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Target
Proteasome subunit beta type-10
Ligand
BDBM50526811
Substrate
n/a
Meas. Tech.
ChEMBL_1909305 (CHEMBL4411751)
IC50
623±n/a nM
Citation
 Johnson, HWB; Lowe, E; Anderl, JL; Fan, A; Muchamuel, T; Bowers, S; Moebius, DC; Kirk, C; McMinn, DL Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem 61:11127-11143 (2018) [PubMed]  Article 
Target
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
  
Inhibitor
Name:
BDBM50526811
Synonyms:
Kzr-616
Type:
Small organic molecule
Emp. Form.:
C30H42N4O8
Mol. Mass.:
586.6765
SMILES:
COc1ccc(cc1)[C@@H](O)[C@H](NC(=O)[C@H](C)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CCCC1)C(=O)[C@@]1(C)CO1 |t:33|
Structure:
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