| Reaction Details |
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 | Report a problem with these data |
| Target | Proprotein convertase subtilisin/kexin type 9 |
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| Ligand | BDBM50581540 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2151333 (CHEMBL5035795) |
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| Ki | 0.230000±n/a nM |
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| Citation |  Tucker, TJ; Embrey, MW; Alleyne, C; Amin, RP; Bass, A; Bhatt, B; Bianchi, E; Branca, D; Bueters, T; Buist, N; Ha, SN; Hafey, M; He, H; Higgins, J; Johns, DG; Kerekes, AD; Koeplinger, KA; Kuethe, JT; Li, N; Murphy, B; Orth, P; Salowe, S; Shahripour, A; Tracy, R; Wang, W; Wu, C; Xiong, Y; Zokian, HJ; Wood, HB; Walji, A A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors. J Med Chem64:16770-16800 (2021) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Proprotein convertase subtilisin/kexin type 9 |
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| Name: | Proprotein convertase subtilisin/kexin type 9 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 74286.93 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q8NBP7 |
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| Residue: | 692 |
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| Sequence: | MGTVSSRRSWWPLPLLLLLLLLLGPAGARAQEDEDGDYEELVLALRSEEDGLAEAPEHGT
TATFHRCAKDPWRLPGTYVVVLKEETHLSQSERTARRLQAQAARRGYLTKILHVFHGLLP
GFLVKMSGDLLELALKLPHVDYIEEDSSVFAQSIPWNLERITPPRYRADEYQPPDGGSLV
EVYLLDTSIQSDHREIEGRVMVTDFENVPEEDGTRFHRQASKCDSHGTHLAGVVSGRDAG
VAKGASMRSLRVLNCQGKGTVSGTLIGLEFIRKSQLVQPVGPLVVLLPLAGGYSRVLNAA
CQRLARAGVVLVTAAGNFRDDACLYSPASAPEVITVGATNAQDQPVTLGTLGTNFGRCVD
LFAPGEDIIGASSDCSTCFVSQSGTSQAAAHVAGIAAMMLSAEPELTLAELRQRLIHFSA
KDVINEAWFPEDQRVLTPNLVAALPPSTHGAGWQLFCRTVWSAHSGPTRMATAVARCAPD
EELLSCSSFSRSGKRRGERMEAQGGKLVCRAHNAFGGEGVYAIARCCLLPQANCSVHTAP
PAEASMGTRVHCHQQGHVLTGCSSHWEVEDLGTHKPPVLRPRGQPNQCVGHREASIHASC
CHAPGLECKVKEHGIPAPQEQVTVACEEGWTLTGCSALPGTSHVLGAYAVDNTCVVRSRD
VSTTGSTSEGAVTAVAICCRSRHLAQASQELQ
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| BDBM50581540 |
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| n/a |
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| Name | BDBM50581540 |
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| Synonyms: | CHEMBL5087487 |
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| Type | Small organic molecule |
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| Emp. Form. | C69H86FN11O12S2 |
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| Mol. Mass. | 1344.616 |
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| SMILES | CO[C@@H](C)[C@@H]1NC(=O)[C@@H]2[C@@H]3CCN2C(=O)[C@H](Cc2c[nH]c4ccc(F)cc24)NC(=O)[C@H](Cc2cccc(C\C=C\CO3)c2)NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)CCSCc2cccc(CSCCNC(=O)[C@]3(C)CCCN3C(=O)[C@H](Cc3ccc(OC)cc3)NC1=O)c2 |r,t:41| |
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| Structure | 
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