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Assay Detail

CHEMBL5378550

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

Binding
Binding affinity to human DYRK1A assessed as dissociation constant
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

Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Lindberg MF, Deau E, Miege F, Greverie M, Roche D, George N, George P, Merlet L, Gavard J, Brugman SJT, Aret E, Tinnemans P, de Gelder R, Sadownik J, Verhofstad E, Sleegers D, Santangelo S, Dairou J, Fernandez-Blanco Á, Dierssen M, Krämer A, Knapp S, Meijer L.
J Med Chem (2023) 66 : 15648 -15670
PubMed 38051674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.85 9.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- 1.0 1 9.56
CHEMBL1802358 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- Kd = 0.276 nM 9.56
CHEMBL1802358 Kd = 7.236 nM 8.14