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Assay Detail

CHEMBL4673836

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Binding
Inhibition of DYRK1A (unknown origin) by [33P]-ATP filter binding kinase assay
20
Total Activities
20
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

Probing the ATP-Binding Pocket of Protein Kinase DYRK1A with Benzothiazole Fragment Molecules.
Rothweiler U,Stensen W,Brandsdal BO,Isaksson J,Leeson FA,Engh RA,Svendsen JS
J Med Chem (2016) 59 : 9814 -9824
PubMed 27736065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.28 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1532203 1 6.40
CHEMBL1213041 1 6.16
CHEMBL4747967 1 6.10
CHEMBL4780479 1 5.96
CHEMBL4794978 1 5.96
CHEMBL4759909 1 5.89
CHEMBL1538954 1 5.64
CHEMBL4556783 1 5.54
CHEMBL4746739 1 5.50
CHEMBL4754469 1 5.41
CHEMBL4784222 1 5.14
CHEMBL4759082 1 4.98
CHEMBL1486796 1 4.91
CHEMBL4741377 1 4.80
CHEMBL2029515 1 4.63
CHEMBL4750244 1 4.58
CHEMBL4743605 1 4.55
CHEMBL4763711 1 4.53
CHEMBL4798633 1 4.46
CHEMBL2206133 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1532203 IC50 = 400.0 nM 6.40
CHEMBL1213041 IC50 = 700.0 nM 6.16
CHEMBL4747967 IC50 = 800.0 nM 6.10
CHEMBL4780479 IC50 = 1100.0 nM 5.96
CHEMBL4794978 IC50 = 1100.0 nM 5.96
CHEMBL4759909 IC50 = 1300.0 nM 5.89
CHEMBL1538954 IC50 = 2300.0 nM 5.64
CHEMBL4556783 IC50 = 2900.0 nM 5.54
CHEMBL4746739 IC50 = 3200.0 nM 5.50
CHEMBL4754469 IC50 = 3900.0 nM 5.41
CHEMBL4784222 IC50 = 7300.0 nM 5.14
CHEMBL4759082 IC50 = 10500.0 nM 4.98
CHEMBL1486796 IC50 = 12300.0 nM 4.91
CHEMBL4741377 IC50 = 15700.0 nM 4.80
CHEMBL2029515 IC50 = 23600.0 nM 4.63
CHEMBL4750244 IC50 = 26500.0 nM 4.58
CHEMBL4743605 IC50 = 28100.0 nM 4.55
CHEMBL4763711 IC50 = 29300.0 nM 4.53
CHEMBL4798633 IC50 = 35000.0 nM 4.46
CHEMBL2206133 IC50 = 36000.0 nM 4.44