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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM518768
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:
BDBM518768
Synonyms:
(3-methoxy-4-((4- methoxyethyl) (methyl)amino)-3- (trifluoromethyl)- 1H-pyrrolo[2,3- b]pyridin-6- yl)amino)phenyl) (morpholino) methanone | US11117892, Example 87
Type:
Small organic molecule
Emp. Form.:
C24H28F3N5O4
Mol. Mass.:
507.5054
SMILES:
COCCN(C)c1cc(Nc2ccc(cc2OC)C(=O)N2CCOCC2)nc2[nH]cc(c12)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: