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Assay Detail

CHEMBL5328508

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Binding
Binding affinity to S1R (unknown origin)
3
Total Activities
3
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 AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.
Dichiara M, Ambrosio FA, Lee SM, Ruiz-Cantero MC, Lombino J, Coricello A, Costa G, Shah D, Costanzo G, Pasquinucci L, Son KN, Cosentino G, González-Cano R, Marrazzo A, Aakalu VK, Cobos EJ, Alcaro S, Amata E.
J Med Chem (2023) 66 : 11447 -11463
PubMed 37535861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.22 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5432062 1 10.89
CHEMBL5402927 1 8.72
CHEMBL39900 SPIPETHIANE 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5432062 Ki = 0.013 nM 10.89
CHEMBL5402927 Ki = 1.9 nM 8.72
CHEMBL39900 SPIPETHIANE Ki = 9.2 nM 8.04