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Target
Importin subunit alpha-1
Ligand
BDBM75085
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
1581±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:
BDBM75085
Synonyms:
(E)-2-Cyano-3-(9-methyl-4-oxo-2-phenoxy-4H-pyrido[1,2-a]pyrimidin-3-yl)-acrylamide | (E)-2-cyano-3-(4-keto-9-methyl-2-phenoxy-pyrido[1,2-a]pyrimidin-3-yl)acrylamide | (E)-2-cyano-3-(9-methyl-4-oxidanylidene-2-phenoxy-pyrido[1,2-a]pyrimidin-3-yl)prop-2-enamide | (E)-2-cyano-3-(9-methyl-4-oxo-2-phenoxy-3-pyrido[1,2-a]pyrimidinyl)-2-propenamide | (E)-2-cyano-3-(9-methyl-4-oxo-2-phenoxypyrido[1,2-a]pyrimidin-3-yl)prop-2-enamide | MLS000333249 | SMR000436562 | cid_946759
Type:
Small organic molecule
Emp. Form.:
C19H14N4O3
Mol. Mass.:
346.3395
SMILES:
Cc1cccn2c1nc(Oc1ccccc1)c(\C=C(/C#N)C(N)=O)c2=O
Structure:
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