Target Information
| Target General Information | Top | |||||
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| Target ID |
T20401
(Former ID: TTDS00306)
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| Target Name |
Carbonic anhydrase II (CA-II)
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| Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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| Gene Name |
CA2
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| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 6 Target-related Diseases | + | ||||
| 1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
| 2 | Essential hypertension [ICD-11: BA00] | |||||
| 3 | Glaucoma [ICD-11: 9C61] | |||||
| 4 | Heart failure [ICD-11: BD10-BD1Z] | |||||
| 5 | Insomnia [ICD-11: 7A00-7A0Z] | |||||
| 6 | Seborrhoeic dermatitis [ICD-11: EA81] | |||||
| Function |
Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate exchange activity of SLC26A6. Essential for bone resorption and osteoclast differentiation.
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| BioChemical Class |
Alpha-carbonic anhydrase
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| UniProt ID | ||||||
| EC Number |
EC 4.2.1.1
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| Sequence |
MSHHWGYGKHNGPEHWHKDFPIAKGERQSPVDIDTHTAKYDPSLKPLSVSYDQATSLRIL
NNGHAFNVEFDDSQDKAVLKGGPLDGTYRLIQFHFHWGSLDGQGSEHTVDKKKYAAELHL VHWNTKYGDFGKAVQQPDGLAVLGIFLKVGSAKPGLQKVVDVLDSIKTKGKSADFTNFDP RGLLPESLDYWTYPGSLTTPPLLECVTWIVLKEPISVSSEQVLKFRKLNFNGEGEPEELM VDNWRPAQPLKNRQIKASFK Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T43XD8 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 9 Approved Drugs | + | ||||
| 1 | Benzthiazide | Drug Info | Approved | High blood pressure | [2], [3], [4] | |
| 2 | Chlorothiazide | Drug Info | Approved | Congestive heart failure | [4], [5], [6] | |
| 3 | Cyclothiazide | Drug Info | Approved | Congestive heart failure | [4], [7], [8] | |
| 4 | Dichlorphenamide | Drug Info | Approved | Chronic glaucoma | [9], [10] | |
| 5 | Dorzolamide | Drug Info | Approved | Open-angle glaucoma | [11], [12] | |
| 6 | Ethinamate | Drug Info | Approved | Insomnia | [13], [14] | |
| 7 | Ethoxzolamide | Drug Info | Approved | Glaucoma/ocular hypertension | [15], [16] | |
| 8 | Salicyclic acid | Drug Info | Approved | Seborrhoeic dermatitis | [4], [17], [18] | |
| 9 | Sulfamylon | Drug Info | Approved | Bacterial infection | [4], [19] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | Curcumin | Drug Info | Phase 3 | Solid tumour/cancer | [22], [23] | |
| 2 | STX-140 | Drug Info | Phase 2 | Osteoporosis | [25] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 253 Inhibitor drugs | + | ||||
| 1 | Benzthiazide | Drug Info | [1], [26] | |||
| 2 | Chlorothiazide | Drug Info | [27] | |||
| 3 | Cyclothiazide | Drug Info | [28] | |||
| 4 | Dichlorphenamide | Drug Info | [29] | |||
| 5 | Dorzolamide | Drug Info | [30] | |||
| 6 | Ethinamate | Drug Info | [31] | |||
| 7 | Ethoxzolamide | Drug Info | [29] | |||
| 8 | Salicyclic acid | Drug Info | [32] | |||
| 9 | Sulfamylon | Drug Info | [33] | |||
| 10 | Curcumin | Drug Info | [34] | |||
| 11 | GUAIACOL | Drug Info | [35] | |||
| 12 | PARABEN | Drug Info | [36] | |||
| 13 | SULTHIAME | Drug Info | [29] | |||
| 14 | PHENOL | Drug Info | [34] | |||
| 15 | STX-140 | Drug Info | [37] | |||
| 16 | FERULIC ACID | Drug Info | [36] | |||
| 17 | (2,2-dimethyl-1,3-dioxolan-4-yl)methyl sulfamate | Drug Info | [38] | |||
| 18 | (2-bromophenyl)difluoromethanesulfonamide | Drug Info | [39] | |||
| 19 | (4-bromophenyl)difluoromethanesulfonamide | Drug Info | [39] | |||
| 20 | 1,2,4-Triazole | Drug Info | [40] | |||
| 21 | 1,4-Dihydro-1-methyl-4-oxo-3-pyridinesulfonamide | Drug Info | [41] | |||
| 22 | 1,4-phenylene disulfamate | Drug Info | [42] | |||
| 23 | 1-(3,4-dichlorophenyl)-3-hydroxyurea | Drug Info | [43] | |||
| 24 | 1-acetamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 25 | 1-Benzyl-1,4-dihydro-4-oxo-3-pyridinesulfonamide | Drug Info | [41] | |||
| 26 | 1-cyclohexylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 27 | 1-pentafluorophenylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 28 | 1-pentenyl-4-(aminosulfonyl)benzoate | Drug Info | [45] | |||
| 29 | 1-valproylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 30 | 2,2,2-Trifluoro-N-(4-sulfamoyl-phenyl)-acetamide | Drug Info | [46] | |||
| 31 | 2,2-Dimethyl-N-(4-sulfamoyl-phenyl)-propionamide | Drug Info | [46] | |||
| 32 | 2,3-dihydro-1H-indene-5-sulfonamide | Drug Info | [29], [47] | |||
| 33 | 2,4-dichloro-5-sulfamoylbenzoic acid | Drug Info | [48] | |||
| 34 | 2,4-Disulfamyltrifluoromethylaniline | Drug Info | [49] | |||
| 35 | 2,6-di-t-butylphenol | Drug Info | [35] | |||
| 36 | 2,6-di-tert-butyl-4-methoxyphenol | Drug Info | [35] | |||
| 37 | 2,6-Difluorobenzenesulfonamide | Drug Info | [50] | |||
| 38 | 2-(4-chlorobenzyloxyamino)-N-hydroxyacetamide | Drug Info | [51] | |||
| 39 | 2-(4-chlorobenzyloxyamino)-N-hydroxyhexanamide | Drug Info | [51] | |||
| 40 | 2-(4-chlorobenzyloxyamino)-N-hydroxypropanamide | Drug Info | [51] | |||
| 41 | 2-(4-hydroxybenzylideneamino)ethanesulfonamide | Drug Info | [52] | |||
| 42 | 2-(4-tert-butylbenzylideneamino)ethanesulfonamide | Drug Info | [52] | |||
| 43 | 2-(benzylideneamino)ethanesulfonamide | Drug Info | [52] | |||
| 44 | 2-(N''-Acetyl-hydrazino)-benzenesulfonamide | Drug Info | [53] | |||
| 45 | 2-acetamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 46 | 2-Acetylamino-indan-5-sulfonic acid hydrate | Drug Info | [47] | |||
| 47 | 2-Amino-benzenesulfonamide | Drug Info | [49] | |||
| 48 | 2-Amino-indan-5-sulfonic acid | Drug Info | [47] | |||
| 49 | 2-butylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 50 | 2-cyclohexylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 51 | 2-ethylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 52 | 2-Hydrazinocarbonyl-benzenesulfonamide | Drug Info | [53] | |||
| 53 | 2-hydrazinylbenzenesulfonamide | Drug Info | [30] | |||
| 54 | 2-Hydroxycinnamic acid | Drug Info | [34] | |||
| 55 | 2-Mercapto-N-(4-sulfamoyl-phenyl)-benzamide | Drug Info | [29], [54] | |||
| 56 | 2-methoxyestradiol-17-O-sulfamate | Drug Info | [37] | |||
| 57 | 2-methoxyestrrone-3-O-sulfamate | Drug Info | [37] | |||
| 58 | 2-Morpholin-4-yl-N-(4-sulfamoyl-phenyl)-acetamide | Drug Info | [55] | |||
| 59 | 2-nonylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 60 | 2-oxo-2H-thiochromene-3-carboxylic acid | Drug Info | [56] | |||
| 61 | 2-pentafluorophenylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 62 | 2-propylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 63 | 2-Sulfamoyl-benzoic acid methyl ester | Drug Info | [53] | |||
| 64 | 2-Sulfhydryl-Ethanol | Drug Info | [40] | |||
| 65 | 2-valproylamido-5-sulfonamidoindane | Drug Info | [44] | |||
| 66 | 3,5-Difluorobenzenesulfonamide | Drug Info | [40] | |||
| 67 | 3-((4-aminophenyl)diazenyl)benzenesulfonamide | Drug Info | [57] | |||
| 68 | 3-((4-hydroxyphenyl)diazenyl)benzenesulfonamide | Drug Info | [57] | |||
| 69 | 3-(3-Phenyl-ureido)-benzenesulfonamide | Drug Info | [46] | |||
| 70 | 3-(4'-Hydroxyphenyl)diazenylbenzenesulfonamide | Drug Info | [57] | |||
| 71 | 3-(4-sulfamoylphenyl)propanoic acid | Drug Info | [29], [49] | |||
| 72 | 3-Amino-benzenesulfonamide | Drug Info | [58] | |||
| 73 | 3-bromophenyl-difluoromethanesulfonamide | Drug Info | [39] | |||
| 74 | 3-Chloro-4-hydrazino-benzenesulfonamide | Drug Info | [53] | |||
| 75 | 3-Fluoro-4-hydrazino-benzenesulfonamide | Drug Info | [53] | |||
| 76 | 3-hydroxy-2-methoxybenzaldehyde | Drug Info | [35] | |||
| 77 | 3-mercapto-N-(4-sulfamoyl-phenyl)-propionamide | Drug Info | [59] | |||
| 78 | 3-Mercuri-4-Aminobenzenesulfonamide | Drug Info | [40] | |||
| 79 | 3-Nitro-benzenesulfonamide | Drug Info | [60] | |||
| 80 | 3-phenyl-5-sulfamoyl-1H-indole-2-carboxamide | Drug Info | [61] | |||
| 81 | 3-phenylprop-1-enylboronic acid | Drug Info | [62] | |||
| 82 | 4,4'-thiodipyridine-3-sulfonamide | Drug Info | [63] | |||
| 83 | 4,6-Dinitro salicylic acid | Drug Info | [64] | |||
| 84 | 4-((4-hydroxyphenyl)diazenyl)benzenesulfonamide | Drug Info | [57] | |||
| 85 | 4-((benzylideneamino)methyl)benzenesulfonamide | Drug Info | [52] | |||
| 86 | 4-(2-AMINOETHYL)BENZENESULFONAMIDE | Drug Info | [29], [65] | |||
| 87 | 4-(2-aminopyrimidin-4-ylamino)benzenesulfonamide | Drug Info | [49] | |||
| 88 | 4-(2-Hydroxy-ethyl)-benzenesulfonamide | Drug Info | [66] | |||
| 89 | 4-(2-Methyl-8-quinolinoxy)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 90 | 4-(2-Phenylacetamido)-3-chlorobenzenesulfonamide | Drug Info | [67] | |||
| 91 | 4-(2-Phenylacetamido)-3-fluorobenzenesulfonamide | Drug Info | [67] | |||
| 92 | 4-(2-Phenylacetamido)benzenesulfonamide | Drug Info | [67] | |||
| 93 | 4-(2-Phenylacetamidoethyl)benzenesulfonamide | Drug Info | [67] | |||
| 94 | 4-(2-Phenylacetamidomethyl)benzenesulfonamide | Drug Info | [67] | |||
| 95 | 4-(2-Propynylthio)pyridine-3-sulfonamide | Drug Info | [63] | |||
| 96 | 4-(2-Pyridin-2-ylacetamido)benzenesulfonamide | Drug Info | [67] | |||
| 97 | 4-(2-Pyridin-4-ylacetamido)benzenesulfonamide | Drug Info | [67] | |||
| 98 | 4-(4-Cyanophenoxy)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 99 | 4-(4-Fluorophenoxy)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 100 | 4-(4-hydroxy-benzylideneamino)-benzenesulfonamide | Drug Info | [52] | |||
| 101 | 4-(4-hydroxybenzylideneamino)benzoic acid | Drug Info | [52] | |||
| 102 | 4-(4-tert-butylbenzylideneamino)benzoic acid | Drug Info | [52] | |||
| 103 | 4-(5-Methyl-2-pirazolino)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 104 | 4-(Allylamino)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 105 | 4-(benzylideneamino)benzenesulfonamide | Drug Info | [52] | |||
| 106 | 4-(benzylideneamino)benzoic acid | Drug Info | [52] | |||
| 107 | 4-(Cyanomethylthio)pyridine-3-sulfonamide | Drug Info | [63] | |||
| 108 | 4-(Hydroxymercury)Benzoic Acid | Drug Info | [40] | |||
| 109 | 4-(hydroxymethyl)benzenesulfonamide | Drug Info | [49] | |||
| 110 | 4-(Methylhydrazino)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 111 | 4-(N-Methyl-hydrazino)-benzenesulfonamide | Drug Info | [68] | |||
| 112 | 4-(N-Oxide-2-pyridylthio)pyridine-3-sulfonamide | Drug Info | [63] | |||
| 113 | 4-(Quinolinoxy)-3-pyridinesulfonamide | Drug Info | [63] | |||
| 114 | 4-Amino-3-bromo-benzenesulfonamide | Drug Info | [49] | |||
| 115 | 4-Amino-3-fluoro-benzenesulfonamide | Drug Info | [66] | |||
| 116 | 4-Amino-3-iodo-benzenesulfonamide | Drug Info | [49] | |||
| 117 | 4-Benzythiopyridine-3-sulfonamide | Drug Info | [63] | |||
| 118 | 4-butylphenylboronic acid | Drug Info | [62] | |||
| 119 | 4-Chloro-N-(5-sulfamoyl-indan-2-yl)-benzamide | Drug Info | [47] | |||
| 120 | 4-CYANOPHENOL | Drug Info | [32] | |||
| 121 | 4-Ethoxy-3-pyridinesulfonamide | Drug Info | [63] | |||
| 122 | 4-ethynyl benzene sulfonamide | Drug Info | [69] | |||
| 123 | 4-Flourobenzenesulfonamide | Drug Info | [40] | |||
| 124 | 4-Hydrazino-benzenesulfonamide | Drug Info | [70] | |||
| 125 | 4-Hydrazinocarbonyl-benzenesulfonamide | Drug Info | [53] | |||
| 126 | 4-isothiocyanatobenzenesulfonamide | Drug Info | [71] | |||
| 127 | 4-Methanesulfonylamino-benzenesulfonamide | Drug Info | [46] | |||
| 128 | 4-Methoxy-3-pyridinesulfonamide | Drug Info | [63] | |||
| 129 | 4-methoxyphenylboronic acid | Drug Info | [62] | |||
| 130 | 4-methoxyphenylsulfamide | Drug Info | [38] | |||
| 131 | 4-Methylamino-benzenesulfonamide | Drug Info | [68] | |||
| 132 | 4-Methylimidazole | Drug Info | [50] | |||
| 133 | 4-methylphenyl-difluoromethanesulfonamide | Drug Info | [39] | |||
| 134 | 4-Methylthiopyridine-3-sulfonamide | Drug Info | [63] | |||
| 135 | 4-Nitro-benzenesulfonamide | Drug Info | [60] | |||
| 136 | 4-nitrophenyl phosphate | Drug Info | [72] | |||
| 137 | 4-nitrophenyl-difluoromethanesulfonamide | Drug Info | [39] | |||
| 138 | 4-nitrophenylsulfamide | Drug Info | [38] | |||
| 139 | 4-phenoxyphenylboronic acid | Drug Info | [62] | |||
| 140 | 4-Sulfonamide-[1-(4-Aminobutane)]Benzamide | Drug Info | [40] | |||
| 141 | 4-Thiocyanato-benzenesulfonamide | Drug Info | [60] | |||
| 142 | 4-[2-(2-Thienyl)acetamidoethyl]benzenesulfonamide | Drug Info | [67] | |||
| 143 | 4-[2-(3-Phenyl-ureido)-ethyl]-benzenesulfonamide | Drug Info | [46] | |||
| 144 | 5-Chlorosalicylic Acid | Drug Info | [64] | |||
| 145 | 5-hydroxy-1-tosyl-1H-pyrrol-2(5H)-one | Drug Info | [73] | |||
| 146 | 6-(aminomethyl)-2H-chromen-2-one | Drug Info | [56] | |||
| 147 | 6-(hydroxymethyl)-2H-chromen-2-one | Drug Info | [56] | |||
| 148 | 6-Amino-benzothiazole-2-sulfonic acid amide | Drug Info | [74] | |||
| 149 | 6-HYDROXY-1,3-BENZOTHIAZOLE-2-SULFONAMIDE | Drug Info | [29] | |||
| 150 | 6-Hydroxy-benzothiazole-2-sulfonic acid amide | Drug Info | [70] | |||
| 151 | 6-hydroxybenzo[d][1,3]oxathiol-2-one | Drug Info | [75] | |||
| 152 | 6-methoxy-2-oxo-2H-chromene-3-carboxylic acid | Drug Info | [56] | |||
| 153 | 6-methyl-2-oxo-2H-chromene-3-carboxylic acid | Drug Info | [56] | |||
| 154 | 6-Nitro-benzothiazole-2-sulfonic acid amide | Drug Info | [60] | |||
| 155 | Acetate Ion | Drug Info | [40] | |||
| 156 | ACETYLSULFANILAMIDE | Drug Info | [46] | |||
| 157 | AL4623 | Drug Info | [40] | |||
| 158 | AL5300 | Drug Info | [40] | |||
| 159 | AL5424 | Drug Info | [40] | |||
| 160 | AL5927 | Drug Info | [40] | |||
| 161 | AL6528 | Drug Info | [40] | |||
| 162 | Al7089a | Drug Info | [40] | |||
| 163 | AL7182 | Drug Info | [40] | |||
| 164 | Allyl 4-(aminosulfonyl)benzoate | Drug Info | [45] | |||
| 165 | Aminobenzolamide derivative | Drug Info | [76] | |||
| 166 | Azide | Drug Info | [77] | |||
| 167 | BENZOLAMIDE | Drug Info | [49] | |||
| 168 | Beta-naphthylboronic acid | Drug Info | [62] | |||
| 169 | Biphenyl-4-ylboronic acid | Drug Info | [62] | |||
| 170 | Carzenide | Drug Info | [45] | |||
| 171 | CATECHOL | Drug Info | [36] | |||
| 172 | COUMARIN | Drug Info | [78] | |||
| 173 | Dansylamide | Drug Info | [40] | |||
| 174 | Decane-1,10-diyl disulfamate | Drug Info | [79] | |||
| 175 | Decyl sulfamate | Drug Info | [79] | |||
| 176 | Di(2,6-di-t-butylphenol) | Drug Info | [35] | |||
| 177 | Di(2,6-diisopropylphenol) | Drug Info | [35] | |||
| 178 | Di(2,6-dimethylphenol) | Drug Info | [35] | |||
| 179 | ELLAGIC ACID | Drug Info | [36] | |||
| 180 | EMATE | Drug Info | [80] | |||
| 181 | ETHYL 3-[4-(AMINOSULFONYL)PHENYL]PROPANOATE | Drug Info | [29] | |||
| 182 | Formic Acid | Drug Info | [40] | |||
| 183 | HYDROSULFIDE | Drug Info | [77] | |||
| 184 | IODIDE | Drug Info | [77] | |||
| 185 | Mercuribenzoic Acid | Drug Info | [40] | |||
| 186 | Methyl 4-(4-hydroxybenzylideneamino)benzoate | Drug Info | [52] | |||
| 187 | Methyl 4-(4-tert-butylbenzylideneamino)benzoate | Drug Info | [52] | |||
| 188 | Methyl Mercury Ion | Drug Info | [40] | |||
| 189 | MMI270 | Drug Info | [51] | |||
| 190 | N-(1-benzofuran-3-ylmethyl)sulfamide | Drug Info | [81] | |||
| 191 | N-(2,3-DIFLUORO-BENZYL)-4-SULFAMOYL-BENZAMIDE | Drug Info | [29] | |||
| 192 | N-(2,6-Diflouro-Benzyl)-4-Sulfamoyl-Benzamide | Drug Info | [40] | |||
| 193 | N-(2-Thienylmethyl)-2,5-Thiophenedisulfonamide | Drug Info | [40] | |||
| 194 | N-(4-cyanophenyl)sulfamide | Drug Info | [82] | |||
| 195 | N-(4-Sulfamoyl-phenyl)-benzamide | Drug Info | [46] | |||
| 196 | N-(4-Sulfamoyl-phenyl)-butyramide | Drug Info | [46] | |||
| 197 | N-(4-Sulfamoyl-phenyl)-isobutyramide | Drug Info | [46] | |||
| 198 | N-(4-Sulfamoyl-phenyl)-propionamide | Drug Info | [46] | |||
| 199 | N-(4-sulfamoylphenylethyl)-4-sulfamoylbenzamide | Drug Info | [83] | |||
| 200 | N-(5-ethyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [84] | |||
| 201 | N-(5-Mercapto-[1,3,4]thiadiazol-2-yl)-acetamide | Drug Info | [85] | |||
| 202 | N-(5-phenyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [84] | |||
| 203 | N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)sulfamide | Drug Info | [84] | |||
| 204 | N-(pentafluorophenyl)sulfamide | Drug Info | [82] | |||
| 205 | N-(phosphonacetyl)-L-aspartate | Drug Info | [86] | |||
| 206 | N-1,3,4-thiadiazol-2-ylsulfamide | Drug Info | [84] | |||
| 207 | N-Benzyl-4-Sulfamoyl-Benzamide | Drug Info | [40] | |||
| 208 | N-hydroxysulfamide | Drug Info | [87] | |||
| 209 | N-hydroxysulfonamides | Drug Info | [88] | |||
| 210 | N-propynyl amidebenzenesulphonide | Drug Info | [89] | |||
| 211 | N-[(4-bromo-1-benzothien-3-yl)methyl]sulfamide | Drug Info | [81] | |||
| 212 | N-[(5-chloro-1-benzothien-3-yl)methyl]sulfamide | Drug Info | [81] | |||
| 213 | N-[2-(1h-Indol-5-Yl)-Butyl]-4-Sulfamoyl-Benzamide | Drug Info | [40] | |||
| 214 | N-[4-(trifluoromethyl)phenyl]sulfamide | Drug Info | [82] | |||
| 215 | N-[5-(ethylthio)-1,3,4-thiadiazol-2-yl]sulfamide | Drug Info | [84] | |||
| 216 | N-[5-(methylthio)-1,3,4-thiadiazol-2-yl]sulfamide | Drug Info | [84] | |||
| 217 | N-{2-[4-(AMINOSULFONYL)PHENYL]ETHYL}ACETAMIDE | Drug Info | [29] | |||
| 218 | NITRATE | Drug Info | [77] | |||
| 219 | NSC-654077 | Drug Info | [54] | |||
| 220 | Octane-1,8-diyl disulfamate | Drug Info | [79] | |||
| 221 | Octyl sulfamate | Drug Info | [79] | |||
| 222 | P-Coumaric Acid | Drug Info | [36] | |||
| 223 | P-tolylboronic acid | Drug Info | [62] | |||
| 224 | PARAOXON | Drug Info | [72] | |||
| 225 | Pentane-1,5-diamine | Drug Info | [90] | |||
| 226 | Pentanoic acid (4-sulfamoyl-phenyl)-amide | Drug Info | [46] | |||
| 227 | Phenethylboronic acid | Drug Info | [62] | |||
| 228 | Phenoxyarsonous acid | Drug Info | [77] | |||
| 229 | Phenyl Boronic acid | Drug Info | [77] | |||
| 230 | Phenyl-phosphonic acid | Drug Info | [86] | |||
| 231 | PHENYLMETHANESULFONAMIDE | Drug Info | [39] | |||
| 232 | PHENYLSULFAMATE | Drug Info | [38] | |||
| 233 | PHENYLSULFAMIDE | Drug Info | [38] | |||
| 234 | PRONTOCIL | Drug Info | [57] | |||
| 235 | Prop-2-ynyl 4-sulfamoylbenzoate | Drug Info | [89] | |||
| 236 | Quinoline-8-sulfonamide | Drug Info | [42] | |||
| 237 | RESORCINOL | Drug Info | [32] | |||
| 238 | SACCHARIN | Drug Info | [66] | |||
| 239 | Sodium 2,3,5,6-tetrafluorobenzoate | Drug Info | [91] | |||
| 240 | SODIUM PERFLUOROHEXANESULFONAMIDE | Drug Info | [92] | |||
| 241 | Sodium trithiocarbonate | Drug Info | [93] | |||
| 242 | SULFAMATE | Drug Info | [77] | |||
| 243 | Sulfamic acid 12-sulfamoyloxy-dodecyl ester | Drug Info | [94] | |||
| 244 | Sulfamic acid 16-sulfamoyloxy-hexadecyl ester | Drug Info | [94] | |||
| 245 | Sulfamic acid 3-sulfamoyloxy-phenyl ester | Drug Info | [94] | |||
| 246 | Sulfamic acid 4-sulfamoyloxy-butyl ester | Drug Info | [94] | |||
| 247 | Sulfamic acid 4-sulfamoyloxymethyl-benzyl ester | Drug Info | [94] | |||
| 248 | Sulfamic acid 7-sulfamoyloxy-heptyl ester | Drug Info | [94] | |||
| 249 | Sulfamic acid benzo[1,3]dioxol-2-ylmethyl ester | Drug Info | [95] | |||
| 250 | Sulfamic acid chroman-2-ylmethyl ester | Drug Info | [95] | |||
| 251 | Syringic Acid | Drug Info | [36] | |||
| 252 | Thioureido sulfonamide | Drug Info | [96] | |||
| 253 | Trecadrine | Drug Info | [97] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Famotidine | Ligand Info | |||||
| Structure Description | Crystal structure of human carbonic anhydrase II in complex with the inhibitor famotidine | PDB:6G3Q | ||||
| Method | X-ray diffraction | Resolution | 1.01 Å | Mutation | No | [98] |
| PDB Sequence |
MSHHWGYGKH
10 NGPEHWHKDF20 PIAKGERQSP30 VDIDTHTAKY40 DPSLKPLSVS50 YDQATSLRIL 60 NNGHAFNVEF70 DDSQDKAVLK80 GGPLDGTYRL90 IQFHFHWGSL100 DGQGSEHTVD 110 KKKYAAELHL120 VHWNTKYGDF131 GKAVQQPDGL141 AVLGIFLKVG151 SAKPGLQKVV 161 DVLDSIKTKG171 KSADFTNFDP181 RGLLPESLDY191 WTYPGSLTTP201 PLLECVTWIV 211 LKEPISVSSE221 QVLKFRKLNF231 NGEGEPEELM241 VDNWRPAQPL251 KNRQIKASFK 261
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| Ligand Name: Acetazolamide | Ligand Info | |||||
| Structure Description | Human carbonic anhydrase II complexed with acetazolamide | PDB:3HS4 | ||||
| Method | X-ray diffraction | Resolution | 1.10 Å | Mutation | No | [99] |
| PDB Sequence |
HWGYGKHNGP
13 EHWHKDFPIA23 KGERQSPVDI33 DTHTAKYDPS43 LKPLSVSYDQ53 ATSLRILNNG 63 HAFNVEFDDS73 QDKAVLKGGP83 LDGTYRLIQF93 HFHWGSLDGQ103 GSEHTVDKKK 113 YAAELHLVHW123 NTKYGDFGKA134 VQQPDGLAVL144 GIFLKVGSAK154 PGLQKVVDVL 164 DSIKTKGKSA174 DFTNFDPRGL184 LPESLDYWTY194 PGSLTTPPLL204 ECVTWIVLKE 214 PISVSSEQVL224 KFRKLNFNGE234 GEPEELMVDN244 WRPAQPLKNR254 QIKASFK |
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HIS4
3.556
TRP5
3.491
GLY6
4.944
HIS10
4.415
ASN11
3.264
GLY12
4.487
HIS15
2.957
TRP16
3.567
LYS18
4.078
ASP19
2.730
PHE20
3.633
GLN92
3.097
HIS94
3.232
HIS96
3.272
GLU106
4.083
VAL109
3.771
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
|
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|
There is no similarity protein (E value < 0.005) for this target
|
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Nitrogen metabolism | hsa00910 | Affiliated Target |
|
| Class: Metabolism => Energy metabolism | Pathway Hierarchy | ||
| Proximal tubule bicarbonate reclamation | hsa04964 | Affiliated Target |
|
| Class: Organismal Systems => Excretory system | Pathway Hierarchy | ||
| Collecting duct acid secretion | hsa04966 | Affiliated Target |
|
| Class: Organismal Systems => Excretory system | Pathway Hierarchy | ||
| Gastric acid secretion | hsa04971 | Affiliated Target |
|
| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Pancreatic secretion | hsa04972 | Affiliated Target |
|
| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Bile secretion | hsa04976 | Affiliated Target |
|
| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Click to Show/Hide the Information of Affiliated Human Pathways | |||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 2.33E-05 |
|---|---|---|---|---|---|
| Closeness centrality | 1.79E-01 | Radiality | 1.30E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 6.00E+00 | Topological coefficient | 5.00E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 6 KEGG Pathways | + | ||||
| 1 | Nitrogen metabolism | |||||
| 2 | Proximal tubule bicarbonate reclamation | |||||
| 3 | Collecting duct acid secretion | |||||
| 4 | Gastric acid secretion | |||||
| 5 | Pancreatic secretion | |||||
| 6 | Bile secretion | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | IL4 Signaling Pathway | |||||
| 2 | EGFR1 Signaling Pathway | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Erythrocytes take up carbon dioxide and release oxygen | |||||
| 2 | Erythrocytes take up oxygen and release carbon dioxide | |||||
| 3 | Reversible hydration of carbon dioxide | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Reversible Hydration of Carbon Dioxide | |||||
| 2 | Uptake of Carbon Dioxide and Release of Oxygen by Erythrocytes | |||||
| 3 | Uptake of Oxygen and Release of Carbon Dioxide by Erythrocytes | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Nature of the inhibition of carbonic anhydrase by acetazolamide and benzthiazide. J Pharmacol Exp Ther. 1961 Mar;131:271-4. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7125). | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 083206. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4835). | |||||
| REF 6 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 084026. | |||||
| REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4167). | |||||
| REF 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 013157. | |||||
| REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6807). | |||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011366. | |||||
| REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6810). | |||||
| REF 12 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 13 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7325). | |||||
| REF 14 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009750. | |||||
| REF 15 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6814). | |||||
| REF 16 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011047. | |||||
| REF 17 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4306). | |||||
| REF 18 | Drug information of Salicyclic acid, 2008. eduDrugs. | |||||
| REF 19 | ClinicalTrials.gov (NCT00634166) Prospective Evaluation of the Effects of Topical Therapy With Sulfamylon For 5% Topical Solution on Autograft Healing in Subjects With Thermal Injuries Requiring Meshed Autografts: A Comparison to a Historical Control Group. U.S. National Institutes of Health. | |||||
| REF 20 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8316). | |||||
| REF 21 | ClinicalTrials.gov (NCT01765296) Phase III Study of CG100649 in Osteoarthritis Patients. U.S. National Institutes of Health. | |||||
| REF 22 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000). | |||||
| REF 23 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | |||||
| REF 24 | Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83. | |||||
| REF 25 | ClinicalTrials.gov (NCT00592579) A Phase 2 Study With Panzem in Patients With Relapsed or Plateau Phase Multiple Myeloma. U.S. National Institutes of Health. | |||||
| REF 26 | Diuretic activity of a dihydro-analog of benzthiazide; (3-benzylthiomethyl-6-chloro-7-sulfamyl-3,4 dihydro-1,2,4 benzothiadiazine, 1,1-dioxide). Chemotherapia (Basel). 1962;4:405-12. | |||||
| REF 27 | Localization of diuretic effects along the loop of Henle: an in vivo microperfusion study in rats. Clin Sci (Lond). 2000 Apr;98(4):481-8. | |||||
| REF 28 | Selective effect of thiazides on the human osteoblast-like cell line MG-63. Kidney Int. 1996 Nov;50(5):1476-82. | |||||
| REF 29 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 30 | Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. Bioorg Med Chem. 2009 Jul 15;17(14):5054-8. | |||||
| REF 31 | Inhibition of carbonic anhydrases I and II by N-unsubstituted carbamate esters. J Biol Chem. 1992 Dec 15;267(35):25044-50. | |||||
| REF 32 | 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 33 | Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases. J Med Chem. 2010 Apr 8;53(7):2913-26. | |||||
| REF 34 | Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. | |||||
| REF 35 | Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols. Bioorg Med Chem. 2009 Apr 15;17(8):3207-11. | |||||
| REF 36 | 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 37 | Structure-activity relationships of C-17 cyano-substituted estratrienes as anticancer agents. J Med Chem. 2008 Mar 13;51(5):1295-308. | |||||
| REF 38 | Inhibition of carbonic anhydrase-II by sulfamate and sulfamide groups: an investigation involving direct thermodynamic binding measurements. J Med Chem. 2006 Jun 15;49(12):3496-500. | |||||
| REF 39 | Carbonic anhydrase inhibitors: inhibition of the human isozymes I, II, VA, and IX with a library of substituted difluoromethanesulfonamides. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5192-6. | |||||
| REF 40 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 41 | Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the... Eur J Med Chem. 2010 Sep;45(9):3656-61. | |||||
| REF 42 | Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors. Bioorg Med Chem. 2009 Jan 15;17(2):553-7. | |||||
| REF 43 | N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4316-20. | |||||
| REF 44 | Indanesulfonamides as carbonic anhydrase inhibitors. Toward structure-based design of selective inhibitors of the tumor-associated isozyme CA IX. J Med Chem. 2006 May 4;49(9):2743-9. | |||||
| REF 45 | Synthesis and structure-activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5429-33. | |||||
| REF 46 | Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozymes IX and XII with a library of aromatic and heteroaromatic sulfonamides. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4862-6. | |||||
| REF 47 | Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5781-6. | |||||
| REF 48 | Synthesis, characterization and antiglaucoma activity of a novel proton transfer compound and a mixed-ligand Zn(II) complex. Bioorg Med Chem. 2010 Jan 15;18(2):930-8. | |||||
| REF 49 | Carbonic anhydrase inhibitors. Characterization and inhibition studies of the most active beta-carbonic anhydrase from Mycobacterium tuberculosis, ... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6649-54. | |||||
| REF 50 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | |||||
| REF 51 | Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with su... Bioorg Med Chem. 2007 Mar 15;15(6):2298-311. | |||||
| REF 52 | Carbonic anhydrase II-induced selection of inhibitors from a dynamic combinatorial library of Schiff's bases. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6014-7. | |||||
| REF 53 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamide... J Med Chem. 2005 Mar 24;48(6):2121-5. | |||||
| REF 54 | Recent developments of carbonic anhydrase inhibitors as potential anticancer drugs. J Med Chem. 2008 Jun 12;51(11):3051-6. | |||||
| REF 55 | Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic... Bioorg Med Chem Lett. 2005 Jan 17;15(2):367-72. | |||||
| REF 56 | Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins. J Med Chem. 2010 Jan 14;53(1):335-44. | |||||
| REF 57 | Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesul... Bioorg Med Chem Lett. 2009 Sep 1;19(17):4929-32. | |||||
| REF 58 | Carbonic anhydrase inhibitors. Inhibition of the membrane-bound human and bovine isozymes IV with sulfonamides. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1149-54. | |||||
| REF 59 | Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. J Med Chem. 2006 Sep 7;49(18):5544-51. | |||||
| REF 60 | Carbonic anhydrase inhibitors: inhibition of human cytosolic isozyme II and mitochondrial isozyme V with a series of benzene sulfonamide derivatives. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5703-7. | |||||
| REF 61 | Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273. J Med Chem. 2009 Jul 9;52(13):4063-7. | |||||
| REF 62 | Carbonic anhydrase inhibitors. Inhibition of the fungal beta-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. Bioorg Med Chem Lett. 2009 May 15;19(10):2642-5. | |||||
| REF 63 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human cytosolic isozymes I and II and transmembrane isozymes IX, XII (cancer-associa... Eur J Med Chem. 2010 Jun;45(6):2396-404. | |||||
| REF 64 | In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II. Bioorg Med Chem. 2008 Oct 15;16(20):9101-5. | |||||
| REF 65 | Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-media... J Med Chem. 2005 Jul 28;48(15):4834-41. | |||||
| REF 66 | Mutation of Phe91 to Asn in human carbonic anhydrase I unexpectedly enhanced both catalytic activity and affinity for sulfonamide inhibitors. Bioorg Med Chem. 2010 Aug 1;18(15):5498-503. | |||||
| REF 67 | Carbonic anhydrase inhibitors. Aromatic/heterocyclic sulfonamides incorporating phenacetyl, pyridylacetyl and thienylacetyl tails act as potent inh... Bioorg Med Chem. 2009 Jul 15;17(14):4894-9. | |||||
| REF 68 | Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglauc... Bioorg Med Chem Lett. 2005 Feb 15;15(4):963-9. | |||||
| REF 69 | Inhibition of carbonic anhydrases with glycosyltriazole benzene sulfonamides. J Med Chem. 2008 Mar 27;51(6):1945-53. | |||||
| REF 70 | 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 71 | Carbonic anhydrase inhibitors: the first on-resin screening of a 4-sulfamoylphenylthiourea library. J Med Chem. 2004 Oct 7;47(21):5224-9. | |||||
| REF 72 | Paraoxon, 4-nitrophenyl phosphate and acetate are substrates of - but not of -, - and -carbonic anhydrases. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6208-12. | |||||
| REF 73 | A novel and one-pot synthesis of new 1-tosyl pyrrol-2-one derivatives and analysis of carbonic anhydrase inhibitory potencies. Bioorg Med Chem. 2010 Jun 15;18(12):4468-74. | |||||
| REF 74 | Carbonic anhydrase inhibitors. Synthesis of water-soluble, topically effective, intraocular pressure-lowering aromatic/heterocyclic sulfonamides co... J Med Chem. 1999 Jul 15;42(14):2641-50. | |||||
| REF 75 | Carbonic anhydrase inhibitors: thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors Bioorg Med Chem Lett. 2008 Jul 15;18(14):3938-41. | |||||
| REF 76 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides d... Bioorg Med Chem Lett. 2004 Dec 6;14(23):5775-80. | |||||
| REF 77 | Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5435-9. | |||||
| REF 78 | 7,8-disubstituted- but not 6,7-disubstituted coumarins selectively inhibit the transmembrane, tumor-associated carbonic anhydrase isoforms IX and X... Bioorg Med Chem Lett. 2010 Dec 15;20(24):7255-8. | |||||
| REF 79 | 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 80 | 2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity. J Med Chem. 2006 Dec 28;49(26):7683-96. | |||||
| REF 81 | Novel, broad-spectrum anticonvulsants containing a sulfamide group: advancement of N-((benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into huma... J Med Chem. 2009 Dec 10;52(23):7528-36. | |||||
| REF 82 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, IX, and XII with N-hydroxy... Bioorg Med Chem Lett. 2005 May 2;15(9):2353-8. | |||||
| REF 83 | Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity. Bioorg Med Chem. 2010 Jul 15;18(14):5081-9. | |||||
| REF 84 | Carbonic anhydrase inhibitors: 2-substituted-1,3,4-thiadiazole-5-sulfamides act as powerful and selective inhibitors of the mitochondrial isozymes ... Bioorg Med Chem Lett. 2008 Dec 15;18(24):6332-5. | |||||
| REF 85 | Carbonic anhydrase inhibitors. Inhibition of the cytosolic and tumor-associated carbonic anhydrase isozymes I, II, and IX with a series of 1,3,4-th... Bioorg Med Chem Lett. 2005 May 2;15(9):2347-52. | |||||
| REF 86 | Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with organic phosphates and phosphonates. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1683-6. | |||||
| REF 87 | Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mamm... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3601-5. | |||||
| REF 88 | Carbonic anhydrase inhibitors: inhibition of isozymes I, II and IV with N-hydroxysulfonamides--a novel class of intraocular pressure lowering agents. J Enzyme Inhib. 1998 Jul;13(4):267-84. | |||||
| REF 89 | A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing". J Med Chem. 2006 Nov 2;49(22):6539-48. | |||||
| REF 90 | Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule. J Med Chem. 2010 Aug 12;53(15):5511-22. | |||||
| REF 91 | Carbonic anhydrase inhibitors. Inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with ali... Bioorg Med Chem. 2009 Apr 1;17(7):2654-7. | |||||
| REF 92 | Synthesis and investigation of inhibition effect of fluorinated sulfonamide derivatives on carbonic anhydrase. Eur J Med Chem. 2010 Mar;45(3):1225-9. | |||||
| REF 93 | Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I, II, III, VII and XIII with less investigated inorganic anions. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1855-7. | |||||
| REF 94 | Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with bis-sulfamates. Bioorg Med Chem Lett. 2005 Feb 1;15(3):579-84. | |||||
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