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Target
Importin subunit alpha-1
Ligand
BDBM75097
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
5998±n/a nM
Citation
 PubChem, PC Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex. PubChem Bioassay (2010)[AID] 
Target
Name:
Importin subunit alpha-1
Synonyms:
IMA1_HUMAN | KPNA2 | RCH1 | SRP1 | karyopherin alpha 2 (RAG cohort 1, importin alpha 1), isoform CRA_b
Type:
Enzyme Catalytic Domain
Mol. Mass.:
57852.15
Organism:
Homo sapiens (Human)
Description:
gi_119609447
Residue:
529
Sequence:
MSTNENANTPAARLHRFKNKGKDSTEMRRRRIEVNVELRKAKKDDQMLKRRNVSSFPDDATSPLQENRNNQGTVNWSVDDIVKGINSSNVENQLQATQAARKLLSREKQPPIDNIIRAGLIPKFVSFLGRTDCSPIQFESAWALTNIASGTSEQTKAVVDGGAIPAFISLLASPHAHISEQAVWALGNIAGDGSVFRDLVIKYGAVDPLLALLAVPDMSSLACGYLRNLTWTLSNLCRNKNPAPPIDAVEQILPTLVRLLHHDDPEVLADTCWAISYLTDGPNERIGMVVKTGVVPQLVKLLGASELPIVTPALRAIGNIVTGTDEQTQVVIDAGALAVFPSLLTNPKTNIQKEATWTMSNITAGRQDQIQQVVNHGLVPFLVSVLSKADFKTQKEAVWAVTNYTSGGTVEQIVYLVHCGIIEPLMNLLTAKDTKIILVILDAISNIFQAAEKLGETEKLSIMIEECGGLDKIEALQNHENESVYKASLSLIEKYFSVEEEEDQNVVPETTSEGYTFQVQDGAPGTFNF
  
Inhibitor
Name:
BDBM75097
Synonyms:
(E)-2-Cyano-3-[2-(4-methoxy-phenoxy)-9-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]-acrylamide | (E)-2-cyano-3-[2-(4-methoxyphenoxy)-9-methyl-4-oxidanylidene-pyrido[1,2-a]pyrimidin-3-yl]prop-2-enamide | (E)-2-cyano-3-[2-(4-methoxyphenoxy)-9-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinyl]-2-propenamide | (E)-2-cyano-3-[2-(4-methoxyphenoxy)-9-methyl-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enamide | (E)-2-cyano-3-[4-keto-2-(4-methoxyphenoxy)-9-methyl-pyrido[1,2-a]pyrimidin-3-yl]acrylamide | MLS000333200 | SMR000436564 | cid_2025178
Type:
Small organic molecule
Emp. Form.:
C20H16N4O4
Mol. Mass.:
376.3654
SMILES:
COc1ccc(Oc2nc3c(C)cccn3c(=O)c2\C=C(/C#N)C(N)=O)cc1
Structure:
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