Reaction Details
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Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM7287
Substrate
n/a
Meas. Tech.
ChEMBL_749963 (CHEMBL1786940)
IC50
>10000±n/a nM
Citation
Power, DP; Lozach, O; Meijer, L; Grayson, DH; Connon, SJ Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones. Bioorg Med Chem Lett 20:4940-4 (2010) [PubMed] Article More Info.:
Target
Name:
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Synonyms:
DYR1A_RAT | Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A | Dyrk | Dyrk1a
Type:
Enzyme Catalytic Domain
Mol. Mass.:
85573.59
Organism:
RAT
Description:
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A 0 RAT::Q63470
Residue:
763
Sequence:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
Inhibitor
Name:
BDBM7287
Synonyms:
8,18-diazatetracyclo[9.7.0.0^{2,7}.0^{12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaen-9-one | CHEMBL430574 | NSC 641166 | Paullone
Type:
Small organic molecule
Emp. Form.:
C16H12N2O
Mol. Mass.:
248.2793
SMILES:
O=C1Cc2c([nH]c3ccccc23)-c2ccccc2N1
Structure:
