Target Validation Information
TTD ID T06569
Target Name Carbonic anhydrase VI (CA-VI)
Type of Target
Successful
Drug Potency against Target Drug Info Ki = 798 nM [8]
Drug Info Ki = 640 nM [7]
Drug Info Ki = 6130 nM [6]
Drug Info Ki = 653 nM [2]
Drug Info Ki = 608 nM [3]
Drug Info Ki = 5500 nM [5]
Drug Info Ki = 4910 nM [9]
Drug Info Ki = 1097 nM [3]
Drug Info Ki = 1582 nM [3]
Drug Info Ki = 55 nM [3]
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-fluoro-benzenesulfonamide Drug Info Ki = 96 nM [3]
4-Amino-3-iodo-benzenesulfonamide Drug Info Ki = 1024 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]
COUMARIN Drug Info Ki = 2000 nM [5]
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]
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]
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]
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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