Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T73495 | Target Info | |||
| Target Name | Glutamate receptor ionotropic kainate 1 (GRIK1) | ||||
| Synonyms |
Glutamate receptor 5; GluR5 kainate receptor; GluR5; GluR-5; GRIK1; Excitatory amino acid receptor 3; EAA3
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| Target Type | Successful Target | ||||
| Gene Name | GRIK1 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Carbonic anhydrase XII (CA-XII) | Successful Target | ||||
| UniProt ID | CAH12_HUMAN | |||||
| Gene Name | CA12 | |||||
| Synonyms |
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 3.8 nM | [1] | ||
| Co-Target Name | Carbonic anhydrase II (CA-II) | Successful Target | ||||
| UniProt ID | CAH2_HUMAN | |||||
| Gene Name | CA2 | |||||
| Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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| Representative Drug(s) | Topiramate | Drug Info | IC50 = 5 nM | [2] | ||
| Co-Target Name | Carbonic anhydrase VI (CA-VI) | Successful Target | ||||
| UniProt ID | CAH6_HUMAN | |||||
| Gene Name | CA6 | |||||
| Synonyms |
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 45 nM | [3] | ||
| Co-Target Name | Glutamate receptor AMPA 2 (GRIA2) | Successful Target | ||||
| UniProt ID | GRIA2_HUMAN | |||||
| Gene Name | GRIA2 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 2; Glutamate receptor 2; GluRK2; GluRB; GluR2; GluR-K2; GluR-B; GluR-2; GluA2; AMPAselective glutamate receptor 2; AMPA-selective glutamate receptor 2
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| Representative Drug(s) | NBQX | Drug Info | Ki = 210 nM | [4] | ||
| Co-Target Name | Carbonic anhydrase I (CA-I) | Successful Target | ||||
| UniProt ID | CAH1_HUMAN | |||||
| Gene Name | CA1 | |||||
| Synonyms |
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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| Representative Drug(s) | Topiramate | Drug Info | IC50 = 250 nM | [2] | ||
| Co-Target Name | Glutamate receptor AMPA 4 (GRIA4) | Successful Target | ||||
| UniProt ID | GRIA4_HUMAN | |||||
| Gene Name | GRIA4 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 4; GluRD; GluR4; GluA4; GRIA4; AMPAselective glutamate receptor 4
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| Representative Drug(s) | NBQX | Drug Info | Ki = 600 nM | [5] | ||
| Co-Target Name | Glutamate receptor AMPA 3 (GRIA3) | Successful Target | ||||
| UniProt ID | GRIA3_HUMAN | |||||
| Gene Name | GRIA3 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 3; GluRK3; GluRC; GluR3; GluA3; GRIA3; AMPAselective glutamate receptor 3
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| Representative Drug(s) | NBQX | Drug Info | Ki = 900 nM | [5] | ||
| Co-Target Name | Glutamate receptor ionotropic (GRI) | Clinical trial Target | ||||
| UniProt ID | GRIA1_HUMAN; GRIA2_HUMAN; GRIA3_HUMAN; GRIA4_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | NBQX | Drug Info | IC50 = 52 nM | [6] | ||
| Co-Target Name | Carbonic anhydrase IX (CA-IX) | Clinical trial Target | ||||
| UniProt ID | CAH9_HUMAN | |||||
| Gene Name | CA9 | |||||
| Synonyms |
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 58 nM | [7] | ||
| Co-Target Name | Carbonic anhydrase VII (CA-VII) | Patented-recorded Target | ||||
| UniProt ID | CAH7_HUMAN | |||||
| Gene Name | CA7 | |||||
| Synonyms |
Carbonic anhydrase 7; Carbonate dehydratase VII
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 0.87 nM | [8] | ||
| Co-Target Name | Carbonic anhydrase V (CA5) | Co-Target | ||||
| UniProt ID | CAH5A_HUMAN; CAH5B_HUMAN | |||||
| Gene Name | CA5A; CA5B | |||||
| Synonyms |
Carbonate dehydratase V; Carbonic anhydrase V; CA-V
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 25.4 nM | [9] | ||
| Co-Target Name | Carbonic anhydrase VB (CA5B) | Co-Target | ||||
| UniProt ID | CAH5B_HUMAN | |||||
| Gene Name | CA5B | |||||
| Synonyms |
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 30 nM | [10] | ||
| Co-Target Name | Carbonic anhydrase XIII (CA13) | Co-Target | ||||
| UniProt ID | CAH13_HUMAN | |||||
| Gene Name | CA13 | |||||
| Synonyms |
Carbonic anhydrase 13; Carbonate dehydratase XIII; CA-XIII
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 47 nM | [11] | ||
| Co-Target Name | Carbonic anhydrase VA (CA5A) | Co-Target | ||||
| UniProt ID | CAH5A_HUMAN | |||||
| Gene Name | CA5A | |||||
| Synonyms |
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
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| Representative Drug(s) | Topiramate | Drug Info | Ki = 63 nM | [12] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Carbonic anhydrase inhibitors: synthesis and inhibition of the human carbonic anhydrase isoforms I, II, IX and XII with benzene sulfonamides incorporating 4- and 3-nitrophthalimide moieties. Bioorg Med Chem. 2014 Mar 1;22(5):1586-95. | ||||
| REF 2 | Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the antipsychotic drug sulpiride. Bioorg Med Chem Lett. 2004 Jan 19;14(2):337-41. | ||||
| REF 3 | 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 4 | Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem. 2005 Jun 30;48(13):4200-3. | ||||
| REF 5 | Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. J Med Chem. 2002 Sep 26;45(20):4383-6. | ||||
| REF 6 | Homology modeling of the ampa receptor: A quantitative predictive tool for the design of novel antagonists. Bioorg Med Chem Lett. 1997 Jun 3;7(11):1437-42. | ||||
| REF 7 | Design, synthesis, and biological evaluation of novel carbohydrate-based sulfamates as carbonic anhydrase inhibitors. J Med Chem. 2011 Mar 10;54(5):1481-9. | ||||
| REF 8 | Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamides. Bioorg Med Chem Lett. 2005 Feb 15;15(4):971-6. | ||||
| REF 9 | Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies. Bioorg Med Chem Lett. 2005 May 2;15(9):2315-20. | ||||
| REF 10 | Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzenesulfonamide derivatives. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4624-7. | ||||
| REF 11 | The coumarin-binding site in carbonic anhydrase accommodates structurally diverse inhibitors: the antiepileptic lacosamide as an example and lead molecule for novel classes of carbonic anhydrase inhibitors. J Med Chem. 2010 Jan 28;53(2):850-4. | ||||
| REF 12 | Carbonic anhydrases as targets for medicinal chemistry. Bioorg Med Chem. 2007 Jul 1;15(13):4336-50. | ||||
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