Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM293540
Substrate
n/a
Meas. Tech.
The DYRK1A kinase assa
Temperature
298.15±n/a K
EC50
1.40±n/a nM
Comments
extracted
Citation
 KC, SKMak, CCEastman, BWCao, JBollu, VMittapalli, GKChiruta, C Isoquinolin-3-yl carboxamides and preparation and use thereof US Patent  US10106527 Publication Date 10/23/2018 
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:
BDBM293540
Synonyms:
US10106527, Compound 222 | US10544128, Compound 222 | US11548872, Compound 222 | US20230286945, Compound 222 | US9951048, Compound 222
Type:
Small organic molecule
Emp. Form.:
C28H31FN8O
Mol. Mass.:
514.5971
SMILES:
CN1CCN(CC1)c1ccc(cn1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn2CCN(CCF)Cc12
Structure:
Search PDB for entries with ligand similarity: