Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 4.2.1.1 extracted from

  • Temperini, C.; Cecchi, A.; Scozzafava, A.; Supuran, C.T.
    Carbonic anhydrase inhibitors. Comparison of chlorthalidone and indapamide X-ray crystal structures in adducts with isozyme II: when three water molecules and the keto-enol tautomerism make the difference (2009), J. Med. Chem., 52, 322-328.
    View publication on PubMed
Search for more literature for 4.2.1.1

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with the inhibitor chlorthalidone Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide efficient inhibitor of only isozymes CA I and II Homo sapiens
acetazolamide promiscuous inhibitor of all isozymes except CA III Homo sapiens
Chlorthalidone chlorthalidone is a medium potency CA I, II, and IV inhibitor, a very effective inhibitor of CA VB, CA VII, CA IX, CA XII, and CA XIII and an ineffective inhibitor of isozymes CA III, VA, VI, and XIV Homo sapiens
ethoxzolamide promiscuous inhibitor of all isozymes except CA III Homo sapiens
indapamide indapamide is a quite ineffective inhibitor of isozymes CA I, II, III, VA, VI, and XIV, a medium potency CA IV and CA VB inhibitor, and a very effective inhibitor of isozymes CA VII, IX, XII, and XIII Homo sapiens
methazolamide promiscuous inhibitor of all isozymes except CA III Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00918
-
-

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 isozyme Homo sapiens
CA II isozyme Homo sapiens
CA III isozyme Homo sapiens
CA IV isozyme Homo sapiens
CA IX isozyme Homo sapiens
CA VA isozyme Homo sapiens
CA VB isozyme Homo sapiens
CA VI isozyme Homo sapiens
CA VII isozyme Homo sapiens
CA XII isozyme Homo sapiens
CA XIV isozyme Homo sapiens
carbonic anhydrase
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000023
-
 indapamide isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000008
-
 ethoxzolamide isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000021
-
 methazolamide isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000025
-
 acetazolamide isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000028
-
 Chlorthalidone isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000034
-
 methazolamide isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000045
-
 Chlorthalidone isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000057
-
 acetazolamide isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000072
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0000075
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000008
-
 ethoxzolamide isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000009
-
 Chlorthalidone isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00001
-
 methazolamide isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00001
-
 indapamide isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000011
-
 acetazolamide isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000012
-
 acetazolamide isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000014
-
 methazolamide isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000019
-
 ethoxzolamide isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000022
-
 ethoxzolamide isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000023
-
 Chlorthalidone isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000025
-
 ethoxzolamide isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000025
-
 acetazolamide isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000025
-
 ethoxzolamide isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000025
-
 ethoxzolamide isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000027
-
 methazolamide isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000034
-
 ethoxzolamide isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000036
-
 indapamide isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000041
-
 acetazolamide isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000043
-
 ethoxzolamide isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000043
-
 methazolamide isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000048
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00005
-
 methazolamide isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000054
-
 acetazolamide isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000062
-
 methazolamide isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000063
-
 acetazolamide isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000065
-
 methazolamide isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000074
-
 acetazolamide isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000089
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA VII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000093
-
 ethoxzolamide isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000102
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA IX, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00011
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA XII, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000138
-
 indapamide isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000138
-
 Chlorthalidone isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000213
-
 indapamide isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00025
-
 acetazolamide isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000274
-
 indapamide isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000348
-
 Chlorthalidone isozyme CA I, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00089
-
 indapamide isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.000917
-
 Chlorthalidone isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0011
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA VA, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0011
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA VB, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.001357
-
 Chlorthalidone isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.001606
-
 indapamide isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00252
-
 indapamide isozyme CA II, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00265
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA VI, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00413
-
 Chlorthalidone isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.00495
-
 indapamide isozyme CA XIV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.0062
-
 methazolamide isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.009
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.011
-
 ethoxzolamide isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.196
-
 Chlorthalidone isozyme CA IV, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.2
-
 acetazolamide isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.23
-
 indapamide isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
0.7
-
 methazolamide isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
1.11
-
 Chlorthalidone isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens
1.4
-
 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide isozyme CA III, in 10 mM HEPES (pH 7.5) and 0.1 M Na2SO4 Homo sapiens