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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM385228
Substrate
n/a
Meas. Tech.
Z-lyte Assay
EC50
0.800±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  US10556885 Publication Date 2/11/2020 
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:
BDBM385228
Synonyms:
US10287267, Compound 528 | US10508099, Compound 528 | US10556885, Compound 528 | US11174244, Compound 528 | US11673881, Compound 528
Type:
Small organic molecule
Emp. Form.:
C21H24N4O2
Mol. Mass.:
364.4409
SMILES:
CO[C@H]1CC[C@@H](CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cncn1C |r,wU:2.1,wD:5.8,(8.57,3.49,;8.57,1.95,;7.23,1.18,;7.19,-.38,;5.85,-1.15,;4.52,-.38,;4.52,1.15,;5.85,1.93,;3.19,-1.15,;3.19,-2.69,;1.85,-.38,;.52,-1.15,;-.82,-.38,;-2.15,-1.15,;-3.48,-.38,;-4.82,-1.15,;-4.82,-2.69,;-3.48,-3.47,;-2.15,-2.69,;-.82,-3.47,;.52,-2.69,;-6.15,-.38,;-7.61,-.86,;-8.52,.38,;-7.61,1.63,;-6.15,1.15,;-4.82,1.93,)|
Structure:
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