Reaction Details |
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Target | Proprotein convertase subtilisin/kexin type 9 |
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Ligand | BDBM50554731 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2050524 (CHEMBL4705223) |
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Ki | 4.0±n/a nM |
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Citation | Alleyne, C; Amin, RP; Bhatt, B; Bianchi, E; Blain, JC; Boyer, N; Branca, D; Embrey, MW; Ha, SN; Jette, K; Johns, DG; Kerekes, AD; Koeplinger, KA; LaPlaca, D; Li, N; Murphy, B; Orth, P; Ricardo, A; Salowe, S; Seyb, K; Shahripour, A; Stringer, JR; Sun, Y; Tracy, R; Wu, C; Xiong, Y; Youm, H; Zokian, HJ; Tucker, TJ Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design. J Med Chem63:13796-13824 (2020) [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 |
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: | MGTVSSRRSWWPLPLLLLLLLLLGPAGARAQEDEDGDYEELVLALRSEEDGLAEAPEHGT
TATFHRCAKDPWRLPGTYVVVLKEETHLSQSERTARRLQAQAARRGYLTKILHVFHGLLP
GFLVKMSGDLLELALKLPHVDYIEEDSSVFAQSIPWNLERITPPRYRADEYQPPDGGSLV
EVYLLDTSIQSDHREIEGRVMVTDFENVPEEDGTRFHRQASKCDSHGTHLAGVVSGRDAG
VAKGASMRSLRVLNCQGKGTVSGTLIGLEFIRKSQLVQPVGPLVVLLPLAGGYSRVLNAA
CQRLARAGVVLVTAAGNFRDDACLYSPASAPEVITVGATNAQDQPVTLGTLGTNFGRCVD
LFAPGEDIIGASSDCSTCFVSQSGTSQAAAHVAGIAAMMLSAEPELTLAELRQRLIHFSA
KDVINEAWFPEDQRVLTPNLVAALPPSTHGAGWQLFCRTVWSAHSGPTRMATAVARCAPD
EELLSCSSFSRSGKRRGERMEAQGGKLVCRAHNAFGGEGVYAIARCCLLPQANCSVHTAP
PAEASMGTRVHCHQQGHVLTGCSSHWEVEDLGTHKPPVLRPRGQPNQCVGHREASIHASC
CHAPGLECKVKEHGIPAPQEQVTVACEEGWTLTGCSALPGTSHVLGAYAVDNTCVVRSRD
VSTTGSTSEGAVTAVAICCRSRHLAQASQELQ
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BDBM50554731 |
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n/a |
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Name | BDBM50554731 |
Synonyms: | CHEMBL4789480 |
Type | Small organic molecule |
Emp. Form. | C69H81F2N15O13S2 |
Mol. Mass. | 1430.601 |
SMILES | C[C@@]12CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1c[nH]c3ccc(F)cc13)NC(=O)[C@H](Cc1c[nH]c3ccc(F)cc13)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CCSCc1cccc(CSC[C@H](NC2=O)C(N)=O)c1 |r| |
Structure |
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