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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50347750
Substrate
n/a
Meas. Tech.
ChEMBL_2214245 (CHEMBL5127377)
IC50
24±n/a nM
Citation
 Tahtouh, T; Durieu, E; Villiers, B; Bruyère, C; Nguyen, TL; Fant, X; Ahn, KH; Khurana, L; Deau, E; Lindberg, MF; Sévère, E; Miege, F; Roche, D; Limanton, E; L'Helgoual'ch, JM; Burgy, G; Guiheneuf, S; Herault, Y; Kendall, DA; Carreaux, F; Bazureau, JP; Meijer, L Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. J Med Chem 65:1396-1417 (2022) [PubMed] 
Target
Name:
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Synonyms:
DYR1A_HUMAN | DYRK | DYRK1A | Dual specificity YAK1-related kinase | Dual specificity YAK1-related kinase 1A (Dyrk1A) | Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) | Dual-specificity tyrosine-phosphorylation regulated kinase 1A | Dual-specificity tyrosine-regulated kinases 1A | HP86 | MNB | MNBH
Type:
Enzyme
Mol. Mass.:
85616.61
Organism:
Homo sapiens (Human)
Description:
Q13627
Residue:
763
Sequence:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
  
Inhibitor
Name:
BDBM50347750
Synonyms:
CHEMBL1802358
Type:
Small organic molecule
Emp. Form.:
C17H13N3O3
Mol. Mass.:
307.3034
SMILES:
O=C1NC(Nc2ccccc2)=NC1=Cc1ccc2OCOc2c1 |w:13.15,c:11|
Structure:
Search PDB for entries with ligand similarity: