Target Validation Information
Target ID T16987
Target Name Carbonic anhydrase XII
Target Type
Successful
Drug Potency against Target PARABEN Drug Info Ki = 6270 nM [1]
MAFENIDE Drug Info Ki = 0.3 nM [2]
SALICYLATE Drug Info Ki = 8800 nM [3]
4-CYANOPHENOL Drug Info Ki = 9200 nM [3]
2-oxo-2H-thiochromene-3-carboxylic acid Drug Info Ki = 10500 nM [4]
4-(Cyanomethylthio)pyridine-3-sulfonamide Drug Info Ki = 15.5 nM [5]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info Ki = 8800 nM [4]
4-(Methylhydrazino)-3-pyridinesulfonamide Drug Info Ki = 8.9 nM [5]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Drug Info Ki = 15.7 nM [5]
7-(benzyloxy)-2H-chromen-2-one Drug Info Ki = 6500 nM [4]
3-Amino-benzenesulfonamide Drug Info Ki = 125 nM [6]
4-Hydrazino-benzenesulfonamide Drug Info Ki = 11 nM [6]
7-butoxy-2H-chromen-2-one Drug Info Ki = 8600 nM [4]
7-propoxy-2H-chromen-2-one Drug Info Ki = 7600 nM [4]
4-(4-Fluorophenoxy)-3-pyridinesulfonamide Drug Info Ki = 6.9 nM [5]
6-(aminomethyl)-2H-chromen-2-one Drug Info Ki = 1500 nM [4]
N-propynyl amidebenzenesulphonide Drug Info Ki = 1 nM [7]
4,4'-thiodipyridine-3-sulfonamide Drug Info Ki = 4.7 nM [5]
Syringic Acid Drug Info Ki = 9010 nM [1]
RESORCINOL Drug Info Ki = 7500 nM [3]
2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Drug Info Ki = 249 nM [8]
N-(pentafluorophenyl)sulfamide Drug Info Ki = 19 nM [9]
CATECHIN Drug Info Ki = 4720 nM [10]
INDISULAM Drug Info Ki = 3.4 nM [11]
Octane-1,8-diyl disulfamate Drug Info Ki = 7.9 nM [12]
4-(hydroxymethyl)benzenesulfonamide Drug Info Ki = 220 nM [13]
4-(2-Propynylthio)pyridine-3-sulfonamide Drug Info Ki = 15.6 nM [5]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Drug Info Ki = 7100 nM [4]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info Ki = 380 nM [14]
PHENOL Drug Info Ki = 9200 nM [10]
Octyl sulfamate Drug Info Ki = 7 nM [12]
Pentanoic acid (4-sulfamoyl-phenyl)-amide Drug Info Ki = 147 nM [8]
4-Benzenesulfonylamino-benzenesulfonamide Drug Info Ki = 68 nM [8]
4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Drug Info Ki = 13 nM [8]
4-Methylamino-benzenesulfonamide Drug Info Ki = 37 nM [13]
2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Drug Info Ki = 31 nM [8]
N-(4-Sulfamoyl-phenyl)-benzamide Drug Info Ki = 21 nM [8]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 8000 nM [4]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 6.7 nM [5]
4-Methanesulfonylamino-benzenesulfonamide Drug Info Ki = 33 nM [8]
N-(4-Sulfamoyl-phenyl)-propionamide Drug Info Ki = 56 nM [8]
N-(4-Sulfamoyl-phenyl)-isobutyramide Drug Info Ki = 138 nM [8]
4-Amino-3-iodo-benzenesulfonamide Drug Info Ki = 11 nM [13]
BENZOLAMIDE Drug Info Ki = 3.8 nM [13]
3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info Ki = 7.3 nM [15]
Prop-2-ynyl 4-sulfamoylbenzoate Drug Info Ki = 8.3 nM [7]
N-hydroxysulfamide Drug Info Ki = 1340 nM [16]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 1.4 nM [17]
SACCHARIN Drug Info Ki = 633 nM [18]
Decyl sulfamate Drug Info Ki = 7.9 nM [12]
CATECHOL Drug Info Ki = 8900 nM [1]
N1-(2-aminoethyl)ethane-1,2-diamine Drug Info Ki = 11400 nM [14]
Pentane-1,5-diamine Drug Info Ki = 450 nM [14]
Sodium N-methylphenylaminomethanesulfonate Drug Info Ki = 5925 nM [15]
FERULIC ACID Drug Info Ki = 9780 nM [1]
Curcumin Drug Info Ki = 3480 nM [10]
5-amino-1,3,4-thiadiazole-2-sulfonamide Drug Info Ki = 34 nM [19]
COUMATE Drug Info Ki = 12 nM [20]
GALLICACID Drug Info Ki = 7780 nM [1]
ELLAGIC ACID Drug Info Ki = 10100 nM [1]
7-phenethoxy-2H-chromen-2-one Drug Info Ki = 7500 nM [4]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 5600 nM [4]
2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 0.39 nM [17]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Drug Info Ki = 4.7 nM [17]
Decane-1,10-diyl disulfamate Drug Info Ki = 8.2 nM [12]
N-(4-cyanophenyl)sulfamide Drug Info Ki = 45 nM [9]
4-(Allylamino)-3-pyridinesulfonamide Drug Info Ki = 16.9 nM [5]
4-(Quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 6.8 nM [5]
COUMARIN Drug Info Ki = 8900 nM [4]
HERNIARIN Drug Info Ki = 9700 nM [4]
3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Drug Info Ki = 7.3 nM [15]
4-Ethoxy-3-pyridinesulfonamide Drug Info Ki = 5.9 nM [5]
1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Drug Info Ki = 28.9 nM [11]
4-(Carbamolymethylthio)pyridine-3-sulfonamide Drug Info Ki = 15.9 nM [5]
1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Drug Info Ki = 45.2 nM [11]
ETHOXYCOUMARIN Drug Info Ki = 8200 nM [4]
P-Coumaric Acid Drug Info Ki = 8010 nM [1]
Carzenide Drug Info Ki = 34 nM [13]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info Ki = 9500 nM [4]
Hexane-1,6-diamine Drug Info Ki = 370 nM [14]
2-hydrazinylbenzenesulfonamide Drug Info Ki = 58 nM [13]
6-Hydroxy-benzothiazole-2-sulfonic acid amide Drug Info Ki = 3.7 nM [13]
4-(N-Methyl-hydrazino)-benzenesulfonamide Drug Info Ki = 11 nM [13]
4-Methylthiopyridine-3-sulfonamide Drug Info Ki = 6.7 nM [5]
4-Amino-3-bromo-benzenesulfonamide Drug Info Ki = 20 nM [13]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 6800 nM [4]
4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Drug Info Ki = 13.8 nM [5]
P-TOLUENESULFONAMIDE Drug Info Ki = 1.8 nM [13]
4-Methoxy-3-pyridinesulfonamide Drug Info Ki = 5.8 nM [5]
2,4-Disulfamyltrifluoromethylaniline Drug Info Ki = 45 nM [13]
2-Amino-benzenesulfonamide Drug Info Ki = 0.85 nM [13]
4-Amino-3-chloro-benzenesulfonamide Drug Info Ki = 3.1 nM [13]
3-(3-Phenyl-ureido)-benzenesulfonamide Drug Info Ki = 10 nM [8]
4-Hydrazino-3-pyridinesulfonamide Drug Info Ki = 10.1 nM [5]
4-Amino-3-fluoro-benzenesulfonamide Drug Info Ki = 1.1 nM [13]
4-(4'-N-Methylphenyl)diazenylbenzenesulfonamide Drug Info Ki = 69.4 nM [15]
4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info Ki = 5 nM [15]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info Ki = 55 nM [13]
4-(4-Cyanophenoxy)-3-pyridinesulfonamide Drug Info Ki = 6.3 nM [5]
Sodium phenylaminomethanesulfonate Drug Info Ki = 6250 nM [15]
2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 2900 nM [4]
3-((4-aminophenyl)diazenyl)benzenesulfonamide Drug Info Ki = 7.3 nM [15]
4-Benzythiopyridine-3-sulfonamide Drug Info Ki = 6.5 nM [5]
ACETYLSULFANILAMIDE Drug Info Ki = 49 nM [8]
N-(4-Sulfamoyl-phenyl)-butyramide Drug Info Ki = 85 nM [8]
2-Amino-indan-5-sulfonic acid Drug Info Ki = 4.8 nM [17]
4-(2-Amino-ethyl)-benzenesulfonamide Drug Info Ki = 3.2 nM [13]
References
REF 1Bioorg 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.
REF 2J Med Chem. 2010 Apr 8;53(7):2913-26.Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.
REF 3Bioorg 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.
REF 4J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
REF 5Eur J Med Chem. 2010 Jun;45(6):2396-404. Epub 2010 Feb 12.Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associated) and XIV with 4-substituted 3-pyridinesulfonamides.
REF 6Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides.
REF 7Bioorg Med Chem Lett. 2007 Feb 15;17(4):987-92. Epub 2006 Nov 17.Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides.
REF 8Bioorg Med Chem Lett. 2005 Nov 1;15(21):4862-6.Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides.
REF 9Bioorg Med Chem Lett. 2005 May 2;15(9):2353-8.Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxysulfamides--a new zinc-binding function in the design of inhibitors.
REF 10Bioorg 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.
REF 11Eur J Med Chem. 2010 Sep;45(9):3656-61. Epub 2010 May 12.Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII.
REF 12J 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.
REF 13Bioorg Med Chem Lett. 2005 Feb 15;15(4):963-9.Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?.
REF 14J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
REF 15Bioorg Med Chem. 2009 Oct 15;17(20):7093-9. Epub 2009 Sep 6.Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XIIover the cytosolic isoforms I and II.
REF 16Bioorg 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.
REF 17Eur J Med Chem. 2008 Dec;43(12):2853-60. Epub 2008 Feb 29.Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation.
REF 18Bioorg Med Chem Lett. 2008 Jan 15;18(2):836-41. Epub 2007 Nov 13.Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potentinhibitors of the tumor-associated isoforms IX and XII.
REF 19Bioorg 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 acetazolamideresides in a less utilized binding pocket than most hydrophobic inhibitors.
REF 20Bioorg 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.

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