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Assay Detail

CHEMBL5251692

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Binding
Binding affinity to human C-terminal his tagged DYRK1A (26 to 490 residues) expressed in Escherichia coli at 5 uM by radiometric analysis
2
Total Activities
2
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

Silmitasertib (CX-4945), a Clinically Used CK2-Kinase Inhibitor with Additional Effects on GSK3β and DYRK1A Kinases: A Structural Perspective.
Grygier P, Pustelny K, Nowak J, Golik P, Popowicz GM, Plettenburg O, Dubin G, Menezes F, Czarna A.
J Med Chem (2023) 66 : 4009 -4024
PubMed 36883902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.31 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1230165 SILMITASERTIB 2.0 1 8.74
CHEMBL269538 HARMINE 1.0 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1230165 SILMITASERTIB Kd = 1.8 nM 8.74
CHEMBL269538 HARMINE Kd = 13.4 nM 7.87