Target
Proprotein convertase subtilisin/kexin type 9
Ligand
BDBM537763
Substrate
n/a
Meas. Tech.
SPR Assay
Kd
1100±n/a nM
Citation
 Serrano-Wu, MHHubbard, BKKaushik, VDaniels, 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:
BDBM537763
Synonyms:
US11248001, Example 170 | US11603523, Example 170
Type:
Small organic molecule
Emp. Form.:
C19H21N5O2S2
Mol. Mass.:
415.532
SMILES:
CCOC(=O)c1ccc2nc(N[C@H]3C[C@@H](C3)Nc3ncc(SC)cn3)sc2c1 |r,wU:12.11,wD:14.16,(10.58,3.54,;9.04,3.54,;8.27,2.2,;6.73,2.2,;5.96,3.54,;5.96,.87,;6.73,-.46,;5.96,-1.8,;4.42,-1.8,;3.39,-2.94,;1.98,-2.32,;.65,-3.09,;-.69,-2.32,;-2.18,-2.71,;-2.57,-1.23,;-1.09,-.83,;-3.91,-.46,;-5.24,-1.23,;-6.58,-.46,;-7.91,-1.23,;-7.91,-2.77,;-9.24,-3.54,;-10.58,-2.77,;-6.58,-3.54,;-5.24,-2.77,;2.14,-.78,;3.65,-.46,;4.42,.87,)|
Structure:
Search PDB for entries with ligand similarity: