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Target
Neutrophil elastase
Ligand
BDBM232342
Substrate
US9346794, MeOSuc-Ala-Ala-Pro-Val-AMC
Meas. Tech.
Human Neutrophil Elastase Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
11.7±n/a nM
Comments
extracted
Citation
 Oost, T; Fiegen, D; Gnamm, C Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity US Patent  US9346794 Publication Date 5/24/2016 
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:
BDBM232342
Synonyms:
US9346794, 46
Type:
Small organic molecule
Emp. Form.:
C27H21F3N6O3S
Mol. Mass.:
566.554
SMILES:
Cc1c(-c2ccnc(c2)C(F)(F)F)c(=O)c(cn1-c1ccncc1)C(=O)NCc1ccc(cc1)S(C)(=O)=NC#N
Structure:
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Substrate
Name:
BDBM211682
Synonyms:
US9290457, MeOSuc-AAPV-AMC
Type:
Substrate
Emp. Form.:
C31H41N5O9
Mol. Mass.:
627.6853
SMILES:
COC(=O)CCC(=O)NC(C)C(=O)NC(C)C(=O)N1CCCC1C(=O)NC(C(C)C)C(=O)Nc1ccc2c(C)cc(=O)oc2c1
Structure:
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