| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
|---|
| Ligand | BDBM586336 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | Alexa Fret |
|---|
| IC50 | 50±n/a nM |
|---|
| 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 |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
|---|
| Name: | Proprotein convertase subtilisin/kexin type 9/Low-density lipoprotein receptor |
|---|
| Synonyms: | Human PCSK9 / LDLR complex |
|---|
| Type: | Protein |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | n/a |
|---|
| Components: | This complex has 2 components. |
|---|
| Component 1 |
| 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
|
|
|
|---|
| Component 2 |
| Name: | Low-density lipoprotein receptor |
|---|
| Synonyms: | LDL receptor | LDLR | LDLR_HUMAN | Low-density lipoprotein receptor |
|---|
| Type: | PROTEIN |
|---|
| Mol. Mass.: | 95343.42 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | ChEMBL_99545 |
|---|
| Residue: | 860 |
|---|
| Sequence: | MGPWGWKLRWTVALLLAAAGTAVGDRCERNEFQCQDGKCISYKWVCDGSAECQDGSDESQ
ETCLSVTCKSGDFSCGGRVNRCIPQFWRCDGQVDCDNGSDEQGCPPKTCSQDEFRCHDGK
CISRQFVCDSDRDCLDGSDEASCPVLTCGPASFQCNSSTCIPQLWACDNDPDCEDGSDEW
PQRCRGLYVFQGDSSPCSAFEFHCLSGECIHSSWRCDGGPDCKDKSDEENCAVATCRPDE
FQCSDGNCIHGSRQCDREYDCKDMSDEVGCVNVTLCEGPNKFKCHSGECITLDKVCNMAR
DCRDWSDEPIKECGTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDIDECQD
PDTCSQLCVNLEGGYKCQCEEGFQLDPHTKACKAVGSIAYLFFTNRHEVRKMTLDRSEYT
SLIPNLRNVVALDTEVASNRIYWSDLSQRMICSTQLDRAHGVSSYDTVISRDIQAPDGLA
VDWIHSNIYWTDSVLGTVSVADTKGVKRKTLFRENGSKPRAIVVDPVHGFMYWTDWGTPA
KIKKGGLNGVDIYSLVTENIQWPNGITLDLLSGRLYWVDSKLHSISSIDVNGGNRKTILE
DEKRLAHPFSLAVFEDKVFWTDIINEAIFSANRLTGSDVNLLAENLLSPEDMVLFHNLTQ
PRGVNWCERTTLSNGGCQYLCLPAPQINPHSPKFTCACPDGMLLARDMRSCLTEAEAAVA
TQETSTVRLKVSSTAVRTQHTTTRPVPDTSRLPGATPGLTTVEIVTMSHQALGDVAGRGN
EKKPSSVRALSIVLPIVLLVFLCLGVFLLWKNWRLKNINSINFDNPVYQKTTEDEVHICH
NQDGYSYPSRQMVSLEDDVA
|
|
|
|---|
| BDBM586336 |
|---|
| n/a |
|---|
| Name | BDBM586336 |
|---|
| Synonyms: | US11530244, Compound 507 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C68H84F2N10O13S2 |
|---|
| Mol. Mass. | 1351.581 |
|---|
| SMILES | CO[C@H](C)[C@@H]1NC(=O)[C@@H]2CC\C=C\COc3cccc(C[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)CCS(=O)Cc4cc(F)cc(CSCCNC(=O)[C@]5(C)CCCN5C(=O)[C@H](Cc5ccc(OC)cc5)NC1=O)c4)C(=O)N[C@@H](Cc1c[nH]c4ccc(F)cc14)C(=O)N2C)c3 |r,t:11| |
|---|
| Structure | 
|
|---|
Search and Browse
