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Target
Proprotein convertase subtilisin/kexin type 9
Ligand
BDBM200318
Substrate
n/a
Meas. Tech.
ChEMBL_2151768 (CHEMBL5036230)
IC50
780±n/a nM
Citation
 Chappie, TA; Abdelmessih, M; Ambroise, CW; Boehm, M; Cai, M; Green, M; Guilmette, E; Steppan, CM; Stevens, LM; Wei, L; Xi, S; Hasson, SA Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators. ACS Med Chem Lett 13:55-62 (2022) [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:
BDBM200318
Synonyms:
US9227956, 3
Type:
Small organic molecule
Emp. Form.:
C23H22ClN7O
Mol. Mass.:
447.92
SMILES:
Cc1cnc2n(nnc2c1)-c1ccc(cc1)C(=O)N([C@@H]1CCCNC1)c1ncccc1Cl |r|
Structure:
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