| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T06569 | ||||
| Target Name | Carbonic anhydrase VI (CA-VI) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | 2,4-Disulfamyltrifluoromethylaniline | Drug Info | Ki = 955 nM | [3] | |
| 2-Amino-benzenesulfonamide | Drug Info | Ki = 772 nM | [3] | ||
| 2-hydrazinylbenzenesulfonamide | Drug Info | Ki = 1090 nM | [3] | ||
| 4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide | Drug Info | Ki = 86 nM | [3] | ||
| 4-(2-Hydroxy-ethyl)-benzenesulfonamide | Drug Info | Ki = 4150 nM | [3] | ||
| 4-(hydroxymethyl)benzenesulfonamide | Drug Info | Ki = 6680 nM | [3] | ||
| 4-Amino-3-bromo-benzenesulfonamide | Drug Info | Ki = 4680 nM | [3] | ||
| 4-Amino-3-chloro-benzenesulfonamide | Drug Info | Ki = 1097 nM | [3] | ||
| 4-Amino-3-fluoro-benzenesulfonamide | Drug Info | Ki = 96 nM | [3] | ||
| 4-Amino-3-iodo-benzenesulfonamide | Drug Info | Ki = 1024 nM | [3] | ||
| 4-amino-6-chlorobenzene-1,3-disulfonamide | Drug Info | Ki = 608 nM | [3] | ||
| 4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamide | Drug Info | Ki = 55 nM | [3] | ||
| 4-CYANOPHENOL | Drug Info | Ki = 13700 nM | [1] | ||
| 4-Hydrazino-benzenesulfonamide | Drug Info | Ki = 1275 nM | [3] | ||
| 6-(aminomethyl)-2H-chromen-2-one | Drug Info | Ki = 1300 nM | [5] | ||
| 6-(hydroxymethyl)-2H-chromen-2-one | Drug Info | Ki = 9300 nM | [5] | ||
| 6-Hydroxy-benzothiazole-2-sulfonic acid amide | Drug Info | Ki = 103 nM | [3] | ||
| 7-butoxy-2H-chromen-2-one | Drug Info | Ki = 13000 nM | [5] | ||
| 7-propoxy-2H-chromen-2-one | Drug Info | Ki = 7400 nM | [5] | ||
| BENZOLAMIDE | Drug Info | Ki = 93 nM | [3] | ||
| Carzenide | Drug Info | Ki = 887 nM | [3] | ||
| CATECHIN | Drug Info | Ki = 4910 nM | [9] | ||
| CL-5343 | Drug Info | Ki = 798 nM | [8] | ||
| COUMARIN | Drug Info | Ki = 2000 nM | [5] | ||
| Coumate | Drug Info | Ki = 653 nM | [2] | ||
| Curcumin | Drug Info | Ki = 9940 nM | [9] | ||
| Decane-1,10-diyl disulfamate | Drug Info | Ki = 1414 nM | [4] | ||
| Decyl sulfamate | Drug Info | Ki = 1334 nM | [4] | ||
| ELLAGIC ACID | Drug Info | Ki = 7060 nM | [6] | ||
| Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate | Drug Info | Ki = 6600 nM | [5] | ||
| FERULIC ACID | Drug Info | Ki = 8450 nM | [6] | ||
| GALLICACID | Drug Info | Ki = 6130 nM | [6] | ||
| HERNIARIN | Drug Info | Ki = 5500 nM | [5] | ||
| Hexane-1,6-diamine | Drug Info | Ki = 720 nM | [7] | ||
| INDISULAM | Drug Info | Ki = 47 nM | [3] | ||
| N1-(2-aminoethyl)ethane-1,2-diamine | Drug Info | Ki = 11500 nM | [7] | ||
| N1-(naphthalen-1-yl)ethane-1,2-diamine | Drug Info | Ki = 640 nM | [7] | ||
| Octane-1,8-diyl disulfamate | Drug Info | Ki = 1020 nM | [4] | ||
| Octyl sulfamate | Drug Info | Ki = 795 nM | [4] | ||
| P-Coumaric Acid | Drug Info | Ki = 6720 nM | [6] | ||
| P-toluenesulfonamide | Drug Info | Ki = 1582 nM | [3] | ||
| PARABEN | Drug Info | Ki = 5700 nM | [6] | ||
| Pentane-1,5-diamine | Drug Info | Ki = 740 nM | [7] | ||
| Salicyclic acid | Drug Info | Ki = 11900 nM | [1] | ||
| SPERMINE | Drug Info | Ki = 990 nM | [7] | ||
| Sulfamylon | Drug Info | Ki = 4800 nM | [3] | ||
| Syringic Acid | Drug Info | Ki = 7550 nM | [6] | ||
| References | |||||
| REF 1 | 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 2 | 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 3 | Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV. J Med Chem. 2009 Feb 12;52(3):646-54. | ||||
| REF 4 | 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 5 | Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44. | ||||
| REF 6 | 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 7 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22. | ||||
| REF 8 | 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 9 | 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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