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Assay Detail

CHEMBL4009149

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 membranes after 120 mins by scintillation counting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Soeberdt M, Molenveld P, Storcken RP, Bouzanne des Mazery R, Sterk GJ, Autar R, Bolster MG, Wagner C, Aerts SN, van Holst FR, Wegert A, Tangherlini G, Frehland B, Schepmann D, Metze D, Lotts T, Knie U, Lin KY, Huang TY, Lai CC, Ständer S, Wünsch B, Abels C.
J Med Chem (2017) 60 : 2526 -2551
PubMed 28218838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.86 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL3634516 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL3634516 Ki = 252.0 nM 6.60