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Literature summary for 3.4.21.37 extracted from

  • Veale, C.A.; Bernstein, P.R.; Bohnert, C.M.; Brown, F.J.; Bryant, C.; Damewood, J.R., Jr.; Earley, R.; Feeney, S.W.; Edwards, P.D.; Gomes, B.; Hulsizer, J.M.; Kosmider, B.J.; Krell, R.D.; Moore, G.; Salcedo, T.W.; Shaw, A.; Silberstein, D.S.; Steelman, G.B.; Stein, M.; Strimpler, A.; Thomas, R.M.; Vacek, E.P.; Williams, J.C.; Wolanin, D.J.; Woolson, S.
    Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase (1997), J. Med. Chem., 40, 3173-3181.
    View publication on PubMed

Application

Application Comment Organism
medicine peptidyl trifluoromethyl ketone inhibitors can achieve high levels of oral activity and bioavailibility, and therefore they may prove useful as therapeutic agents in the treatment of diseases in which elastase is implicated Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-1-[(S)-2-(4-methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide
-
Homo sapiens
alpha-ketobenzoxazoles
-
Homo sapiens
difluoro-beta-ketoamides
-
Homo sapiens
difluoromethyleneamines
-
Homo sapiens
ICI 200,355
-
Homo sapiens
ICI 219,680
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1R)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-(benzoylamino)-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
additional information peptidyl trifluoromethyl ketone inhibitors can achieve high levels of oral activity and bioavailibility, and therefore they may prove useful as therapeutic agents in the treatment of diseases in which elastase is implicated Homo sapiens
trifluoromethylketones
-
Homo sapiens
ZD8321
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000035
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
Homo sapiens
0.00000035
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
0.00000038
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
0.00000085
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
0.0000011
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
0.0000015
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
0.0000017
-
L-Prolinamide, N-(phenoxycarbonyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
0.0000026
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
0.000003
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
0.0000031
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
0.0000033
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
Homo sapiens
0.0000034
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-[[(1,1-dimethylethoxy)carbonyl]amino]-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
0.0000038
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-3,3-difluoro-4-(methylamino)-1-(1-methylethyl)-2,4-dioxobutyl]-
-
Homo sapiens
0.0000064
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-(benzoylamino)-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
0.0000067
-
(S)-1-[(S)-2-(4-methoxybenzamido)-3-methylbutyryl]-N-[(S)-2-methyl-1-(trifluoroacetyl)propyl]pyrrolidine-2-carboxamide
-
Homo sapiens
0.000015
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens
0.000058
-
L-Prolinamide, N-(4-methoxybenzoyl)-L-valyl-N-[(1R)-3,3-difluoro-1-(1-methylethyl)-2,4-dioxo-4-[(2-pyridinylmethyl)amino]butyl]-
-
Homo sapiens
0.00013
-
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-4-amino-3,3-difluoro-1-(1-methylethyl)-2-oxobutyl]-
-
Homo sapiens