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Assay Detail

CHEMBL5034571

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Binding
Inhibition of DYRK2 (unknown origin) by ADP hunter plus assay
10
Total Activities
10
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

Fragment-Derived Selective Inhibitors of Dual-Specificity Kinases DYRK1A and DYRK1B.
Lee Walmsley D, Murray JB, Dokurno P, Massey AJ, Benwell K, Fiumana A, Foloppe N, Ray S, Smith J, Surgenor AE, Edmonds T, Demarles D, Burbridge M, Cruzalegui F, Kotschy A, Hubbard RE.
J Med Chem (2021) 64 : 8971 -8991
PubMed 34143631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.21 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5082044 1 7.85
CHEMBL5083159 1 7.85
CHEMBL5088687 1 7.52
CHEMBL5073598 1 7.30
CHEMBL5081341 1 7.22
CHEMBL5093650 1 7.10
CHEMBL5092157 1 6.82
CHEMBL5092828 1 6.68
CHEMBL5092245 1 6.52
CHEMBL5078833 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5082044 IC50 = 14.0 nM 7.85
CHEMBL5083159 IC50 = 14.0 nM 7.85
CHEMBL5088687 IC50 = 30.0 nM 7.52
CHEMBL5073598 IC50 = 50.0 nM 7.30
CHEMBL5081341 IC50 = 60.0 nM 7.22
CHEMBL5093650 IC50 = 80.0 nM 7.10
CHEMBL5092157 IC50 = 150.0 nM 6.82
CHEMBL5092828 IC50 = 210.0 nM 6.68
CHEMBL5092245 IC50 = 300.0 nM 6.52
CHEMBL5078833 IC50 > 10000.0 nM -