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Target
Importin subunit alpha-1
Ligand
BDBM75025
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
9416±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:
BDBM75025
Synonyms:
4-[4-(dimethylamino)phenyl]-1-methyl-2-(methylthio)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile | 4-[4-(dimethylamino)phenyl]-1-methyl-2-(methylthio)-6-oxo-5-pyrimidinecarbonitrile | 4-[4-(dimethylamino)phenyl]-1-methyl-2-methylsulfanyl-6-oxidanylidene-pyrimidine-5-carbonitrile | 4-[4-(dimethylamino)phenyl]-1-methyl-2-methylsulfanyl-6-oxopyrimidine-5-carbonitrile | 4-[4-(dimethylamino)phenyl]-6-keto-1-methyl-2-(methylthio)pyrimidine-5-carbonitrile | MLS000766800 | SMR000339696 | cid_694212
Type:
Small organic molecule
Emp. Form.:
C15H16N4OS
Mol. Mass.:
300.379
SMILES:
CSc1nc(-c2ccc(cc2)N(C)C)c(C#N)c(=O)n1C
Structure:
Search PDB for entries with ligand similarity: