| Reaction Details |
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 | Report a problem with these data |
| Target | Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
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| Ligand | BDBM586440 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Alexa Fret |
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| IC50 | 50±n/a nM |
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| Citation |  Ricardo, A; Tucker, TJ; Boyer, NC; Stringer, JR; LaPlaca, DM; Kerekes, AD; Wu, C; Ha, SN; Youm, H; Embrey, MW; Bianchi, E; Branca, D; Ingenito, R; Costantini, W; Santoprete, A; Costante, R; Conte, I; Colarusso, S; Gilbert, EJ; Shahripour, A; Xiong, Y Cyclic polypeptides for PCSK9 inhibition US Patent US11530244 Publication Date 12/20/2022 |
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| More Info.: | Get all data from this article, Assay Method |
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| Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
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| Name: | Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
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| Synonyms: | Human PCSK9 / LDLR complex |
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| Type: | Protein |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 2 components. |
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| Component 1 |
| 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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| Component 2 |
| Name: | Low-density lipoprotein receptor |
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| Synonyms: | LDL receptor | LDLR | LDLR_HUMAN | Low-density lipoprotein receptor |
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| Type: | PROTEIN |
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| Mol. Mass.: | 95343.42 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_99545 |
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| Residue: | 860 |
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| Sequence: | MGPWGWKLRWTVALLLAAAGTAVGDRCERNEFQCQDGKCISYKWVCDGSAECQDGSDESQ
ETCLSVTCKSGDFSCGGRVNRCIPQFWRCDGQVDCDNGSDEQGCPPKTCSQDEFRCHDGK
CISRQFVCDSDRDCLDGSDEASCPVLTCGPASFQCNSSTCIPQLWACDNDPDCEDGSDEW
PQRCRGLYVFQGDSSPCSAFEFHCLSGECIHSSWRCDGGPDCKDKSDEENCAVATCRPDE
FQCSDGNCIHGSRQCDREYDCKDMSDEVGCVNVTLCEGPNKFKCHSGECITLDKVCNMAR
DCRDWSDEPIKECGTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDIDECQD
PDTCSQLCVNLEGGYKCQCEEGFQLDPHTKACKAVGSIAYLFFTNRHEVRKMTLDRSEYT
SLIPNLRNVVALDTEVASNRIYWSDLSQRMICSTQLDRAHGVSSYDTVISRDIQAPDGLA
VDWIHSNIYWTDSVLGTVSVADTKGVKRKTLFRENGSKPRAIVVDPVHGFMYWTDWGTPA
KIKKGGLNGVDIYSLVTENIQWPNGITLDLLSGRLYWVDSKLHSISSIDVNGGNRKTILE
DEKRLAHPFSLAVFEDKVFWTDIINEAIFSANRLTGSDVNLLAENLLSPEDMVLFHNLTQ
PRGVNWCERTTLSNGGCQYLCLPAPQINPHSPKFTCACPDGMLLARDMRSCLTEAEAAVA
TQETSTVRLKVSSTAVRTQHTTTRPVPDTSRLPGATPGLTTVEIVTMSHQALGDVAGRGN
EKKPSSVRALSIVLPIVLLVFLCLGVFLLWKNWRLKNINSINFDNPVYQKTTEDEVHICH
NQDGYSYPSRQMVSLEDDVA
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| BDBM586440 |
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| n/a |
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| Name | BDBM586440 |
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| Synonyms: | US11530244, Compound 437 |
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| Type | Small organic molecule |
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| Emp. Form. | C58H61F2N13O12 |
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| Mol. Mass. | 1170.1816 |
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| SMILES | NC(=O)[C@@H]1Cc2ccc(CNC(=O)CCCC(=O)NCC(=O)N[C@@H](Cc3c[nH]c4ccc(F)cc34)C(=O)N[C@@H](Cc3c[nH]c4ccc(F)cc34)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N1)cc2 |r| |
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| Structure | 
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