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Assay Detail

CHEMBL5138110

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

Binding
Inhibition of 6xHis-tagged rat DYRK1A (1 to 502 residues) expressed in Escherichia coli BL21(DE3) using FKHR as substrate incubated for 30 mins in presence of ATP by UFLC based analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

DYRK1A inhibitors for disease therapy: Current status and perspectives.
Liu T, Wang Y, Wang J, Ren C, Chen H, Zhang J.
Eur J Med Chem (2022) 229 : 114062 -114062
PubMed 34954592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.47 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4292553 1 7.68
CHEMBL5196629 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4292553 IC50 = 20.7 nM 7.68
CHEMBL5196629 IC50 = 56.6 nM 7.25