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Target
Importin subunit alpha-1
Ligand
BDBM75014
Substrate
n/a
Meas. Tech.
Fluorescence Cell-Free Homogeneous Counterscreen to Identify Inhibitors of the RanGTP-Importin-beta complex.
EC50
>500000±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:
BDBM75014
Synonyms:
2-[2-[5-(4-bromophenyl)-3-(4-fluorophenyl)-3,4-dihydropyrazol-2-yl]-2-oxidanylidene-ethyl]sulfanyl-6,7-dihydro-5H-[1,3,4]thiadiazolo[3,2-a][1,3]diazepin-8-one | 2-[2-[5-(4-bromophenyl)-3-(4-fluorophenyl)-3,4-dihydropyrazol-2-yl]-2-oxoethyl]sulfanyl-6,7-dihydro-5H-[1,3,4]thiadiazolo[3,2-a][1,3]diazepin-8-one | 2-[[2-[3-(4-bromophenyl)-5-(4-fluorophenyl)-2-pyrazolin-1-yl]-2-keto-ethyl]thio]-6,7-dihydro-5H-[1,3,4]thiadiazolo[3,2-a][1,3]diazepin-8-one | 2-[[2-[5-(4-bromophenyl)-3-(4-fluorophenyl)-3,4-dihydropyrazol-2-yl]-2-oxoethyl]thio]-6,7-dihydro-5H-[1,3,4]thiadiazolo[3,2-a][1,3]diazepin-8-one | MLS000419107 | SMR000319827 | cid_5227427
Type:
Small organic molecule
Emp. Form.:
C23H19BrFN5O2S2
Mol. Mass.:
560.462
SMILES:
Fc1ccc(cc1)C1CC(=NN1C(=O)CSC1=NN2CCCC(=O)N=C2S1)c1ccc(Br)cc1 |c:10,26,t:18|
Structure:
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