Target Information
| Target General Information | Top | |||||
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| Target ID |
T30374
(Former ID: TTDS00023)
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| Target Name |
Gamma-aminobutyric acid uptake (GABAU)
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| Synonyms |
GABA uptake
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Epilepsy/seizure [ICD-11: 8A61-8A6Z] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Tiagabine | Drug Info | Approved | Epilepsy | [2], [3] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | Tiagabine | Drug Info | [1] | |||
| 2 | NNC 05-2045 | Drug Info | [4] | |||
| 3 | (R)-nipecotic acid | Drug Info | [5] | |||
| 4 | Cis-4-hydroxynipecotic acid | Drug Info | [6] | |||
| 5 | NNC 711 | Drug Info | [7] | |||
| 6 | THPO | Drug Info | [8] | |||
| 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 | |||||
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| Co-Targets | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. | |||||
| 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: 4818). | |||||
| REF 3 | Use of second-generation antiepileptic drugs in the pediatric population. Paediatr Drugs. 2008;10(4):217-54. | |||||
| REF 4 | GABA-level increasing and anticonvulsant effects of three different GABA uptake inhibitors. Neuropharmacology. 2000 Sep;39(12):2399-407. | |||||
| REF 5 | GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr Pharm Des. 2000 Aug;6(12):1193-209. | |||||
| REF 6 | GABA uptake inhibitors. Synthesis and effects on audiogenic seizures of ester prodrugs of nipecotic acid, guvacine and cis-4-hydroxynipecotic acid. Drug Des Deliv. 1987 Sep;2(1):9-21. | |||||
| REF 7 | Effects of NNC 711, a GABA uptake inhibitor, on pentylenetetrazol-induced seizures in developing and adult rats. Naunyn Schmiedebergs Arch Pharmacol. 1998 Sep;358(3):334-41. | |||||
| REF 8 | Anticonvulsant activity of intracerebroventricularly administered glial GABA uptake inhibitors and other GABAmimetics in chemical seizure models. Epilepsy Res. 1989 Jul-Aug;4(1):34-41. | |||||
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