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Literature summary for 4.2.1.1 extracted from

  • Guezel, O.; Innocenti, A.; Scozzafava, A.; Salman, A.; Supuran, C.T.
    Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inhibitors of human mitochondrial isoforms VA and VB (2009), Bioorg. Med. Chem., 17, 4894-4899.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-(2-phenylacetamido)-3-bromobenzenesulfonamide
-
Homo sapiens
4-(2-phenylacetamido)-3-chlorobenzenesulfonamide
-
Homo sapiens
4-(2-phenylacetamido)-3-fluorobenzenesulfonamide
-
Homo sapiens
4-(2-phenylacetamido)benzenesulfonamide
-
Homo sapiens
4-(2-phenylacetamidoethyl)benzenesulfonamide
-
Homo sapiens
4-(2-phenylacetamidomethyl)benzenesulfonamide
-
Homo sapiens
4-(2-pyridin-2-ylacetamido)benzenesulfonamide
-
Homo sapiens
4-(2-pyridin-4-ylacetamido)benzenesulfonamide
-
Homo sapiens
4-(2-pyridin-4-ylacetamidoethyl)benzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamidoethyl]benzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamidomethyl]benzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamido]-3-bromobenzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamido]-3-chlorobenzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamido]-3-fluorobenzenesulfonamide
-
Homo sapiens
4-[2-(2-thienyl)acetamido]benzenesulfonamide
-
Homo sapiens
5-(2-phenylacetamido)-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
5-[2-(2-thienyl)acetamido]-1,3,4-thiadiazole-2-sulfonamide
-
Homo sapiens
acetazolamide
-
Homo sapiens
topiramate
-
Homo sapiens
zonisamide
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol isoforms CA I and CA II Homo sapiens 5829
-
mitochondrion isoforms CA VA and CA VB Homo sapiens 5739
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
CO2 + H2O Homo sapiens
-
H2CO3
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P35218
-
-
Homo sapiens Q9Y2D0
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CO2 + H2O
-
Homo sapiens H2CO3
-
r

Synonyms

Synonyms Comment Organism
CA I isoform Homo sapiens
CA II isoform Homo sapiens
CA VA isoform Homo sapiens
CA VB isoform Homo sapiens
carbonic anhydrase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0054
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens acetazolamide
0.0059
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-bromobenzenesulfonamide
0.0061
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-(2-phenylacetamido)-1,3,4-thiadiazole-2-sulfonamide
0.0067
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)benzenesulfonamide
0.0068
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-2-ylacetamido)benzenesulfonamide
0.0068
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-2-ylacetamido)benzenesulfonamide
0.0069
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-fluorobenzenesulfonamide
0.007
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]benzenesulfonamide
0.0071
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-bromobenzenesulfonamide
0.0072
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]benzenesulfonamide
0.0072
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidomethyl]benzenesulfonamide
0.0073
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamido)benzenesulfonamide
0.0074
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-[2-(2-thienyl)acetamido]-1,3,4-thiadiazole-2-sulfonamide
0.0075
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-bromobenzenesulfonamide
0.0076
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-[2-(2-thienyl)acetamido]-1,3,4-thiadiazole-2-sulfonamide
0.0076
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamidoethyl)benzenesulfonamide
0.0077
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-chlorobenzenesulfonamide
0.0079
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-fluorobenzenesulfonamide
0.0079
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)benzenesulfonamide
0.008
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidoethyl]benzenesulfonamide
0.0081
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidoethyl)benzenesulfonamide
0.0081
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-fluorobenzenesulfonamide
0.0081
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-chlorobenzenesulfonamide
0.0082
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-chlorobenzenesulfonamide
0.0082
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidoethyl)benzenesulfonamide
0.0083
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-fluorobenzenesulfonamide
0.0083
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidomethyl)benzenesulfonamide
0.0084
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-(2-phenylacetamido)-1,3,4-thiadiazole-2-sulfonamide
0.0086
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-chlorobenzenesulfonamide
0.0087
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-bromobenzenesulfonamide
0.009
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamido)benzenesulfonamide
0.0091
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidomethyl]benzenesulfonamide
0.0093
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamidoethyl)benzenesulfonamide
0.01
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens topiramate
0.0102
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidoethyl]benzenesulfonamide
0.012
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens acetazolamide
0.02
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens zonisamide
0.03
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens topiramate
0.035
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens zonisamide
0.05
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]benzenesulfonamide
0.05
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-chlorobenzenesulfonamide
0.051
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-[2-(2-thienyl)acetamido]-1,3,4-thiadiazole-2-sulfonamide
0.051
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-(2-phenylacetamido)-1,3,4-thiadiazole-2-sulfonamide
0.052
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-bromobenzenesulfonamide
0.052
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidomethyl]benzenesulfonamide
0.053
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidoethyl]benzenesulfonamide
0.054
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidomethyl)benzenesulfonamide
0.056
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens zonisamide
0.058
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-chlorobenzenesulfonamide
0.06
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidomethyl]benzenesulfonamide
0.06
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidoethyl)benzenesulfonamide
0.061
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]benzenesulfonamide
0.061
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-chlorobenzenesulfonamide
0.061
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-fluorobenzenesulfonamide
0.063
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-(2-phenylacetamido)-1,3,4-thiadiazole-2-sulfonamide
0.063
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens acetazolamide
0.063
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens topiramate
0.067
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-fluorobenzenesulfonamide
0.067
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidoethyl)benzenesulfonamide
0.068
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamidoethyl]benzenesulfonamide
0.069
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-2-ylacetamido)benzenesulfonamide
0.071
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamido)benzenesulfonamide
0.072
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 5-[2-(2-thienyl)acetamido]-1,3,4-thiadiazole-2-sulfonamide
0.073
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamidoethyl)benzenesulfonamide
0.074
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamido)benzenesulfonamide
0.075
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidomethyl)benzenesulfonamide
0.075
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-2-ylacetamido)benzenesulfonamide
0.077
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-chlorobenzenesulfonamide
0.084
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-bromobenzenesulfonamide
0.086
-
carbonic anhydrase VA, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamidomethyl)benzenesulfonamide
0.097
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-pyridin-4-ylacetamidoethyl)benzenesulfonamide
0.107
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)benzenesulfonamide
0.108
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)benzenesulfonamide
0.161
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-fluorobenzenesulfonamide
0.25
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens acetazolamide
0.25
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens topiramate
0.263
-
carbonic anhydrase I, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-bromobenzenesulfonamide
0.39
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-[2-(2-thienyl)acetamido]-3-fluorobenzenesulfonamide
0.395
-
carbonic anhydrase II, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens 4-(2-phenylacetamido)-3-bromobenzenesulfonamide
6.033
-
carbonic anhydrase VB, in 10 mM HEPES (pH 7.4), 0.1 M Na2SO4 or NaClO4, at 25°C Homo sapiens zonisamide