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

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