Target Validation Information
TTD ID T16987
Target Name Carbonic anhydrase XII (CA-XII)
Type of Target
Successful
Drug Potency against Target 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide Drug Info Ki = 28.9 nM [17]
1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide Drug Info Ki = 45.2 nM [17]
2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide Drug Info Ki = 31 nM [4]
2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide Drug Info Ki = 249 nM [4]
2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 0.39 nM [7]
2,4-Disulfamyltrifluoromethylaniline Drug Info Ki = 45 nM [1]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Drug Info Ki = 4.7 nM [7]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 1.4 nM [7]
2-Amino-benzenesulfonamide Drug Info Ki = 0.85 nM [1]
2-Amino-indan-5-sulfonic acid Drug Info Ki = 4.8 nM [7]
2-hydrazinylbenzenesulfonamide Drug Info Ki = 58 nM [1]
2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 2900 nM [12]
2-oxo-2H-thiochromene-3-carboxylic acid Drug Info Ki = 10500 nM [12]
3-((4-aminophenyl)diazenyl)benzenesulfonamide Drug Info Ki = 7.3 nM [11]
3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info Ki = 7.3 nM [11]
3-(3-Phenyl-ureido)-benzenesulfonamide Drug Info Ki = 10 nM [4]
3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide Drug Info Ki = 7.3 nM [11]
3-Amino-benzenesulfonamide Drug Info Ki = 125 nM [3]
4,4'-thiodipyridine-3-sulfonamide Drug Info Ki = 4.7 nM [15]
4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide Drug Info Ki = 5 nM [11]
4-(2-AMINOETHYL)BENZENESULFONAMIDE Drug Info Ki = 3.2 nM [1]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info Ki = 55 nM [1]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 6.7 nM [15]
4-(2-Propynylthio)pyridine-3-sulfonamide Drug Info Ki = 15.6 nM [15]
4-(4'-N-Methylphenyl)diazenylbenzenesulfonamide Drug Info Ki = 69.4 nM [11]
4-(4-Cyanophenoxy)-3-pyridinesulfonamide Drug Info Ki = 6.3 nM [15]
4-(4-Fluorophenoxy)-3-pyridinesulfonamide Drug Info Ki = 6.9 nM [15]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Drug Info Ki = 15.7 nM [15]
4-(Allylamino)-3-pyridinesulfonamide Drug Info Ki = 16.9 nM [15]
4-(Carbamolymethylthio)pyridine-3-sulfonamide Drug Info Ki = 15.9 nM [15]
4-(Cyanomethylthio)pyridine-3-sulfonamide Drug Info Ki = 15.5 nM [15]
4-(hydroxymethyl)benzenesulfonamide Drug Info Ki = 220 nM [1]
4-(Methylhydrazino)-3-pyridinesulfonamide Drug Info Ki = 8.9 nM [15]
4-(N-Methyl-hydrazino)-benzenesulfonamide Drug Info Ki = 11 nM [1]
4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide Drug Info Ki = 13.8 nM [15]
4-(Quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 6.8 nM [15]
4-Amino-3-bromo-benzenesulfonamide Drug Info Ki = 20 nM [1]
4-Amino-3-chloro-benzenesulfonamide Drug Info Ki = 3.1 nM [1]
4-Amino-3-fluoro-benzenesulfonamide Drug Info Ki = 1.1 nM [1]
4-Amino-3-iodo-benzenesulfonamide Drug Info Ki = 11 nM [1]
4-Benzenesulfonylamino-benzenesulfonamide Drug Info Ki = 68 nM [4]
4-Benzythiopyridine-3-sulfonamide Drug Info Ki = 6.5 nM [15]
4-CYANOPHENOL Drug Info Ki = 9200 nM [8]
4-Ethoxy-3-pyridinesulfonamide Drug Info Ki = 5.9 nM [15]
4-Hydrazino-3-pyridinesulfonamide Drug Info Ki = 10.1 nM [15]
4-Hydrazino-benzenesulfonamide Drug Info Ki = 11 nM [3]
4-Methanesulfonylamino-benzenesulfonamide Drug Info Ki = 33 nM [4]
4-Methoxy-3-pyridinesulfonamide Drug Info Ki = 5.8 nM [15]
4-Methylamino-benzenesulfonamide Drug Info Ki = 37 nM [1]
4-Methylthiopyridine-3-sulfonamide Drug Info Ki = 6.7 nM [15]
4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide Drug Info Ki = 13 nM [4]
6-(aminomethyl)-2H-chromen-2-one Drug Info Ki = 1500 nM [12]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info Ki = 9500 nM [12]
6-Hydroxy-benzothiazole-2-sulfonic acid amide Drug Info Ki = 3.7 nM [1]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 6800 nM [12]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 8000 nM [12]
7-(benzyloxy)-2H-chromen-2-one Drug Info Ki = 6500 nM [12]
7-butoxy-2H-chromen-2-one Drug Info Ki = 8600 nM [12]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Drug Info Ki = 7100 nM [12]
7-phenethoxy-2H-chromen-2-one Drug Info Ki = 7500 nM [12]
7-propoxy-2H-chromen-2-one Drug Info Ki = 7600 nM [12]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 5600 nM [12]
ACETYLSULFANILAMIDE Drug Info Ki = 49 nM [4]
BENZOLAMIDE Drug Info Ki = 3.8 nM [1]
Carzenide Drug Info Ki = 34 nM [1]
CATECHIN Drug Info Ki = 4720 nM [20]
CATECHOL Drug Info Ki = 8900 nM [13]
CL-5343 Drug Info Ki = 34 nM [19]
COUMARIN Drug Info Ki = 8900 nM [12]
Coumate Drug Info Ki = 12 nM [9]
Curcumin Drug Info Ki = 3480 nM [20]
Decane-1,10-diyl disulfamate Drug Info Ki = 8.2 nM [10]
Decyl sulfamate Drug Info Ki = 7.9 nM [10]
ELLAGIC ACID Drug Info Ki = 10100 nM [13]
ETHOXYCOUMARIN Drug Info Ki = 8200 nM [12]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info Ki = 8800 nM [12]
FERULIC ACID Drug Info Ki = 9780 nM [13]
GALLICACID Drug Info Ki = 7780 nM [13]
HERNIARIN Drug Info Ki = 9700 nM [12]
Hexane-1,6-diamine Drug Info Ki = 370 nM [18]
INDISULAM Drug Info Ki = 3.4 nM [17]
N-(4-cyanophenyl)sulfamide Drug Info Ki = 45 nM [2]
N-(4-Sulfamoyl-phenyl)-benzamide Drug Info Ki = 21 nM [4]
N-(4-Sulfamoyl-phenyl)-butyramide Drug Info Ki = 85 nM [4]
N-(4-Sulfamoyl-phenyl)-isobutyramide Drug Info Ki = 138 nM [4]
N-(4-Sulfamoyl-phenyl)-propionamide Drug Info Ki = 56 nM [4]
N-(pentafluorophenyl)sulfamide Drug Info Ki = 19 nM [2]
N-hydroxysulfamide Drug Info Ki = 1340 nM [16]
N-propynyl amidebenzenesulphonide Drug Info Ki = 1 nM [5]
N1-(2-aminoethyl)ethane-1,2-diamine Drug Info Ki = 11400 nM [18]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info Ki = 380 nM [18]
Octane-1,8-diyl disulfamate Drug Info Ki = 7.9 nM [10]
Octyl sulfamate Drug Info Ki = 7 nM [10]
P-Coumaric Acid Drug Info Ki = 8010 nM [13]
P-toluenesulfonamide Drug Info Ki = 1.8 nM [1]
PARABEN Drug Info Ki = 6270 nM [13]
Pentane-1,5-diamine Drug Info Ki = 450 nM [18]
Pentanoic acid (4-sulfamoyl-phenyl)-amide Drug Info Ki = 147 nM [4]
PHENOL Drug Info Ki = 9200 nM [20]
Prop-2-ynyl 4-sulfamoylbenzoate Drug Info Ki = 8.3 nM [5]
RESORCINOL Drug Info Ki = 7500 nM [8]
SACCHARIN Drug Info Ki = 633 nM [6]
Salicyclic acid Drug Info Ki = 8800 nM [8]
Sodium N-methylphenylaminomethanesulfonate Drug Info Ki = 5925 nM [11]
Sodium phenylaminomethanesulfonate Drug Info Ki = 6250 nM [11]
Sulfamylon Drug Info Ki = 0.3 nM [14]
Syringic Acid Drug Info Ki = 9010 nM [13]
References
REF 1 Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglauc... Bioorg Med Chem Lett. 2005 Feb 15;15(4):963-9.
REF 2 Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxy... Bioorg Med Chem Lett. 2005 May 2;15(9):2353-8.
REF 3 Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.
REF 4 Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4862-6.
REF 5 Inhibition of membrane-associated carbonic anhydrase isozymes IX, XII and XIV with a library of glycoconjugate benzenesulfonamides. Bioorg Med Chem Lett. 2007 Feb 15;17(4):987-92.
REF 6 Carbonic anhydrase inhibitors: copper(II) complexes of polyamino-polycarboxylamido aromatic/heterocyclic sulfonamides are very potent inhibitors of... Bioorg Med Chem Lett. 2008 Jan 15;18(2):836-41.
REF 7 Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. Eur J Med Chem. 2008 Dec;43(12):2853-60.
REF 8 Carbonic anhydrase inhibitors: inhibition of mammalian isoforms I-XIV with a series of substituted phenols including paracetamol and salicylic acid. Bioorg Med Chem. 2008 Aug 1;16(15):7424-8.
REF 9 Carbonic anhydrase inhibitors. Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-r... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4282-6.
REF 10 Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-bi... J Med Chem. 2009 Oct 8;52(19):5990-8.
REF 11 Carbonic anhydrase inhibitors. Diazenylbenzenesulfonamides are potent and selective inhibitors of the tumor-associated isozymes IX and XII over the... Bioorg Med Chem. 2009 Oct 15;17(20):7093-9.
REF 12 Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44.
REF 13 Carbonic anhydrase inhibitors. Inhibition of mammalian isoforms I-XIV with a series of natural product polyphenols and phenolic acids. Bioorg Med Chem. 2010 Mar 15;18(6):2159-2164.
REF 14 Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. J Med Chem. 2010 Apr 8;53(7):2913-26.
REF 15 Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associa... Eur J Med Chem. 2010 Jun;45(6):2396-404.
REF 16 Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mamm... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5.
REF 17 Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the... Eur J Med Chem. 2010 Sep;45(9):3656-61.
REF 18 Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
REF 19 Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a l... Bioorg Med Chem Lett. 2010 Aug 1;20(15):4376-81.
REF 20 Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3.

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