Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM518775
Substrate
n/a
Meas. Tech.
Enzyme Activity Assay
IC50
55±n/a nM
Citation
 Choi, HGKo, ECho, JSon, JBKo, YKPark, JKim, SYKang, SYLee, SRyu, HYKim, NDKim, SBLee, SKim, DLee, SJCho, SLee, KYu, KChoi, MKoo, JWHoe, 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:
BDBM518775
Synonyms:
(R)-(4-((4-((1- hydroxy-3- methylbutan-2-yl) amino)-3- (trifluoromethyl)- 1H-pyrrolo[2,3- b]amino)-3- methoxyphenyl) (4-morpholino- piperidin-1-yl) methanone | US11117892, Example 91
Type:
Small organic molecule
Emp. Form.:
C30H39F3N6O4
Mol. Mass.:
604.6637
SMILES:
COc1cc(ccc1Nc1cc(N[C@@H](CO)C(C)C)c2c(c[nH]c2n1)C(F)(F)F)C(=O)N1CCC(CC1)N1CCOCC1 |r|
Structure:
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