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 | 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|
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 |