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Target
Neutrophil elastase
Ligand
BDBM50066999
Substrate
n/a
Meas. Tech.
ChEMBL_220433 (CHEMBL842598)
IC50
0.450000±n/a nM
Citation
 Macdonald, SJ; Dowle, MD; Harrison, LA; Spooner, JE; Shah, P; Johnson, MR; Inglis, GG; Clarke, GD; Belton, DJ; Smith, RA; Molloy, CR; Dixon, M; Murkitt, G; Godward, RE; Skarzynski, T; Singh, OM; Kumar, KA; Hodgson, ST; McDonald, E; Hardy, GW; Finch, H; Humphreys, DC; Fleetwood, G Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams. Bioorg Med Chem Lett 11:243-6 (2001) [PubMed]  Article 
Target
Name:
Neutrophil elastase
Synonyms:
Bone marrow serine protease | Chymotrypsin | Coagulation factor X | ELA2 | ELANE | ELNE_HUMAN | Elastase | Elastase-2 | HLE | Human leukocyte elastase | Leukocyte elastase | Leukocyte elastase (HLE) | Medullasin | Neutrophil elastase | Neutrophil elastase (HNE) | Neutrophil elastase (NE) | PMN elastase | Thrombin | Trypsin
Type:
Enzyme
Mol. Mass.:
28532.38
Organism:
Homo sapiens (Human)
Description:
P08246
Residue:
267
Sequence:
MTLGRRLACLFLACVLPALLLGGTALASEIVGGRRARPHAWPFMVSLQLRGGHFCGATLIAPNFVMSAAHCVANVNVRAVRVVLGAHNLSRREPTRQVFAVQRIFENGYDPVNLLNDIVILQLNGSATINANVQVAQLPAQGRRLGNGVQCLAMGWGLLGRNRGIASVLQELNVTVVTSLCRRSNVCTLVRGRQAGVCFGDSGSPLVCNGLIHGIASFVRGGCASGLYPDAFAPVAQFVNWIDSIIQRSEDNPCPHPRDPDPASRTH
  
Inhibitor
Name:
BDBM50066999
Synonyms:
(S)-3,3-Diethyl-2-[4-(4-methyl-piperazine-1-carbonyl)-phenoxy]-4-oxo-azetidine-1-carboxylic acid ((R)-1-benzo[1,3]dioxol-5-yl-butyl)-amide | (S)-N-((R)-1-(benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(1-methylpiperazine-4-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide | CHEMBL310871 | L-694458
Type:
Small organic molecule
Emp. Form.:
C31H40N4O6
Mol. Mass.:
564.6725
SMILES:
CCC[C@@H](NC(=O)N1[C@@H](Oc2ccc(cc2)C(=O)N2CCN(C)CC2)C(CC)(CC)C1=O)c1ccc2OCOc2c1 |r|
Structure:
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