Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR00210
Target NameCarbonic anhydrase VI    
Type of TargetResearch target    
Drug Potency against Targetoctane-1,8-diyl disulfamateKi = 1020 nM[1]
4-amino-3-iodobenzenesulfonamideKi = 1024 nM[2]
6-hydroxybenzo[d]thiazole-2-sulfonamideKi = 103 nM[2]
2-hydrazinylbenzenesulfonamideKi = 1090 nM[2]
4-amino-3-chlorobenzenesulfonamideKi = 1097 nM[2]
N1-(2-aminoethyl)ethane-1,2-diamineKi = 11500 nM[3]
SALICYLATEKi = 11900 nM[4]
4-hydrazinylbenzenesulfonamideKi = 1275 nM[2]
6-(aminomethyl)-2H-chromen-2-oneKi = 1300 nM[5]
7-butoxy-2H-chromen-2-oneKi = 13000 nM[5]
decyl sulfamateKi = 1334 nM[1]
4-CYANOPHENOLKi = 13700 nM[4]
decane-1,10-diyl disulfamateKi = 1414 nM[1]
P-TOLUENESULFONAMIDEKi = 1582 nM[2]
COUMARINKi = 2000 nM[5]
4-(2-hydroxyethyl)benzenesulfonamideKi = 4150 nM[2]
4-amino-3-bromobenzenesulfonamideKi = 4680 nM[2]
INDISULAMKi = 47 nM[2]
MAFENIDEKi = 4800 nM[2]
CATECHINKi = 4910 nM[6]
4-amino-N-(4-sulfamoylbenzyl)benzenesulfonamideKi = 55 nM[2]
HERNIARINKi = 5500 nM[5]
PARABENKi = 5700 nM[7]
4-amino-6-chlorobenzene-1,3-disulfonamideKi = 608 nM[2]
GALLICACIDKi = 6130 nM[7]
N1-(naphthalen-1-yl)ethane-1,2-diamineKi = 640 nM[3]
COUMATEKi = 653 nM[8]
ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylateKi = 6600 nM[5]
4-(hydroxymethyl)benzenesulfonamideKi = 6680 nM[2]
p-Coumaric AcidKi = 6720 nM[7]
ELLAGIC ACIDKi = 7060 nM[7]
hexane-1,6-diamineKi = 720 nM[3]
pentane-1,5-diamineKi = 740 nM[3]
7-propoxy-2H-chromen-2-oneKi = 7400 nM[5]
Syringic AcidKi = 7550 nM[7]
2-aminobenzenesulfonamideKi = 772 nM[2]
octyl sulfamateKi = 795 nM[1]
5-amino-1,3,4-thiadiazole-2-sulfonamideKi = 798 nM[9]
FERULIC ACIDKi = 8450 nM[7]
4-(2-aminopyrimidin-4-ylamino)benzenesulfonamideKi = 86 nM[2]
Carzenide;Para-Carboxybenzenesulfonamide (Weak Carbonic Anhydrase Inhibitor)Ki = 887 nM[2]
BENZOLAMIDEKi = 93 nM[2]
6-(hydroxymethyl)-2H-chromen-2-oneKi = 9300 nM[5]
2,4-DisulfamyltrifluoromethylanilineKi = 955 nM[2]
4-amino-3-fluorobenzenesulfonamideKi = 96 nM[2]
SPERMINEKi = 990 nM[3]
CURCUMINKi = 9940 nM[6]
Ref 1J 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. To Reference
Ref 2J 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. To Reference
Ref 3J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. To Reference
Ref 4Bioorg 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. To Reference
Ref 5J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. To Reference
Ref 6Bioorg 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. To Reference
Ref 7Bioorg 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. To Reference
Ref 8Bioorg 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. To Reference
Ref 9Bioorg 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 acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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