Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T94823 | Target Info | |||
Target Name | Xaa-Pro dipeptidase (PEPD) | ||||
Synonyms |
X-Pro dipeptidase; Proline dipeptidase; Prolidase; PEPD; Imidodipeptidase
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Target Type | Literature-reported Target | ||||
Gene Name | PEPD | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
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Compound Name |
JTP-4819
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Discontinued in Phase 2 | Compound Info | ||
Synonyms |
JTP-3399
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Activity |
IC50 ~ 100000 nM
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[1] | |||
Compound Name |
(2S)-1-[(2S,3S)-3-Amino-2-hydroxy-5-methylhexanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL309274; BDBM50078390
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Activity |
IC50 = 59000 nM
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[2] | |||
Compound Name |
(2S)-1-[3-Amino-4-(2-fluorophenyl)butanoyl]-N-[[4-(trifluoromethyl)phenyl]methyl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL435882
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
(2S)-1-[3-Amino-4-(2-fluorophenyl)butanoyl]-N-[4-(2H-tetrazol-5-yl)butyl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL184346
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
(2R)-2-[4-[[[(2S)-1-[3-Amino-4-(2,3,4,5,6-pentafluorophenyl)butanoyl]pyrrolidine-2-carbonyl]amino]methyl]phenoxy]-3-methylbutanoic acid;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL183289
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
Methyl 2-[4-[[[(4R)-3-[3-amino-4-(2-fluorophenyl)butanoyl]-1,3-thiazolidine-4-carbonyl]amino]methyl]phenyl]acetate;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL186482
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
(2R)-2-[4-[[[(2S)-1-[3-Amino-4-(2,5-difluorophenyl)butanoyl]pyrrolidine-2-carbonyl]amino]methyl]phenoxy]-3-methylbutanoic acid;2,2,2-trifluoroacetic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL364102
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
(2S)-1-[(2S,4R)-1-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-4-hydroxypyrrolidine-2-carbonyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL2369857
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Activity |
IC50 = 110000 nM
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[2] | |||
Compound Name |
(2S)-1-[(2S)-1-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]pyrrolidine-2-carbonyl]-N-[(2S)-1-[[(2S)-1-[[(2R)-1-amino-1-oxo-3-sulfanylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL78505; BDBM50078393
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Activity |
IC50 = 130000 nM
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[2] | |||
Click to Show/Hide the Information of All Poor Binders |
Non Binders of This Target (in total, 7 non binders) | Download | Top | |||
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Compound Name |
Aminolevulinic acid hci
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Approved | Compound Info | ||
Synonyms |
Aminolevulinic acid; 5-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid; 106-60-5; 5-Aminolevulinate; delta-aminolevulinic acid; Pentanoic acid, 5-amino-4-oxo-; Aladerm; 5-Amino-4-oxovaleric acid; Kerastick; Ameluz; Aminolevulinate; 5-ALA; delta-ALA; 5-Amino-4-oxopentanoate; 5-amino-levulinate; 5-amino-levulinic acid; 5-amino-4-oxo-pentanoic acid; CCRIS 8958; UNII-88755TAZ87; EINECS 203-414-1; Levulinic acid, 5-amino-; CHEMBL601; 4-oxo-5-amino-pentanoic acid; CHEBI:17549; ZGXJTSGNIOSYLO-UHFFFAOYSA-N; 88755TAZ87; Levulan (TN)
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Activity |
Ki = 960000 nM
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[4] | |||
Compound Name |
(2S)-1-[(2R,3R)-3-Amino-2-hydroxy-5-methylhexanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL81423; BDBM50078392
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Activity |
IC50 = 410000 nM
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[2] | |||
Compound Name |
(1R,2R)-2-(2-Aminoacetyl)cyclohexane-1-carboxylic acid;hydrochloride
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Investigative | Compound Info | ||
Synonyms |
CHEMBL95756
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Activity |
Ki = 1100000 nM
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[4] | |||
Compound Name |
(2S)-N-[(2S)-1-Amino-1-oxopropan-2-yl]-1-[2-(hydroxycarbamoyl)cyclohexanecarbonyl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL80368; BDBM50078395
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Activity |
IC50 = 1700000 nM
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[2] | |||
Compound Name |
(2S)-N-[(2S)-1-Amino-1-oxopropan-2-yl]-1-(2-sulfanylcyclopentanecarbonyl)pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL79083; BDBM50078396; (S)-1-(2-Mercapto-cyclopentanecarbonyl)-pyrrolidine-2-carboxylic acid ((S)-1-carbamoyl-ethyl)-amide
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Activity |
IC50 > 2000000 nM
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[2] | |||
Compound Name |
(2S)-1-[(3R,4S)-4-Amino-3-hydroxy-6-methylheptanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL78482; BDBM50078399
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Activity |
IC50 > 2000000 nM
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[2] | |||
Compound Name |
2-[(S)-2-((S)-1-Carbamoyl-ethylcarbamoyl)-pyrrolidin-1-yl]-4-phenyl-butyric acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL311925; BDBM50078398
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Activity |
IC50 > 2000000 nM
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[2] | |||
Click to Show/Hide the Information of All Non Binders |
References | Top | ||||
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REF 1 | Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors. J Med Chem. 2010 May 13;53(9):3423-38. | ||||
REF 2 | Apstatin analogue inhibitors of aminopeptidase P, a bradykinin-degrading enzyme. J Med Chem. 1999 Jul 1;42(13):2394-402. | ||||
REF 3 | Potent and selective proline derived dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5151-5. | ||||
REF 4 | Peptide mimics of glycylproline as inhibitors of prolidase. Bioorg Med Chem Lett. 1995 Dec 7;5(23):2825-8. |
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