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Assay Detail

CHEMBL3266323

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

Binding
Displacement of [3H]DTG from Wistar Hannover rat liver sigma 2 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent and σ receptors binding properties.
Abate C, Niso M, Marottoli R, Riganti C, Ghigo D, Ferorelli S, Ossato G, Perrone R, Lacivita E, Lamb DC, Berardi F.
J Med Chem (2014) 57 : 3314 -3323
PubMed 24697311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.65 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3259961 1 8.18
CHEMBL3259962 1 8.16
CHEMBL282433 DITOLYLGUANIDINE 1 7.61
CHEMBL3259960 1 7.51
CHEMBL3259963 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3259961 Ki = 6.57 nM 8.18
CHEMBL3259962 Ki = 6.9 nM 8.16
CHEMBL282433 DITOLYLGUANIDINE Ki = 24.6 nM 7.61
CHEMBL3259960 Ki = 31.2 nM 7.51
CHEMBL3259963 Ki = 161.0 nM 6.79