Target Validation Information
TTD ID T31992
Target Name Carbonic anhydrase XIV (CA-XIV)
Type of Target
Successful
Drug Potency against Target 2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 6.5 nM [3]
2,4-Disulfamyltrifluoromethylaniline Drug Info Ki = 680 nM [1]
2-acetamido-2,3-dihydro-1H-indene-5-sulfonic acid Drug Info Ki = 68 nM [3]
2-amino-2,3-dihydro-1H-indene-5-sulfonamide Drug Info Ki = 5.8 nM [3]
2-Amino-benzenesulfonamide Drug Info Ki = 6500 nM [1]
2-Amino-indan-5-sulfonic acid Drug Info Ki = 82 nM [3]
2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 8200 nM [7]
2-oxo-2H-thiochromene-3-carboxylic acid Drug Info Ki = 7800 nM [7]
3-Amino-benzenesulfonamide Drug Info Ki = 4800 nM [1]
4,4'-thiodipyridine-3-sulfonamide Drug Info Ki = 160 nM [9]
4-(2-AMINOETHYL)BENZENESULFONAMIDE Drug Info Ki = 2900 nM [1]
4-(2-Hydroxy-ethyl)-benzenesulfonamide Drug Info Ki = 3255 nM [1]
4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 70 nM [9]
4-(2-Propynylthio)pyridine-3-sulfonamide Drug Info Ki = 56.4 nM [9]
4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide Drug Info Ki = 152 nM [9]
4-(Allylamino)-3-pyridinesulfonamide Drug Info Ki = 143 nM [9]
4-(Carbamolymethylthio)pyridine-3-sulfonamide Drug Info Ki = 142 nM [9]
4-(Cyanomethylthio)pyridine-3-sulfonamide Drug Info Ki = 140 nM [9]
4-(hydroxymethyl)benzenesulfonamide Drug Info Ki = 3840 nM [1]
4-(Methylhydrazino)-3-pyridinesulfonamide Drug Info Ki = 95.7 nM [9]
4-(Quinolinoxy)-3-pyridinesulfonamide Drug Info Ki = 59.7 nM [9]
4-Amino-3-bromo-benzenesulfonamide Drug Info Ki = 15 nM [1]
4-Amino-3-chloro-benzenesulfonamide Drug Info Ki = 21 nM [1]
4-Amino-3-fluoro-benzenesulfonamide Drug Info Ki = 180 nM [1]
4-Amino-3-iodo-benzenesulfonamide Drug Info Ki = 79 nM [1]
4-AMINOPHENOL Drug Info Ki = 10100 nM [4]
4-Benzythiopyridine-3-sulfonamide Drug Info Ki = 68.2 nM [9]
4-Ethoxy-3-pyridinesulfonamide Drug Info Ki = 52.2 nM [9]
4-Hydrazino-3-pyridinesulfonamide Drug Info Ki = 93.4 nM [9]
4-Hydrazino-benzenesulfonamide Drug Info Ki = 1450 nM [1]
4-Methylthiopyridine-3-sulfonamide Drug Info Ki = 98.3 nM [9]
6-(aminomethyl)-2H-chromen-2-one Drug Info Ki = 46 nM [7]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info Ki = 6200 nM [7]
6-Hydroxy-benzothiazole-2-sulfonic acid amide Drug Info Ki = 48 nM [1]
6-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 3200 nM [7]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 8600 nM [7]
7-(benzyloxy)-2H-chromen-2-one Drug Info Ki = 5600 nM [7]
7-butoxy-2H-chromen-2-one Drug Info Ki = 8700 nM [7]
7-methoxy-2-oxo-2H-chromene-4-carboxylic acid Drug Info Ki = 8800 nM [7]
7-phenethoxy-2H-chromen-2-one Drug Info Ki = 8400 nM [7]
7-propoxy-2H-chromen-2-one Drug Info Ki = 8600 nM [7]
8-methoxy-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 48 nM [7]
BENZOLAMIDE Drug Info Ki = 33 nM [1]
Carzenide Drug Info Ki = 780 nM [1]
CATECHIN Drug Info Ki = 11550 nM [12]
CL-5343 Drug Info Ki = 280 nM [11]
COUMARIN Drug Info Ki = 48 nM [7]
Coumate Drug Info Ki = 755 nM [5]
Curcumin Drug Info Ki = 11730 nM [12]
Decane-1,10-diyl disulfamate Drug Info Ki = 852 nM [6]
Decyl sulfamate Drug Info Ki = 711 nM [6]
ELLAGIC ACID Drug Info Ki = 8910 nM [8]
ETHOXYCOUMARIN Drug Info Ki = 8900 nM [7]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info Ki = 6100 nM [7]
FERULIC ACID Drug Info Ki = 9430 nM [8]
GALLICACID Drug Info Ki = 7030 nM [8]
HERNIARIN Drug Info Ki = 9000 nM [7]
Hexane-1,6-diamine Drug Info Ki = 640 nM [10]
INDISULAM Drug Info Ki = 104 nM [9]
N-propynyl amidebenzenesulphonide Drug Info Ki = 11.3 nM [2]
N1-(2-aminoethyl)ethane-1,2-diamine Drug Info Ki = 10100 nM [10]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info Ki = 590 nM [10]
Octane-1,8-diyl disulfamate Drug Info Ki = 605 nM [6]
Octyl sulfamate Drug Info Ki = 390 nM [6]
P-Coumaric Acid Drug Info Ki = 6680 nM [8]
PARABEN Drug Info Ki = 6160 nM [8]
Pentane-1,5-diamine Drug Info Ki = 500 nM [10]
PHENOL Drug Info Ki = 11500 nM [12]
Prop-2-ynyl 4-sulfamoylbenzoate Drug Info Ki = 83 nM [2]
RESORCINOL Drug Info Ki = 10700 nM [4]
SPERMINE Drug Info Ki = 860 nM [10]
Sulfamylon Drug Info Ki = 3200 nM [1]
Syringic Acid Drug Info Ki = 9140 nM [8]
TRIENTINE Drug Info Ki = 12100 nM [10]
References
REF 1 Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3828-33.
REF 2 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 3 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 4 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 5 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 6 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 7 Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44.
REF 8 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 9 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 10 Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22.
REF 11 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 12 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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