Reaction Details
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Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM5655
Substrate
n/a
Meas. Tech.
ChEMBL_819992 (CHEMBL2032667)
IC50
300±n/a nM
Citation
Nguyen, TB; Lozach, O; Surpateanu, G; Wang, Q; Retailleau, P; Iorga, BI; Meijer, L; Guéritte, F Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases. J Med Chem 55:2811-9 (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:
BDBM5655
Synonyms:
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]-4H-chromen-4-one | CHEMBL428690 | Flavopiridol | US10294218, Example Flavopiridol | US9617225, Flavopiridol
Type:
Small organic molecule
Emp. Form.:
C21H20ClNO5
Mol. Mass.:
401.84
SMILES:
CN1CC[C@@H]([C@H](O)C1)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccccc1Cl |r|
Structure:
