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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50596124
Substrate
n/a
Meas. Tech.
ChEMBL_2219461 (CHEMBL5132795)
IC50
4000±n/a nM
Citation
 Miyazaki, Y; Kikuchi, M; Umezawa, K; Descamps, A; Nakamura, D; Furuie, G; Sumida, T; Saito, K; Kimura, N; Niwa, T; Sumida, Y; Umehara, T; Hosoya, T; Kii, I Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A. Eur J Med Chem 227:0 (2022) [PubMed]  Article
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:
BDBM50596124
Synonyms:
CHEMBL5173788
Type:
Small organic molecule
Emp. Form.:
C31H23NO2S2Si
Mol. Mass.:
533.735
SMILES:
[#6]-[#8]-c1ccc(\[#6]=[#6]-2/[#16]-[#6](=S)-[#7]-[#6]-2=O)cc1C#C[Si;v4](c1ccccc1)(c1ccccc1)c1ccccc1
Structure:
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