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Assay Detail

CHEMBL3379239

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

Binding
Displacement of [3H]-DTG from sigma-2 receptor in rat liver membrane in presence of (+)-pentazocine
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
Bourgeois C, Werfel E, Galla F, Lehmkuhl K, Torres-Gómez H, Schepmann D, Kögel B, Christoph T, Straßburger W, Englberger W, Soeberdt M, Hüwel S, Galla HJ, Wünsch B.
J Med Chem (2014) 57 : 6845 -6860
PubMed 25062506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.98 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL3323513 1 5.80
CHEMBL3323509 1 5.63
CHEMBL3299002 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL3323513 Ki = 1590.0 nM 5.80
CHEMBL3323509 Ki = 2340.0 nM 5.63
CHEMBL3299002 Ki = 4340.0 nM 5.36