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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50538084
Substrate
n/a
Meas. Tech.
ChEMBL_1972143 (CHEMBL4604961)
IC50
6.0±n/a nM
Citation
 Liu, YA; Jin, Q; Zou, Y; Ding, Q; Yan, S; Wang, Z; Hao, X; Nguyen, B; Zhang, X; Pan, J; Mo, T; Jacobsen, K; Lam, T; Wu, TY; Petrassi, HM; Bursulaya, B; DiDonato, M; Gordon, WP; Liu, B; Baaten, J; Hill, R; Nguyen-Tran, V; Qiu, M; Zhang, YQ; Kamireddy, A; Espinola, S; Deaton, L; Ha, S; Harb, G; Jia, Y; Li, J; Shen, W; Schumacher, AM; Colman, K; Glynne, R; Pan, S; McNamara, P; Laffitte, B; Meeusen, S; Molteni, V; Loren, J Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J Med Chem 63:2958-2973 (2020) [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:
BDBM50538084
Synonyms:
CHEMBL4647659
Type:
Small organic molecule
Emp. Form.:
C25H27FN6O4
Mol. Mass.:
494.5181
SMILES:
CC(C)Oc1ccc(F)c(c1)-c1cnc(N)c(n1)C(=O)Nc1cnccc1N1CCC[C@H](C1)C(O)=O |r|
Structure:
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