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((8'Z)-pentadecenyl)-salicylic acid
-
a noncompetitive inhibitor isolated from Gingko biloba leaves
(+)-gallocatechin
-
IC50: 0.000109 mM, expected to be useful for preventing and curing of Alzheimers disease
(-)-epicatechin
-
IC50: 0.0281 mM, noncompetitive inhibition
(-)-epicatechin 3-O-gallate
-
0.000052 mM, noncompetitive inhibition
(-)-epicatechin gallate
-
IC50: 10.2 mM, expected to be useful for preventing and curing of Alzheimers disease
(-)-epigallocatechin gallate
-
IC50: 0.000142 mM, expected to be useful for preventing and curing of Alzheimers disease
(1R,3S,4S,5S)-1,3,4-tris(acetyloxy)-5-([(2E)-3-[3,4-bis(acetyloxy)phenyl]prop-2-enoyl]oxy)cyclohexanecarboxylic acid
-
81.9% inhibition at 0.5 mM
(1R,3S,4S,5S)-3-[[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]-1,4,5-trihydroxycyclohexanecarboxylic acid
-
88% inhibition at 0.5 mM
(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoic acid
-
93.8% inhibition at 0.5 mM
(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoic acid
-
29.4% inhibition at 0.5 mM
(2E)-3-(4-methoxyphenyl)prop-2-enoic acid
-
less than 10% inhibition at 0.5 mM
(2E)-3-phenylprop-2-enoic acid
-
16.1% inhibition at 0.5 mM
(2E)-3-[3,4-bis(acetyloxy)phenyl]prop-2-enoic acid
-
72.9% inhibition at 0.5 mM
(2R)-1-(1-[[3-(azepan-1-ylcarbonyl)phenyl]carbonyl]-L-prolyl)pyrrolidine-2-carbonitrile
50% inhibition at 4.6 nM
(2R)-1-(1-[[4-(pyrrolidin-1-ylcarbonyl)phenyl]carbonyl]-L-prolyl)pyrrolidine-2-carbonitrile
50% inhibition at 1.6 nM
(2R)-1-[1-(4-azepan-1-yl-4-oxobutanoyl)-L-prolyl]pyrrolidine-2-carbonitrile
50% inhibition at 0.76 nM
(2R)-1-[1-(4-oxo-4-pyrrolidin-1-ylbutanoyl)-L-prolyl]pyrrolidine-2-carbonitrile
50% inhibition at 2.9 nM
(2R)-1-[1-(5-azepan-1-yl-3,3-dimethyl-5-oxopentanoyl)-L-prolyl]pyrrolidine-2-carbonitrile
50% inhibition at 0.39 nM
(2R)-1-[1-(5-azepan-1-yl-5-oxopentanoyl)-L-prolyl]pyrrolidine-2-carbonitrile
50% inhibition at 1.2 nM
(2S)-1-(4-phenylbutanoyl)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidine
-
(2S)-1-({(2S,4S)-4-[2-(1,3-Dihydro-2H-isoindol-2-yl)-2-oxo- ethyl]-5-oxopyrrolidin-2-yl}carbonyl)-4,4-difluoropyrrolidine-2- carbonitrile
-
potent and selective inhibitor of FAP, 0.01 mM used in assay conditions
(2S)-1-octanoyl-2-(pyrrolidin-1-ylcarbonyl)pyrrolidine
-
(2S)-1-[1-(2,3-dihydro-1H-inden-2-ylacetyl)-L-prolyl]pyrrolidine-2-carbaldehyde
-
-
(2S)-1-[1-(2,3-dihydro-1H-inden-2-ylacetyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[1-(3-[[(2S)-2-(cyclopentylcarbonyl)pyrrolidin-1-yl]carbonyl]benzoyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[1-(4-phenylbutanoyl)-L-prolyl]pyrrolidine-2-carbaldehyde
-
(2S)-1-[1-(4-phenylbutanoyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[1-[(3-[[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]carbonyl]phenyl)carbonyl]-D-prolyl]pyrrolidine-2-carbaldehyde
-
functional CHO group is the principal factor determining the inhibition kinetics
(2S)-1-[1-[(3-[[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]carbonyl]phenyl)carbonyl]-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile
(2S,2'S)-1,1'-(benzene-1,3-diyldicarbonyl)bis[2-(pyrrolidin-1-ylcarbonyl)pyrrolidine]
-
-
(2S,3aS,7aS)-1-[[(1R,2R)-2-phenylcyclopropyl]carbonyl]-2-(1,3-thiazolidin-3-ylcarbonyl)octahydro-1H-indole
-
S-17092
(3S)-3-(pyrrolidin-1-ylcarbonyl)-6-[[4-(trifluoromethyl)benzyl]oxy]-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(2,4-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(2,5-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(3,4-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(3,5-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(3,5-difluorobenzyl)oxy]-8-(phenylsulfonyl)-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(4-fluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(4-tert-butylbenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-6-[(4-tert-butylbenzyl)oxy]-8-(phenylsulfonyl)-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-(phenylsulfonyl)-3-(pyrrolidin-1-ylcarbonyl)-6-[[4-(trifluoromethyl)benzyl]oxy]-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-3-(pyrrolidin-1-ylcarbonyl)-6-(2,2,2-trifluoroethoxy)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-3-(pyrrolidin-1-ylcarbonyl)-6-[[4-(trifluoromethyl)benzyl]oxy]-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-(2-phenylethyl)-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(3,4-dichlorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(3,4-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(3,5-difluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(3-chloro-4-fluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(4-chlorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(4-fluorobenzyl)oxy]-3-(1H-pyrazol-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(4-fluorobenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[(4-methoxybenzyl)oxy]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-8-acetyl-6-[2-(4-fluorophenyl)ethyl]-3-(pyrrolidin-1-ylcarbonyl)-2,3-dihydroindolizin-5(1H)-one
-
-
(3S)-N-benzyl-3-[[(2S)-2-(chloroacetyl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroisoquinoline-2(1H)-carboxamide
-
(4R)-3-octanoyl-4-(pyrrolidin-1-ylcarbonyl)-1,3-thiazolidine
-
(5R,7S,8S,9S)-8,9-dihydroxy-2,2-dimethyl-4-oxo-1,3-dioxaspiro[4.5]dec-7-yl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
88.3% inhibition at 0.5 mM
(6S)-1,3-dichloro-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-(cyclohexylmethoxy)-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-(naphthalen-2-ylmethoxy)-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-(pyridin-4-ylmethoxy)-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-phenoxy-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(2-phenylethyl)amino]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(3,4-dichlorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(3,4-difluorobenzyl)amino]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(3,4-difluorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(3-chloro-4-fluorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(3-chlorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(4-fluorobenzyl)amino]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[(4-fluorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
(6S)-1-chloro-3-[2-(3,4-dichlorophenyl)ethoxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-3-[2-(4-fluorophenyl)ethoxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-6-(pyrrolidin-1-ylcarbonyl)-3-[(2,3,5-trifluorobenzyl)oxy]-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-1-chloro-6-(pyrrolidin-1-ylcarbonyl)-3-[[4-(trifluoromethyl)benzyl]oxy]-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(6S)-3-(benzylamino)-1-chloro-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(E)-1-(3-(4-methoxyphenyl)acryloyl)pyrrolidine-2-carboxylic acid
-
less than 10% inhibition at 0.5 mM
(E)-4-(3-(2-(methoxycarbonyl)pyrrolidin-1-yl)-3-oxoprop-1-enyl)-1,2-phenylene-diacetate
-
98.3% inhibition at 0.5 mM
(E)-methyl 1-(3-(3,4-dihydroxyphenyl)acryloyl)pyrrolidine-2-carboxylate
-
96.3% inhibition at 0.5 mM
(E)-methyl 1-(3-(3-(3,4-dihydroxyphenyl)acryloyloxy)-1,4,5-trihydroxycyclohexanecarbonyl)pyrrolidine-2-carboxylate
-
75.5% inhibition at 0.5 mM
(E)-methyl 1-(3-(4-methoxyphenyl)acryloyl)pyrrolidine-2-carboxylate
-
42.8% inhibition at 0.5 mM
(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile
(S)-valinyl-(R)-boroproline
-
-
1,2,3,4,6-penta-O-galloyl-beta-D-glucose
-
IC50: 170 nM
1,2,3,4,6-pentagalloyl glucopyranoside
-
specific, noncompetitive, and strong inhibition
1,2,3,6-tetra-O-galloyl-beta-D-glucose
-
IC50: 25 nM
1,2,3,6-tetragalloyl alloside
-
specific, noncompetitive, and strong inhibition
1,2,3-trigalloyl glucopyranoside
-
specific, noncompetitive, and strong inhibition
1,2,6-tri-O-galloylglucose
-
IC50: 0.00044 mM, noncompetitive inhibition
1,2,6-trigalloyl alloside
-
specific, noncompetitive, and strong inhibition
1,2,6-trigalloyl glucopyranoside
-
from Euphorbia helioscopia, specific, noncompetitive, and strong inhibition
1,2-oxazolidin-2-yl[(2S,3aS,7aS)-1-[[(1R,2R)-2-phenylcyclopropyl]carbonyl]octahydro-1H-indol-2-yl]methanone
-
-
1,3,6-trigalloyl alloside
-
specific, noncompetitive, and strong inhibition
1,3-dibenzyl-4-(benzylamino)-5-(methoxycarbonyl)-1H-3,1-benzimidazol-3-ium iodide
-
-
1,3-dicyclohexyl-4-(cyclohexylamino)-5-(methoxycarbonyl)-1H-3,1-benzimidazol-3-ium iodide
-
-
1-(2-(1-oxoisoindolin-2-acetyl))-(R)-boroproline
-
-
1-(3-oxo-3-[(2S)-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]propyl)-3-phenylquinoxalin-2(1H)-one
-
1-(4-oxo-4-[(2S)-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]butyl)-3-phenylquinoxalin-2(1H)-one
-
1-(4-phenylbutanoyl)-2(S)-(pyridine-2-carbonyl)pyrrolidine
-
-
1-(4-phenylbutanoyl)-2(S)-(thiophene-2-carbonyl)pyrrolidin
-
-
1-(cyclopent-1-en-1-ylcarbonyl)-N-(2-phenylethyl)-L-prolinamide
-
1-(cyclopent-1-enecarbonyl)-D-proline benzylamide
-
-
1-(cyclopent-1-enecarbonyl)-L-proline benzylamide
-
-
1-(cyclopent-1-enecarbonyl)-L-proline phenethylamide
-
-
1-benzyl-3-cyclohexyl-4-(cyclohexylamino)-5-(methoxycarbonyl)-1H-3,1-benzimidazol-3-ium iodide
-
-
1-benzyl-3-cyclohexyl-4-(cyclohexylamino)-5-(methoxymethyl)-1H-3,1-benzimidazol-3-ium iodide
-
-
1-cinnamoylpyrrolidine-2-carboxylic acid
-
14.6% inhibition at 0.5 mM
1-[(2R,5S)-2-(propan-2-yl)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-4-(pyridin-3-yl)butan-1-one
-
1-[(2R,5S)-2-tert-butyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-4-phenylbutan-1-one
-
1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-2-[(2R)-1,2,3,4-tetrahydronaphthalen-2-yl]ethanone
-
-
1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-2-[(2S)-1,2,3,4-tetrahydronaphthalen-2-yl]ethanone
-
-
1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-4-(thiophen-2-yl)butan-1-one
-
-
1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]octan-1-one
-
-
1-[2-oxo-2-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]ethyl]-3-phenylquinoxalin-2(1H)-one
-
-
1-[[(2S)-1-(4-phenylbutanoyl)pyrrolidin-2-yl]carbonyl]pyrrolidin-2-one
-
-
2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone
-
50% inhibition at 0.15 mM
2',4'-dihydroxy-6'-methoxy-3',5'-dimethyldihydrochalcone
-
50% inhibition at 0.098 mM
2',4'-dihydroxy-6'-methoxy-3'-methylchalcone
-
50% inhibition at 0.0375 mM
2',4'-dihydroxy-6'-methoxy-3'-methyldihydrochalcone
-
50% inhibition at 0.0125 mM
2'-hydroxy-4',6'-dimethoxy-3'-methylchalcone
-
50% inhibition above 0.2 mM
2'-hydroxy-4',6'-dimethoxy-3'-methyldihydrochalcone
-
50% inhibition at 0.158 mM
2(S)-(aroyl)-1-(4-phenylbutanoyl)pyrrolidines
-
-
-
2(S)-(cycloalk-1-enecarbonyl)-1-(4-phenyl-butanoyl)pyrrolidines
-
-
-
2(S)-(cyclohex-1-enecarbonyl)-1-(4-phenylbutanoyl)pyrrolidine
-
-
2(S)-(cyclopent-1-enecarbonyl)-1-(4-phenylbutanoyl)pyrrolidine
-
-
2(S)-(furan-2-carbonyl)-1-(4-phenylbutanoyl)pyrrolidine
-
-
2,3-dihydro-1H-inden-2-yl[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]methanone
-
-
2,3-dihydro-1H-pyrrol-1-yl[(2S,3aS,7aS)-1-[[(1R,2R)-2-phenylcyclopropyl]carbonyl]octahydro-1H-indol-2-yl]methanone
-
-
2,5-dihydro-1H-pyrrol-1-yl[(2S,3aS,7aS)-1-[[(1R,2R)-2-phenylcyclopropyl]carbonyl]octahydro-1H-indol-2-yl]methanone
-
-
2-(2,3-dihydro-1H-inden-2-yl)-1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]ethanone
-
-
2-(3-[(2S)-4,4-difluoro-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]-3-oxopropyl) isoindole-1,3(2H)-dione
-
2-(4-oxo-4-[(2S)-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]butyl)-1H-isoindole-1,3(2H)-dione
-
2-hydroxy-1-[(2S)-1-[1-[(3-[[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]carbonyl]phenyl)carbonyl]-D-prolyl]pyrrolidin-2-yl]ethanone
-
functional CHO group is the principal factor determining the inhibition kinetics
2-oxo-kolavenic acid
-
terpenoid from the bark of Xylopia aethiopia, 34% inhibition at 1mM
2-[2-oxo-2-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]ethyl]-1H-isoindole-1,3(2H)-dione
-
-
2-[2-[(2S)-4,4-difluoro-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]-2-oxoethyl]-1H-isoindole-1,3(2H)-dione
-
-
2-[3-oxo-3-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]propyl]-1H-isoindole-1,3(2H)-dione
-
3,3-dimethyl glutaric acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 13 nM
3,5,4'-trihydroxystilbene 4'-O-beta-D-(2-O-galloyl)glucopyranoside
-
IC50: 0.003 mM, noncompetitive inhibition
3,5,4'-trihydroxystilbene 4'-O-beta-D-(6-O-galloyl)glucopyranoside
-
IC50: 0.0149 mM, noncompetitive inhibition
3,5,4'-trihydroxystilbene 4'-O-beta-D-glucopyranoside
-
IC50: 0.0229 mM, noncompetitive inhibition
3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-5(R)-tert-butyl-L-Pro-pyrrolidine
-
IC50: 460 nM
3-(2(S)-benzoyl-pyrrolidine-1-carbonyl)-benzoyl-L-Pro-pyrrolidine
-
IC50: 18 nM
3-(2,3-dihydro-1H-inden-2-yl)-1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]propan-1-one
-
-
3-(3-oxo-3-[(2S)-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]propyl)-5,5-diphenylimidazolidine-2,4-dione
-
3-(4-oxo-4-[(2S)-2-(pyrrolidinocarbonyl)pyrrolidin-1-yl]butyl)-5,5-diphenylimidazolidine-2,4-dione
-
3-({4-[2-(E)-styrylphenoxy]butanoyl}-L-4-hydroxyprolyl)-thiazolidine
-
SUAM-14746, selective prolyl oligopeptidase inhibitor
3-benzyl-4-(benzylamino)-5-(methoxycarbonyl)-1-methyl-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-4-(cyclohexylamino)-1-ethyl-5-[(prop-2-en-1-yloxy)carbonyl]-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-4-(cyclohexylamino)-1-methyl-5-[(prop-2-en-1-yloxy)carbonyl]-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-4-(cyclohexylamino)-5-(methoxycarbonyl)-1-(4-methylphenyl)-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-4-(cyclohexylamino)-5-(methoxycarbonyl)-1-methyl-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-4-(cyclohexylamino)-5-(methoxycarbonyl)-1-[(1S)-1-phenylethyl]-1H-3,1-benzimidazol-3-ium iodide
-
-
3-cyclohexyl-N-[(2S)-1-oxo-3-phenyl-1-[(2S)-2-(piperidin-1-ylcarbonyl)pyrrolidin-1-yl]propan-2-yl]propanamide
-
3-O-galloylepigallocatechin-(4-8)-epigallocetechin 3-O-gallate
-
IC50: 440 nM
3-[3-oxo-3-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]propyl]-5,5-diphenylimidazolidine-2,4-dione
-
-
33mer of gluten-derived peptide
-
-
4-(2,3-dihydro-1H-inden-2-yl)-1-[(2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]butan-1-one
-
-
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
-
4-(2-aminoethyl)benzenesulfonyl fluoride
-
inhibition of extracellular isozyme
4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride
-
complete inhibition at 10 mM
4-(4-chlorophenyl)-8-(ethoxycarbonyl)-5-methyl-2,3-dihydrofuro[3,2-c]quinolin-5-ium iodide
-
-
4-(4-hydroxyphenyl)-2-butanone 4'-O-beta-D-(2,6-di-O-galloyl)glucopyranoside
-
IC50: 0.0105 mM, noncompetitive inhibition
4-(4-hydroxyphenyl)-2-butanone 4'-O-beta-D-(2-O-galloyl-6-O-cinnamoyl)glucopyranoside
-
IC50: 690 nM, noncompetitive inhibition
4-(4-hydroxyphenyl)-2-butanone 4'-O-beta-D-(6-O-galloyl-2-O-cinnamoyl)glucopyranoside
-
IC50: 0.082 mM, noncompetitive inhibition
4-(4-iodophenyl)butanoyl-L-prolyl-pyrrolidine
-
-
4-(4-[123I]iodophenyl)butanoyl-L-prolyl-2(S)-cyanopyrrolidine
-
-
4-([[(3S)-8-acetyl-5-oxo-3-(pyrrolidin-1-ylcarbonyl)-1,2,3,5-tetrahydroindolizin-6-yl]oxy]methyl)benzonitrile
-
-
4-chloromercuribenzoate
-
14% residual activity at 0.2 mM
4-Chloromercuriphenylsulfonate
4-hydroxymercuriphenylsulfonate
-
-
4-phenyl-1-[(2S)-2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]butan-1-one
-
-
4-phenyl-1-[(2S)-2-[[(2S)-2-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidin-1-yl]butan-1-one
-
4-phenyl-1-[(3S)-3-(pyrrolidin-1-ylcarbonyl)-3,4-dihydroisoquinolin-2(1H)-yl]butan-1-one
-
-
4-phenyl-1-[(4R)-4-(1,3-thiazolidin-3-ylcarbonyl)-1,3-thiazolidin-3-yl]butan-1-one
-
-
4-phenyl-1-[(4S)-4-(1,3-thiazolidin-3-ylcarbonyl)-1,3-thiazolidin-3-yl]butan-1-one
-
-
4-phenyl-1-[2-(pyrrolidin-1-ylcarbonyl)cyclopent-1-en-1-yl]butan-1-one
-
4-phenyl-1-[5-(pyrrolidin-1-ylcarbonyl)cyclopent-1-en-1-yl]butan-1-one
-
4-phenyl-butanoyl-L-prolyl-2(S)-cyanopyrrolidine
4-phenylbutanoyl-2(S)-(2-oxocyclopentanecarbonyl)-pyrrolidine
-
IC50: 260 nM
4-phenylbutanoyl-2(S)-(3-phenylpropionyl)pyrrolidine
-
IC50: 0.024 mM
4-phenylbutanoyl-2(S)-(cyclohexanecarbonyl)pyrrolidine
-
IC50: 1100 nM
4-phenylbutanoyl-2(S)-(cyclopentanecarbonyl)pyrrolidine
-
IC50: 30 nM
4-phenylbutanoyl-2(S)-(phenylacetyl)pyrrolidine
-
IC50: 3600 nM
4-phenylbutanoyl-2(S)-benzylpyrrolidine
-
IC50: 23 nM
4-phenylbutanoyl-2(S)-isobutanoylpyrrolidine
-
IC50: 620 nM
4-phenylbutanoyl-5(R)-methyl-L-Pro-2(S)-(hydroxyacetyl)pyrrolidine
-
IC50: 0.15 nM
4-phenylbutanoyl-5(R)-methyl-L-Pro-pyrrolidine
-
IC50: 0.71 nM
4-phenylbutanoyl-5(R)-t-butyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine
-
-
4-phenylbutanoyl-5(R)-t-butyl-L-prolyl-pyrrolidine
-
-
4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine
-
IC50: 0.26 nM
4-phenylbutanoyl-5(R)-tert-butyl-L-Pro-pyrrolidine
-
IC50: 1.2 nM
4-phenylbutanoyl-5(R)-tert-butyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine
-
4-phenylbutanoyl-5(S)-methyl-L-Pro-pyrrolidine
-
IC50: 1.4 nM
4-phenylbutanoyl-L-Pro-2(S)-(hydroxyacetyl)-pyrrolidine
-
IC50: 0.24 nM
4-phenylbutanoyl-L-Pro-pyrrolidine
-
IC50: 2.2 nM
4-phenylbutanoyl-L-prolyl-2(S)-(cyclopentanecarbonyl)-pyrrolidine
-
IC%0: 1010 nM
4-phenylbutanoyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine
-
IC50: 0.2 nM
4-phenylbutanoyl-L-prolyl-2(S)-acetylpyrrolidine
-
IC50: 170 nM
4-phenylbutanoyl-L-prolyl-2(S)-benzoylpyrrolidine
-
IC50: 210 nM
4-phenylbutanoyl-L-prolyl-2(S)-cyanopyrrolidine
-
4-phenylbutanoyl-L-prolyl-2(S)cyanopyrrolidine
-
-
4-phenylbutanoyl-L-prolyl-pyrrolidine
-
i.e. SUAM-1221
4-toluenesulfonamide
-
98% residual activity at 0.2 mM
5,5'-dithio-bis(2-nitrobenzoic acid)
-
enzyme from brain
5,5'-dithio-bis-(2-nitrobenzoic acid)
-
complete inhibition at 5 mM
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5-(4-chlorophenyl)-9-(ethoxycarbonyl)-6-methyl-3,4-dihydro-2H-pyrano[3,2-c]quinolin-6-ium iodide
-
-
5-(methoxycarbonyl)-3-(4-methoxyphenyl)-4-[(4-methoxyphenyl)amino]-1-methyl-1H-3,1-benzimidazol-3-ium iodide
-
-
5-cyano-3-cyclohexyl-4-(cyclohexylamino)-1-methyl-1H-3,1-benzimidazol-3-ium iodide
-
-
6-((10'Z)-heptadecenyl)salicylic acid
-
a noncompetitive inhibitor isolated from Gingko biloba leaves
6-(10Z-heptadecenyl)salicylic acid
-
isolated from leaves of Ginkgo biloba, noncompetitive, 50% inhibition at 0.00062 mM
6-(8Z-pentadecenyl)salicylic acid
-
isolated from leaves of Ginkgo biloba, noncompetitive, 50% inhibition at 0.00086 mM
7-hydroxy-5-methoxy-6,8-dimethylflavanone
-
14% inhibition at 0.5 mM
8-(ethoxycarbonyl)-5-methyl-4-naphthalen-1-yl-2,3-dihydrofuro[3,2-c]quinolin-5-ium iodide
-
-
9-(ethoxycarbonyl)-6-methyl-5-phenyl-3,4-dihydro-2H-pyrano[3,2-c]quinolin-6-ium iodide
-
-
9H-fluoren-9-ylmethyl [(2S)-5-carbamimidamido-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopentan-2-yl]carbamate
-
-
acetonyl geraniin
-
specific, noncompetitive, and strong inhibition
acetyl-5(R)-tert-butyl-L-Pro-pyrrolidine
-
IC50: 7100 nM
adipic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 68 nM
AEBSF
1 mM, 12% inhibition
alpha-/beta-carotene
-
mixture of alpha- and beta-form, 64.4% inhibition at 0.5 mM
alpha-ketobenzothiazol
-
enzyme from serum
alpha2-gliadin 33-mer peptide
-
POP inhibitor
-
amastatin
-
0.1 mM, 97% inhibition
arachidonic acid
-
50% inhibition at 0.0534 mM
ARI-3099
-
i.e. N-(pyridine-4-carbonyl)-D-Ala-boro-L-Pro
ARI-3531
-
selective inhibitor, i.e. N-(pyridine-3-carbonyl)-L-Val-boroproline
Ba2+
-
48% residual activity at 10 mM
benzoyl-L-Pro-pyrrolidine
-
IC50: 66 nM
benzyl (1S,2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]cyclohexanecarboxylate
-
-
benzyl (2S)-2-(1,3-oxazolidin-3-ylcarbonyl)pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-([(2S)-2-[(5-phenyl-4,5-dihydro-1,2-oxazol-3-yl)carbonyl]pyrrolidin-1-yl]carbonyl)pyrrolidine-1-carboxylate
-
benzyl (2S)-2-[(1-oxido-1,3-thiazolidin-3-yl)carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[(2S)-2-formylpyrrolidine-1-carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
benzyl (2S)-2-[[(2S)-2-([5-[(benzyloxy)methyl]-1,2-oxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
benzyl (2S)-2-[[(2S)-2-([5-[(benzyloxy)methyl]-4,5-dihydro-1,2-oxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]-2,3-dihydro-1H-indole-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]-5-oxopyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
benzyl trachyloban-19-oic acid
-
terpenoid from the bark of Xylopia aethiopia, 50% inhibition at 0.037 mM
benzyl [(2R)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate
-
0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts
benzyl [(2R,3R,7aS)-3-cyano-2-methyl-5-oxohexahydropyrrolo[2,1-b][1,3]oxazol-6-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells
benzyl [(2S)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate
-
0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts
benzyl [(3R,6R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
benzyl [(3R,6R,8aS)-3-cyano-5-oxohexahydro-5H-[1,3]thiazolo[3,2-a]pyridin-6-yl]carbamate
-
0.1 mM, more than 50% inhibition in extracts from astrocyte-derived cells, extracts from brain-derived endothelial cells and extracts from fibroblasts
benzyl [(3R,6S,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells
benzyl [(3R,6S,8aS)-3-cyano-5-oxohexahydro-5H-[1,3]thiazolo[3,2-a]pyridin-6-yl]carbamate
-
0.1 mM, more than 50% inhibition in extracts from astrocyte-derived cells, extracts from brain-derived endothelial cells and extracts from fibroblasts
benzyl [(3R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]oxazol-6-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from fibroblasts
benzyl [(3S,6R,7aR)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells
benzyl [(3S,6S,7aR)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and brain-derived endothelial cells
benzyl [(4S,7S,8aS)-4-cyano-6-oxohexahydro-2H-pyrrolo[2,1-b][1,3]thiazin-7-yl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from fibroblasts
benzyl [2-(2-cyanopiperidin-1-yl)-2-oxoethyl]carbamate
-
0.1 mM, 10-50% inhibition in extracts from brain-derived endothelial cells and extracts from fibroblasts, more than 50% inhibition in extracts from astrocyte-derived cells
benzyl [2-[(2R)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate
-
0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts
benzyl [2-[(2S)-2-(chloroacetyl)pyrrolidin-1-yl]-2-oxoethyl]carbamate
-
-
benzyl [2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate
-
0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts
benzylcarbamoyl-5(R)-tert-butyl-L-prolyl-pyrrolidine
-
IC50: 2.0 nM
benzylcarbamoyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine
-
Benzyloxycarbonyl-Ala-Ala-Pro diazomethyl ketone
-
-
benzyloxycarbonyl-Gly-Gly-Pro-CH2Cl
-
enzyme from kidney
benzyloxycarbonyl-Gly-Pro-beta-naphthylamide
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
benzyloxycarbonyl-L-methionyl-2(S)-cyanopyrrolidine
-
-
benzyloxycarbonyl-L-Pro-L-prolinal
-
IC50: 0.4 nM
benzyloxycarbonyl-Pro-L-prolinal
-
IC50: 0.33 nM
benzyloxycarbonyl-Pro-Pro-OH
-
-
benzyloxycarbonyl-Pro-prolinal
benzyloxycarbonyl-Pro-pyrrolidine
-
-
benzyloxycarbonyl-Pro-thiazolidine
-
-
benzyloxycarbonyl-proline-prolinal
benzyloxycarbonyl-prolyl-prolinal
-
-
benzyloxycarbonyl-thioPro-thiazolidine
-
-
benzyloxycarbonyl-thioPro-thioprolinal
-
-
benzyloxycarbonyl-thioprolyl-thioprolinal
-
specific inhibitor of prolyl oligopeptidase
benzyloxycarbonyl-thioprolylthiazolidine
-
-
benzyloxycarbonyl-thioprolylthioprolinal
-
enzyme from lymphocyte
betulin
-
50% inhibition at 0.101 mM
bixanin
-
specific and noncompetitive inhibition
Boc-5(R)-tert-butyl-L-Pro-pyrrolidine
-
IC50: 2.2 nM
Boc-5(S)-tert-butyl-L-Pro-pyrrolidine
-
IC50: 9.2 nM
Boc-L-Pro-pyrrolidine
-
IC50: 29 nM
buspirone
-
25% inhibition at 0.01 mM
calcitonin gene-related peptide
-
-
-
caproyl-L-Pro-((2S)-hydroxyacetyl)pyrrolidine
-
-
carbamazepine
-
mechanism, reverses the effect of drugs
Cbz-Pro-CN
-
0.1 mM, 10-50% inhibition in extracts from brain-derived endothelial cells
Cbz-Pro-NH2
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from fibroblasts
Chloromethylketone derivatives
chlorpromazine
-
55% inhibition at 0.01 mM
cis-3,5,4'-trihydroxystilbene 4'-O-beta-D-(6-O-galloyl)glucopyranoside
-
IC50: 0.0028 mM, noncompetitive inhibition
citalopram
-
27% inhibition at 0.01 mM
clozapine
-
40% inhibition at 0.01 mM
corilagin
-
specific, noncompetitive, and strong inhibition
cyclopent-2-ene-1,2-dicarboxylic acid 2-benzylamide 1-[2(S)-(hydroxyacetyl)-H-pyrrolidine]amide
-
cyclosporine A
-
the activating effect of methotrexate dominates the inhibitory effect of cyclosporine A
desipramine
-
20% inhibition at 0.01 mM
DFP
0.1 mM, 100% inhibition
diethyl dicarbonate
-
enzyme from brain
diisopropyl fluorophosphate
diisopropylfluorophosphate
diprotin
-
0.1 mM, complete inhibition
docosahexaenoic acid
-
50% inhibition at 0.0462 mM
duloxetine
-
21% inhibition at 0.01 mM
E-64
Lyophyllum cinerascens
-
-
eicosapentaenoic acid
-
50% inhibition at 0.0994 mM
elaeocarpusin
-
specific, noncompetitive, and strong inhibition
ent-kaur-16-en-19-oic acid
-
terpenoid from the bark of Xylopia aethiopia, 50% inhibition at 0.060 mM
epi-betulinic acid
-
50% inhibition at 0.015 mM
escitalopram
-
39% inhibition at 0.01 mM
euphorscopin
-
specific, noncompetitive, and strong inhibition
fluoxetine
-
an antidepressant
flupenthixol
-
56% inhibition at 0.01 mM
gallic acid 4-O-beta-D-(6-O-galloyl)glucopyranoside
-
IC50: 0.00939 mM, noncompetitive inhibition
geraniin
-
specific, noncompetitive, and strong inhibition
glutaric acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 48 nM
glycinyl-(R)-boroproline
-
-
helioscopin B
-
specific, noncompetitive, and strong inhibition
helioscopinin A
-
specific, noncompetitive, and strong inhibition
helioscopinin B
-
specific, noncompetitive, and strong inhibition
hetero-chitooligosaccharides
-
hetero-chitooligosaccharides with different degrees of sulfatization, or deacetylation, preparation and inhibitory potency, competitive enzyme inhibition, overview
-
hispidulin
-
0.1 mM, 43% enzyme inhibition
imipramine
-
29% inhibition at 0.01 mM
interferon-alpha
-
IFN-alpha
-
isophthalic acid (L-proline methyl ester) L-prolyl-pyrrolidine amide
-
IC50: 54 nM
isophthalic acid 2(S)-(cyclopentanecarbonyl)pyrrolidine (L-proline methyl ester) amide
-
IC50: 640 nM
isophthalic acid 2(S)-(cyclopentanecarbonyl)pyrrolidine L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine amide
-
IC50: 0.61 nM, log P: 0.2, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid 2(S)-(cyclopentanecarbonyl)pyrrolidine-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine amide
-
-
isophthalic acid 2(S)-(cyclopentanecarbonyl)pyrrolidine-L-prolyl-2(S)-cyanopyrrolidine amide
-
-
isophthalic acid 2(S)-(cyclopentylcarbonyl)pyrrolidine L-prolyl-pyrrolidine amide
-
IC50: 14 nM, log P: 1.1, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid 2(S)-(cylcohexanecarbonyl)pyrrolidine L-prolyl-2(S)-cynaopyrrolidine amide
-
IC50: 0.72 nM
isophthalic acid 2(S)-(cylcopentanecarbonyl)pyrrolidine L-prolyl-2(S)-cynaopyrrolidine amide
-
IC50: 1.1 nM, log P: 0.8, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid 2(S)-acetylpyrrolidine L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine amide
-
IC50: 1.2 nM
isophthalic acid 2(S)-acetylpyrrolidine L-prolyl-2(S)-cynaopyrrolidine amide
-
IC50: 4.2 nM, log P: -0.6, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid 2(S)-acetylpyrrolidine L-prolyl-pyrrolidine amide
-
IC50: 65 nM
isophthalic acid 2(S)-benzoylpyrrolidine L-prolyl-2(S)-cynaopyrrolidine amide
-
IC50: 1.3 nM, log P: 1.1, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid 2(S)-benzoylpyrrolidine L-prolyl-pyrrolidine amide
-
IC50: 18 nM
isophthalic acid 2(S)-isobutanoylpyrrolidine L-prolyl-2(S)-cynaopyrrolidine amide
-
IC50: 1.6 nM, log P: 0.3, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid bis(L-prolyl-pyrrolidine) amide
isophthalic acid bis-2(S)-(cyclopentanecarbonyl)pyrrolidine amide
-
IC50: 78 nM, log P: 2.7, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid bis-2(S)-acetylpyrrolidine amide
-
54% inhibition at 0.1 nM
isophthalic acid L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine L-prolyl-pyrrolidine amide
isophthalic acid L-prolyl-2(S)-cyanopyrrolidine L-prolyl-pyrrolidine amide
-
IC50: 1.5 nM
isophthalic acid L-prolyl-pyrrolidine L-prolyl-L-prolinal amide
-
IC50: 1.3 nM
isophthalic acid L-prolylbenzylamine L-prolyl-pyrrolidine amide
-
IC50: 31 nM
jolkinin
-
specific, noncompetitive, and strong inhibition
ketanserin
-
mixed type inhibitor, 49% inhibition at 0.01 mM
kolavenic acid
-
terpenoid from the bark of Xylopia aethiopia, 50% inhibition at 0.099 mM
L-1-tosylamido-2-phenylethylchloromethyl ketone
-
-
lamotrigine
-
22% inhibition at 0.01 mM
levomepromazine
-
32% inhibition at 0.01 mM
licuroside
-
IC50: 0.0265 mM, noncompetitive inhibition
linoleic acid
-
50% inhibition at 0.0438 mM
macranganin
-
from Euphorbia fisheriana, specific, noncompetitive, and strong inhibition
methyl (1R,3S,4S,5S)-3-[[(2E)-3-(3,4-dihydroxyphenyl)prop-2-enoyl]oxy]-1,4,5-trihydroxycyclohexanecarboxylate
-
92.6% inhibition at 0.5 mM
methyl (2E)-3-(3,4-dihydroxyphenyl)prop-2-enoate
-
90.5% inhibition at 0.5 mM
methyl (2E)-3-(4-methoxyphenyl)prop-2-enoate
-
22% inhibition at 0.5 mM
methyl (2E)-3-phenylprop-2-enoate
-
20% inhibition at 0.5 mM
methyl (3R,6R,7aS)-6-[[(benzyloxy)carbonyl]amino]-5-oxohexahydropyrrolo[2,1-b][1,3]thiazole-3-carboxylate
-
0.1 mM, 10-50% inhibition in extracts from fibroblasts
methyl (3R,6S,7aS)-6-[[(benzyloxy)carbonyl]amino]-5-oxohexahydropyrrolo[2,1-b][1,3]thiazole-3-carboxylate
-
0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from fibroblasts
methyl 1-cinnamoylpyrrolidine-2-carboxylate
-
less than 10% inhibition at 0.5 mM
methyl 2-(cyclohexylamino)-3-[cyclohexyl(formyl)amino]-4-(methylamino)benzoate
-
-
methyl 3-cyclohexyl-4-(cyclohexylamino)-1-methyl-2,3-dihydro-1H-benzimidazole-5-carboxylate
-
-
methyl trachyloban-19-oic acid
-
terpenoid from the bark of Xylopia aethiopia, 50% inhibition at 0.045 mM
mianserin
-
15% inhibition at 0.01 mM
N-(1-naphthalenecarbonyl)glycinyl-(R)-boroproline
-
-
N-(benzoyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-2-chloro-4-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-2-fluoro-4-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-3-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-3-carbonyl)glycinyl-(R)-boroproline
-
-
N-(pyridine-3-chloro-4-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-3-fluoro-4-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(pyridine-4-carbonyl)glycinyl-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-alaninyl-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-butyl(glycinyl)-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-ethyl(glycinyl)-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-methioninyl-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-phenyl(glycinyl)-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-propyl(glycinyl)-(R)-boroproline
-
-
N-(quinoline-4-carbonyl)-(R)-serinyl-(R)-boroproline
-
-
N-acetyl-(R)-alaninyl-(R)-boroproline
-
-
N-Alpha-benzyloxycarbonyl-Ala-Pro
-
-
N-benzyloxycarbonyl-L-prolyl-L-prolinal
-
i.e. Z-Pro-prolinal
N-benzyloxycarbonyl-thioprolyl-thioprolinaldimethylacetal
-
-
N-Benzyloxycarbonyl-valyl-prolinal
-
-
N-carbobenzoxy-Leu-Leu-Leu-COH
-
the proteasome inhibitor
N-carbobenzoxy-prolyl-prolinal
-
ZPP
N-methyllaurotetanine
-
-
N-p-tosyl-L-phenylalanine chloromethylketone
67.2% inhibition at 0.001 mM
N-p-tosyl-L-phenylalanine-chloromethylketone
-
-
N-[(2S)-1-[(2S)-2-formylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]-4-phenylbutanamide
-
-
N-[(2S)-3-methyl-1-oxo-1-[(2S)-2-(piperidin-1-ylcarbonyl)pyrrolidin-1-yl]butan-2-yl]-3-phenoxybenzamide
-
Nalpha-tosyl-L-lysine chloromethylketone
38.3% inhibition at 0.001 mM
Nalpha-tosyl-L-lysine-chloromethylketone
-
-
orinithine decarboxylase
-
-
-
oroxylin A
-
0.1 mM, 20% enzyme inhibition
oroxyloside
-
0.1 mM, 34% enzyme inhibition
p-hydroxymercuribenzoate
-
-
Pancreatic basic trypsin inhibitor
-
-
-
PCMBS
-
enzyme from kidney
phenyl (2S)-2-(((2S)-2-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-1-yl)carbonyl)pyrrolidine-1-carboxylate
-
phenyl (2S)-2-(((2S)-2-(isoxazol-3-ylcarbonyl)pyrrolidin-yl)carbonyl)pyrrolidine-1-carboxylate
-
phenyl (2S)-2-([(2S)-2-[(5-phenylisoxazol-3-yl)carbonyl]pyrrolidin-1-yl]carbonyl)pyrrolidine-1-carboxylate
-
phenyl (2S)-2-[[(2S)-2-([5-[(2E)-3-phenylprop-2-en-1-yl]isoxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
50% inhibition at 0.01 mM, inhibition of parasite invasion into host cells
phenyl (2S)-2-[[(2S)-2-[[5-(trimethylsilyl)isoxazol-3-yl]carbonyl]pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
phenylmethanesulfonyl fluoride
-
PE and POP are partially resistant to phenylmethanesulfonyl fluoride, a generic serine protease inhibitor that has a low efficiency in inhibiting POP
phenylmethylsulfonyl fluoride
phthalic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 0.021 mM
pimozide
-
11% inhibition at 0.01 mM
prazosin
-
91% inhibition at 0.01 mM
prochlorperazine
-
77% inhibition at 0.01 mM
promazine
-
64% inhibition at 0.01 mM
propeptin
-
a netural inhibitor of POP isolated from Microbispora sp. strain SNA-115
puromycin
-
0.1 mM, 97% inhibition
reboxetine
-
13% inhibition at 0.01 mM
reserpine
-
18% inhibition at 0.01 mM
rhodionin
-
IC50: 0.022 mM
rhodiosin
-
IC50: 0.041 mM
risperidone
-
56% inhibition at 0.01 mM
ritanserin
-
33% inhibition at 0.01 mM
rugosin E
-
from Euphorbia supina, specific, noncompetitive, and strong inhibition
salicylic acid
-
50% inhibition at 1.65 mM
Sn2+
-
87% residual activity at 0.2 mM
Soybean trypsin inhibitor
-
succinic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 77 nM
supinanin
-
specific, noncompetitive, and strong inhibition
teracatain
-
specific, noncompetitive, and strong inhibition
terephthalic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 81 nM
tert-butyl (2S)-2-(pyrrolidin-1-ylcarbonyl)pyrrolidine-1-carboxylate
-
tert-butyl [(2S)-3-methyl-1-(1,3-thiazolidin-3-yl)-1-thioxobutan-2-yl]carbamate
-
-
thioridazine
-
non-competitive inhibitor, 91% inhibition at 0.01 mM
TLCK
0.1 mM, 73.2% inhibition
tosyllysylchloromethane
-
enzyme from brain
tosylphenylalanylchloromethane
-
enzyme from brain, partly
TPCK
0.1 mM, 91.1% inhibition
trachyloban-19-oic acid
-
terpenoid from the bark of Xylopia aethiopia, 50% inhibition at 0.164 mM
Tyr-Pro-Ile-Pro-Phe
-
inhibitory peptide isolated from grapes of Cabernet Sauvignon
Val-Glu-Ile-Pro-Glu
-
inhibitory peptide isolated from grapes of Cabernet Sauvignon
Valproate
-
competitive inhibitor, 56% inhibition at 0.5 mM
Z-Ala-Pro-chloromethylketone
Z-Arg-Pro-chloromethylketone
Z-L-Pro-prolinal
-
50% inhibition at 0.0000022 mM
Z-L-prolyl-L-prolinal
-
-
Z-Pro-Pro-aldehyde-dimethyl acetal
-
Z-Pro-Pro-aldehyde-dimethylacetal
Z-Pro-Pro-dimethyl acetal aldehyde
-
irreversible inhibitor
Z-thioprolyl-thioprolinal-dimethylacetal
-
physiological effects, overview
[(1R,2R)-2-phenylcyclopropyl][(2S,3aS,7aS)-2-(1,3-thiazolidin-3-ylcarbonyl)octahydro-1H-indol-1-yl]methanone
-
-
[(1R,2R)-2-phenylcyclopropyl][(2S,3aS,7aS)-2-(1H-pyrrol-1-ylcarbonyl)octahydro-1H-indol-1-yl]methanone
-
-
[(1R,2R)-2-phenylcyclopropyl][(2S,3aS,7aS)-2-(pyrrolidin-1-ylcarbonyl)octahydro-1H-indol-1-yl]methanone
-
-
[(1R,2R)-2-phenylcyclopropyl][(3S)-3-(pyrrolidin-1-ylcarbonyl)-2-azabicyclo[2.2.2]oct-2-yl]methanone
-
-
[(2R)-1-[N-(2,5-dichlorobenzoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile
i.e. KYP-2047, hyperbolic kinetics of KYP-2047 binding to human PREP with pseudo-firstorder rate constant, Van't Hoff plot for binding of KYP-2047 to human PREP, a covalent bond is formed between the nitrile group of KYP-2047 and the active site serine
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile
i.e. KYP-2047
(6S)-1-chloro-3-[(4-fluorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
is co-crystallized within the catalytic site of a human chimeric POP protein which provides a more detailed understanding of how these inhibitors interact with the key residues within the catalytic pocket
(6S)-1-chloro-3-[(4-fluorobenzyl)oxy]-6-(pyrrolidin-1-ylcarbonyl)-7,8-dihydropyrrolo[1,2-a]pyrazin-4(6H)-one
-
-
(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile
-
KYP-2047, most potent inhibitor
(S)-1-((S)-1-(4-phenylbutanoyl)-pyrrolidine-2-carbonyl)pyrrolidine-2-carbonitrile
-
KYP-2047, most potent inhibitor
1,10-phenanthroline
Lyophyllum cinerascens
-
-
1,10-phenanthroline
-
about 59% inhibition at 10 mM
3,4-dichloroisocoumarin
-
enzyme from lymphocyte
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
77.3% inhibition at 0.1 mM
4-Chloromercuriphenylsulfonate
-
not
4-Chloromercuriphenylsulfonate
-
-
4-Chloromercuriphenylsulfonate
-
-
4-Chloromercuriphenylsulfonate
-
weak
4-Chloromercuriphenylsulfonate
-
-
4-phenyl-butanoyl-L-prolyl-2(S)-cyanopyrrolidine
-
KYP-2047
4-phenyl-butanoyl-L-prolyl-2(S)-cyanopyrrolidine
-
KYP-204, 0.1 mM and 0.5 mM concentrations significantly inhibit enzyme activity in tissue homogenate
aesculitannin B
-
noncompetitive
aesculitannin B
-
noncompetitive
Al3+
-
65% residual activity at 10 mM
Al3+
-
34.5% residual activity at 1 mM
antipain
-
-
antipain
32.4% inhibition at 0.02 mM
Aprotinin
-
89% residual activity at 1 mM
Aprotinin
-
inhibition of extracellular isozyme
Aprotinin
1.4% inhibition at 0.05 mM
bacitracin
-
-
bacitracin
-
50% inhibition at 0.129 mM
bacitracin
-
50% inhibition at 0.130 mM
benzamidine
-
-
benzamidine
3.7% inhibition at 0.01 mM
benzamidine
1 mM, 7.2% inhibition
benzyl (2S)-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl (2S)-2-[[(2S)-2-formylpyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
-
benzyl [(3R,6R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
-
0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts
benzyl [(3R,6R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate
-
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
-
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
Ascidia sp.
-
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
-
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
Lyophyllum cinerascens
-
-
benzyloxycarbonyl-Gly-Pro-CH2Cl
-
enzyme from kidney and brain
benzyloxycarbonyl-Gly-Pro-CH2Cl
-
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-Prolinal, inhibition of cytsolic isozyme, but no inhibition of the extracellular isozyme in serum
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
Lyophyllum cinerascens
-
-
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
-
benzyloxycarbonyl-Pro-prolinal
-
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
i.e. Z-Pro-prolinal
benzyloxycarbonyl-Pro-prolinal
-
benzyloxycarbonyl-proline-prolinal
-
specific inhibition
benzyloxycarbonyl-proline-prolinal
-
specific inhibition
benzyloxycarbonyl-proline-prolinal
specific inhibition
benzyloxycarbonyl-proline-prolinal
-
specific inhibition
benzyloxycarbonyl-proline-prolinal
-
specific inhibition
bestatin
-
-
bestatin
-
0.5 mM, 97% inhibition
bestatin
2.3% inhibition at 0.001 mM
Boc-Asn-Phe-Pro-aldehyde
-
Boc-Asn-Phe-Pro-aldehyde
-
-
Boc-Asn-Phe-Pro-aldehyde
-
-
Ca2+
-
-
Ca2+
83.9% residual activity at 1 mM
Cd2+
-
enzyme from lymphocyte
Cd2+
-
complete inhibition at 0.05 mM
Chloromethylketone derivatives
-
-
Chloromethylketone derivatives
-
-
Chloromethylketone derivatives
-
-
Chloromethylketone derivatives
-
-
Co2+
-
48% residual activity at 0.2 mM
Co2+
-
enzyme from lymphocyte
Cu2+
-
12% residual activity at 1 mM
Cu2+
-
14.1% residual activity at 1 mM
Cu2+
-
13% residual activity at 0.2 mM
Cu2+
-
enzyme from lymphocyte
Cu2+
-
57% residual activity at 1 mM
Cu2+
91.2% residual activity at 1 mM
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
Ascidia sp.
-
-
diisopropyl fluorophosphate
-
enzyme from hypophysis, eye-lens and brain
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
13% residual activity at 0.2 mM
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
enzyme from brain, lymphocyte and serum
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
Lyophyllum cinerascens
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
enzyme from kidney and brain
diisopropyl fluorophosphate
-
enzyme from brain and skin
diisopropyl fluorophosphate
complete inhibition at 0.1 mM
diisopropyl fluorophosphate
-
enzyme from brain and muscle
diisopropyl fluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
-
-
dithiothreitol
-
-
dithiothreitol
-
86% residual activity at 5 mM
E64
-
-
E64
6.5% inhibition at 0.01 mM
EDTA
-
37.3% residual activity at 10 mM
EDTA
-
93% residual activity at 0.2 mM
EDTA
Lyophyllum cinerascens
-
-
EDTA
-
94% residual activity at 1 mM
EDTA
3.8% inhibition at 1 mM
EDTA
91.2% residual activity at 30 mM
epicatechin
-
noncompetitive
epicatechin
-
noncompetitive
Fe2+
-
55% residual activity at 10 mM
Fe2+
-
80.6% residual activity at 1 mM
Hg2+
-
enzyme from hypophysis and brain
Hg2+
-
complete inhibition at 0.2 mM
Hg2+
-
enzyme from lymphocyte
Hg2+
Lyophyllum cinerascens
-
-
Hg2+
-
complete inhibition at 0.05 mM
iodoacetamide
-
enzyme from brain
iodoacetamide
-
87% residual activity at 0.2 mM
iodoacetamide
-
enzyme from kidney
iodoacetamide
-
enzyme from brain
iodoacetamide
-
23.61% residual activity at 10 mM
iodoacetate
Lyophyllum cinerascens
-
-
iodoacetate
-
enzyme from brain
iodoacetate
98.3% residual activity at 1 mM
isolinderalactone
-
competitive
isolinderalactone
-
competitive
isophthalic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 26 nM
isophthalic acid bis(L-prolyl-pyrrolidine) amide
-
IC50: 26 nM, log O = -0.2, the log P value is a first prediction of the blood-brain barrier penetrability
isophthalic acid L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine L-prolyl-pyrrolidine amide
-
0.00039 nM
isophthalic acid L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine L-prolyl-pyrrolidine amide
-
IC50: 0.39 nM
JTP-4819
-
-
JTP-4819
-
i.e. (S)-2-[[(S)-2-(hydroxyacetyl)-1-yrrolidinyl]carbonyl]-N-(phenylmethyl)-1-pyrrolidinecarboxamide
JTP-4819
-
a selective POP inhibitor, physiological effects, overview
JTP-4819
-
used the tight-binding inhibitor JTP-4819 covalently coupled with fluorescein (FJTP) as a tool to study the changes on expression and localization of POP protein
JTP-4819
-
i.e. (S)-2-[[(S)-2-(hydroxyacetyl)-1-pyrrolidinyl]carbonyl]-N(phenylmethyl)-1-pyrrolidinecarboxamide
JTP-4819
-
i.e. (S)-2-[[(S)-2-(hydroxyacetyl)-1-yrrolidinyl]carbonyl]-N-(phenylmethyl)-1-pyrrolidinecarboxamide
JTP-4819
-
a selective POP inhibitor, physiological effects, overview
JTP-4819
-
a selective POP inhibitor, physiological effects, overview
JTP-4819
-
i.e. (S)-2-[[(S)-2-(hydroxyacetyl)-1-yrrolidinyl]carbonyl]-N-(phenylmethyl)-1-pyrrolidinecarboxamide, improves learning deficits in rats with dorsal hippocampal lesions
JTP-4819
-
a selective POP inhibitor, physiological effects, overview
JTP-4819
-
a selective POP inhibitor, physiological effects, overview
K+
-
92.2% residual activity at 1 mM
K+
-
63% residual activity at 1 mM
K+
88.8% residual activity at 1 mM
KYP-2047
-
i.e. 4-phenylbutanoyl-L-prolyl-2(S)cyanopyrrolidine
KYP-2047
-
i.e. 4-phenylbutanoyl-l-prolyl-2(S)-cyanopyrrolidine, highly potent covalent reversible competitive inhibitor
KYP-2047
-
i.e. 4-phenylbutanoyl-L-prolyl-(2S)-cyanopyrrolidine
KYP-2047
-
selective inhibitor, i.e (2S)-1[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinylcarbonyl]-2-pyrrolidinecarbonitrile
KYP-2047
-
specific inhibitor, complete inhibition at 0.06 mM
KYP-2047
-
i.e. 4-phenylbutanoyl-l-prolyl-2(S)-cyanopyrrolidine
leupeptin
-
86% residual activity at 1 mM
leupeptin
2.3% inhibition at 0.02 mM
leupeptin
0.1 mM, 46.2% inhibition
linderalactone
-
competitive
linderalactone
-
competitive
linderene
-
competitive
linderene acetate
-
competitive
linderene acetate
-
competitive
lithium
-
reverses the effect of the drugs
lithium
-
mechanism, reverses the effect of drugs
lupeol
-
50% inhibition at 0.065 mM
lupeol
-
0.1 mM, 5% enzyme inhibition
Mg2+
-
97% residual activity at 10 mM
Mg2+
-
87.3% residual activity at 1 mM
Mg2+
-
87% residual activity at 1 mM
Mg2+
90.1 % residual activity at 1 mM
Mn2+
-
30% residual activity at 10 mM
Mn2+
-
24.3% residual activity at 1 mM
Mn2+
-
93% residual activity at 0.2 mM
Mn2+
-
87% residual activity at 1 mM
Mn2+
90.4% residual activity at 1 mM
N-ethylmaleimide
-
-
N-ethylmaleimide
-
50% residual activity at 0.2 mM
N-ethylmaleimide
-
complete inhibition at 10 mM
Na+
-
93.1% residual activity at 1 mM
Na+
92.3% residual activity at 1 mM
NEM
-
enzyme from hypophysis and eye-lens
NEM
-
enzyme from brain and skin
Ni2+
-
86% residual activity at 0.2 mM
Ni2+
-
58% residual activity at 0.05 mM
o-phenanthroline
-
79% residual activity at 0.2 mM
oleic acid
-
50% inhibition at 0.031 mM
oleic acid
-
50% inhibition at 0.0236 mM
ONO-1603
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
PCMB
-
-
PCMB
-
enzyme from lymphocyte
PCMB
Lyophyllum cinerascens
-
-
PCMB
-
enzyme from kidney and brain
PCMB
-
enzyme from brain and skin
PCMB
0.1 mM, 98% inhibition
Pefabloc SC
-
-
Pefabloc SC
12% inhibition at 1 mM
pepstatin A
-
-
pepstatin A
7.3% inhibition at 0.001 mM
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
97% residual activity at 1 mM
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
18% residual activity at 1 mM
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
47.6% inhibition at 1 mM
phenylmethylsulfonyl fluoride
96% residual activity at 1 mM
PMSF
Ascidia sp.
-
-
PMSF
-
enzyme from lymphocyte
PMSF
Lyophyllum cinerascens
-
-
PMSF
-
enzyme from brain and partly enzyme from skin
PMSF
1 mM, 18% inhibition
rosmarinic acid
-
non-competitive inhibitor
S 17092
-
selective enzyme inhibitor, pharmacodynamics and pharmacokinetics, overview
S 17092
-
physiological effects, overview
S 17092
-
selective enzyme inhibitor, pharmacodynamics and pharmacokinetics, overview
S 17092
-
physiological effects, overview
S 17092
-
physiological effects, overview
S 17092
-
selective enzyme inhibitor, pharmacodynamics and pharmacokinetics, overview
S 17092
-
physiological effects, overview
S 17092
-
physiological effects, overview
S-17092
-
-
S-17092
-
i.e. (2S,3aS,7aS)-1-[(R,R)-2-phenylcyclopropyl]-2-[(thiazolidin-3-yl)carbonyl]octahydro-1H-indole, specific enzyme inhibitor
S-17092
-
i.e. (2S,3aS,7aS)-1-[[(R,R)-2-phenylcyclopropyl]carbonyl]-2-[(thiazolidin-3-yl)carbonyl] octahydro-1H-indole
S-17092
-
i.e. (2S,3aS,7aS)-1-[[(R,R)-2-phenylcyclopropyl]carbonyl]-2-[(thiazolidin-3-yl)carbonyl] octahydro-1H-indole
S-17092
-
i.e. (2S,3aS,7aS)-1-[[(R,R)-2-phenylcyclopropyl]carbonyl]-2-[(thiazolidin-3-yl)carbonyl] octahydro-1H-indole
Soybean trypsin inhibitor
-
-
-
Soybean trypsin inhibitor
12.3% inhibition at 0.01 mM
-
SUAM 14746
-
i.e. 3-([4-[2-(E)-styrylphenoxy]butanoyl]-L-4-hydroxyprolyl)thiazolidine
SUAM 14746
i.e. 3-([4-[2-(E)-styrylphenoxy]butanoyl]-L-4-hydroxyprolyl)thiazolidine
SUAM-1221
-
-
SUAM-14746
-
-
SUAM-14746
-
specific inhibitor, complete inhibition at 0.03 mM
UAMC-00021
-
-
Valproic acid
-
reverses the effect of the drugs
Valproic acid
-
mechanism, reverses the effect of drugs
Valproic acid
-
an antimanic drug
Y-29794 oxalate
-
-
Z-Ala-Pro-aldehyde
-
-
Z-Ala-Pro-chloromethylketone
-
-
Z-Ala-Pro-chloromethylketone
complete inhibition at 0.001 mM
Z-Arg-Pro-aldehyde
-
-
Z-Arg-Pro-chloromethylketone
-
-
Z-Arg-Pro-chloromethylketone
-
Z-Gly-Pro-aldehyde
-
-
Z-Lys-Pro-aldehyde
-
-
Z-Pro
-
-
Z-Pro
41.1% inhibition at 0.1 mM
Z-Pro-Pro
-
-
Z-Pro-Pro
37.6% inhibition at 0.1 mM
Z-Pro-Pro-aldehyde
-
-
Z-Pro-Pro-aldehyde
complete inhibition at 0.001 mM
Z-Pro-Pro-aldehyde-dimethylacetal
-
-
Z-Pro-Pro-aldehyde-dimethylacetal
-
-
Z-Pro-prolinal
-
-
Z-Pro-prolinal
-
a transition state analog inhibitor, binding structure
Z-Pro-prolinal
-
30% residual activity at 0.1 mM
Z-Pro-prolinal
-
a transition state analog inhibitor, binding structure
Z-Pro-prolinal
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physiological effects, overview
Z-Pro-prolinal
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specific inhibitor
Z-Pro-prolinal
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with high potency but relatively poor stability
Z-Tyr-Pro-aldehyde
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Zn2+
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91% residual activity at 10 mM
Zn2+
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31.2% residual activity at 1 mM
Zn2+
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61% residual activity at 0.2 mM
Zn2+
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enzyme from lymphocyte
Zn2+
91.3% residual activity at 1 mM
ZTTA
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i.e. N-benzyloxycarbonyl-thioprolyl-thioprolinal-dimethylacetal
ZTTA
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i.e. N-benzyloxycarbonyl-thioprolyl-thioprolinal-dimethylacetal
ZTTA
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i.e. N-benzyloxycarbonyl-thioprolyl-thioprolinal-dimethylacetal
additional information
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the enzyme is completely resistant to digestion with pepsin
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additional information
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additional information
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different N-blocked L-proline-containing compounds and derivatives
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additional information
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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comparison of inhibitory effects of methylchalcones on enzyme, trypsin and thrombin
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additional information
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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endogenous inhibitor
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additional information
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resistant to: PMSF, thyorphan, E64 and phosphoramidon
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additional information
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at least 3 galloyl groups are required for strong inhibition activity by Euphorbiaceae plants, poor inhibition by 1-galloyl glucopyranoside, 1,6-digalloyl glucopyranoside, 2,6-digalloyl glucopyranoside, 2-galloyl galactose, 6-galloyl-1-O-(4-gallate)-glucopyranoside, 6-galloyl-1-O-(phloroglucinol)-glucopyranoside, gallic acid, furosin, anthricin, gomisin A, tigloyl gomisin, 8-C-(glucopyranosyl)-kaempferol, 3-O-galloyl shikimate, 4-O-galloyl shikimate, 3-O-(2-galloyl-glucopyranosyl)-quercetin, quercetin-3-O-glucopyranoside, alpha-viniferin, 5-O-galloylquininc acid, and shizarin, overview
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additional information
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no inhibition by lithium, carbamazepime, desipramine, fluoxetine, and olanzapine
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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not inhibited by cyclosporine A
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additional information
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not inhibited by huperzine A
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additional information
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additional information
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no inhibition by lithium, carbamazepime, desipramine, fluoxetine, and olanzapine
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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inhibitor binding structure
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additional information
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not inhibited by p-aminobenzamidine, 1,10-phenanthroline and 2-mercaptoethanol
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additional information
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no effect by SH-reagents and metal chelators
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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additional information
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no inhibition by lithium, carbamazepime, desipramine, fluoxetine, and olanzapine
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additional information
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structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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not inhibited by carbamazepine, bupropion, diazepam, fluoxetine, haloperidol, lithium, maprotiline, mirtazapine, moclobemide, pargyline, pinoline, scopolamine, selegiline, sulpiride, venlafaxine, and valpraote at 0.01 mM concentration
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additional information
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not diisopropyl fluorophosphate, p-chloromercuriphenylsulfonic acid
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additional information
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inhibitor synthesis, overview
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additional information
structure-function relationship of inhibitors, specificity at the P2 and S3 position, overview
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additional information
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specific dipeptidyl peptidase IV inhibitor HIV-1 tat (1-9) fragment with sequence H-Met-Asp-Pro-Val-Asp-Pro-Asn-Ile-Glu-OH
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