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Literature summary for 3.4.21.59 extracted from

  • Lee, C.S.; Liu, W.; Sprengeler, P.A.; Somoza, J.R.; Janc, J.W.; Sperandio, D.; Spencer, J.R.; Green, M.J.; McGrath, M.E.
    Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles (2006), Bioorg. Med. Chem. Lett., 16, 4036-4040.
    View publication on PubMed
Search for more literature for 3.4.21.59

Inhibitors

Inhibitors Comment Organism Structure
benzyl 4-[(3-[N2-[(benzyloxy)carbonyl]-L-lysyl]-1,2,4-oxadiazol-5-yl)methyl]piperazine-1-carboxylate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-([5-[4-(benzylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-([5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-([5-[4-([2-[3-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-([5-[4-([2-[4-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(2-thiophen-2-ylethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(3,4-dimethylbenzyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(3-methylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(4-phenylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-1-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-2-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-methoxybenzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[(2E)-3-phenylprop-2-en-1-yl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,4-dichlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate10n
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,5-difluorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[2-(4-fluorophenoxy)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
benzyl [(1S)-5-amino-1-[[5-(4-[[4-(2-fluorobenzyl)piperazin-1-yl]carbonyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
ethyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
ethyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
additional information design of potent and selective enzyme inhibitors based on alpha-keto-[1,2,4]-oxadiazoles, overview Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-1,3-benzodioxole-5-carboxamide
-
 Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,4-difluorobenzamide
-
 Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,5-difluorobenzamide
-
 Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3-fluorobenzamide
-
 Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-chlorobenzamide
-
 Homo sapiens
N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-fluorobenzamide
-
 Homo sapiens
N-[2-(3-chlorophenyl)ethyl]-4-([3-[N2-(2,2-dimethylpropanoyl)-L-lysyl]-1,2,4-oxadiazol-5-yl]methyl)benzamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
beta-tryptase
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000015
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,5-difluorobenzamide
-
 Homo sapiens
0.0000017
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3-fluorobenzamide
-
 Homo sapiens
0.0000017
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-3,4-difluorobenzamide
-
 Homo sapiens
0.0000018
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000018
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-fluorobenzamide
-
 Homo sapiens
0.0000019
-
 ethyl [(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000019
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-4-chlorobenzamide
-
 Homo sapiens
0.000002
-
 N-[2-(3-chlorophenyl)ethyl]-4-([3-[N2-(2,2-dimethylpropanoyl)-L-lysyl]-1,2,4-oxadiazol-5-yl]methyl)benzamide
-
 Homo sapiens
0.0000021
-
 N-[(1S)-5-amino-1-[[5-(4-[[2-(3-chlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]-1,3-benzodioxole-5-carboxamide
-
 Homo sapiens
0.0000024
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(2-thiophen-2-ylethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000028
-
 ethyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.0000029
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[2-(4-fluorophenoxy)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000003
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000032
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(3-phenylpropyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000035
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,5-difluorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000036
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[(2E)-3-phenylprop-2-en-1-yl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000037
-
 benzyl [(1S)-5-amino-1-([5-[4-(2,3-dihydro-1H-inden-2-ylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.0000058
-
 benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.0000082
-
 benzyl [(1S)-5-amino-1-([5-[4-([2-[3-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.0000099
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(3-methylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000011
-
 benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000011
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-2-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000012
-
 benzyl [(1S)-5-amino-1-([5-[4-(benzyloxy)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.000013
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(naphthalen-1-ylmethyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000016
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[2-(3,4-dichlorophenyl)ethyl]carbamoyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000034
-
 benzyl [(1S)-5-amino-1-[(5-[[4-(4-phenylbutanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.000037
-
 benzyl [(1S)-5-amino-1-([5-[4-(benzylcarbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.000039
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(3,4-dimethylbenzyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.00006
-
 benzyl [(1S)-5-amino-1-[(5-[4-[(4-phenylbutyl)carbamoyl]benzyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.00014
-
 benzyl [(1S)-5-amino-1-[[5-(4-[[4-(2-fluorobenzyl)piperazin-1-yl]carbonyl]benzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens
0.00022
-
 benzyl [(1S)-5-amino-1-([5-[4-([2-[4-(trifluoromethyl)phenyl]ethyl]carbamoyl)benzyl]-1,2,4-oxadiazol-3-yl]carbonyl)pentyl]carbamate
-
 Homo sapiens
0.00023
-
 benzyl [(1S)-5-amino-1-[(5-[[4-(3-phenylpropanoyl)piperazin-1-yl]methyl]-1,2,4-oxadiazol-3-yl)carbonyl]pentyl]carbamate
-
 Homo sapiens
0.00047
-
 benzyl 4-[(3-[N2-[(benzyloxy)carbonyl]-L-lysyl]-1,2,4-oxadiazol-5-yl)methyl]piperazine-1-carboxylate
-
 Homo sapiens
0.00077
-
 benzyl [(1S)-5-amino-1-[[5-(4-methoxybenzyl)-1,2,4-oxadiazol-3-yl]carbonyl]pentyl]carbamate
-
 Homo sapiens