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Literature summary for 3.1.1.1 extracted from

  • Hicks, L.D.; Hyatt, J.L.; Stoddard, S.; Tsurkan, L.; Edwards, C.C.; Wadkins, R.M.; Potter, P.M.
    Improved, selective, human intestinal carboxylesterase inhibitors designed to modulate 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (Irinotecan, CPT-11) toxicity (2009), J. Med. Chem., 52, 3742-3752.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development development and application of hiCE-specific inhibitors designed to selectively modulate drug hydrolysis in vivo Homo sapiens
pharmacology development and application of hiCE-specific inhibitors designed to selectively modulate drug hydrolysis in vivo Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4S)-4,11-diethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
-
Homo sapiens
(4S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl 1,4'-bipiperidine-1'-carboxylate
-
Homo sapiens
2,4-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
2,5-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
3,4-difluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
3,4-difluoro-N-(4-(phenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
4,6-dimethyl-N1,N3-diphenylbenzene-1,3-disulfonamide
-
Homo sapiens
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)-3-methylbenzoic acid
-
Homo sapiens
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)-N-methyl benzamide
-
Homo sapiens
4-(N-(4-(4-fluorophenylsulfonamido)phenyl)sulfamoyl)benzoic acid
-
Homo sapiens
4-bromo-N-(4-ethoxyphenyl)benzene sulfonamide
-
Homo sapiens
4-chloro-N-(4-(4-fluorophenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
4-chloro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
4-chloro-N-(4-ethoxyphenyl)benzene sulfonamide
-
Homo sapiens
4-fluoro-N-(4-(4-methoxy phenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
4-fluoro-N-(4-(4-methylphenylsulfonamido)phenyl)benzene sulfonamide
-
Homo sapiens
7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin i.e. irinotecan or CPT-11, an antitumor prodrug Homo sapiens
additional information development and evaluation of a class of benzene sulfonamide inhibitors, quantitative structure-activity relationship, QSAR, modeling, overview Homo sapiens
N,N'-(1,4-phenylene)bis(2,3-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(2,4,5-trichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(2,5-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(2,6-difluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(2-fluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3,4,5-trifluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3,4-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3,4-difluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3,5-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3,5-difluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3-bromobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(3-fluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(4-fluoro-2-methylbenzene sulfonamide)
-
Homo sapiens
N,N'-(1,4-phenylene)bis(4-fluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-fluoro-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetrafluoro-1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3,4-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3,5-dichlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3-bromobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(3-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-bromobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,3,5,6-tetramethyl-1,4-phenylene)bis(4-fluorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,5-dibromo-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2,5-dibromo-1,4-phenylene)bisbenzene sulfonamide
-
Homo sapiens
N,N'-(2,5-dichloro-1,4-phenylene)bis(4-chlorobenzene sulfonamide)
-
Homo sapiens
N,N'-(2-chloro-1,4-phenylene)dibenzene sulfonamide
-
Homo sapiens
N,N'-(2-methyl-1,4-phenylene)benzene sulfonamide
-
Homo sapiens
N,N'-(2-methylbenzene-1,4-diyl)dibenzenesulfonamide
-
Homo sapiens
N,N'-(disulfanediyldibenzene-4,1-diyl)dimethanesulfonamide
-
Homo sapiens
N,N'-1,4-phenylenebis-2-naphthalene sulfonamide
-
Homo sapiens
N,N'-9H-fluorene-2,7-diylbis(3,4,5-trifluorobenzenesulfonamide)
-
Homo sapiens
N,N'-9H-fluorene-2,7-diylbis(3-bromobenzenesulfonamide)
-
Homo sapiens
N,N'-9H-fluorene-2,7-diylbis(3-chlorobenzenesulfonamide)
-
Homo sapiens
N,N'-9H-fluorene-2,7-diylbis(4-chlorobenzenesulfonamide)
-
Homo sapiens
N,N'-9H-fluorene-2,7-diyldibenzenesulfonamide
-
Homo sapiens
N,N'-benzene-1,4-diyldibenzenesulfonamide
-
Homo sapiens
N-(4-(4-fluoromethylphenylsulfonamido)phenyl)-2,5-dimethylbenzene sulfonamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozymes CE1 and intestinal CE
-

Source Tissue

Source Tissue Comment Organism Textmining
intestine human intestinal CE, hiCE Homo sapiens
-

Synonyms

Synonyms Comment Organism
HCE1
-
Homo sapiens
hiCE
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000079
-
-
Homo sapiens N,N'-9H-fluorene-2,7-diylbis(3,4,5-trifluorobenzenesulfonamide)
0.0000252
-
-
Homo sapiens N,N'-9H-fluorene-2,7-diylbis(4-chlorobenzenesulfonamide)
0.0000984
-
-
Homo sapiens N,N'-9H-fluorene-2,7-diyldibenzenesulfonamide
0.0001
-
-
Homo sapiens N,N'-9H-fluorene-2,7-diylbis(3-chlorobenzenesulfonamide)
0.00057
-
-
Homo sapiens N,N'-9H-fluorene-2,7-diylbis(3-bromobenzenesulfonamide)