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Assay Detail

CHEMBL5225132

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Binding
Binding affinity to human sigma 2 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of mixed σ<sub>1</sub>R/σ<sub>2</sub>R ligands with antiproliferative and anticancer effects.
Fallica AN, Ciaffaglione V, Modica MN, Pittalà V, Salerno L, Amata E, Marrazzo A, Romeo G, Intagliata S.
Bioorg Med Chem (2022) 73 : 117032 -117032
PubMed 36202063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.38 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.75
CHEMBL50112 1 7.60
CHEMBL190883 1 6.77
CHEMBL4088272 1 5.86
CHEMBL5270434 1 5.81
CHEMBL305881 1 4.49
CHEMBL2170062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 18.0 nM 7.75
CHEMBL50112 Ki = 25.2 nM 7.60
CHEMBL190883 Ki = 170.0 nM 6.77
CHEMBL4088272 Ki = 1377.0 nM 5.86
CHEMBL5270434 Ki = 1542.0 nM 5.81
CHEMBL305881 Ki = 32100.0 nM 4.49
CHEMBL2170062 Ki > 1000.0 nM -