Assay Detail

CHEMBL5378545

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Binding

Inhibition of human DYRK1A using DYRKtide peptide as substrate measured after 70 mins by ADP-GloTM luminescence proximity assay

ChEMBL ↗

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Target

Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗

Open DB target context

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Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Dual specificity tyrosine-phosphorylation-regulated kinase 1A

CHEMBL2292

Anchored from Assay target.

Protein identity Dual specificity tyrosine-phosphorylation-regulated kinase 1A

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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
IC50	1	8.66	8.66

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	8.66

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)-	IC50	=	2.2	nM	8.66