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Assay Detail

CHEMBL3405394

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Binding
Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in Sprague-Dawley rat liver membranes after 120 mins by beta counting in presence of (+)-pentazocine
10
Total Activities
10
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

Synthesis and evaluation of tetrahydroindazole derivatives as sigma-2 receptor ligands.
Wu ZW, Song SY, Li L, Lu HL, Lieberman B, Huang YS, Mach RH.
Bioorg Med Chem (2015) 23 : 1463 -1471
PubMed 25752422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.13 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.71
CHEMBL3401447 1 7.33
CHEMBL3401452 1 7.13
CHEMBL3401450 1 7.05
CHEMBL3401451 1 6.85
CHEMBL3401449 1 6.09
CHEMBL3401446 1 4.95
CHEMBL3401448 1 4.74
CHEMBL3401454 1 4.74
CHEMBL3401453 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 19.4 nM 7.71
CHEMBL3401447 Ki = 46.6 nM 7.33
CHEMBL3401452 Ki = 74.5 nM 7.13
CHEMBL3401450 Ki = 89.8 nM 7.05
CHEMBL3401451 Ki = 142.0 nM 6.85
CHEMBL3401449 Ki = 820.0 nM 6.09
CHEMBL3401446 Ki = 11350.0 nM 4.95
CHEMBL3401448 Ki = 18250.0 nM 4.74
CHEMBL3401454 Ki = 18400.0 nM 4.74
CHEMBL3401453 Ki = 21500.0 nM 4.67