Target
Importin subunit alpha-1
Ligand
BDBM74552
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
15960±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:
BDBM74552
Synonyms:
6-Methyl-2-[4-(thiophene-2-carbonyl)-piperazin-1-yl]-quinoline-3-carbonitrile | 6-methyl-2-(4-thiophen-2-ylcarbonylpiperazin-1-yl)quinoline-3-carbonitrile | 6-methyl-2-[4-(2-thenoyl)piperazino]quinoline-3-carbonitrile | 6-methyl-2-[4-(thiophene-2-carbonyl)piperazin-1-yl]quinoline-3-carbonitrile | 6-methyl-2-[4-[oxo(thiophen-2-yl)methyl]-1-piperazinyl]-3-quinolinecarbonitrile | MLS000029929 | SMR000005589 | cid_648602
Type:
Small organic molecule
Emp. Form.:
C20H18N4OS
Mol. Mass.:
362.448
SMILES:
Cc1ccc2nc(N3CCN(CC3)C(=O)c3cccs3)c(cc2c1)C#N
Structure:
Search PDB for entries with ligand similarity: