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Target
Proprotein convertase subtilisin/kexin type 9
Ligand
BDBM50543443
Substrate
n/a
Meas. Tech.
ChEMBL_1989157 (CHEMBL4622704)
IC50
0.930000±n/a nM
Citation
 Sabnis, RW Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders. ACS Med Chem Lett 11:1671-1673 (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:
BDBM50543443
Synonyms:
CHEMBL4638184
Type:
Small organic molecule
Emp. Form.:
C48H56Cl2FN7O6
Mol. Mass.:
916.906
SMILES:
C[C@@H]1N(Cc2c(F)cc(Cl)cc2Oc2ccc(cc2)-c2cnc(CNC3CCC3)n2C)C(=O)C[C@@H](CC2CC2)C(=O)N2CCC[C@@](Cc3ccc(Cl)cc3)(C2)NC(=O)[C@H](CO)NC1=O |r|
Structure:
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