Protein Information

General Information of the Protein

Protein ID	PT00992
Protein Name	Neutrophil elastase
Secondarily Protein Name	Bone marrow serine protease Elastase-2 Human leukocyte elastase Medullasin PMN elastase
Gene Name	ELANE
Secondarily Gene Name	ELA2
Sequence	MTLGRRLACLFLACVLPALLLGGTALASEIVGGRRARPHAWPFMVSLQLRGGHFCGATLIAPNFVMSAAHCVANVNVRAVRVVLGAHNLSRREPTRQVFAVQRIFENGYDPVNLLNDIVILQLNGSATINANVQVAQLPAQGRRLGNGVQCLAMGWGLLGRNRGIASVLQELNVTVVTSLCRRSNVCTLVRGRQAGVCFGDSGSPLVCNGLIHGIASFVRGGCASGLYPDAFAPVAQFVNWIDSIIQRSEDNPCPHPRDPDPASRTH Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Protease > Serine protease > Serine protease PA clan > Serine protease S1A subfamily
Function	Serine protease that modifies the functions of natural killer cells, monocytes and granulocytes. Inhibits C5a-dependent neutrophil enzyme release and chemotaxis (PubMed:15140022). Promotes cleavage of GSDMB, thereby inhibiting pyroptosis (PubMed:36899106). Capable of killing E.coli but not S.aureus in vitro; digests outer membrane protein A (ompA) in E.coli and K.pneumoniae (PubMed:10947984). Show/Hide
Uniprot ID	Primary ID: P08246 Secondarily ID: P09649 Q6B0D9 Q6LDP5 Show/Hide
Ensembl ID	ENSG00000197561
HGNC ID	HGNC:3309
Subcellular Location	Cytoplasmic vesicle Phagosome

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000100 , U-937

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0662436 Compound Info	1-((1R,2R)-1-cyano-2-phenylcyclopropylamino)-3-(3-fluorothiophen-2-yl)-1-oxopropan-2-aminium 2,2,2-trifluoroacetate Show/Hide	C19H17F4N3O3S	2
1	IC50 = 170 nM Bioactivity Info	TI LI LO TS
2	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0700060 Compound Info	(S)-1-((1R,2R)-1-cyano-2-phenylcyclopropylamino)-1-oxo-3-(thiophen-2-yl)propan-2-aminium 2,2,2-trifluoroacetate Show/Hide	C19H18F3N3O3S	2
1	IC50 = 220 nM Bioactivity Info	TI LI LO TS
2	IC50 > 50000 nM Bioactivity Info	TI LI LO TS
CP0662437 Compound Info	Trifluoro-acetate(S)-1-((1S,2S)-1-cyano-2-phenyl-cyclopropylcarbamoyl)-2-(2-fluoro-phenyl)-ethyl-ammonium Show/Hide	C21H19F4N3O3	1
1	IC50 = 1900 nM Bioactivity Info	TI LI LO TS
CP0700059 Compound Info	(S)-1-((1S,2S)-1-cyano-2-phenylcyclopropylamino)-1-oxo-3-(thiophen-2-yl)propan-2-aminium 2,2,2-trifluoroacetate Show/Hide	C19H18F3N3O3S	1
1	IC50 > 30000 nM Bioactivity Info	TI LI LO TS
CP0064686 Compound Info	2-Amino-N-[(S)-3-diazo-1-(4-iodo-benzyl)-2-oxo-propyl]-acetamide Show/Hide	C12H13IN4O2	1
1	IC50 > 50000 nM Bioactivity Info	TI LI LO TS

Biochemical Assays

Clinical Information about the Protein

Target 1 ( Neutrophil elastase (NE) )

Target Type	Clinical trial Target
Disease	8 Target-related Diseases				8
1	Hepatic fibrosis [ICD-11: DB93.0]
2	Chronic obstructive pulmonary disease [ICD-11: CA22]
3	Bronchiectasis [ICD-11: CA24]
4	Cystic fibrosis [ICD-11: CA25]
5	Acute lung injury [ICD-11: NB32.3]
6	Phlegmy cough [ICD-11: SA80-SA8Z]
7	Pyoderma gangrenosum [ICD-11: EB21]
8	Pulmonary disease [ICD-11: 1B10-1F85]
Approved Drug(s)	1 Approved Drug				1
1	Sivelestat sodium hydrate	Drug Info	Phase 4	Acute lung injury
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	Epigallocatechin gallate	Drug Info	Phase 3	Hepatic fibrosis
2	AZD9668	Drug Info	Phase 2	Chronic obstructive pulmonary disease
3	BAY 85-8501	Drug Info	Phase 2	Bronchiectasis
4	L-694,458	Drug Info	Phase 2	Cystic fibrosis
5	Sivelestat	Drug Info	Phase 3	Pyoderma gangrenosum
Discontinued Drug(s)	4 Discontinued Drugs				4
1	MR-889	Drug Info	Discontinued in Phase 3	Phlegmy cough
2	ZD-8321	Drug Info	Discontinued in Phase 2	Acute lung injury
3	AE-3763	Drug Info	Discontinued in Phase 1	Chronic obstructive pulmonary disease
4	ZD-0892	Drug Info	Discontinued in Phase 1	Chronic obstructive pulmonary disease
Investigative Drug(s)	1 Investigative Drug				1
1	AX-9657	Drug Info	Investigative	Pulmonary disease