Target
Importin subunit alpha-1
Ligand
BDBM75032
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
13840±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:
BDBM75032
Synonyms:
MLS000691962 | N,N-dimethyl-N'-[7-(2-thienyl)[1,2,4]triazolo[1,5-a]pyrimidin-2-yl]iminoformamide | N,N-dimethyl-N'-(7-thiophen-2-yl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methanimidamide | N,N-dimethyl-N'-[7-(2-thienyl)-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl]formamidine | SMR000334002 | cid_2767358
Type:
Small organic molecule
Emp. Form.:
C12H12N6S
Mol. Mass.:
272.329
SMILES:
CN(C)C=Nc1nc2nccc(-c3cccs3)n2n1
Structure:
Search PDB for entries with ligand similarity: