Target
Importin subunit alpha-1
Ligand
BDBM75104
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
15420±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:
BDBM75104
Synonyms:
7-Methyl-2-[4-(3,4,5-trimethoxy-benzoyl)-[1,4]diazepan-1-yl]-quinoline-3-carbonitrile | 7-methyl-2-[4-(3,4,5-trimethoxybenzoyl)-1,4-diazepan-1-yl]quinoline-3-carbonitrile | 7-methyl-2-[4-(3,4,5-trimethoxyphenyl)carbonyl-1,4-diazepan-1-yl]quinoline-3-carbonitrile | 7-methyl-2-[4-[oxo-(3,4,5-trimethoxyphenyl)methyl]-1,4-diazepan-1-yl]-3-quinolinecarbonitrile | MLS000881240 | SMR000006851 | cid_646289
Type:
Small organic molecule
Emp. Form.:
C26H28N4O4
Mol. Mass.:
460.5249
SMILES:
COc1cc(cc(OC)c1OC)C(=O)N1CCCN(CC1)c1nc2cc(C)ccc2cc1C#N
Structure:
Search PDB for entries with ligand similarity: