Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T15882 | Target Info | |||
| Target Name | Leukocyte proteinase-3 (PRTN3) | ||||
| Synonyms |
Wegener autoantigen; PR3; PR-3; P29; Neutrophil proteinase 4; NP4; NP-4; Myeloblastin; MBN; Leukocyte proteinase 3; CANCA antigen; C-ANCA antigen; AGP7
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| Target Type | Clinical trial Target | ||||
| Gene Name | PRTN3 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 7 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Sivelestat
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Phase 4 | Compound Info | ||
| Synonyms |
127373-66-4; UNII-DWI62G0P59; 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid; Elastase Inhibitor IV; C20H22N2O7S; N-(2-(4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino)benzoyl)aminoacetic acid; Sivelestat (ONO-5046); LY544349; CHEMBL76688; LY 544349; DWI62G0P59; Glycine, N-(2-(((4-(2,2-dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)-; N-(o-(p-Pivaloyloxybenzene)sulfonylaminobenzoyl)glycine
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
(2S)-2-Amino-N-[(1R,2R)-1-cyano-2-phenylcyclopropyl]-3-thiophen-2-ylpropanamide;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL516292
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
cis-(S)-2-Amino-N-((1R,2R)-1-cyano-2-phenylcyclopropyl)-3-(thiophen-2-yl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1078411; BDBM50310690; (2S)-N-[[(1R)-1alpha-Cyano-2beta-phenylcyclopropane]-1-yl]-2-amino-3-(2-thienyl)propanamide
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| Activity |
IC50 ~ 50000 nM
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[3] | |||
| Compound Name |
(3S)-1-Diazo-3-[(aminoacetyl)amino]-4-(4-iodophenyl)-2-butanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL450997; BDBM50270029; 2-Amino-N-[(S)-3-diazo-1-(4-iodo-benzyl)-2-oxo-propyl]-acetamide
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
1-Phenyl-2-(5-carboxybenzoxazole-2-ylthiomethyl)-5-(pivaloyloxy)-1,4-dihydropyridine-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093806; BDBM50444295
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
6-(((5-(Cyclopropanecarboxamido)-1,3,4-thiadiazol-2-yl)thio)methyl)-4-oxo-4H-pyran-3-yl 3-fluorobenzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3093805; BDBM50444298; ZINC11025900; AKOS024657172; MCULE-3931999485; SR-01000021298; SR-01000021298-1; F2532-0362
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| Activity |
IC50 ~ 134000 nM
|
[4] | |||
| Compound Name |
2-[(5-Amino-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(3,5-dichlorophenyl)-2-phenylacetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3219672; AKOS033611139; MCULE-4764172078; Z18355736
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| Activity |
IC50 ~ 139000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors. J Med Chem. 2013 Dec 12;56(23):9802-6. | ||||
| REF 2 | Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J Biol Chem. 2007 Jul 20;282(29):20836-46. | ||||
| REF 3 | Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5392-6. | ||||
| REF 4 | Structure based virtual screening for discovery of novel human neutrophil elastase inhibitors. Medchemcomm. 2012;3:1299-304. | ||||
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