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Target
Proteasome subunit beta type-8
Ligand
BDBM50277733
Substrate
n/a
Meas. Tech.
ChEMBL_502029 (CHEMBL981240)
IC50
238±n/a nM
Citation
Zhou, HJ; Aujay, MA; Bennett, MK; Dajee, M; Demo, SD; Fang, Y; Ho, MN; Jiang, J; Kirk, CJ; Laidig, GJ; Lewis, ER; Lu, Y; Muchamuel, T; Parlati, F; Ring, E; Shenk, KD; Shields, J; Shwonek, PJ; Stanton, T; Sun, CM; Sylvain, C; Woo, TM; Yang, J Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem 52:3028-38 (2009) [PubMed] Article
More Info.:
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:
BDBM50277733
Synonyms:
(2S)-3-methoxy-2-[(2S)-3-methoxy-2-[(5-methyl-1,2-oxazol-3-yl)formamido]propanamido]-N-[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]propanamide | CHEMBL484156
Type:
Small organic molecule
Emp. Form.:
C22H34N4O8
Mol. Mass.:
482.5274
SMILES:
COC[C@H](NC(=O)[C@H](COC)NC(=O)c1cc(C)on1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1 |r|