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Assay Detail

CHEMBL5046166

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Binding
Inhibition of DYRK1B (unknown origin) measured after 6 hrs in presence of ATP by Z'-LYTE 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

Selective Macrocyclic Inhibitors of DYRK1A/B.
Powell CE, Hatcher JM, Jiang J, Vatsan PS, Che J, Gray NS.
ACS Med Chem Lett (2022) 13 : 577 -585
PubMed 35450378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.97 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5086263 1 8.30
CHEMBL5089965 1 7.75
CHEMBL5093741 1 7.72
CHEMBL5075321 1 7.26
CHEMBL5075335 1 7.16
CHEMBL5081601 1 6.84
CHEMBL5079894 1 6.82
CHEMBL5086482 1 6.27
CHEMBL5089643 1 6.03
CHEMBL5088208 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5086263 IC50 = 5.0 nM 8.30
CHEMBL5089965 IC50 = 18.0 nM 7.75
CHEMBL5093741 IC50 = 19.0 nM 7.72
CHEMBL5075321 IC50 = 55.0 nM 7.26
CHEMBL5075335 IC50 = 70.0 nM 7.16
CHEMBL5081601 IC50 = 146.0 nM 6.84
CHEMBL5079894 IC50 = 150.0 nM 6.82
CHEMBL5086482 IC50 = 533.0 nM 6.27
CHEMBL5089643 IC50 = 929.0 nM 6.03
CHEMBL5088208 IC50 = 3050.0 nM 5.52