Reaction Details  Report a problem with these data
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50251505
Substrate
n/a
Meas. Tech.
ChEBML_1683762
IC50
2142±n/a nM
Citation
 Shaw, SJ; Goff, DA; Lin, N; Singh, R; Li, W; McLaughlin, J; Baltgalvis, KA; Payan, DG; Kinsella, TM Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. Bioorg Med Chem Lett 27:2617-2621 (2017) [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:
BDBM50251505
Synonyms:
CHEMBL4068096
Type:
Small organic molecule
Emp. Form.:
C14H13N3O
Mol. Mass.:
239.2725
SMILES:
COc1cccc2c(c[nH]c12)-c1ccnc(N)c1
Structure:
Search PDB for entries with ligand similarity: