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Literature summary for 4.2.1.1 extracted from

  • Syrjaenen, L.; Vermelho, A.B.; Rodrigues, I.d.e..A.; Corte-Real, S.; Salonen, T.; Pan, P.; Vullo, D.; Parkkila, S.; Capasso, C.; Supuran, C.T.
    Cloning, characterization, and inhibition studies of a beta-carbonic anhydrase from Leishmania donovani chagasi, the protozoan parasite responsible for leishmaniasis (2013), J. Med. Chem., 56, 7372-7381.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
using the baculovirus expression system as a His-tagged fusion protein Leishmania chagasi

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(3-bromobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(3-methoxybenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(4-chlorobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(4-fluorobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(4-methylpentan-2-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(2Z)-2-benzylidene-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide
-
Leishmania chagasi
(4S,6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide
-
Leishmania chagasi
1,2-benzothiazol-3(2H)-one 1,1-dioxide
-
Leishmania chagasi
1-(1,2-benzoxazol-3-yl)methanesulfonamide
-
Leishmania chagasi
2-(hydroxymethyl)-4-nitro-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide
-
Leishmania chagasi
2-methoxy-N-[(1-methylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide
-
Leishmania chagasi
3,5-dichloro-2-hydroxybenzenesulfonamide
-
Leishmania chagasi
3-aminobenzenesulfonamide
-
Leishmania chagasi
4,5-dichlorobenzene-1,3-disulfonamide
-
Leishmania chagasi
4-(1,1-dioxido-1,2-thiazinan-2-yl)benzenesulfonamide
-
Leishmania chagasi
4-(2-aminoethyl)benzenesulfonamide
-
Leishmania chagasi
4-(2-hydroxyethyl)benzenesulfonamide
-
Leishmania chagasi
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide
-
Leishmania chagasi
4-(aminomethyl)benzenesulfonamide
-
Leishmania chagasi
4-(hydroxymethyl)benzenesulfonamide
-
Leishmania chagasi
4-amino-3-bromobenzenesulfonamide
-
Leishmania chagasi
4-amino-3-chlorobenzenesulfonamide
-
Leishmania chagasi
4-amino-3-fluorobenzenesulfonamide
-
Leishmania chagasi
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide
-
Leishmania chagasi
4-amino-6-chlorobenzene-1,3-disulfonamide
-
Leishmania chagasi
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide
-
Leishmania chagasi
4-amino-N-(4-sulfamoylphenyl)benzenesulfonamide
-
Leishmania chagasi
4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide
-
Leishmania chagasi
4-Aminobenzenesulfonamide
-
Leishmania chagasi
4-hydroxybenzenesulfonamide
-
Leishmania chagasi
4-sulfamoylbenzoic acid
-
Leishmania chagasi
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide
-
Leishmania chagasi
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
-
Leishmania chagasi
5-([(4-aminophenyl)sulfonyl]amino)-1,3,4-thiadiazole-2-sulfonamide
-
Leishmania chagasi
5-amino-1,3,4-thiadiazole-2-sulfonamide
-
Leishmania chagasi
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide
-
Leishmania chagasi
5-[(phenylsulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide
-
Leishmania chagasi
6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
-
Leishmania chagasi
6-ethoxy-1,3-benzothiazole-2-sulfonamide
-
Leishmania chagasi
acetazolamide
-
Leishmania chagasi
benzene-1,3-disulfonamide
-
Leishmania chagasi
benzenesulfonamide
-
Leishmania chagasi
N-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide
-
Leishmania chagasi
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
-
Leishmania chagasi
N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide
-
Leishmania chagasi
N-[(2E)-3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide
-
Leishmania chagasi
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate
-
Leishmania chagasi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0158
-
CO2 pH 7.5, 20°C Leishmania chagasi

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
35000
-
SDS-PAGE Leishmania chagasi

Organism

Organism UniProt Comment Textmining
Leishmania chagasi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CO2 + H2O
-
Leishmania chagasi H2CO3
-
?

Synonyms

Synonyms Comment Organism
beta-carbonic anhydrase
-
Leishmania chagasi
LdcCA
-
Leishmania chagasi

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
935000
-
CO2 pH 7.5, 20°C Leishmania chagasi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000134
-
(2Z)-2-(3-bromobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000184
-
(2Z)-2-(4-chlorobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000195
-
(2Z)-2-(4-methylpentan-2-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000279
-
(2Z)-2-benzylidene-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000331
-
(2Z)-2-(4-fluorobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000401
-
(2Z)-2-(3-methoxybenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000502
-
6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide pH 7.5, 20°C Leishmania chagasi
0.0000502
-
2-(hydroxymethyl)-4-nitro-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.0000515
-
6-ethoxy-1,3-benzothiazole-2-sulfonamide pH 7.5, 20°C Leishmania chagasi
0.0000596
-
4-sulfamoylbenzoic acid pH 7.5, 20°C Leishmania chagasi
0.0000734
-
4-amino-N-[2-(4-sulfamoylphenyl)ethyl]benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000074
-
N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.0000871
-
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.0000871
-
N-[(2E)-3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide pH 7.5, 20°C Leishmania chagasi
0.0000917
-
acetazolamide pH 7.5, 20°C Leishmania chagasi
0.0000917
-
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide pH 7.5, 20°C Leishmania chagasi
0.0000951
-
5-([(4-aminophenyl)sulfonyl]amino)-1,3,4-thiadiazole-2-sulfonamide pH 7.5, 20°C Leishmania chagasi
0.0000953
-
(2Z)-2-(4-chlorobenzylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.000136
-
4-amino-N-(4-sulfamoylphenyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000144
-
(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.000152
-
(2Z)-2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-N-(5-sulfanyl-1,3,4-thiadiazol-2-yl)hydrazinecarboxamide pH 7.5, 20°C Leishmania chagasi
0.000189
-
4,5-dichlorobenzene-1,3-disulfonamide pH 7.5, 20°C Leishmania chagasi
0.000227
-
4-(2-hydroxyethyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000236
-
5-[(phenylsulfonyl)amino]-1,3,4-thiadiazole-2-sulfonamide pH 7.5, 20°C Leishmania chagasi
0.000316
-
N-(3-chloro-1H-indol-7-yl)benzene-1,4-disulfonamide pH 7.5, 20°C Leishmania chagasi
0.000338
-
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000389
-
4-(hydroxymethyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000433
-
5-imino-4-methyl-4,5-dihydro-1,3,4-thiadiazole-2-sulfonamide pH 7.5, 20°C Leishmania chagasi
0.000584
-
5-amino-1,3,4-thiadiazole-2-sulfonamide pH 7.5, 20°C Leishmania chagasi
0.000705
-
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000764
-
(4R)-4-(ethylamino)-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-dioxide pH 7.5, 20°C Leishmania chagasi
0.000806
-
(4S,6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide pH 7.5, 20°C Leishmania chagasi
0.000834
-
4-(1,1-dioxido-1,2-thiazinan-2-yl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.000927
-
4-hydroxybenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.004819
-
4-amino-6-chlorobenzene-1,3-disulfonamide pH 7.5, 20°C Leishmania chagasi
0.00596
-
3-aminobenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.00842
-
4-amino-3-bromobenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.00891
-
benzene-1,3-disulfonamide pH 7.5, 20°C Leishmania chagasi
0.009058
-
4-amino-3-chlorobenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.009083
-
4-amino-6-(trifluoromethyl)benzene-1,3-disulfonamide pH 7.5, 20°C Leishmania chagasi
0.009135
-
3,5-dichloro-2-hydroxybenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.009251
-
4-Aminobenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.0156
-
4-amino-3-fluorobenzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
4-(aminomethyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
4-(2-aminoethyl)benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
4-[(2-aminopyrimidin-4-yl)amino]benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
benzenesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
1-(1,2-benzoxazol-3-yl)methanesulfonamide pH 7.5, 20°C Leishmania chagasi
0.1
-
1,2-benzothiazol-3(2H)-one 1,1-dioxide pH 7.5, 20°C Leishmania chagasi
0.1
-
[(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate pH 7.5, 20°C Leishmania chagasi
0.1
-
2-methoxy-N-[(1-methylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide pH 7.5, 20°C Leishmania chagasi

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
59000
-
CO2 pH 7.5, 20°C Leishmania chagasi