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Assay Detail

CHEMBL4022076

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

Binding
Displacement of (+)-[3H]-ditolylguanidine from recombinant rat sigma 2 receptor expressed in rat PC12 cell membranes after 90 mins in presence of sigma 1 receptor blocker (+)-SKF-10047 by scintillation counting method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma intracellular receptor 2 (CHEMBL4105864)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Reevaluation of fenpropimorph as a σ receptor ligand: Structure-affinity relationship studies at human σ1 receptors.
Sguazzini E, Schmidt HR, Iyer KA, Kruse AC, Dukat M.
Bioorg Med Chem Lett (2017) 27 : 2912 -2919
PubMed 28495085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.78 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101014 1 7.86
CHEMBL4083034 1 7.50
CHEMBL4071509 1 7.18
CHEMBL4098546 1 7.11
CHEMBL372700 FENPROPIMORPH 1 6.07
CHEMBL4090823 1 6.03
CHEMBL1562542 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101014 Ki = 13.8 nM 7.86
CHEMBL4083034 Ki = 31.5 nM 7.50
CHEMBL4071509 Ki = 66.1 nM 7.18
CHEMBL4098546 Ki = 77.9 nM 7.11
CHEMBL372700 FENPROPIMORPH Ki = 854.0 nM 6.07
CHEMBL4090823 Ki = 930.0 nM 6.03
CHEMBL1562542 Ki = 2019.0 nM 5.70