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Target
Proprotein convertase subtilisin/kexin type 9
Ligand
BDBM50565593
Substrate
n/a
Meas. Tech.
ChEMBL_2092914 (CHEMBL4774177)
EC50
40±n/a nM
Citation
 Xie, H; Yang, K; Winston-McPherson, GN; Stapleton, DS; Keller, MP; Attie, AD; Smith, KA; Tang, W From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators. Eur J Med Chem 206:0 (2020) [PubMed]  Article 
Target
Name:
Proprotein convertase subtilisin/kexin type 9
Synonyms:
NARC-1 | NARC1 | Neural apoptosis-regulated convertase 1 | PC9 | PCSK9 | PCSK9_HUMAN | Proprotein convertase 9 | Proprotein convertase subtilisin/kexin type 9 | Proprotein convertase subtilisin/kexin type 9 (PCSK9) | Subtilisin/kexin type 9 | Subtilisin/kexin-like protease PC9
Type:
Enzyme
Mol. Mass.:
74286.93
Organism:
Homo sapiens (Human)
Description:
Q8NBP7
Residue:
692
Sequence:
MGTVSSRRSWWPLPLLLLLLLLLGPAGARAQEDEDGDYEELVLALRSEEDGLAEAPEHGTTATFHRCAKDPWRLPGTYVVVLKEETHLSQSERTARRLQAQAARRGYLTKILHVFHGLLPGFLVKMSGDLLELALKLPHVDYIEEDSSVFAQSIPWNLERITPPRYRADEYQPPDGGSLVEVYLLDTSIQSDHREIEGRVMVTDFENVPEEDGTRFHRQASKCDSHGTHLAGVVSGRDAGVAKGASMRSLRVLNCQGKGTVSGTLIGLEFIRKSQLVQPVGPLVVLLPLAGGYSRVLNAACQRLARAGVVLVTAAGNFRDDACLYSPASAPEVITVGATNAQDQPVTLGTLGTNFGRCVDLFAPGEDIIGASSDCSTCFVSQSGTSQAAAHVAGIAAMMLSAEPELTLAELRQRLIHFSAKDVINEAWFPEDQRVLTPNLVAALPPSTHGAGWQLFCRTVWSAHSGPTRMATAVARCAPDEELLSCSSFSRSGKRRGERMEAQGGKLVCRAHNAFGGEGVYAIARCCLLPQANCSVHTAPPAEASMGTRVHCHQQGHVLTGCSSHWEVEDLGTHKPPVLRPRGQPNQCVGHREASIHASCCHAPGLECKVKEHGIPAPQEQVTVACEEGWTLTGCSALPGTSHVLGAYAVDNTCVVRSRDVSTTGSTSEGAVTAVAICCRSRHLAQASQELQ
  
Inhibitor
Name:
BDBM50565593
Synonyms:
CHEMBL4779800
Type:
Small organic molecule
Emp. Form.:
C24H24F2N4O2
Mol. Mass.:
438.4698
SMILES:
Cn1c(nc2ccc(F)cc12)C(=O)c1cn(CCCN2CCOCC2)c2c(F)cccc12
Structure:
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