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Target
Proprotein convertase subtilisin/kexin type 9
Ligand
BDBM537759
Substrate
n/a
Meas. Tech.
SPR Assay
Kd
1100±n/a nM
Citation
 Serrano-Wu, MH; Hubbard, BK; Kaushik, V; Daniels, D PCSK9 inhibitors and methods of use thereof US Patent  US11603523 Publication Date 3/14/2023 
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:
BDBM537759
Synonyms:
US11248001, Example 166 | US11603523, Example 166
Type:
Small organic molecule
Emp. Form.:
C16H17N5OS
Mol. Mass.:
327.404
SMILES:
CSc1cnc(N[C@H]2C[C@@H](C2)Nc2nc3ccccc3o2)nc1 |r,wU:7.6,wD:9.11,(-8.65,-1.43,;-7.32,-2.2,;-5.98,-1.43,;-5.98,.11,;-4.65,.88,;-3.32,.11,;-1.98,.88,;-.65,.11,;.84,.51,;1.24,-.98,;-.25,-1.38,;2.57,-1.75,;3.9,-.98,;4.07,.55,;5.57,.87,;6.34,2.2,;7.88,2.2,;8.65,.87,;7.88,-.46,;6.34,-.46,;5.31,-1.61,;-3.32,-1.43,;-4.65,-2.2,)|
Structure:
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