Reaction Details
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Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50216159
Substrate
n/a
Meas. Tech.
ChEMBL_825077 (CHEMBL2045871)
IC50
200±n/a nM
Citation
Deslandes, S; Lamoral-Theys, D; Frongia, C; Chassaing, S; Bruyère, C; Lozach, O; Meijer, L; Ducommun, B; Kiss, R; Delfourne, E Synthesis and biological evaluation of analogs of the marine alkaloids granulatimide and isogranulatimide. Eur J Med Chem 54:626-36 (2012) [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:
BDBM50216159
Synonyms:
5-hydroxy-pyrrolo[3',4':5,6]indolizino[8,7-b]indole-1,3-(2H,8H)-dione | CHEMBL239698
Type:
Small organic molecule
Emp. Form.:
C16H9N3O3
Mol. Mass.:
291.261
SMILES:
Oc1ccc2[nH]c3c4cccn4c4C(=O)NC(=O)c4c3c2c1
Structure:
