Compound name
Leucettine L41
Protein family
Protein Kinase
Target name
DYRK1A
Affinity biochemical (nM)
7.8
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001025a
SMILES
O=C1N=C(NC2=CC=CC=C2)N/C1=C\C3=CC=C4C(OCO4)=C3
InChIKey
PGPHHJBZEGSUNE-JYRVWZFOSA-N
NCBI gene ID
1859
UniProt ID
Q13627
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
Kd ELECT competition-binding assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/jm301034u
Affinity biochemical relation
=
Selectivity platform
KINOMEscan (DiscoverX)
Selectivity platform number of targets
402
Selectivity remarks
Screened at 10 µM, closest targets as % of control: CLK3 (2%), GSK3A (9.8%), HIPK1/3 (0.75%/ 3.8%), IRAK1 (2.8%), TAOK1 (8.8%), TYK2(JH1 domain-pseudokinase) (9.0%); Kd follow-up by DiscoverX: Kd(CLK3) = 1100 nM, Kd(GSK3A) = 550 nM, Kd(HIPK1/3) = 320 /230 nM, Kd(IRAK1) = 930 nM, Kd(TAOK1) = 1700 nM; Selective against 148 proteins from mouse brain (Competition Affinity Chromatography (KinAffinity, by Kinaxo Biotechnologies, Evotec)), closest targets: Kd,free(SLK) = 21 nM, Kd,free(DYRK1A) = 65 nM, Kd,free(CSNK2A1) = 326 nM, Kd,free(CSNK2N) = 382 nM, others > 500 nM
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/jm301034u
Selectivity Number of Off-targets
6