Therapeutic Targets Database
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Target Validation Information
TTD IDTTDR00209
Target NameCarbonic anhydrase IV    
Type of TargetResearch target    
Drug Potency against TargetSPERMINEKi = 10 nM[1]
[Fe(CN)6]4-Ki = 10000 nM[2]
Syringic AcidKi = 10600 nM[3]
FERULIC ACIDKi = 10800 nM[3]
CATECHOLKi = 10900 nM[3]
SALICYLATEKi = 11100 nM[4]
BENZOLAMIDEKi = 12 nM[5]
PYRUVATE SODIUMKi = 14500 nM[6]
6-(aminomethyl)-2H-chromen-2-oneKi = 15000 nM[7]
N-(5-Sulfamoyl-[1,3,4]thiadiazol-2-yl)-benzamideKi = 21 nM[8]
2-Propyl-pentanoic acid 4-sulfamoyl-benzylamideKi = 210 nM[8]
COUMATEKi = 24 nM[9]
Sodium; MalonateKi = 2800 nM[6]
2-Propyl-pentanoic acid 4-sulfamoyl-benzyl esterKi = 333 nM[8]
4-(2-Amino-ethyl)-benzenesulfonamideKi = 3570 nM[10]
4-Amino-3-chloro-benzenesulfonamideKi = 450 nM[10]
hexane-1,6-diamineKi = 450 nM[1]
2,4-DisulfamyltrifluoromethylanilineKi = 4830 nM[10]
CATECHINKi = 4900 nM[11]
CURCUMINKi = 4970 nM[11]
pentane-1,5-diamineKi = 52 nM[1]
Phenyl-phosphonic acidKi = 5400 nM[12]
N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamideKi = 5540 nM[13]
N1-(naphthalen-1-yl)ethane-1,2-diamineKi = 58 nM[1]
7-(benzyloxy)-2H-chromen-2-oneKi = 5800 nM[7]
Ditiocarb sodiumKi = 6500 nM[14]
decyl sulfamateKi = 67.6 nM[15]
COUMARINKi = 6800 nM[7]
ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylateKi = 7200 nM[7]
N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamideKi = 7580 nM[13]
4-Hydrazino-benzenesulfonamideKi = 7700 nM[10]
6-(hydroxymethyl)-2H-chromen-2-oneKi = 7700 nM[7]
3-Amino-benzenesulfonamideKi = 7750 nM[10]
PARABENKi = 7780 nM[3]
SPARFOSIC ACIDKi = 79 nM[12]
octyl sulfamateKi = 79.9 nM[15]
HERNIARINKi = 8300 nM[7]
N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamideKi = 8300 nM[13]
trisodium phosphateKi = 84 nM[16]
octane-1,8-diyl disulfamateKi = 84.1 nM[15]
N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamideKi = 8400 nM[13]
6-methyl-2-oxo-2H-chromene-3-carboxylic acidKi = 8500 nM[7]
MAFENIDEKi = 8600 nM[10]
N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamideKi = 8640 nM[13]
sodium phenylarsonateKi = 870 nM[17]
Phenylarsonic acidKi = 870 nM[18]
SULFAMIDEKi = 880 nM[19]
phenylboronic acidKi = 880 nM[17]
1-(3,4-dichlorophenyl)-3-hydroxyureaKi = 890 nM[20]
N-1,3,4-thiadiazol-2-ylsulfamideKi = 8910 nM[13]
ELLAGIC ACIDKi = 9080 nM[3]
decane-1,10-diyl disulfamateKi = 91.2 nM[15]
4-Amino-3-fluoro-benzenesulfonamideKi = 910 nM[10]
4-Amino-3-iodo-benzenesulfonamideKi = 920 nM[10]
SULFAMATEKi = 930 nM[18]
sodium sulfamateKi = 930 nM[17]
5-amino-1,3,4-thiadiazole-2-sulfonamideKi = 940 nM[21]
PHENOLKi = 9500 nM[11]
4-Amino-3-bromo-benzenesulfonamideKi = 96 nM[10]
p-Coumaric AcidKi = 9600 nM[3]
2-oxo-2H-chromene-3-carboxylic acidKi = 9700 nM[7]
GALLICACIDKi = 9800 nM[3]
SODIUM PHOSPHATE, DIBASIC, ANHYDROUSKi = 9800 nM[16]
[Cu(CN)2]-Ki = 9800 nM[2]
SODIUM CITRATEKi = 99 nM[6]
Sodium; OxalateKi = 99 nM[6]
Carbamoyl phosphate; di sodiumKi = 9900 nM[16]
aminocarbonyl dihydrogen phosphateKi = 9900 nM[12]
sodium trithiocarbonateKi = 9900 nM[14]
Ref 1J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. To Reference
Ref 2Bioorg Med Chem Lett. 2005 Apr 1;15(7):1909-13.Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides. To Reference
Ref 3Bioorg Med Chem. 2010 Mar 15;18(6):2159-64. Epub 2010 Feb 6.Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. To Reference
Ref 4Bioorg Med Chem. 2008 Aug 1;16(15):7424-8. Epub 2008 Jun 13.Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. To Reference
Ref 5Bioorg Med Chem Lett. 2003 Sep 1;13(17):2867-73.Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide. To Reference
Ref 6Bioorg Med Chem Lett. 2005 Feb 1;15(3):573-8.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. To Reference
Ref 7J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. To Reference
Ref 8J Med Chem. 2002 Jan 17;45(2):312-20.Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. To Reference
Ref 9Bioorg Med Chem Lett. 2008 Aug 1;18(15):4282-6. Epub 2008 Jul 5.Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. To Reference
Ref 10Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. To Reference
Ref 11Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. Epub 2010 Jul 13.Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. To Reference
Ref 12Bioorg Med Chem Lett. 2005 Mar 15;15(6):1683-6.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates. To Reference
Ref 13Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV. To Reference
Ref 14Bioorg Med Chem Lett. 2009 Apr 1;19(7):1855-7. Epub 2009 Feb 26.Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I, II, III, VII and XIII with less investigated inorganic anions. To Reference
Ref 15J Med Chem. 2009 Oct 8;52(19):5990-8.Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors. To Reference
Ref 16Bioorg Med Chem Lett. 2004 Dec 6;14(23):5763-7.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet. To Reference
Ref 17Bioorg Med Chem Lett. 2009 Feb 15;19(4):1155-8. Epub 2008 Dec 25.Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions. To Reference
Ref 18Bioorg Med Chem Lett. 2004 Dec 6;14(23):5769-73.Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. To Reference
Ref 19Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5. Epub 2010 Apr 28.Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV. To Reference
Ref 20Bioorg Med Chem Lett. 2006 Aug 15;16(16):4316-20. Epub 2006 Jun 12.N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors. To Reference
Ref 21Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81. Epub 2010 Jun 17.Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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