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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM484632
Substrate
n/a
Meas. Tech.
Kinase Assay
EC50
5.00±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:
BDBM484632
Synonyms:
US10934297, Compound 26 | US11713320, Compound 26
Type:
Small organic molecule
Emp. Form.:
C24H29FN6O
Mol. Mass.:
436.5251
SMILES:
FC1CN(C[C@H]2CC[C@@H](CC2)NC(=O)c2n[nH]c3ccc(cc23)-c2cnn(c2)C2CC2)C1 |r,wU:5.4,wD:8.11,(8.49,5.81,;7,5.41,;6.23,4.07,;4.9,4.84,;3.41,4.44,;3.01,2.96,;4.1,1.87,;3.7,.38,;2.21,-.02,;1.13,1.07,;1.52,2.56,;1.82,-1.51,;.33,-1.9,;-.76,-.81,;-.07,-3.39,;.83,-4.64,;-.07,-5.88,;-1.54,-5.41,;-2.87,-6.18,;-4.2,-5.41,;-4.2,-3.87,;-2.87,-3.1,;-1.54,-3.87,;-5.54,-3.1,;-7,-3.57,;-7.91,-2.33,;-7,-1.08,;-5.54,-1.56,;-7.4,.41,;-7,1.89,;-8.49,1.5,;5.67,6.18,)|
Structure:
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