Target
Proteasome subunit beta type-8
Ligand
BDBM50277889
Substrate
n/a
Meas. Tech.
ChEMBL_502029 (CHEMBL981240)
IC50
14±n/a nM
Citation
 Zhou, HJAujay, MABennett, MKDajee, MDemo, SDFang, YHo, MNJiang, JKirk, CJLaidig, GJLewis, ERLu, YMuchamuel, TParlati, FRing, EShenk, KDShields, JShwonek, PJStanton, TSun, CMSylvain, CWoo, TMYang, 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 
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:
BDBM50277889
Synonyms:
CARFILZOMIB | CHEMBL451887
Type:
Small organic molecule
Emp. Form.:
C40H57N5O7
Mol. Mass.:
719.9099
SMILES:
CC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1 |r|
Structure:
Search PDB for entries with ligand similarity: