Cloned (Comment) | Organism |
---|---|
expression of UCH-L1 in H1299 cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | silencing of UCH-L1 by expression of siRNA in H1299 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(3E)-1-(3,4-dichlorobenzyl)-4-methoxy-5-phenyl-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0061 mM | Homo sapiens | |
(3E)-1-(3,4-dichlorobenzyl)-5-iodo-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.00094 mM; IC50: 0.016 mM | Homo sapiens | |
(3E)-1-(3,4-dichlorobenzyl)-5-methoxy-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0029 mM | Homo sapiens | |
(3E)-1-{2-bromo-2-[3-(trifluoromethyl)phenyl]ethyl}-5-chloro-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0095 mM | Homo sapiens | |
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carbonitrile | IC50: 0.012 mM | Homo sapiens | |
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxamide | IC50: 0.0041 mM | Homo sapiens | |
(3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxylic acid | IC50: 0.05 mM | Homo sapiens | |
(3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0034 mM | Homo sapiens | |
(3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | IC50: 0.078 mM | Homo sapiens | |
(3E)-5-bromo-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.00081 mM | Homo sapiens | |
(3E)-5-chloro-1-(2,3-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0027 mM | Homo sapiens | |
(3E)-5-chloro-1-(2,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0012 mM | Homo sapiens | |
(3E)-5-chloro-1-(2,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.00088 mM | Homo sapiens | |
(3E)-5-chloro-1-(2-chloro-5-fluorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0065 mM | Homo sapiens | |
(3E)-5-chloro-1-(2-naphthylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.014 mM | Homo sapiens | |
(3E)-5-chloro-1-(2-phenylethyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.019 mM | Homo sapiens | |
(3E)-5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0018 mM; IC50: 0.017 mM | Homo sapiens | |
(3E)-5-chloro-1-(3,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0013 mM | Homo sapiens | |
(3E)-5-chloro-1-(3-chloro-4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.021 mM | Homo sapiens | |
(3E)-5-chloro-1-(3-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.013 mM | Homo sapiens | |
(3E)-5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.012 mM | Homo sapiens | |
(3E)-5-chloro-1-(4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.052 mM | Homo sapiens | |
(3E)-5-chloro-1-[2-(3,4-dichlorophenoxy)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0062 mM | Homo sapiens | |
(3E)-5-chloro-1-[2-(3,4-dichlorophenyl)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0013 mM | Homo sapiens | |
(3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.018 mM | Homo sapiens | |
(3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | IC50: 0.321 mM | Homo sapiens | |
(3E)-5-chloro-1-[3-(3,4-dichlorophenyl)propyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.016 mM | Homo sapiens | |
(3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.006 mM; IC50: 0.036 mM | Homo sapiens | |
(3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | IC50: 0.114 mM | Homo sapiens | |
(3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.012 mM | Homo sapiens | |
(3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | IC50: 0.013 mM | Homo sapiens | |
(3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0088 mM | Homo sapiens | |
(3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | IC50: 0.045 mM | Homo sapiens | |
(3E)-5-chloro-1-{1-[3-(trichloromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0034 mM | Homo sapiens | |
(3E)-5-chloro-1-{1-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | IC50: 0.022 mM | Homo sapiens | |
(3E)-5-chloro-1-{2-ethoxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.095 mM | Homo sapiens | |
(3E)-5-chloro-1-{2-hydroxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.019 mM | Homo sapiens | |
(3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0041 mM | Homo sapiens | |
(3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | IC50: 0.08 mM | Homo sapiens | |
(3E)-5-chloro-7-methyl-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.012 mM | Homo sapiens | |
(3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0061 mM | Homo sapiens | |
(3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | IC50: 0.043 mM | Homo sapiens | |
(3E)-6-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0058 mM | Homo sapiens | |
5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | IC50: 0.0018 mM | Homo sapiens | |
5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-oxime | IC50: 0.012 mM | Homo sapiens | |
isatin O-acyl oximes | reversible and competitive inhibition, inhibitory potency and features of the drivatives, specific inhibition of UCH-L1, poor inhibition of UCH-L3, IC50 values, overview | Homo sapiens | |
additional information | IC50 above 0.1 mM: (3E)-5-chloro-1-(pyridin-3-ylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime), (3E)-5-chloro-1-(pyridin-4-ylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime), 4-({(3E)-3-[(acetyloxy)imino]-5-chloro-2-oxo-2,3-dihydro-1H-indol-1-yl}methyl)benzoic acid | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Homo sapiens | - |
two isozymes UCH-L1 and UCH-L3 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
H358 cell | non-small cell lung cancer cell line | Homo sapiens | - |
additional information | no expression of UCH-L1 in healthy lung tissue | Homo sapiens | - |
NCI-H1299 cell | lung cancer cell line | Homo sapiens | - |
NCI-H1299 cell | non-small cell lung cancer cell line | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ubiquitin-7-amido-4-methylcoumarin + H2O | UCH-L1 and UCH-L3 | Homo sapiens | ubiquitin + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UCH-L1 | - |
Homo sapiens |
UCH-L3 | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics of isatin O-acyl oximes, overview | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00081 | - |
IC50: 0.00081 mM | Homo sapiens | (3E)-5-bromo-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.00088 | - |
IC50: 0.00088 mM | Homo sapiens | (3E)-5-chloro-1-(2,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.00094 | - |
IC50: 0.00094 mM | Homo sapiens | (3E)-1-(3,4-dichlorobenzyl)-5-iodo-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0012 | - |
IC50: 0.0012 mM | Homo sapiens | (3E)-5-chloro-1-(2,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0013 | - |
IC50: 0.0013 mM | Homo sapiens | (3E)-5-chloro-1-[2-(3,4-dichlorophenyl)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0013 | - |
IC50: 0.0013 mM | Homo sapiens | (3E)-5-chloro-1-(3,5-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0018 | - |
IC50: 0.0018 mM | Homo sapiens | (3E)-5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0018 | - |
IC50: 0.0018 mM | Homo sapiens | 5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0027 | - |
IC50: 0.0027 mM | Homo sapiens | (3E)-5-chloro-1-(2,3-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0029 | - |
IC50: 0.0029 mM | Homo sapiens | (3E)-1-(3,4-dichlorobenzyl)-5-methoxy-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0034 | - |
IC50: 0.0034 mM | Homo sapiens | (3E)-5-chloro-1-{1-[3-(trichloromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0034 | - |
IC50: 0.0034 mM | Homo sapiens | (3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0041 | - |
IC50: 0.0041 mM | Homo sapiens | (3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0041 | - |
IC50: 0.0041 mM | Homo sapiens | (3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxamide | |
0.0058 | - |
IC50: 0.0058 mM | Homo sapiens | (3E)-6-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.006 | - |
IC50: 0.006 mM | Homo sapiens | (3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0061 | - |
IC50: 0.0061 mM | Homo sapiens | (3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0061 | - |
IC50: 0.0061 mM | Homo sapiens | (3E)-1-(3,4-dichlorobenzyl)-4-methoxy-5-phenyl-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0062 | - |
IC50: 0.0062 mM | Homo sapiens | (3E)-5-chloro-1-[2-(3,4-dichlorophenoxy)ethyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0065 | - |
IC50: 0.0065 mM | Homo sapiens | (3E)-5-chloro-1-(2-chloro-5-fluorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0088 | - |
IC50: 0.0088 mM | Homo sapiens | (3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.0095 | - |
IC50: 0.0095 mM | Homo sapiens | (3E)-1-{2-bromo-2-[3-(trifluoromethyl)phenyl]ethyl}-5-chloro-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.012 | - |
IC50: 0.012 mM | Homo sapiens | (3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.012 | - |
IC50: 0.012 mM | Homo sapiens | 5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-oxime | |
0.012 | - |
IC50: 0.012 mM | Homo sapiens | (3E)-5-chloro-1-(4-chlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.012 | - |
IC50: 0.012 mM | Homo sapiens | (3E)-5-chloro-7-methyl-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.012 | - |
IC50: 0.012 mM | Homo sapiens | (3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carbonitrile | |
0.013 | - |
IC50: 0.013 mM | Homo sapiens | (3E)-5-chloro-1-[4-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | |
0.013 | - |
IC50: 0.013 mM | Homo sapiens | (3E)-5-chloro-1-(3-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.014 | - |
IC50: 0.014 mM | Homo sapiens | (3E)-5-chloro-1-(2-naphthylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.016 | - |
IC50: 0.016 mM | Homo sapiens | (3E)-1-(3,4-dichlorobenzyl)-5-iodo-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.016 | - |
IC50: 0.016 mM | Homo sapiens | (3E)-5-chloro-1-[3-(3,4-dichlorophenyl)propyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.017 | - |
IC50: 0.017 mM | Homo sapiens | (3E)-5-chloro-1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.018 | - |
IC50: 0.018 mM | Homo sapiens | (3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.019 | - |
IC50: 0.019 mM | Homo sapiens | (3E)-5-chloro-1-{2-hydroxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.019 | - |
IC50: 0.019 mM | Homo sapiens | (3E)-5-chloro-1-(2-phenylethyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.021 | - |
IC50: 0.021 mM | Homo sapiens | (3E)-5-chloro-1-(3-chloro-4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.022 | - |
IC50: 0.022 mM | Homo sapiens | (3E)-5-chloro-1-{1-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | |
0.036 | - |
IC50: 0.036 mM | Homo sapiens | (3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.043 | - |
IC50: 0.043 mM | Homo sapiens | (3E)-5-fluoro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | |
0.045 | - |
IC50: 0.045 mM | Homo sapiens | (3E)-5-chloro-1-{1-[2-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | |
0.05 | - |
IC50: 0.05 mM | Homo sapiens | (3E)-3-[(acetyloxy)imino]-1-(3,4-dichlorobenzyl)-2-oxoindoline-5-carboxylic acid | |
0.052 | - |
IC50: 0.052 mM | Homo sapiens | (3E)-5-chloro-1-(4-methoxybenzyl)-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.078 | - |
IC50: 0.078 mM | Homo sapiens | (3E)-5-(trifluoromethoxy)-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | |
0.08 | - |
IC50: 0.08 mM | Homo sapiens | (3E)-5-chloro-1-{2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-oxime | |
0.095 | - |
IC50: 0.095 mM | Homo sapiens | (3E)-5-chloro-1-{2-ethoxy-2-[3-(trifluoromethyl)phenyl]ethyl}-1H-indole-2,3-dione 3-(O-acetyloxime) | |
0.1 | - |
IC50 above 0.1 mM: (3E)-5-chloro-1-(pyridin-3-ylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime), (3E)-5-chloro-1-(pyridin-4-ylmethyl)-1H-indole-2,3-dione 3-(O-acetyloxime), 4-({(3E)-3-[(acetyloxy)imino]-5-chloro-2-oxo-2,3-dihydro-1H-indol-1-yl}methyl)benzoi | Homo sapiens | additional information | |
0.114 | - |
IC50: 0.114 mM | Homo sapiens | (3E)-5-chloro-1-[3-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime | |
0.321 | - |
IC50: 0.321 mM | Homo sapiens | (3E)-5-chloro-1-[2-(trifluoromethyl)benzyl]-1H-indole-2,3-dione 3-oxime |