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Assay Detail

CHEMBL5324496

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Binding
Binding affinity to sigma1 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 non-opioid intracellular receptor 1 (CHEMBL287)
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 7.14 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53325 1 9.42
CHEMBL61479 SIRAMESINE 2.0 1 7.77
CHEMBL4846092 1 7.20
CHEMBL5395401 1 6.28
CHEMBL5426155 1 6.25
CHEMBL5189158 1 5.89
CHEMBL4297605 ROLUPERIDONE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53325 Ki = 0.38 nM 9.42
CHEMBL61479 SIRAMESINE Ki = 17.0 nM 7.77
CHEMBL4846092 Ki = 63.0 nM 7.20
CHEMBL5395401 Ki = 530.0 nM 6.28
CHEMBL5426155 Ki = 560.0 nM 6.25
CHEMBL5189158 Ki = 1279.0 nM 5.89
CHEMBL4297605 ROLUPERIDONE Ki >= 1000.0 nM -