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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM439136
Substrate
n/a
Meas. Tech.
Kinase Assay
EC50
16.0±n/a nM
Citation
 KC, SK; Mittapalli, GK; Chiruta, C; Hofilena, BJ; Mak, CC; Eastman, BW; Bollu, V 6-(5-membered heteroaryl)isoquinolin-3-yl carboxamides and preparation and use thereof US Patent  US10604514 Publication Date 3/31/2020 
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:
BDBM439136
Synonyms:
US10604514, Compound 12
Type:
Small organic molecule
Emp. Form.:
C25H31N5O2
Mol. Mass.:
433.5459
SMILES:
CN1CCN(CC1)[C@H]1CC[C@@H](CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1coc(C)n1 |r,wU:7.7,wD:10.14,(11.29,3.85,;9.96,3.08,;9.96,1.54,;8.62,.77,;7.29,1.54,;7.29,3.08,;8.62,3.85,;5.96,.77,;5.96,-.77,;4.62,-1.54,;3.29,-.77,;3.29,.77,;4.62,1.54,;1.95,-1.54,;1.95,-3.08,;.62,-.77,;-.71,-1.54,;-2.05,-.77,;-3.38,-1.54,;-4.71,-.77,;-6.05,-1.54,;-6.05,-3.08,;-4.71,-3.85,;-3.38,-3.08,;-2.05,-3.85,;-.71,-3.08,;-7.38,-.77,;-7.38,.77,;-8.85,1.25,;-9.75,,;-11.29,,;-8.85,-1.25,)|
Structure:
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