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Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors

Nishimori, I.; Minakuchi, T.; Onishi, S.; Vullo, D.; Scozzafava, A.; Supuran, C.T.; J. Med. Chem. 50, 381-388 (2007)

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
4.2.1.1
-
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
4.2.1.1
2-aminobenzenesulfonamide
-
Homo sapiens
4.2.1.1
2-hydrazinobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(2-aminoethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(2-hydroxyethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(aminomethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(aminosulfonyl)benzoic acid
-
Homo sapiens
4.2.1.1
4-(hydroxymethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-bromobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-chlorobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-fluorobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-iodobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
-
Homo sapiens
4.2.1.1
4-amino-6-chlorobenzene-1,3-disulfonamide
-
Homo sapiens
4.2.1.1
4-amino-N-[4-(aminosulfonyl)benzyl]benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-N-{2-[4-(aminosulfonyl)phenyl]ethyl}benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-Aminobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-hydrazinobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-methylbenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
-
Homo sapiens
4.2.1.1
5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-amino-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-{[(4-aminophenyl)sulfonyl]amino}-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
6-hydroxy-1,3-benzothiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
acetazolamide
-
Homo sapiens
4.2.1.1
benzolamide
-
Homo sapiens
4.2.1.1
brinzolamide
-
Homo sapiens
4.2.1.1
dichlorophenamide
-
Homo sapiens
4.2.1.1
dorzolamide
-
Homo sapiens
4.2.1.1
ethoxzolamide
-
Homo sapiens
4.2.1.1
indisulam
-
Homo sapiens
4.2.1.1
methazolamide
-
Homo sapiens
4.2.1.1
sulpiride
-
Homo sapiens
4.2.1.1
topiramate
-
Homo sapiens
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
4.2.1.1
Homo sapiens
P23280
-
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.2.1.1
CO2 + H2O
-
681312
Homo sapiens
H2CO3
-
-
-
?
Ki Value [mM]
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
4.2.1.1
0.0000008
-
sulpiride
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.0000009
-
brinzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00001
-
dorzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00001
-
methazolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000011
-
acetazolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000024
-
4-amino-N-[2-[4-(aminosulfonyl)phenyl]ethyl]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000043
-
ethoxzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000045
-
topiramate
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000047
-
indisulam
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000055
-
4-amino-N-[4-(aminosulfonyl)benzyl]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000073
-
5-[[(4-aminophenyl)sulfonyl]amino]-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000079
-
dichlorophenamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000086
-
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000093
-
benzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000096
-
4-amino-3-fluorobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000103
-
6-hydroxy-1,3-benzothiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000114
-
5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000608
-
4-amino-6-chlorobenzene-1,3-disulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00074
-
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000772
-
2-aminobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000798
-
5-amino-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000813
-
4-(2-aminoethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000887
-
4-(aminosulfonyl)benzoic acid
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000941
-
4-Aminobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000955
-
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001024
-
4-amino-3-iodobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00109
-
2-hydrazinobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001097
-
4-amino-3-chlorobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001275
-
4-hydrazinobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001582
-
4-methylbenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00415
-
4-(2-hydroxyethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00468
-
4-amino-3-bromobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.0048
-
4-(aminomethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00668
-
4-(hydroxymethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
4.2.1.1
-
Homo sapiens
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
4.2.1.1
2-aminobenzenesulfonamide
-
Homo sapiens
4.2.1.1
2-hydrazinobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(2-aminoethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(2-hydroxyethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(aminomethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-(aminosulfonyl)benzoic acid
-
Homo sapiens
4.2.1.1
4-(hydroxymethyl)benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-bromobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-chlorobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-fluorobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-3-iodobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
-
Homo sapiens
4.2.1.1
4-amino-6-chlorobenzene-1,3-disulfonamide
-
Homo sapiens
4.2.1.1
4-amino-N-[4-(aminosulfonyl)benzyl]benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-amino-N-{2-[4-(aminosulfonyl)phenyl]ethyl}benzenesulfonamide
-
Homo sapiens
4.2.1.1
4-Aminobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-hydrazinobenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-methylbenzenesulfonamide
-
Homo sapiens
4.2.1.1
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
-
Homo sapiens
4.2.1.1
5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-amino-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
5-{[(4-aminophenyl)sulfonyl]amino}-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
6-hydroxy-1,3-benzothiazole-2-sulfonamide
-
Homo sapiens
4.2.1.1
acetazolamide
-
Homo sapiens
4.2.1.1
benzolamide
-
Homo sapiens
4.2.1.1
brinzolamide
-
Homo sapiens
4.2.1.1
dichlorophenamide
-
Homo sapiens
4.2.1.1
dorzolamide
-
Homo sapiens
4.2.1.1
ethoxzolamide
-
Homo sapiens
4.2.1.1
indisulam
-
Homo sapiens
4.2.1.1
methazolamide
-
Homo sapiens
4.2.1.1
sulpiride
-
Homo sapiens
4.2.1.1
topiramate
-
Homo sapiens
Ki Value [mM] (protein specific)
EC Number
Ki Value [mM]
Ki Value maximum [mM]
Inhibitor
Commentary
Organism
Structure
4.2.1.1
0.0000008
-
sulpiride
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.0000009
-
brinzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00001
-
dorzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00001
-
methazolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000011
-
acetazolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000024
-
4-amino-N-[2-[4-(aminosulfonyl)phenyl]ethyl]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000043
-
ethoxzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000045
-
topiramate
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000047
-
indisulam
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000055
-
4-amino-N-[4-(aminosulfonyl)benzyl]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000073
-
5-[[(4-aminophenyl)sulfonyl]amino]-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000079
-
dichlorophenamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000086
-
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000093
-
benzolamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000096
-
4-amino-3-fluorobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000103
-
6-hydroxy-1,3-benzothiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000114
-
5-(2-chlorophenyl)-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000608
-
4-amino-6-chlorobenzene-1,3-disulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00074
-
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000772
-
2-aminobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000798
-
5-amino-1,3,4-thiadiazole-2-sulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000813
-
4-(2-aminoethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000887
-
4-(aminosulfonyl)benzoic acid
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000941
-
4-Aminobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.000955
-
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001024
-
4-amino-3-iodobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00109
-
2-hydrazinobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001097
-
4-amino-3-chlorobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001275
-
4-hydrazinobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.001582
-
4-methylbenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00415
-
4-(2-hydroxyethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00468
-
4-amino-3-bromobenzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.0048
-
4-(aminomethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
4.2.1.1
0.00668
-
4-(hydroxymethyl)benzenesulfonamide
20°C, pH 7.5, full-length recombinant hCA VI
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
4.2.1.1
CO2 + H2O
-
681312
Homo sapiens
H2CO3
-
-
-
?