3.4.23.16: HIV-1 retropepsin
This is an abbreviated version!
For detailed information about HIV-1 retropepsin, go to the full flat file.
Word Map on EC 3.4.23.16
-
3.4.23.16
-
antiretroviral
-
ritonavir
-
transcriptase
-
saquinavir
-
indinavir
-
nelfinavir
-
hiv-infected
-
lopinavir
-
polyproteins
-
flap
-
darunavir
-
amprenavir
-
drug-resistant
-
anti-hiv
-
atazanavir
-
virological
-
haart
-
gag-pol
-
peptidomimetic
-
virion
-
p-glycoprotein
-
lipodystrophy
-
non-nucleoside
-
integrase
-
cross-resistance
-
isostere
-
nonpeptidic
-
zidovudine
-
nevirapine
-
virus-1
-
tipranavir
-
cyp3a4
-
nnrti
-
drug-drug
-
treatment-experienced
-
lamivudine
-
didanosine
-
ritonavir-boosted
-
autoprocessing
-
efavirenz
-
protease-inhibitor
-
stavudine
-
treatment-naive
-
analysis
-
raltegravir
-
zalcitabine
-
plasmepsins
-
antiretroviral-naive
-
pi-based
-
pharmacology
-
drug development
-
medicine
-
hiv-rna
-
lipoatrophy
- 3.4.23.16
-
antiretroviral
- ritonavir
- transcriptase
- saquinavir
- indinavir
- nelfinavir
-
hiv-infected
- lopinavir
- polyproteins
- flap
- darunavir
- amprenavir
-
drug-resistant
-
anti-hiv
- atazanavir
-
virological
-
haart
- gag-pol
-
peptidomimetic
- virion
- p-glycoprotein
- lipodystrophy
-
non-nucleoside
-
integrase
-
cross-resistance
- isostere
-
nonpeptidic
- zidovudine
- nevirapine
- virus-1
- tipranavir
- cyp3a4
-
nnrti
-
drug-drug
-
treatment-experienced
- lamivudine
- didanosine
-
ritonavir-boosted
-
autoprocessing
- efavirenz
-
protease-inhibitor
- stavudine
-
treatment-naive
- analysis
- raltegravir
- zalcitabine
-
plasmepsins
-
antiretroviral-naive
-
pi-based
- pharmacology
- drug development
- medicine
-
hiv-rna
-
lipoatrophy
Reaction
specific for a P1 residue that is hydrophobic, and P1' variable, but often Pro =
Synonyms
CRF01_AE protease, Gag protease, HIV aspartyl protease, HIV PR, HIV protease, HIV-1 aspartyl protease, HIV-1 PR, HIV-1 protease, HIV-1 proteinase, HIV-1PR, HIV-2 protease, HIVPR, human immunodeficiency virus 1 protease, human immunodeficiency virus 1 retropepsin, human immunodeficiency virus protease, human immunodeficiency virus type 1 protease, human immunodeficiency virus type I protease, More, PR, PR1, PR2, retropepsin, retroproteinase
ECTree
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KI Value
KI Value on EC 3.4.23.16 - HIV-1 retropepsin
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0.00011
((S)-1-(N'-(3',5'-difluoro-biphenyl-4-ylmethyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxyindan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000018
((S)-1-(N'-(4'-acetylamino-biphenyl-4-ylmethyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethylpropyl)-carbamic acid methyl ester
-
wild-type protein
0.000008
((S)-1-(N'-(4-benzo[1,3]dioxol-5-yl-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxyindan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000023
((S)-1-(N'-benzyl-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000082
((S)-1-(N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-phenethyl-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000017
((S)-1-(N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-[4-(1-methyl-1H-pyrazol-4-yl)-benzyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000028
((S)-1-(N'-[4-(3,5-dimethyl-isoxazol-4-yl)-benzyl]-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethylpropyl)-carbamic acid methyl ester
-
wild-type protein
0.0000029 - 0.00003
((S)-1-[N'-(4-bromo-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
0.000012
((S)-1-[N'-biphenyl-4-ylmethyl-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0000017 - 0.000016
((S)-1-[N'-[(S)-3-Hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
0.0000012 - 0.000016
((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-3-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
0.0000023
((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-4-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.0006
(1-Benzyl-3-benzylcarbamoyl-3,3-difluoro-2-oxo-propyl)-carbamic acid benzyl ester
-
-
0.000053
(2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-4,4,4-trifluoro-3-methylbut-2-enamide
-
-
0.00061
(2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-4-oxopent-2-enamide
-
-
0.013
(2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(5-methylisoxazol-4-yl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-4,4,4-trifluoro-3-methylbut-2-enamide
-
-
0.00000038
(2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(1R,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide
-
-
0.0000212
(2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(2R,5S)-2-hydroxy-5-methylcyclopentyl]amino]-5-oxopentyl]-N-tert-butyl-4-(3-pyridin-3-ylpropanoyl)piperazine-2-carboxamide
-
-
0.0000019
(2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-2-hydroxy-3-methylbutanamide
-
-
0.0000025
(2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-2-hydroxy-3-methylbutanamide
-
-
0.00000062
(2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-2-hydroxy-3-methylbutanamide
-
-
0.00000029
(2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-2-hydroxy-3-methylbutanamide
-
-
0.00000082
(2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-2,3-dimethylbutanamide
-
-
0.000000063
(2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-2-hydroxy-3-methylbutanamide
-
-
0.000000004
(2S)-N-[(1S,2R,3S,4S)-1-benzyl-2,3-dihydroxy-4-[[(2S)-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanoyl]amino]-5-phenylpentyl]-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide
-
-
0.000000112
(2S)-N-[(1S,2S,4S)-1-benzyl-2-hydroxy-4-[[(2S)-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanoyl]amino]-5-phenylpentyl]-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide
-
-
0.000000063 - 0.000005
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
0.000000011
(2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide)
-
-
0.000000012
(2S,2'S)-N,N'-[(2S,3S,4S,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide)
-
-
0.000006 - 0.000012
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-dicyclohexylhexane-3,4-diol
0.0000013 - 0.000009
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-diphenylhexane-3,4-diol
0.0000023 - 0.000014
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-6-cyclohexyl-1-phenylhexane-3,4-diol
0.0000045
(2S,4S)-2-[(1R)-2-(benzylamino)-2-oxo-1-[(phenylacetyl)amino]ethyl]-N-[(1S)-1-hydroxy-2-phenylethyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00000011
(2S,4S)-N-[(1R,2R)-4-[(1H-benzimidazol-2-ylmethyl)amino]-1-benzyl-2-hydroxy-4-oxobutyl]-2-[(1R)-1-(benzylcarbamoyl)-3-oxo-4-phenylbutyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000053 - 0.00067
(2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide
0.000000068
(3aR,4R,7aS)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.00000065
(3aR,5r,6aS)-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.000000005
(3aR,7aR)-octahydro-1-benzofuran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.000009
(3aR,7aR)-octahydro-1H-inden-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.0000000027
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.00000001
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.000000085
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl {(2S,3R)-3-hydroxy-4-[{[4-(hydroxymethyl)phenyl]sulfonyl}(2-methylpropyl)amino]-1-phenylbutan-2-yl}carbamate
-
pH and temperature not specified in the publication
0.00000029
(3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.000000099
(3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate
-
GRL-02031
0.00000031
(3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate
-
-
0.00000031
(3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-4-(4-amino-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate
-
-
0.00000011
(3aS,5R,7aR)-hexahydro-4H-furo[2,3-b]pyran-5-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.00000037
(3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-3-hydroxypentanamide
-
-
0.00000086
(3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-3-hydroxypentanamide
-
-
0.00000034
(3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-3-hydroxypentanamide
-
-
0.012
(3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(5-methylisoxazol-4-yl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3-methylpent-4-enamide
-
-
0.00000013
(3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide
-
-
0.0000007
(3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide
-
-
0.000000067
(3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide
-
-
0.0000025
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
0.00000031
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-3-hydroxy-4-[(4R)-4-[[4-(hydroxymethyl)-2-methylbenzyl]carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.00000101
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-4-[(4-amino-2-methylbenzyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.0000000052 - 0.00000203
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
0.00000085
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-yl-carbamate
-
-
0.00000028
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(2S,3R)-4-(4-amino-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate
-
-
0.00000028
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate
-
-
0.00000012
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate
-
-
0.000000035
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate
-
-
0.00000031
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((R)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate
-
-
0.00000085
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate
-
-
0.00000024
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((S)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate
-
-
0.000002
(3R,4aR,8aR)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-(phenylsulfanyl)butyl]decahydroisoquinoline-3-carboxamide
-
-
0.0000191
(3R,4S,5S,6S)-2,7-dibenzyl-3,6-bis(phenoxymethyl)-1,2,7-thiadiazepane-4,5-diol 1,1-dioxide
-
-
0.0000862
(3S)-tetrahydrofuran-3-yl [(2S,3R)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
-
0.00000021
(3S)-tetrahydrofuran-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.00000143
(4aR,7aS)-octahydrocyclopenta[b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.0000053
(4aS,7aR)-hexahydro-2H-furo[3,4-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
pH and temperature not specified in the publication
0.000000041
(4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-1,3-thiazolidine-4-carboxamide
-
-
0.0000000055
(4R)-N-tert-butyl-3-[(2S,3S)-3-([(2,6-dimethylphenoxy)acetyl]amino)-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.0000122
(4R,5S,6S,7S)-1,3-dibenzyl-5,6-dihydroxy-4,7-bis(phenoxymethyl)-1,3-diazepan-2-one
-
-
0.00000078
(5R)-1,3-dioxepan-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.000000063 - 0.00001054
(5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000212
(5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000033
(5S)-3-(3,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000000008 - 0.0000034
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000236
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000006 - 0.0000035
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000015 - 0.00000169
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.00000002 - 0.00000268
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000113 - 0.00000655
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000319
(5S)-3-(3-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000004 - 0.0000019
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000317
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000073 - 0.00000204
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000128 - 0.00000957
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000207 - 0.00000956
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000122 - 0.00000389
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000051 - 0.00000476
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000086 - 0.00000245
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.00000013 - 0.0000163
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000006 - 0.0000074
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.00000565 - 0.00006734
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000136 - 0.0000054
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000049 - 0.00000174
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000252
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000235 - 0.00000457
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000286 - 0.00000749
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000196 - 0.00001015
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000206 - 0.0000055
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
0.000000142 - 0.00000436
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000239 - 0.0000106
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000016 - 0.0000125
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000347
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000147
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000117 - 0.00000648
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000167 - 0.00001078
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000025 - 0.00000416
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000033 - 0.00000121
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
0.000000097 - 0.00000186
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000026 - 0.00000338
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000016 - 0.00000296
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.00000015 - 0.0000035
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000232 - 0.00000518
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.00000008 - 0.00000212
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000133 - 0.000003
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000003 - 0.00000245
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000136 - 0.00000571
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000225 - 0.00000995
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
0.000000385
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000736 - 0.00004046
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
0.000000448
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.461
(R)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
-
0.00000007
(R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3,4-methylenedioxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000134
(R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000152
(R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000138
(R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000163
(R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3,4-methylenedioxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000255
(R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.00000031
(R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.000000311
(R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
-
-
0.0262
(S)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
-
0.00000075
(S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide
-
-
0.000000861
(S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide
-
-
0.000000804
(S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide
-
-
0.0343
(S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid tert-butylamide
-
-
0.1486
(S,S,S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid [1-(1-tert-butylcarbamoyl-2-methyl-propylcarbamoyl)-2-methyl-butyl]-amide
-
-
0.000003
1,3,4,7-tetrabenzyl-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.292
1-(benzyl[[(2S)-1-oxo-3-phenylpropan-2-yl]carbamoyl]amino)-L-prolyl-N-tert-butyl-L-valinamide
-
-
0.099
1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-L-prolyl-N-tert-butyl-L-valinamide
-
-
0.574
1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-N-tert-butyl-L-prolinamide
-
-
0.0000006
2-[2-[5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-2,6-diphenyl-hexanoylamino]-3-methyl-butyrylamino]-3-methyl-butyric acid methyl ester
-
-
0.000003
2-[2-[5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-2-methyl-6-phenyl-hexanoylamino]-3-methyl-butyrylamino]-3-methyl-butyric acid methyl ester
-
-
0.0000012
2-[2-[5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-6-phenyl-2-propyl-hexanoylamino]-3-methyl-butyrylamino]-3-methyl-butyric acid methyl ester
-
-
0.000004
2-[2-[5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-6-phenyl-hexanoylamino]-3-methyl-butyrylamino]-3-methyl-butyric acid methyl ester
-
-
0.00005 - 0.00038
3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide
0.000042 - 0.00026
3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide
0.0000023
3-[3-[2-[2-(isoquinolin-5-yloxy)-acetylamino]-3-methylsulfanyl-propionylamino]-2-methoxy-4-phenyl-butyryl]-5,5-dimethyl-thiazolidine-4-carboxylic acid tert-butylamide
-
-
0.00007 - 0.00026
4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis[[4-(trifluoromethyl)benzyl]sulfamoyl]]dibenzamide
0.00024
4,7-dibenzyl-1,3-bis(2-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0011
4,7-dibenzyl-1,3-bis(2-ethoxyethyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.000034
4,7-dibenzyl-1,3-bis(2-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.000036
4,7-dibenzyl-1,3-bis(3,3-dimethylbutyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000014
4,7-dibenzyl-1,3-bis(3-bromobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.00000089
4,7-dibenzyl-1,3-bis(3-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.000003
4,7-dibenzyl-1,3-bis(3-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.000027
4,7-dibenzyl-1,3-bis(4-bromobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000052
4,7-dibenzyl-1,3-bis(4-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000014
4,7-dibenzyl-1,3-bis(4-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000013
4,7-dibenzyl-1,3-bis(cyclobutylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.000037
4,7-dibenzyl-1,3-bis(cyclohexylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000043
4,7-dibenzyl-1,3-bis(cyclopentylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000021
4,7-dibenzyl-1,3-bis(cyclopropylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.00006
4,7-dibenzyl-1,3-bis[2-(ethenyloxy)ethyl]-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000014
4,7-dibenzyl-1,3-dibutyl-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0001
4,7-dibenzyl-1,3-diethyl-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.00026
4,7-dibenzyl-1,3-diheptyl-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.0000046
4,7-dibenzyl-1,3-dihexyl-5,6-dihydroxy-1,3-diazepan-2-one
-
-
0.00011
4,7-dibenzyl-1-decyl-5,6-dihydroxy-3-nonyl-1,3-diazepan-2-one
-
-
0.0019
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methoxybenzyl)-1,3-diazepan-2-one
-
-
0.00079
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methoxyethyl)-1,3-diazepan-2-one
-
-
0.0000072
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methylprop-2-en-1-yl)-1,3-diazepan-2-one
-
-
0.000049
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methylpropyl)-1,3-diazepan-2-one
-
-
0.00000012
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-hydroxybenzyl)-1,3-diazepan-2-one
-
-
0.00000042
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-iodobenzyl)-1,3-diazepan-2-one
-
-
0.0000016
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methoxybenzyl)-1,3-diazepan-2-one
-
-
0.0000071
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbenzyl)-1,3-diazepan-2-one
-
-
0.0000018
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbut-2-en-1-yl)-1,3-diazepan-2-one
-
-
0.000012
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbutyl)-1,3-diazepan-2-one
-
-
0.0000028
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-nitrobenzyl)-1,3-diazepan-2-one
-
-
0.00000012
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-hydroxybenzyl)-1,3-diazepan-2-one
-
-
0.00016
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methoxybenzyl)-1,3-diazepan-2-one
-
-
0.0000058
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methylbenzyl)-1,3-diazepan-2-one
-
-
0.0000071
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methylpentyl)-1,3-diazepan-2-one
-
-
0.00003
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(5-methylhexyl)-1,3-diazepan-2-one
-
-
0.000085
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(naphthalen-1-ylmethyl)-1,3-diazepan-2-one
-
-
0.00000031
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(naphthalen-2-ylmethyl)-1,3-diazepan-2-one
-
-
0.00014
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-2-ylmethyl)-1,3-diazepan-2-one
-
-
0.0000098
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-3-ylmethyl)-1,3-diazepan-2-one
-
-
0.000089
4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-4-ylmethyl)-1,3-diazepan-2-one
-
-
0.0078
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[2-(2-methoxyethoxy)ethyl]-1,3-diazepan-2-one
-
-
0.004
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[2-(morpholin-4-yl)ethyl]-1,3-diazepan-2-one
-
-
0.00000014
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[3-(hydroxymethyl)benzyl]-1,3-diazepan-2-one
-
-
0.000022
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[3-(trifluoromethyl)benzyl]-1,3-diazepan-2-one
-
-
0.00000034 - 0.0017
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(hydroxymethyl)benzyl]-1,3-diazepan-2-one
0.000051
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(trifluoromethyl)benzyl]-1,3-diazepan-2-one
-
-
0.0000052
4,7-dibenzyl-5,6-dihydroxy-1,3-di(prop-2-en-1-yl)-1,3-diazepan-2-one
-
-
0.000022
4,7-dibenzyl-5,6-dihydroxy-1,3-di(prop-2-yn-1-yl)-1,3-diazepan-2-one
-
-
0.0058
4,7-dibenzyl-5,6-dihydroxy-1,3-dimethyl-1,3-diazepan-2-one
-
-
0.0000016
4,7-dibenzyl-5,6-dihydroxy-1,3-dipentyl-1,3-diazepan-2-one
-
-
0.0000079
4,7-dibenzyl-5,6-dihydroxy-1,3-dipropyl-1,3-diazepan-2-one
-
-
0.00000127
4-amino-N-[(2R,3S)-3-{[(aminooxy)carbonyl]amino}-2-hydroxy-4-phenylbutyl]-N-{[(2S)-5-oxopyrrolidin-2-yl]methyl}benzenesulfonamide
-
-
0.0016
4-[[(6-[[(4-aminothiophen-2-yl)carbonyl]amino]-1,3-benzoxazol-2-yl)carbonyl]amino]thiophene-2-carboxylic acid
-
wild-type protein
0.0000052
Ac-His-Gly-Trp-Ile-PSI[N-CH(CH2(CH3)2)-CH(OH)-CH2-CH2-C(O)]-Glu-His-Gly-Asp-NH2
-
-
0.00002
acetyl-pepstatin
-
pH 4.7, competitive versus YVSQNFPIVQNR
0.000027
allyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.0000025
bis-[[N-(1S,2R)-2,3-dihydro-2-hydroxy-1H-inden-1-yl]-2S-phenyl-3-yl-propionamide] sulfoximine
-
-
0.5
E-R-Q-A-N-r-F-L-G-K-I
-
above, wild-type enzyme, mutant V82A enzyme, and mutant I84V enzyme
0.000034
ethyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.002755
methyl (7S,10R,16S)-10-benzyl-13-(4-bromobenzyl)-10-hydroxy-7-isopropyl-17,17-dimethyl-6,9,15-trioxo-2-oxa-5,8,13,14-tetraazaoctadecan-16-ylcarbamate
-
wild-type protein
0.0000032
methyl (7S,10S,16S)-10-benzyl-13-(4-bromobenzyl)-10-hydroxy-7-isopropyl-17,17-dimethyl-6,9,15-trioxo-2-oxa-5,8,13,14-tetraazaoctadecan-16-ylcarbamate
-
wild-type protein
0.00124
methyl (S)-1-(2-((R)-3-benzyl-3-hydroxy-4-((S)-3-methyl-1-(methylamino)-1-oxobutan-2-ylamino)-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.0022
methyl (S)-1-(2-((R)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.0000029
methyl (S)-1-(2-((S)-3-benzyl-3-hydroxy-4-((S)-3-methyl-1-(methylamino)-1-oxobutan-2-ylamino)-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.0000011
methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.000001
methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-3-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.000002
methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-4-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.0000017
methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate
-
wild-type protein
0.0061
methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate
-
wild-type protein
0.000005
methyl [(2S)-1-[2-[(2S)-2-benzyl-2-hydroxy-3-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-3-oxopropyl]-2-[4-(pyridin-3-yl)benzyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
-
wild-type protein
0.0000028
methyl [(2S)-1-[2-[(4R)-4-benzyl-4-hydroxy-5-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-2-[4-(pyridin-4-yl)benzyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
-
wild-type protein
0.000000289 - 0.00000368
methyl [3-[(5S)-5-([(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
0.000000163 - 0.00000444
methyl [3-[(5S)-5-[[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]carbamoyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
0.00046
N-methyl bis-[N-(2,2-dimethyl-8,8a-dihydro-3aH-indeno[(1S,2R)-1,2]-oxazol-3-yl) 2R-benzyl-3-yl propianamide] sulfoximine
-
-
0.0024
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-2-thiophen-3-ylacetamide
-
-
0.0011
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]pyridazine-4-carboxamide
-
-
0.00051
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-2,4,5-trifluoro-3-hydroxybenzamide
-
-
0.00058
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-2-methylbenzamide
-
-
0.0011
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3,4,5-trihydroxybenzamide
-
-
0.00005
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3,4-dihydroxybenzamide
-
-
0.00004
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3-fluoro-2-methylbenzamide
-
-
0.00000013
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-3-hydroxybenzamide
-
-
0.00000024
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-4-oxohexanamide
-
-
0.00000017
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]cyclopropane-1,1-dicarboxamide
-
-
0.0000015
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-3-hydroxybenzamide
-
-
0.0000042
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-4-oxohexanamide
-
-
0.00000079
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]cyclopropane-1,1-dicarboxamide
-
-
0.00000012
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-3-hydroxybenzamide
-
-
0.000000062
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-4-oxohexanamide
-
-
0.00000021
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]cyclopropane-1,1-dicarboxamide
-
-
0.000141
N-[(1S,2R)-1-benzyl-3-[(butylsulfonyl)(3-chlorobenzyl)amino]-2-hydroxypropyl]-2,3-dichlorobenzamide
-
-
0.00065
N-[(1S,2R)-1-benzyl-3-[(butylsulfonyl)(3-chlorobenzyl)amino]-2-hydroxypropyl]-2-bromo-3-methylbenzamide
-
-
0.000000027
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide
-
-
0.00000012
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide
-
-
0.00000012
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide
-
-
0.00000031
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide
-
-
0.0000016
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide
-
-
0.00000021
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide
-
-
0.000000036
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide
-
-
0.000000063
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide
-
-
0.00000013
N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide
-
-
0.000000062 - 0.000007
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
0.000000039 - 0.0000018
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
0.000000046 - 0.00000192
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
0.000058 - 0.0029
N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
0.000024 - 0.000372
N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
0.00000058
N1-[1-Benzyl-3-(2-tert-butylcarbamoyl-pyrrolidin-1-yl)-2-methoxy-3-oxo-propyl]-2-[2-(naphthalen-1-yloxy)-acetylamino]-succinamide
-
-
0.000033
N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-L-alaninamide
-
-
0.000000084
N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-L-valinamide
-
-
0.000000038
N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-L-valinamide
-
-
0.000000033
N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-L-valinamide
-
-
0.000000099
N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-L-valinamide
-
-
0.000000014
N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-L-valinamide
-
-
0.000000057
N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-L-valinamide
-
-
0.000029 - 0.00027
N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide
0.000000002 - 0.000000227
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
0.0000006 - 0.00043
N2-[(2S)-2-[(3R)-5-[(1S)-1-(L-alanylamino)ethyl]-3-benzyl-2,3,6,7-tetrahydro-1H-azepin-1-yl]propanoyl]-N-[(1S,2S,4R)-1-benzyl-2-hydroxy-4-[5-(2-methylpropanoyl)-1H-imidazol-2-yl]-5-phenylpentyl]-L-valinamide
0.00002
N2-[(2S,4S,5S)-5-(acetylamino)-6-cyclohexyl-4-hydroxy-2-(1-methylethyl)hexanoyl]-L-glutaminyl-L-argininamide
-
-
0.00035
phenyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.00002
tert-butyl N-[(1R,2S)-1-benzyl-3-[(4S)-7-fluoro-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]-2-hydroxypropyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.000186
tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-7-(trifluoromethyl)-1,3,4,5-tetrahydro-2H-1lambda6,-2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.0001
tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-8-(trifluoromethyl)-1,3,4,5-tetrahydro-2H-1lambda6,-2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.000019
tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-7-methoxy-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate
-
in 50 mM sodium acetate, pH 5.5, 100 mM NaCl, 1 mg/ml bovine serum albumin, at 30°C
0.000001
[1-(1-Benzyl-3-benzylcarbamoyl-3,3-difluoro-2-oxo-propylcarbamoyl)-2-methyl-propyl]-carbamic acid benzyl ester
-
-
0.0000029
((S)-1-[N'-(4-bromo-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.00003
((S)-1-[N'-(4-bromo-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
L63P/V82T/I84V mutant protein
0.0000017
((S)-1-[N'-[(S)-3-Hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.000016
((S)-1-[N'-[(S)-3-Hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
L63P/V82T/I84V mutant protein
0.0000012
((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-3-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
wild-type protein
0.000016
((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-3-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester
-
L63P/V82T/I84V mutant protein
0.000000063
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
-
wild-type protein
0.00000088
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
-
D30N/L63P/N88D mutant protein
0.0000011
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000013
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
-
I50V/A71V mutant protein
0.000005
(2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000006
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-dicyclohexylhexane-3,4-diol
-
native enzyme
0.000012
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-dicyclohexylhexane-3,4-diol
-
mutant enzyme V82A
0.0000013
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-diphenylhexane-3,4-diol
-
native enzyme
0.000009
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-diphenylhexane-3,4-diol
-
mutant enzyme V82A
0.0000023
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-6-cyclohexyl-1-phenylhexane-3,4-diol
-
native enzyme
0.000014
(2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-6-cyclohexyl-1-phenylhexane-3,4-diol
-
mutant enzyme V82A
0.000053
(2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide
-
wild-type protein
0.00013
(2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide
-
D30N/L63P/N88D mutant protein
0.00014
(2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.00067
(2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.0000000052
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
GRL-0355
0.00000203
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate
-
-
0.000000063
(5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00001054
(5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000000008
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
wild-type protein
0.000000039
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
D30N/L63P/N88D mutant protein
0.00000016
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000014
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
I50V/A71V mutant protein
0.0000034
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000006
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
wild-type protein
0.00000024
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
D30N/L63P/N88D mutant protein
0.00000072
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000023
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
I50V/A71V mutant protein
0.0000035
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000015
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000169
(5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000002
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000268
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000113
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000655
(5S)-3-(3-aminophenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000004
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
wild-type protein
0.00000018
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
D30N/L63P/N88D mutant protein
0.00000078
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000001
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
I50V/A71V mutant protein
0.0000019
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000073
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000204
(5S)-3-(4-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000128
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000957
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000207
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000956
(5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000122
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000389
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000051
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000476
(5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000086
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000245
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000013
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000163
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000006
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
wild-type protein
0.00000027
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
D30N/L63P/N88D mutant protein
0.000001
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000042
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
I50V/A71V mutant protein
0.0000074
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00000565
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00006734
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000136
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000054
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000049
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000174
(5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000235
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000457
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000286
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000749
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000196
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00001015
(5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000206
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000055
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000142
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000436
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000239
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000106
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000016
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
wild-type protein
0.00000059
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
D30N/L63P/N88D mutant protein
0.0000021
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000077
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.0000125
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
-
I50V/A71V mutant protein
0.000000117
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000648
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000167
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00001078
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000025
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000416
(5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000033
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000121
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000097
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000186
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000026
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000338
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000016
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000296
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000015
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.0000035
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000232
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000518
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000008
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000212
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000133
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000003
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000003
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000245
(5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000136
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000571
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000225
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000995
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000736
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00004046
(5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00005
3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide
-
wild-type protein
0.000066
3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide
-
D30N/L63P/N88D mutant protein
0.00014
3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00038
3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000042
3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide
-
wild-type protein
0.000079
3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000085
3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide
-
D30N/L63P/N88D mutant protein
0.00026
3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000036
-
mutant I84V, pH 5.5
0.00026
4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis(benzylsulfamoyl)]dibenzamide
-
wild-type, pH 5.5
0.0014
4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis(benzylsulfamoyl)]dibenzamide
-
mutant I50V, pH 5.5
0.00007
-
wild-type, pH 5.5
0.00012
4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis[[4-(trifluoromethyl)benzyl]sulfamoyl]]dibenzamide
-
mutant I84V, pH 5.5
0.00026
4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis[[4-(trifluoromethyl)benzyl]sulfamoyl]]dibenzamide
-
mutant I50V, pH 5.5
0.00000034
-
-
0.0017
4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(hydroxymethyl)benzyl]-1,3-diazepan-2-one
-
-
0.0000022
Ace-T-I-Nle-r-Nle-Q-R
-
pH 5.0, 25°C, wild-type enzyme
0.000022
mutant enzyme PRS17, at pH 5.6 and 37°C
0.000024
Ace-TINlerNleQR
mutant enzyme PRV82A, at pH 5.6 and 37°C
0.000075
Ace-TINlerNleQR
wild type enzyme, at pH 5.6 and 37°C
0.000000021
-
pH 4.7, 37°C, recombinant LAI wild-type enzyme
0.00000004
AG1776
-
pH 4.7, 37°C, recombinant V6 wild-type enzyme
0.0000022
AG1776
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I84V
0.0000056
AG1776
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I54V/I84V
0.0000094
AG1776
-
pH 4.7, 37°C, recombinant V6 mutant I54V/I84V
0.00000015
amprenavir
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.00000017
amprenavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.00000039
amprenavir
wild type enzyme, at pH 5.0 and 20°C
0.000001
amprenavir
mutant enzyme V32I/I47V/V82I, at pH 4.0 and 28°C
0.0000014
amprenavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00000324
amprenavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.0000035
amprenavir
mutant enzyme V32I/I47V/V82I, at pH 5.8 and 28°C
0.00000033
atazanavir
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.00000049
atazanavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000005
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000000025
darunavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00000004
darunavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.00000004
darunavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.0000031
indinavir
-
pH 4.7, 37°C, recombinant LAI wild-type enzyme
0.000021
indinavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000062
indinavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I84V
0.000069
indinavir
-
pH 4.7, 37°C, recombinant V6 wild-type enzyme
0.002914
indinavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I54V/I84V
0.004235
indinavir
-
pH 4.7, 37°C, recombinant V6 mutant I54V/I84V
0.0000009
lopinavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000289
methyl [3-[(5S)-5-([(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000368
methyl [3-[(5S)-5-([(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000000163
methyl [3-[(5S)-5-[[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]carbamoyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
wild type enzyme, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.00000444
methyl [3-[(5S)-5-[[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]carbamoyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate
mutant enzyme L10I/L63P/A71V/G73S/I84V/L90M, in 0.1 M sodium acetate, 1 M sodium chloride, 1 mM EDTA, 1 mM dithiothreitol, 2% (v/v) DMSO, and 1 mg/ml bovine serum albumin, at pH 4.7 and 22°C
0.000128
-
mutant I84V, pH 5.5
0.00027
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(4-amino-N-benzylbenzenesulfonamide)
-
wild-type, pH 5.5
0.001
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(4-amino-N-benzylbenzenesulfonamide)
-
mutant I50V, pH 5.5
0.00033
-
mutant I84V, pH 5.5
0.00039
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(4-iodobenzyl)benzenesulfonamide]
-
wild-type, pH 5.5
0.0014
N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(4-iodobenzyl)benzenesulfonamide]
-
mutant I50V, pH 5.5
0.000000062
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
-
wild-type protein
0.00000084
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
-
D30N/L63P/N88D mutant protein
0.0000035
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000053
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
-
I50V/A71V mutant protein
0.000007
N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000039
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
wild-type protein
0.00000012
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
D30N/L63P/N88D mutant protein
0.000000724
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
I50V/A71V mutant protein
0.00000108
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000018
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000046
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
wild-type protein
0.00000031
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
D30N/L63P/N88D mutant protein
0.000000724
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000001713
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00000192
N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide
-
I50V/A71V mutant protein
0.000058
N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
wild-type protein
0.00013
N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
D30N/L63P/N88D mutant protein
0.0013
N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0029
N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000024
N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
wild-type protein
0.000063
N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
D30N/L63P/N88D mutant protein
0.00036
N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000372
N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000029
N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide
-
D30N/L63P/N88D mutant protein
0.000033
N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide
-
wild-type protein
0.000095
N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.00027
N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000000002
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
-
wild-type protein
0.000000063
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
-
I50V/A71V mutant protein
0.000000094
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
-
D30N/L63P/N88D mutant protein
0.000000117
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000000227
N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.0000006
N2-[(2S)-2-[(3R)-5-[(1S)-1-(L-alanylamino)ethyl]-3-benzyl-2,3,6,7-tetrahydro-1H-azepin-1-yl]propanoyl]-N-[(1S,2S,4R)-1-benzyl-2-hydroxy-4-[5-(2-methylpropanoyl)-1H-imidazol-2-yl]-5-phenylpentyl]-L-valinamide
-
-
0.00043
N2-[(2S)-2-[(3R)-5-[(1S)-1-(L-alanylamino)ethyl]-3-benzyl-2,3,6,7-tetrahydro-1H-azepin-1-yl]propanoyl]-N-[(1S,2S,4R)-1-benzyl-2-hydroxy-4-[5-(2-methylpropanoyl)-1H-imidazol-2-yl]-5-phenylpentyl]-L-valinamide
-
-
0.0000012
nelfinavir
-
pH 4.7, 37°C, recombinant LAI wild-type enzyme
0.000017
nelfinavir
-
pH 4.7, 37°C, recombinant V6 wild-type enzyme
0.000019
nelfinavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000023
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant I54V
0.000024
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant I84V
0.000052
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I84V
0.000116
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I
0.000563
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I54V/I84V
0.001259
nelfinavir
-
pH 4.7, 37°C, recombinant V6 mutant I54V/I84V
0.0000007
ritonavir
-
pH 4.7, 37°C, recombinant LAI wild-type enzyme
0.0000028
ritonavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.000003
ritonavir
-
pH 4.7, 37°C, recombinant V6 wild-type enzyme
0.0000065
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I
0.0000109
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant I54V
0.0000165
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant I84V
0.0000345
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I84V
0.0000624
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant M46I/I54V/I84V
0.0000932
ritonavir
-
pH 4.7, 37°C, recombinant V6 mutant I54V/I84V
0.000514
mutant enzyme PRS17, at pH 5.6 and 37°C
0.00053
RVLrFEANle
mutant enzyme PRV82A, at pH 5.6 and 37°C
0.00217
RVLrFEANle
wild type enzyme, at pH 5.6 and 37°C
0.00000007
saquinavir
mutant enzyme V32I/I47V/V82I, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.00000011
saquinavir
wild type enzyme, in 0.5 M potassium phosphate buffer, pH 5.6, containing 10% (v/v) glycerol, 2 mM EDTA, 10 mM dithiothreitol, 4 M NaCl, at 37°C
0.000078
saquinavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
0.0000015
-
wild-type enzyme
0.0000041
tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2
-
mutant A71V/V82T/I84V enzyme
0.000033
-
wild-type enzyme
0.001
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2
-
mutant A71V/V82T/I84V enzyme
0.00000015
-
wild-type enzyme
0.000086
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2
-
mutant A71V/V82T/I84V enzyme
0.00000002
-
wild-type enzyme
0.00000026
tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2
-
mutant A71V/V82T/I84V enzyme
0.000000014
tipranavir
-
L10I/G48V/I54V/L63P/V82A mutant protein
0.000000032
tipranavir
-
L10I/L63P/A71V/G73S/I84V/L90M mutant protein
additional information
-
87% inhibition at 0.01 mM
additional information
bis-[(L-valine-N-methylamide)-2-phenyl-3-yl-propionamide] sulfoxide
-
90% inhibition at 0.01 mM
additional information
bis-[(L-valine-N-methylamide)-2-phenyl-3-yl-propionamide] sulfoximine
-
99% inhibition at 0.01 mM
additional information
bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfide
-
51% inhibition at 0.01 mM
additional information
bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoxide
-
50% inhibition at 0.01 mM
additional information
bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide]sulfoximine
-
54% inhibition at 0.01 mM
additional information
bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfide
-
41% inhibition at 0.01 mM
additional information
bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoxide
-
47% inhibition at 0.01 mM
additional information
bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoximine
-
87% inhibition at 0.01 mM
additional information
additional information
-
kinetic and thermodynamic characterization of HIV-1 protease inhibitors using a biosensor-based method, overview
-
additional information
additional information
-
influence of mutations (D30N, N88D, L90M, A71V, D30N/A71V, D30N/N88D, D30N/L90M, D30N/L63P/A71V/L90M) on the Ki-values for saquinavir, ritonavir, indinavir, nelfinavir, and lopinavir
-
additional information
additional information
-
influence of mutations (D30N, N88D, L90M, D30N/L90M, D30N/N88D, N88D/L90M) on Ki-values for ritonavir, indinavir, nelfinavir, saquinavir, amprenavir, lopinavir, atazanavir, tipranavir
-