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Assay Detail

CHEMBL5138107

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Binding
Inhibition of N-terminal GST-fused full-length human DYRK1A (1 to 763 residues) expressed in baculovirus expression system using myelin basic protein peptide as substrate preincubated with substrate for 40 mins followed by compound addition measured after 1 hr in presence of ATP by TR-FRET assay
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

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 1 7.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269538 HARMINE 1.0 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269538 HARMINE IC50 = 12.0 nM 7.92