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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM385200
Substrate
n/a
Meas. Tech.
The screening assay for DYRK1A kinase activity
EC50
2.70±n/a nM
Citation
 KC, SK; Mittapalli, GK; Hofilena, BJ; Marakovits, JT; Chiruta, C; Mak, CC; Cao, J Isoquinolin-3-yl carboxamides and preparation and use thereof US Patent  US10287267 Publication Date 5/14/2019 
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:
BDBM385200
Synonyms:
US10287267, Compound 365 | US10508099, Compound 365 | US10556885, Compound 365 | US11174244, Compound 365 | US11673881, Compound 365
Type:
Small organic molecule
Emp. Form.:
C20H23N5O
Mol. Mass.:
349.4295
SMILES:
Cn1cc(cn1)-c1ccc2cnc(NC(=O)[C@H]3CC[C@H](N)CC3)cc2c1 |r,wU:19.20,wD:16.16,(-8.38,3.21,;-7.61,1.88,;-6.15,1.41,;-6.15,-.13,;-7.61,-.61,;-8.52,.64,;-4.82,-.9,;-4.82,-2.44,;-3.48,-3.21,;-2.15,-2.44,;-.82,-3.21,;.52,-2.44,;.52,-.9,;1.85,-.13,;3.19,-.9,;3.19,-2.44,;4.52,-.13,;5.85,-.9,;7.19,-.13,;7.19,1.41,;8.52,2.18,;5.85,2.18,;4.52,1.41,;-.82,-.13,;-2.15,-.9,;-3.48,-.13,)|
Structure:
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