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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM484630
Substrate
n/a
Meas. Tech.
Kinase Assay
EC50
2.00±n/a nM
Citation
 Kc, SK; Mak, CC; Mittapalli, GK; Hofilena, BJ; Eastman, BW; Cao, J; Chiruta, C; Bollu, V 5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof US Patent  US10934297 Publication Date 3/2/2021 
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:
BDBM484630
Synonyms:
US10934297, Compound 24 | US11713320, Compound 24
Type:
Small organic molecule
Emp. Form.:
C22H26F2N6O
Mol. Mass.:
428.4782
SMILES:
Cn1cc(cn1)-c1cc2c(n[nH]c2cc1F)C(=O)N[C@H]1CC[C@H](CN2CC(F)C2)CC1 |r,wU:22.25,wD:19.21,(-7.69,.41,;-7.29,-1.08,;-5.83,-1.56,;-5.83,-3.1,;-7.29,-3.57,;-8.2,-2.33,;-4.49,-3.87,;-3.16,-3.1,;-1.83,-3.87,;-.36,-3.39,;.54,-4.64,;-.36,-5.88,;-1.83,-5.41,;-3.16,-6.18,;-4.49,-5.41,;-5.83,-6.18,;.04,-1.9,;-1.05,-.81,;1.52,-1.51,;1.92,-.02,;3.41,.38,;3.81,1.87,;2.72,2.96,;3.12,4.44,;4.61,4.84,;5.94,4.07,;6.71,5.41,;8.2,5.81,;5.38,6.18,;1.23,2.56,;.83,1.07,)|
Structure:
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