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Assay Detail

CHEMBL5338152

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant GST-fused human DYRK1A expressed in Escherichia coli using myelin basic protein as substrate incubated for 10 mins by liquid scintillation counting method
1
Total Activities
1
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

Publication

Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
Ţînţaş ML, Peauger L, Barré A, Papamicaël C, Besson T, Sopkovà-de Oliveira Santos J, Gembus V, Levacher V.
RSC Med Chem (2024) 15 : 963 -980
PubMed 38516603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.62 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1232500 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1232500 IC50 = 240.0 nM 6.62