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TargetProprotein convertase subtilisin/kexin type 9
LigandBDBM50554737
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2050524 (CHEMBL4705223)
Ki 6.3±n/a nM
Citation Alleyne, CAmin, RPBhatt, BBianchi, EBlain, JCBoyer, NBranca, DEmbrey, MWHa, SNJette, KJohns, DGKerekes, ADKoeplinger, KALaPlaca, DLi, NMurphy, BOrth, PRicardo, ASalowe, SSeyb, KShahripour, AStringer, JRSun, YTracy, RWu, CXiong, YYoum, HZokian, HJTucker, TJ Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design. J Med Chem63:13796-13824 (2020) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Proprotein convertase subtilisin/kexin type 9
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:
MGTVSSRRSWWPLPLLLLLLLLLGPAGARAQEDEDGDYEELVLALRSEEDGLAEAPEHGT
TATFHRCAKDPWRLPGTYVVVLKEETHLSQSERTARRLQAQAARRGYLTKILHVFHGLLP
GFLVKMSGDLLELALKLPHVDYIEEDSSVFAQSIPWNLERITPPRYRADEYQPPDGGSLV
EVYLLDTSIQSDHREIEGRVMVTDFENVPEEDGTRFHRQASKCDSHGTHLAGVVSGRDAG
VAKGASMRSLRVLNCQGKGTVSGTLIGLEFIRKSQLVQPVGPLVVLLPLAGGYSRVLNAA
CQRLARAGVVLVTAAGNFRDDACLYSPASAPEVITVGATNAQDQPVTLGTLGTNFGRCVD
LFAPGEDIIGASSDCSTCFVSQSGTSQAAAHVAGIAAMMLSAEPELTLAELRQRLIHFSA
KDVINEAWFPEDQRVLTPNLVAALPPSTHGAGWQLFCRTVWSAHSGPTRMATAVARCAPD
EELLSCSSFSRSGKRRGERMEAQGGKLVCRAHNAFGGEGVYAIARCCLLPQANCSVHTAP
PAEASMGTRVHCHQQGHVLTGCSSHWEVEDLGTHKPPVLRPRGQPNQCVGHREASIHASC
CHAPGLECKVKEHGIPAPQEQVTVACEEGWTLTGCSALPGTSHVLGAYAVDNTCVVRSRD
VSTTGSTSEGAVTAVAICCRSRHLAQASQELQ
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  Blast E-value cutoff:
BDBM50554737
n/a
NameBDBM50554737
Synonyms:CHEMBL4776000
TypeSmall organic molecule
Emp. Form.C71H86F2N14O12S2
Mol. Mass.1429.656
SMILESCC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)CCSCc2cccc(CSCCNC(=O)[C@]3(C)CCCN3C(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc3c[nH]c4ccc(F)cc34)NC(=O)[C@H](Cc3c[nH]c4ccc(F)cc34)NC1=O)c2 |r|
Structure
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