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Assay Detail

CHEMBL5034580

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

Binding
Inhibition of DYRK3 (unknown origin) by TR FRET assay
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

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 2 7.19 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088687 1 7.52
CHEMBL5093650 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088687 IC50 = 30.0 nM 7.52
CHEMBL5093650 IC50 = 140.0 nM 6.85