Target Validation Information
Target ID T53378
Target Name Carbonic anhydrase IV
Target Type
Successful
Drug Potency against Target 5-amino-1,3,4-thiadiazole-2-sulfonamide Drug Info Ki = 940 nM [531013]
ELLAGIC ACID Drug Info Ki = 9080 nM [530751]
6-(hydroxymethyl)-2H-chromen-2-one Drug Info Ki = 7700 nM [530514]
2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 9700 nM [530514]
SPERMINE Drug Info Ki = 10 nM [530998]
COUMATE Drug Info Ki = 24 nM [529605]
CATECHIN Drug Info Ki = 4900 nM [531068]
Phenyl-phosphonic acid Drug Info Ki = 5400 nM [527462]
SPARFOSIC ACID Drug Info Ki = 79 nM [527462]
Aminocarbonyl dihydrogen phosphate Drug Info Ki = 9900 nM [527462]
Sodium trithiocarbonate Drug Info Ki = 9900 nM [530003]
Decane-1,10-diyl disulfamate Drug Info Ki = 91.2 nM [530359]
Phenylarsonic acid Drug Info Ki = 870 nM [527260]
CATECHOL Drug Info Ki = 10900 nM [530751]
FERULIC ACID Drug Info Ki = 10800 nM [530751]
N-1,3,4-thiadiazol-2-ylsulfamide Drug Info Ki = 8910 nM [529794]
Carbamoyl phosphate disodium Drug Info Ki = 9900 nM [527259]
SODIUM PHOSPHATE, DIBASIC, ANHYDROUS Drug Info Ki = 9800 nM [527259]
N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide Drug Info Ki = 7580 nM [529794]
HERNIARIN Drug Info Ki = 8300 nM [530514]
6-(aminomethyl)-2H-chromen-2-one Drug Info Ki = 15000 nM [530514]
7-(benzyloxy)-2H-chromen-2-one Drug Info Ki = 5800 nM [530514]
N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide Drug Info Ki = 8400 nM [529794]
N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide Drug Info Ki = 8640 nM [529794]
N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide Drug Info Ki = 5540 nM [529794]
BENZOLAMIDE Drug Info Ki = 12 nM [526877]
1-(3,4-dichlorophenyl)-3-hydroxyurea Drug Info Ki = 890 nM [528240]
[Cu(CN)2]- Drug Info Ki = 9800 nM [527492]
Octane-1,8-diyl disulfamate Drug Info Ki = 84.1 nM [530359]
3-Amino-benzenesulfonamide Drug Info Ki = 7750 nM [527415]
4-Amino-3-chloro-benzenesulfonamide Drug Info Ki = 450 nM [527415]
MAFENIDE Drug Info Ki = 8600 nM [527415]
PHENOL Drug Info Ki = 9500 nM [531068]
Trisodium phosphate Drug Info Ki = 84 nM [527259]
6-methyl-2-oxo-2H-chromene-3-carboxylic acid Drug Info Ki = 8500 nM [530514]
4-Amino-3-fluoro-benzenesulfonamide Drug Info Ki = 910 nM [527415]
[Fe(CN)6]4- Drug Info Ki = 10000 nM [527492]
SODIUM CITRATE Drug Info Ki = 99 nM [527390]
N1-(naphthalen-1-yl)ethane-1,2-diamine Drug Info Ki = 58 nM [530998]
4-(2-Amino-ethyl)-benzenesulfonamide Drug Info Ki = 3570 nM [527415]
Octyl sulfamate Drug Info Ki = 79.9 nM [530359]
SULFAMATE Drug Info Ki = 930 nM [527260]
Ethyl 7-methoxy-2-oxo-2H-chromene-3-carboxylate Drug Info Ki = 7200 nM [530514]
4-Amino-3-bromo-benzenesulfonamide Drug Info Ki = 96 nM [527415]
4-Amino-3-iodo-benzenesulfonamide Drug Info Ki = 920 nM [527415]
4-Hydrazino-benzenesulfonamide Drug Info Ki = 7700 nM [527415]
2,4-Disulfamyltrifluoromethylaniline Drug Info Ki = 4830 nM [527415]
N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide Drug Info Ki = 8300 nM [529794]
Syringic Acid Drug Info Ki = 10600 nM [530751]
SALICYLATE Drug Info Ki = 11100 nM [529562]
COUMARIN Drug Info Ki = 6800 nM [530514]
Sodium sulfamate Drug Info Ki = 930 nM [529905]
Phenyl Boronic acid Drug Info Ki = 880 nM [529905]
Sodium phenylarsonate Drug Info Ki = 870 nM [529905]
Curcumin Drug Info Ki = 4970 nM [531068]
Malonate sodium Drug Info Ki = 2800 nM [527390]
PYRUVATE SODIUM Drug Info Ki = 14500 nM [527390]
Pentane-1,5-diamine Drug Info Ki = 52 nM [530998]
SULFAMIDE Drug Info Ki = 880 nM [530922]
Hexane-1,6-diamine Drug Info Ki = 450 nM [530998]
2-Propyl-pentanoic acid 4-sulfamoyl-benzyl ester Drug Info Ki = 333 nM [526241]
N-(5-Sulfamoyl-[1,3,4]thiadiazol-2-yl)-benzamide Drug Info Ki = 21 nM [526241]
2-Propyl-pentanoic acid 4-sulfamoyl-benzylamide Drug Info Ki = 210 nM [526241]
GALLICACID Drug Info Ki = 9800 nM [530751]
P-Coumaric Acid Drug Info Ki = 9600 nM [530751]
PARABEN Drug Info Ki = 7780 nM [530751]
Decyl sulfamate Drug Info Ki = 67.6 nM [530359]
References
Ref 531013Bioorg 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 530751Bioorg 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 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 529605Bioorg 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 531068Bioorg 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 527462Bioorg Med Chem Lett. 2005 Mar 15;15(6):1683-6.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
Ref 527462Bioorg Med Chem Lett. 2005 Mar 15;15(6):1683-6.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
Ref 527462Bioorg Med Chem Lett. 2005 Mar 15;15(6):1683-6.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates.
Ref 530003Bioorg Med Chem Lett. 2009 Apr 1;19(7):1855-7. Epub 2009 Feb 26.Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I, II, III, VII and XIII with less investigated inorganic anions.
Ref 530359J 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.
Ref 527260Bioorg Med Chem Lett. 2004 Dec 6;14(23):5769-73.Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.
Ref 530751Bioorg 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 530751Bioorg 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 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 527259Bioorg Med Chem Lett. 2004 Dec 6;14(23):5763-7.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Ref 527259Bioorg Med Chem Lett. 2004 Dec 6;14(23):5763-7.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Ref 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 526877Bioorg Med Chem Lett. 2003 Sep 1;13(17):2867-73.Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide.
Ref 528240Bioorg Med Chem Lett. 2006 Aug 15;16(16):4316-20. Epub 2006 Jun 12.N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors.
Ref 527492Bioorg Med Chem Lett. 2005 Apr 1;15(7):1909-13.Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides.
Ref 530359J 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.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 531068Bioorg 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 527259Bioorg Med Chem Lett. 2004 Dec 6;14(23):5763-7.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with phosphates, carbamoyl phosphate, and the phosphonate antiviral drug foscarnet.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527492Bioorg Med Chem Lett. 2005 Apr 1;15(7):1909-13.Carbonic anhydrase inhibitors. Inhibition of isozymes I, II, IV, V and IX with complex fluorides, chlorides and cyanides.
Ref 527390Bioorg Med Chem Lett. 2005 Feb 1;15(3):573-8.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 530359J 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.
Ref 527260Bioorg Med Chem Lett. 2004 Dec 6;14(23):5769-73.Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.
Ref 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 527415Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54.Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides.
Ref 529794Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. Epub 2008 Nov 1.Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes VA and VB over the cytosolic and membrane-associated carbonic anhydrases I, II and IV.
Ref 530751Bioorg 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 529562Bioorg 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 530514J Med Chem. 2010 Jan 14;53(1):335-44.Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins.
Ref 529905Bioorg Med Chem Lett. 2009 Feb 15;19(4):1155-8. Epub 2008 Dec 25.Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions.
Ref 529905Bioorg Med Chem Lett. 2009 Feb 15;19(4):1155-8. Epub 2008 Dec 25.Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions.
Ref 529905Bioorg Med Chem Lett. 2009 Feb 15;19(4):1155-8. Epub 2008 Dec 25.Carbonic anhydrase inhibitors: the membrane-associated isoform XV is highly inhibited by inorganic anions.
Ref 531068Bioorg 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 527390Bioorg Med Chem Lett. 2005 Feb 1;15(3):573-8.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.
Ref 527390Bioorg Med Chem Lett. 2005 Feb 1;15(3):573-8.Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 530922Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5. Epub 2010 Apr 28.Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV.
Ref 530998J Med Chem. 2010 Aug 12;53(15):5511-22.Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule.
Ref 526241J Med Chem. 2002 Jan 17;45(2):312-20.Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties.
Ref 526241J Med Chem. 2002 Jan 17;45(2):312-20.Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties.
Ref 526241J Med Chem. 2002 Jan 17;45(2):312-20.Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties.
Ref 530751Bioorg 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 530751Bioorg 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 530751Bioorg 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 530359J 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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