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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50347747
Substrate
n/a
Meas. Tech.
ChEMBL_756286 (CHEMBL1805099)
IC50
110±n/a nM
Citation
 Debdab, M; Carreaux, F; Renault, S; Soundararajan, M; Fedorov, O; Filippakopoulos, P; Lozach, O; Babault, L; Tahtouh, T; Baratte, B; Ogawa, Y; Hagiwara, M; Eisenreich, A; Rauch, U; Knapp, S; Meijer, L; Bazureau, JP Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem 54:4172-86 (2011) [PubMed]  Article
Target
Name:
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Synonyms:
DYR1A_RAT | Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A | Dyrk | Dyrk1a
Type:
Enzyme Catalytic Domain
Mol. Mass.:
85573.59
Organism:
RAT
Description:
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A 0 RAT::Q63470
Residue:
763
Sequence:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
  
Inhibitor
Name:
BDBM50347747
Synonyms:
CHEMBL1802355
Type:
Small organic molecule
Emp. Form.:
C18H15N3O4
Mol. Mass.:
337.3294
SMILES:
COc1ccc(NC2=NC(=Cc3ccc4OCOc4c3)C(=O)N2)cc1 |w:10.10,t:7|
Structure:
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