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Literature summary for 2.5.1.18 extracted from

  • Yang, X.; Liu, G.; Li, H.; Zhang, Y.; Song, D.; Li, C.; Wang, R.; Liu, B.; Liang, W.; Jing, Y.; Zhao, G.
    Novel oxadiazole analogues derived from ethacrynic acid: design, synthesis, and structure-activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation (2010), J. Med. Chem., 53, 1015-1022.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-methoxyphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
Homo sapiens
5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
Homo sapiens
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
Homo sapiens
5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
Homo sapiens
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
-
Homo sapiens
5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazole
-
Homo sapiens
5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazole
-
Homo sapiens
Ethacrynic acid inhibits isozyme GSTP1-1 Homo sapiens
additional information antitumor and antirpoliferative activities of inhibitors versus cancer cell lines, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
Homo sapiens
-
HL-60 cell
-
Homo sapiens
-
MCF-10A cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-
PC-3 cell
-
Homo sapiens
-
T-47D cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information structure-activity relationships, overview Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
More structure-activity relationships, overview Homo sapiens

Synonyms

Synonyms Comment Organism
glutathione S-transferase P1-1
-
Homo sapiens
GST P1-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
0.0007
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
0.0007
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
0.0013
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
0.0014
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
0.0018
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
0.002
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
0.002
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
0.002
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
0.0021
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
0.0021
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-chloro-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
0.0023
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
0.0024
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
0.0029
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
0.0032
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-bromo-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
0.0033
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
0.0033
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-nitrobenzyl)-1,2,4-oxadiazol
0.0034
-
-
Homo sapiens Ethacrynic acid
0.0034
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-hydroxyphenyl)-1,2,4-oxadiazol
0.0035
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
0.0036
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-phenyl-1,2,4-oxadiazol
0.0038
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-methoxyphenyl)-1,2,4-oxadiazol
0.0039
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol
0.0039
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-fluorophenyl)-1,2,4-oxadiazol
0.004
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dimethyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
0.004
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
0.005
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[3-methyl-4-(2-methylene-1-oxopropyl)phenoxymethyl]-3-methyl-1,2,4-oxadiazol
0.0054
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-chlorobenzyl)-1,2,4-oxadiazol
0.04
-
25°C, isozyme GSTP1-1 Homo sapiens 5-[2,3-dichloro-4-(2-methylene-1-oxobutyl)phenoxymethyl]-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazol