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Assay Detail

CHEMBL5324497

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Binding
Binding affinity to sigma2 receptor (unknown origin) assessed as inhibition constant
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

Discovery of WLB-89462, a New Drug-like and Highly Selective σ<sub>2</sub> Receptor Ligand with Neuroprotective Properties.
Christmann U, Díaz JL, Pascual R, Bordas M, Álvarez I, Monroy X, Porras M, Yeste S, Reinoso RF, Merlos M, Vela JM, Almansa C.
J Med Chem (2023) 66 : 12499 -12519
PubMed 37607512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.47 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61479 SIRAMESINE 2.0 1 9.92
CHEMBL5426155 1 9.37
CHEMBL53325 1 9.17
CHEMBL4846092 1 8.10
CHEMBL4297605 ROLUPERIDONE 3.0 1 8.09
CHEMBL5189158 1 7.34
CHEMBL5395401 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61479 SIRAMESINE Ki = 0.12 nM 9.92
CHEMBL5426155 Ki = 0.43 nM 9.37
CHEMBL53325 Ki = 0.68 nM 9.17
CHEMBL4846092 Ki = 8.0 nM 8.10
CHEMBL4297605 ROLUPERIDONE Ki = 8.2 nM 8.09
CHEMBL5189158 Ki = 46.0 nM 7.34
CHEMBL5395401 Ki = 47.0 nM 7.33