL3299005 1 6.30
CHEMBL3634395 1 6.28
CHEMBL3634397 1 5.99
CHEMBL58033 (-)-U-50488 1 -
CHEMBL603370 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267495 NALFURAFINE Ki = 0.37 nM 9.43
CHEMBL70 MORPHINE Ki = 2.0 nM 8.70
CHEMBL80 NALOXONE Ki = 2.5 nM 8.60
CHEMBL3634516 Ki = 58.0 nM 7.24
CHEMBL3634515 Ki = 80.0 nM 7.10
CHEMBL3634398 Ki = 130.0 nM 6.89
CHEMBL3299005 Ki = 497.0 nM 6.30
CHEMBL3634515 Ki = 512.0 nM 6.29
CHEMBL3634395 Ki = 520.0 nM 6.28
CHEMBL3634397 Ki = 1020.0 nM 5.99
CHEMBL58033 (-)-U-50488 Ki - -
CHEMBL603370 Ki - -