Literature summary for 3.4.19.12 extracted from

Liu, Y.; Lashuel, H.A.; Choi, S.; Xing, X.; Case, A.; Ni, J.; Yeh, L.A.; Cuny, G.D.; Stein, R.L.; Lansbury, P.T., Jr.
Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line (2003), Chem. Biol., 10, 837-846.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression of UCH-L1 in H1299 cells	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
additional information	silencing of UCH-L1 by expression of siRNA in H1299 cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
(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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Homo sapiens	-	two isozymes UCH-L1 and UCH-L3	-

Source Tissue

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 and Products (Substrate)

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

Synonyms	Comment	Organism
UCH-L1	-	Homo sapiens
UCH-L3	-	Homo sapiens

Ki Value [mM]

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	IC50 Value Maximum	Comment	Organism	Inhibitor
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