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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