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Assay Detail

CHEMBL2211451

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Binding
Binding affinity to sigma 1 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
Yu LF, Zhang HK, Gunosewoyo H, Kozikowski AP.
ACS Med Chem Lett (2012) 3 : 1054 -1058
PubMed 23641311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.06 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203549 1 8.68
CHEMBL60542 (+)-PENTAZOCINE 1 8.51
CHEMBL76806 1 8.44
CHEMBL814 FLUVOXAMINE 4.0 1 7.44
CHEMBL809 SERTRALINE 4.0 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203549 Ki = 2.1 nM 8.68
CHEMBL60542 (+)-PENTAZOCINE Ki = 3.1 nM 8.51
CHEMBL76806 Ki = 3.6 nM 8.44
CHEMBL814 FLUVOXAMINE Ki = 36.0 nM 7.44
CHEMBL809 SERTRALINE Ki = 57.0 nM 7.24