Reaction Details Report a problem with these data
Target
Neutrophil elastase
Ligand
BDBM252427
Substrate
US9458113, MeOSuc-AAPV-AMC
Meas. Tech.
Human Neutrophil Elastase Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
<1±n/a nM
Comments
extracted
Citation
Peters, S; Anderskewitz, R; Gnamm, C; Hoesch, H; Morschhaeuser, G; Oost, T; Ries, UJ Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity US Patent US9458113 Publication Date 10/4/2016
More Info.:
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:
BDBM252427
Synonyms:
US9458113, 20.b
Type:
Small organic molecule
Emp. Form.:
C29H23F3N4O3
Mol. Mass.:
532.5131
SMILES:
CN1[C@@H](C2=C(CCCC2=O)N(C1=O)c1cccc(c1)C(F)(F)F)c1ccc(cc1-c1ccn(C)c(=O)c1)C#N |r,t:3|