Target
Cathepsin E
Ligand
BDBM50305527
Substrate
n/a
Meas. Tech.
ChEMBL_604246 (CHEMBL1050391)
IC50
0.400000±n/a nM
Citation
 Lerchner, AMachauer, RBetschart, CVeenstra, SRueeger, HMcCarthy, CTintelnot-Blomley, MJaton, ALRabe, SDesrayaud, SEnz, AStaufenbiel, MPaganetti, PRondeau, JMNeumann, U Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application. Bioorg Med Chem Lett 20:603-7 (2010) [PubMed]  Article 
Target
Name:
Cathepsin E
Synonyms:
3.4.23.34 | CATE_HUMAN | CTSE | Cathepsin E form I | Cathepsin E form II
Type:
Enzyme
Mol. Mass.:
43298.99
Organism:
Homo sapiens (Human)
Description:
P14091
Residue:
396
Sequence:
MKTLLLLLLVLLELGEAQGSLHRVPLRRHPSLKKKLRARSQLSEFWKSHNLDMIQFTESCSMDQSAKEPLINYLDMEYFGTISIGSPPQNFTVIFDTGSSNLWVPSVYCTSPACKTHSRFQPSQSSTYSQPGQSFSIQYGTGSLSGIIGADQVSVEGLTVVGQQFGESVTEPGQTFVDAEFDGILGLGYPSLAVGGVTPVFDNMMAQNLVDLPMFSVYMSSNPEGGAGSELIFGGYDHSHFSGSLNWVPVTKQAYWQIALDNIQVGGTVMFCSEGCQAIVDTGTSLITGPSDKIKQLQNAIGAAPVDGEYAVECANLNVMPDVTFTINGVPYTLSPTAYTLLDFVDGMQFCSSGFQGLDIHPPAGPLWILGDVFIRQFYSVFDRGNNRVGLAPAVP
  
Inhibitor
Name:
BDBM50305527
Synonyms:
(4S)-4-[(1R)-1-hydroxy-2-({1-[3-(1-methylethyl)phenyl]cyclopropyl}amino)ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1~6,10~]docosa-1(21),6(22),7,9,17,19-hexaen-2-one | (S)-4-{(R)-1-Hydroxy-2-[1-(3-isopropyl-phenyl)-cyclopropylamino]-ethyl}-19-methoxymethyl-11-oxa-3,16-diaza-tricyclo[15.3.1.1*6,10*]docosa-1(21),6(22),7,9,17,19-hexaen-2-one | CHEMBL595066
Type:
Small organic molecule
Emp. Form.:
C35H45N3O4
Mol. Mass.:
571.7495
SMILES:
COCc1cc2NCCCCOc3cccc(C[C@H](NC(=O)c(c1)c2)[C@H](O)CNC1(CC1)c1cccc(c1)C(C)C)c3 |r|
Structure:
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