Reaction Details Report a problem with these data
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM385380
Substrate
n/a
Meas. Tech.
Kinase Assay
EC50
1.40±n/a nM
Citation
 KC, SK; Mittapalli, GK; Hofilena, BJ; Marakovits, JT; Chiruta, C; Mak, CC; Cao, J Isoquinolin-3-yl carboxamides and preparation and use thereof US Patent  US11174244 Publication Date 11/16/2021 
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:
BDBM385380
Synonyms:
US10287267, Compound 1091 | US11174244, Compound 1091 | US11673881, Compound 1091
Type:
Small organic molecule
Emp. Form.:
C26H32N6O2
Mol. Mass.:
460.5713
SMILES:
CN1CCN(CC1)C(=O)[C@H]1CC[C@@H](CC1)C(=O)Nc1cc2cc(ccc2cn1)-c1cnn(C)c1 |r,wU:12.16,wD:9.9,(11.19,-1.16,;9.85,-.39,;8.52,-1.16,;7.19,-.39,;7.19,1.16,;8.52,1.93,;9.85,1.16,;5.85,1.93,;5.85,3.47,;4.52,1.16,;3.19,1.93,;1.85,1.16,;1.85,-.39,;3.19,-1.16,;4.52,-.39,;.52,-1.16,;.52,-2.7,;-.82,-.39,;-2.15,-1.16,;-3.48,-.39,;-4.82,-1.16,;-6.15,-.39,;-7.48,-1.16,;-7.48,-2.7,;-6.15,-3.47,;-4.82,-2.7,;-3.48,-3.47,;-2.15,-2.7,;-8.82,-.39,;-10.28,-.86,;-11.19,.38,;-10.28,1.63,;-11.05,2.96,;-8.82,1.15,)|
Structure:
Search PDB for entries with ligand similarity: