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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM518780
Substrate
n/a
Meas. Tech.
Enzyme Activity Assay
IC50
55±n/a nM
Citation
 Choi, HG; Ko, E; Cho, J; Son, JB; Ko, YK; Park, J; Kim, SY; Kang, SY; Lee, S; Ryu, HY; Kim, ND; Kim, SB; Lee, S; Kim, D; Lee, SJ; Cho, S; Lee, K; Yu, K; Choi, M; Koo, JW; Hoe, H Pyrrolo-pyridine derivative compound, method for preparing same, and pharmaceutical composition containing same as active ingredient for prevention or treatment of protein kinase-related diseases US Patent  US11117892 Publication Date 9/14/2021 
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:
BDBM518780
Synonyms:
(4-((4- (cyclopropylamino)- 3- (trifluoromethyl)- 1-((2- (trimethylsilyl) ethoxy)methyl)- 1H-pyrrolo[2,3- b]pyridin-6-yl)3- methoxyphenyl) (4- morpholino- piperidine-1- yl)methanone | US11117892, Example 94
Type:
Small organic molecule
Emp. Form.:
C28H33F3N6O3
Mol. Mass.:
558.5952
SMILES:
COc1cc(ccc1Nc1cc(NC2CC2)c2c(c[nH]c2n1)C(F)(F)F)C(=O)N1CCC(CC1)N1CCOCC1
Structure:
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