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Target
A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436
Ligand
BDBM50595627
Substrate
n/a
Meas. Tech.
ChEMBL_2217291 (CHEMBL5130423)
IC50
>10000±n/a nM
Citation
 Koester, DC; Marx, VM; Williams, S; Jiricek, J; Dauphinais, M; René, O; Miller, SL; Zhang, L; Patra, D; Chen, YL; Cheung, H; Gable, J; Lakshminarayana, SB; Osborne, C; Galarneau, JR; Kulkarni, U; Richmond, W; Bretz, A; Xiao, L; Supek, F; Wiesmann, C; Honnappa, S; Be, C; Mäser, P; Kaiser, M; Ritchie, R; Barrett, MP; Diagana, TT; Sarko, C; Rao, SPS Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT). J Med Chem 65:11776-11787 (2022) [PubMed]  Article
Target
Name:
A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436
Synonyms:
20S proteasome | 26S proteosome
Type:
n/a
Mol. Mass.:
n/a
Description:
Combinations of UniProts
Components:
This complex has 19 components.
Component 1
Name:
Proteasome subunit beta type-2
Synonyms:
20S proteasome | PSB2_HUMAN | PSMB2 | Proteasome Macropain subunit
Type:
PROTEIN
Mol. Mass.:
22837.53
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1294233
Residue:
201
Sequence:
MEYLIGIQGPDYVLVASDRVAASNIVQMKDDHDKMFKMSEKILLLCVGEAGDTVQFAEYIQKNVQLYKMRNGYELSPTAAANFTRRNLADCLRSRTPYHVNLLLAGYDEHEGPALYYMDYLAALAKAPFAAHGYGAFLTLSILDRYYTPTISRERAVELLRKCLEELQKRFILNLPTFSVRIIDKNGIHDLDNISFPKQGS
  
Component 2
Name:
Proteasome subunit beta type-1
Synonyms:
PSB1_HUMAN | PSC5 | PSMB1 | Proteasome component C5 | Proteasome subunit beta type-1/beta type-5
Type:
PROTEIN
Mol. Mass.:
26493.62
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1366691
Residue:
241
Sequence:
MLSSTAMYSAPGRDLGMEPHRAAGPLQLRFSPYVFNGGTILAIAGEDFAIVASDTRLSEGFSIHTRDSPKCYKLTDKTVIGCSGFHGDCLTLTKIIEARLKMYKHSNNKAMTTGAIAAMLSTILYSRRFFPYYVYNIIGGLDEEGKGAVYSFDPVGSYQRDSFKAGGSASAMLQPLLDNQVGFKNMQNVEHVPLSLDRAMRLVKDVFISAAERDVYTGDALRICIVTKEGIREETVSLRKD
  
Component 3
Name:
Proteasome subunit beta type-5
Synonyms:
20S proteasome chymotrypsin-like | 26S proteosome | LMPX | MB1 | PSB5_HUMAN | PSMB5 | Proteasome Macropain subunit MB1 | Proteasome subunit beta type-1/beta type-5 | X
Type:
Protein
Mol. Mass.:
28480.96
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
263
Sequence:
MALASVLERPLPVNQRGFFGLGGRADLLDLGPGSLSDGLSLAAPGWGVPEEPGIEMLHGTTTLAFKFRHGVIVAADSRATAGAYIASQTVKKVIEINPYLLGTMAGGAADCSFWERLLARQCRIYELRNKERISVAAASKLLANMVYQYKGMGLSMGTMICGWDKRGPGLYYVDSEGNRISGATFSVGSGSVYAYGVMDRGYSYDLEVEQAYDLARRAIYQATYRDAYSGGAVNLYHVREDGWIRVSSDNVADLHEKYSGSTP
  
Component 4
Name:
Proteasome subunit beta type-8
Synonyms:
26S proteosome | LMP7 | Low molecular mass protein 7 | Macropain subunit C13 | Multicatalytic endopeptidase complex subunit C13 | PSB8_HUMAN | PSMB5i | PSMB8 | Proteasome component C13 | Proteasome subunit beta type-8 | Proteasome subunit beta-5i | RING10 | Y2
Type:
PROTEIN
Mol. Mass.:
30357.49
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1446797
Residue:
276
Sequence:
MALLDVCGAPRGQRPESALPVAGSGRRSDPGHYSFSMRSPELALPRGMQPTEFFQSLGGDGERNVQIEMAHGTTTLAFKFQHGVIAAVDSRASAGSYISALRVNKVIEINPYLLGTMSGCAADCQYWERLLAKECRLYYLRNGERISVSAASKLLSNMMCQYRGMGLSMGSMICGWDKKGPGLYYVDEHGTRLSGNMFSTGSGNTYAYGVMDSGYRPNLSPEEAYDLGRRAIAYATHRDSYSGGVVNMYHMKEDGWVKVESTDVSDLLHQYREANQ
  
Component 5
Name:
Proteasome subunit beta type-9
Synonyms:
LMP2 | Low molecular mass protein 2 | Macropain chain 7 | Multicatalytic endopeptidase complex chain 7 | PSB9_HUMAN | PSMB6i | PSMB9 | Proteasome chain 7 | Proteasome subunit beta-1i | RING12 | Really interesting new gene 12 protein
Type:
PROTEIN
Mol. Mass.:
23256.49
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
219
Sequence:
MLRAGAPTGDLPRAGEVHTGTTIMAVEFDGGVVMGSDSRVSAGEAVVNRVFDKLSPLHERIYCALSGSAADAQAVADMAAYQLELHGIELEEPPLVLAAANVVRNISYKYREDLSAHLMVAGWDQREGGQVYGTLGGMLTRQPFAIGGSGSTFIYGYVDAAYKPGMSPEECRRFTTDAIALAMSRDGSSGGVIYLVTITAAGVDHRVILGNELPKFYDE
  
Component 6
Name:
Proteasome subunit beta type-6
Synonyms:
LMPY | Macropain delta chain | Multicatalytic endopeptidase complex delta chain | PSB6_HUMAN | PSMB6 | Proteasome delta chain | Proteasome subunit Y | Y
Type:
PROTEIN
Mol. Mass.:
25349.89
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
239
Sequence:
MAATLLAARGAGPAPAWGPEAFTPDWESREVSTGTTIMAVQFDGGVVLGADSRTTTGSYIANRVTDKLTPIHDRIFCCRSGSAADTQAVADAVTYQLGFHSIELNEPPLVHTAASLFKEMCYRYREDLMAGIIIAGWDPQEGGQVYSVPMGGMMVRQSFAIGGSGSSYIYGYVDATYREGMTKEECLQFTANALALAMERDGSSGGVIRLAAIAESGVERQVLLGDQIPKFAVATLPPA
  
Component 7
Name:
Proteasome subunit alpha type-1
Synonyms:
30 kDa prosomal protein | HC2 | Macropain subunit C2 | Multicatalytic endopeptidase complex subunit C2 | NU | PROS-30 | PROS30 | PSA1_HUMAN | PSC2 | PSMA1 | Proteasome component C2 | Proteasome nu chain
Type:
PROTEIN
Mol. Mass.:
29555.77
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
263
Sequence:
MFRNQYDNDVTVWSPQGRIHQIEYAMEAVKQGSATVGLKSKTHAVLVALKRAQSELAAHQKKILHVDNHIGISIAGLTADARLLCNFMRQECLDSRFVFDRPLPVSRLVSLIGSKTQIPTQRYGRRPYGVGLLIAGYDDMGPHIFQTCPSANYFDCRAMSIGARSQSARTYLERHMSEFMECNLNELVKHGLRALRETLPAEQDLTTKNVSIGIVGKDLEFTIYDDDDVSPFLEGLEERPQRKAQPAQPADEPAEKADEPMEH
  
Component 8
Name:
Proteasome subunit alpha type-2
Synonyms:
HC3 | Macropain subunit C3 | Multicatalytic endopeptidase complex subunit C3 | PSA2_HUMAN | PSC3 | PSMA2 | Proteasome component C3
Type:
PROTEIN
Mol. Mass.:
25900.29
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
234
Sequence:
MAERGYSFSLTTFSPSGKLVQIEYALAAVAGGAPSVGIKAANGVVLATEKKQKSILYDERSVHKVEPITKHIGLVYSGMGPDYRVLVHRARKLAQQYYLVYQEPIPTAQLVQRVASVMQEYTQSGGVRPFGVSLLICGWNEGRPYLFQSDPSGAYFAWKATAMGKNYVNGKTFLEKRYNEDLELEDAIHTAILTLKESFEGQMTEDNIEVGICNEAGFRRLTPTEVKDYLAAIA
  
Component 9
Name:
Proteasome subunit alpha type-3
Synonyms:
HC8 | Macropain subunit C8 | Multicatalytic endopeptidase complex subunit C8 | PSA3_HUMAN | PSC8 | PSMA3 | Proteasome component C8
Type:
PROTEIN
Mol. Mass.:
28426.36
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
255
Sequence:
MSSIGTGYDLSASTFSPDGRVFQVEYAMKAVENSSTAIGIRCKDGVVFGVEKLVLSKLYEEGSNKRLFNVDRHVGMAVAGLLADARSLADIAREEASNFRSNFGYNIPLKHLADRVAMYVHAYTLYSAVRPFGCSFMLGSYSVNDGAQLYMIDPSGVSYGYWGCAIGKARQAAKTEIEKLQMKEMTCRDIVKEVAKIIYIVHDEVKDKAFELELSWVGELTNGRHEIVPKDIREEAEKYAKESLKEEDESDDDNM
  
Component 10
Name:
Proteasome subunit alpha type-4
Synonyms:
HC9 | Macropain subunit C9 | Multicatalytic endopeptidase complex subunit C9 | PSA4_HUMAN | PSC9 | PSMA4 | Proteasome component C9 | Proteasome subunit L
Type:
PROTEIN
Mol. Mass.:
29486.50
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
261
Sequence:
MSRRYDSRTTIFSPEGRLYQVEYAMEAIGHAGTCLGILANDGVLLAAERRNIHKLLDEVFFSEKIYKLNEDMACSVAGITSDANVLTNELRLIAQRYLLQYQEPIPCEQLVTALCDIKQAYTQFGGKRPFGVSLLYIGWDKHYGFQLYQSDPSGNYGGWKATCIGNNSAAAVSMLKQDYKEGEMTLKSALALAIKVLNKTMDVSKLSAEKVEIATLTRENGKTVIRVLKQKEVEQLIKKHEEEEAKAEREKKEKEQKEKDK
  
Component 11
Name:
Proteasome subunit alpha type-5
Synonyms:
Macropain zeta chain | Multicatalytic endopeptidase complex zeta chain | PSA5_HUMAN | PSMA5 | Proteasome zeta chain
Type:
PROTEIN
Mol. Mass.:
26398.14
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
241
Sequence:
MFLTRSEYDRGVNTFSPEGRLFQVEYAIEAIKLGSTAIGIQTSEGVCLAVEKRITSPLMEPSSIEKIVEIDAHIGCAMSGLIADAKTLIDKARVETQNHWFTYNETMTVESVTQAVSNLALQFGEEDADPGAMSRPFGVALLFGGVDEKGPQLFHMDPSGTFVQCDARAIGSASEGAQSSLQEVYHKSMTLKEAIKSSLIILKQVMEEKLNATNIELATVQPGQNFHMFTKEELEEVIKDI
  
Component 12
Name:
Proteasome subunit alpha type-6
Synonyms:
27 kDa prosomal protein | Macropain iota chain | Multicatalytic endopeptidase complex iota chain | PROS-27 | PROS27 | PSA6_HUMAN | PSMA6 | Proteasome iota chain | p27K
Type:
PROTEIN
Mol. Mass.:
27399.66
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
246
Sequence:
MSRGSSAGFDRHITIFSPEGRLYQVEYAFKAINQGGLTSVAVRGKDCAVIVTQKKVPDKLLDSSTVTHLFKITENIGCVMTGMTADSRSQVQRARYEAANWKYKYGYEIPVDMLCKRIADISQVYTQNAEMRPLGCCMILIGIDEEQGPQVYKCDPAGYYCGFKATAAGVKQTESTSFLEKKVKKKFDWTFEQTVETAITCLSTVLSIDFKPSEIEVGVVTVENPKFRILTEAEIDAHLVALAERD
  
Component 13
Name:
Proteasome subunit alpha type-7
Synonyms:
HSPC | PSA7_HUMAN | PSMA7 | Proteasome subunit RC6-1 | Proteasome subunit XAPC7
Type:
PROTEIN
Mol. Mass.:
27891.04
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
248
Sequence:
MSYDRAITVFSPDGHLFQVEYAQEAVKKGSTAVGVRGRDIVVLGVEKKSVAKLQDERTVRKICALDDNVCMAFAGLTADARIVINRARVECQSHRLTVEDPVTVEYITRYIASLKQRYTQSNGRRPFGISALIVGFDFDGTPRLYQTDPSGTYHAWKANAIGRGAKSVREFLEKNYTDEAIETDDLTIKLVIKALLEVVQSGGKNIELAVMRRDQSLKILNPEEIEKYVAEIEKEKEENEKKKQKKAS
  
Component 14
Name:
Proteasome subunit alpha-type 8
Synonyms:
PSMA7L | PSMA8 | PSMA8_HUMAN | Proteasome subunit alpha type-7-like
Type:
PROTEIN
Mol. Mass.:
28537.53
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
256
Sequence:
MASRYDRAITVFSPDGHLFQVEYAQEAVKKGSTAVGIRGTNIVVLGVEKKSVAKLQDERTVRKICALDDHVCMAFAVLTIFIGLTADARVVINRARVECQSHKLTVEDPVTVEYITRFIATLKQKYTQSNGRRPFGISALIVGFDDDGISRLYQTDPSGTYHAWKANAIGRSAKTVREFLEKNYTEDAIASDSEAIKLAIKALLEVVQSGGKNIELAIIRRNQPLKMFSAKEVELYVTEIEKEKEEAEKKKSKKSV
  
Component 15
Name:
Proteasome subunit beta type-10
Synonyms:
LMP10 | Low molecular mass protein 10 | MECL1 | Macropain subunit MECl-1 | Multicatalytic endopeptidase complex subunit MECl-1 | PSB10_HUMAN | PSMB10 | Proteasome MECl-1 | Proteasome subunit beta-2i
Type:
PROTEIN
Mol. Mass.:
28940.51
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
273
Sequence:
MLKPALEPRGGFSFENCQRNASLERVLPGLKVPHARKTGTTIAGLVFQDGVILGADTRATNDSVVADKSCEKIHFIAPKIYCCGAGVAADAEMTTRMVASKMELHALSTGREPRVATVTRILRQTLFRYQGHVGASLIVGGVDLTGPQLYGVHPHGSYSRLPFTALGSGQDAALAVLEDRFQPNMTLEAAQGLLVEAVTAGILGDLGSGGNVDACVITKTGAKLLRTLSSPTEPVKRSGRYHFVPGTTAVLTQTVKPLTLELVEETVQAMEVE
  
Component 16
Name:
Proteasome subunit beta type-11
Synonyms:
PSB11_HUMAN | PSMB11 | Proteasome subunit beta-5t
Type:
PROTEIN
Mol. Mass.:
32529.58
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
300
Sequence:
MALQDVCKWQSPDTQGPSPHLPRAGGWAVPRGCDPQTFLQIHGPRLAHGTTTLAFRFRHGVIAAADTRSSCGSYVACPASCKVIPVHQHLLGTTSGTSADCATWYRVLQRELRLRELREGQLPSVASAAKLLSAMMSQYRGLDLCVATALCGWDRSGPELFYVYSDGTRLQGDIFSVGSGSPYAYGVLDRGYRYDMSTQEAYALARCAVAHATHRDAYSGGSVDLFHVRESGWEHVSRSDACVLYVELQKLLEPEPEEDASHAHPEPATAHRAAEDRELSVGPGEVTPGDSRMPAGTETV
  
Component 17
Name:
Proteasome subunit beta type-3
Synonyms:
PSB3_HUMAN | PSMB3 | Proteasome chain 13 | Proteasome component C10-II | Proteasome theta chain
Type:
PROTEIN
Mol. Mass.:
22948.68
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
205
Sequence:
MSIMSYNGGAVMAMKGKNCVAIAADRRFGIQAQMVTTDFQKIFPMGDRLYIGLAGLATDVQTVAQRLKFRLNLYELKEGRQIKPYTLMSMVANLLYEKRFGPYYTEPVIAGLDPKTFKPFICSLDLIGCPMVTDDFVVSGTCAEQMYGMCESLWEPNMDPDHLFETISQAMLNAVDRDAVSGMGVIVHIIEKDKITTRTLKARMD
  
Component 18
Name:
Proteasome subunit beta type-4
Synonyms:
26 kDa prosomal protein | HsBPROS26 | HsN3 | Macropain beta chain | Multicatalytic endopeptidase complex beta chain | PROS-26 | PROS26 | PSB4_HUMAN | PSMB4 | Proteasome beta chain | Proteasome chain 3
Type:
PROTEIN
Mol. Mass.:
29202.40
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
264
Sequence:
MEAFLGSRSGLWAGGPAPGQFYRIPSTPDSFMDPASALYRGPITRTQNPMVTGTSVLGVKFEGGVVIAADMLGSYGSLARFRNISRIMRVNNSTMLGASGDYADFQYLKQVLGQMVIDEELLGDGHSYSPRAIHSWLTRAMYSRRSKMNPLWNTMVIGGYADGESFLGYVDMLGVAYEAPSLATGYGAYLAQPLLREVLEKQPVLSQTEARDLVERCMRVLYYRDARSYNRFQIATVTEKGVEIEGPLSTETNWDIAHMISGFE
  
Component 19
Name:
Proteasome subunit beta type-7
Synonyms:
Macropain chain Z | Multicatalytic endopeptidase complex chain Z | PSB7_HUMAN | PSMB7 | Proteasome subunit Z | Z
Type:
PROTEIN
Mol. Mass.:
29968.13
Organism:
Homo sapiens (Human)
Description:
ChEMBL_106197
Residue:
277
Sequence:
MAAVSVYAPPVGGFSFDNCRRNAVLEADFAKRGYKLPKVRKTGTTIAGVVYKDGIVLGADTRATEGMVVADKNCSKIHFISPNIYCCGAGTAADTDMTTQLISSNLELHSLSTGRLPRVVTANRMLKQMLFRYQGYIGAALVLGGVDVTGPHLYSIYPHGSTDKLPYVTMGSGSLAAMAVFEDKFRPDMEEEEAKNLVSEAIAAGIFNDLGSGSNIDLCVISKNKLDFLRPYTVPNKKGTRLGRYRCEKGTTAVLTEKITPLEIEVLEETVQTMDTS
  
Inhibitor
Name:
BDBM50595627
Synonyms:
CHEMBL5205510
Type:
Small organic molecule
Emp. Form.:
C18H19F2N3O2
Mol. Mass.:
347.3592
SMILES:
C\C=C\c1cnc(cc1Nc1ccccc1F)C(=O)NC[C@@H](F)CO |r|
Structure:
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