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Assay Detail

CHEMBL3830258

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

Binding
Displacement of [3H]di-o-tolylgluanidine from sigma 2 receptor in rat liver membranes after 2 hrs by scintillation counting
8
Total Activities
8
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

Oxa-Pictet-Spengler reaction as key step in the synthesis of novel σ receptor ligands with 2-benzopyran structure.
Knappmann I, Schepmann D, Wünsch B.
Bioorg Med Chem (2016) 24 : 4045 -4055
PubMed 27396684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.83 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827079 1 7.70
CHEMBL282433 DITOLYLGUANIDINE 1 7.70
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL3828752 1 6.97
CHEMBL3827403 1 6.63
CHEMBL3828326 1 6.21
CHEMBL3827149 1 6.21
CHEMBL3827274 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827079 Ki = 20.0 nM 7.70
CHEMBL282433 DITOLYLGUANIDINE Ki = 20.2 nM 7.70
CHEMBL54 HALOPERIDOL Ki = 78.1 nM 7.11
CHEMBL3828752 Ki = 107.0 nM 6.97
CHEMBL3827403 Ki = 234.0 nM 6.63
CHEMBL3828326 Ki = 617.0 nM 6.21
CHEMBL3827149 Ki = 610.0 nM 6.21
CHEMBL3827274 Ki = 785.0 nM 6.11