Target Information

Target General Information

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Target ID

T22839 (Former ID: TTDR00230)

Target Name

Pancreatic elastase 1 (CELA1)

Synonyms

Elastase; CELA1

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Gene Name

CELA1

Target Type

Successful target

[1]

Disease

[+] 2 Target-related Diseases

Alpha-1-antitrypsin deficiency [ICD-11: 5C5A]

Bronchitis [ICD-11: CA20]

Function

Acts upon elastin.

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BioChemical Class

Peptidase

UniProt ID

CELA1_HUMAN

EC Number

EC 3.4.21.36

Sequence

MLVLYGHSTQDLPETNARVVGGTEAGRNSWPSQISLQYRSGGSRYHTCGGTLIRQNWVMT
AAHCVDYQKTFRVVAGDHNLSQNDGTEQYVSVQKIVVHPYWNSDNVAAGYDIALLRLAQS
VTLNSYVQLGVLPQEGAILANNSPCYITGWGKTKTNGQLAQTLQQAYLPSVDYAICSSSS
YWGSTVKNTMVCAGGDGVRSGCQGDSGGPLHCLVNGKYSVHGVTSFVSSRGCNVSRKPTV
FTQVSAYISWINNVIASN

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

Drugs and Modes of Action

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Approved Drug(s)

[+] 2 Approved Drugs

Alpha 1-PI

Drug Info

Approved

Alpha-1 antitrypsin deficiency

[1], [2]

Erdosteine

Drug Info

Approved

Bronchitis

[1]

Clinical Trial Drug(s)

[+] 1 Clinical Trial Drugs

Sivelestat

Drug Info

Phase 3

Pyoderma gangrenosum

[3]

Discontinued Drug(s)

[+] 5 Discontinued Drugs

Mdl 101,146

Drug Info

Terminated

Inflammation

[4]

PBI-1101

Drug Info

Terminated

Inflammation

[5]

SSR-69071

Drug Info

Terminated

Chronic obstructive pulmonary disease

[6]

SYN-1134

Drug Info

Terminated

Cystic fibrosis

[7]

WIN-63759

Drug Info

Terminated

Emphysema

[8]

Mode of Action

[+] 2 Modes of Action

Inhibitor

[+] 15 Inhibitor drugs

Alpha 1-PI

Drug Info

[9]

Sivelestat

Drug Info

[10]

Mdl 101,146

Drug Info

[11]

PBI-1101

Drug Info

[12]

SSR-69071

Drug Info

[13]

SYN-1134

Drug Info

[14]

(2-BROMOETHYL)(2-'FORMYL-4'-AMINOPHENYL) ACETATE

Drug Info

[16]

(Tert-Butyloxycarbonyl)-Alanyl-Alanyl-Amine

Drug Info

[11]

Acetate Ion

Drug Info

[11]

Acetyl-Ala-Ala-Pro-Ala-trifluromethane

Drug Info

[17]

Acetyl-Pro-Ala-Pro-Ala-trifluoro methane

Drug Info

[17]

Dimethylformamide

Drug Info

[18]

Grassystatin a

Drug Info

[19]

MOLASSAMIDE

Drug Info

[20]

Para-Isopropylaniline

Drug Info

[11]

Modulator

[+] 2 Modulator drugs

Erdosteine

Drug Info

[1]

WIN-63759

Drug Info

[15]

Cell-based Target Expression Variations

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Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Similarity Proteins

Different Human System Profiles of Target

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Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Similarity Proteins

There is no similarity protein (E value < 0.005) for this target

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 2

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003666)

REF 3

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 4

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007771)

REF 5

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018032)

REF 6

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014569)

REF 7

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018646)

REF 8

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007449)

REF 9

Elastase inhibitors. J Soc Biol. 2001;195(2):143-50.

REF 10

Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both acute respiratory distress syndrome... Shock. 2010 Jan;33(1):14-8.

REF 11

How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

REF 12

CN patent application no. 1813706, Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage.

REF 13

Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem. 2011 Aug 19;286(33):28889-901.

REF 14

EP patent application no. 1292314, Method for treating respiratory disorders associated with pulmonary elastic fiber injury comprising the use of glycosaminoglycans.

REF 15

Biological activity of WIN 63759, an orally bioavailable inhibitor of human neutrophil elastase. Drug Development Research Volume 34, Issue 3, pages 306-316, March 1995.

REF 16

The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.

REF 17

Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, ... J Med Chem. 1990 Jan;33(1):394-407.

REF 18

Liver disease associated with occupational exposure to the solvent dimethylformamide. Ann Intern Med. 1988 May;108(5):680-6.

REF 19

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.

REF 20

Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis. J Nat Prod. 2010 Mar 26;73(3):459-62.

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