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Target
Proteasome subunit beta type-8
Ligand
BDBM50069989
Substrate
n/a
Meas. Tech.
ChEMBL_2027962 (CHEMBL4682120)
IC50
2.0±n/a nM
Citation
 Xie, SC; Gillett, DL; Spillman, NJ; Tsu, C; Luth, MR; Ottilie, S; Duffy, S; Gould, AE; Hales, P; Seager, BA; Charron, CL; Bruzzese, F; Yang, X; Zhao, X; Huang, SC; Hutton, CA; Burrows, JN; Winzeler, EA; Avery, VM; Dick, LR; Tilley, L Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome. J Med Chem 61:10053-10066 (2018) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM50069989
Synonyms:
(R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid | (R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-6-carboxamido)propanamido)butylboronic acid | BORTEZOMIB | CHEMBL325041 | Dipeptidyl boronic acid derivative | LDP-341 | N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE | PS-341 | Peptidyl boronic acid derivative | US11542283, Compound Velcade | Velcade | cid_387447
Type:
Small organic molecule
Emp. Form.:
C19H25BN4O4
Mol. Mass.:
384.237
SMILES:
CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1cnccn1)B(O)O |r|
Structure:
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