| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-04-16 16:48:07 |
| Primary Accession Number |
DB00898 |
| Secondary Accession Number |
|
| Name |
Ethanol |
| Drug Type |
|
| Description |
A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in alcoholic beverages. [PubChem] |
| Synonyms |
- Absolute Alcohol
- Absolute Ethanol
- Alcohol
- Alcohol Anhydrous
- Alcohol, Dehydrated
- Alcohol, Diluted
- Alcool Ethylique
- Alcool Etilico
- Alkohol
- Alkoholu Etylowego
- Aminoethanol
- Beta-Aminoethanol
- Beta-Aminoethyl Alcohol
- Beta-Ethanolamine
- Beta-Hydroxyethylamine
- Caswell No. 426
- Dehydrated Ethanol
- Denatured Alcohol
- Denatured Ethanol
- ETA
- Etanolo
- Ethanol 200 Proof
- Ethanol Anhydrous
- Ethanol Extra Pure
- Ethyl Alcohol
- Ethyl Alcohol Anhydrous
- Ethyl Alcohol, Anhydrous
- Ethyl Alcohol, Denatured
- Ethyl Hydrate
- Ethyl Hydroxide
- Ethylol
- Ethylolamine
- HSDB 531
- Methylcarbinol
- USAF EK-1597
|
| Brand Names |
- Aethanol
- Aethylalkohol
- Alcare Hand Degermer
- Algrain
- Anhydrol
- Colamine
- Denatured Alcohol Cd-10
- Denatured Alcohol Cd-5
- Denatured Alcohol Cd-5a
- Denatured Alcohol Sd-1
- Denatured Alcohol Sd-13a
- Denatured Alcohol Sd-17
- Denatured Alcohol Sd-23a
- Denatured Alcohol Sd-28
- Denatured Alcohol Sd-30
- Denatured Alcohol Sd-39b
- Denatured Alcohol Sd-39c
- Denatured Alcohol Sd-3a
- Denatured Alcohol Sd-40m
- Envision Conditioner Pdd 9020
- Ethanol Absolute
- Ethanol Absolute Bp
- Ethanol, Silent Spirit
- Ethyl Alcohol & Water, 10%
- Ethyl Alcohol & Water, 20%
- Ethyl Alcohol & Water, 30%
- Ethyl Alcohol & Water, 40%
- Ethyl Alcohol & Water, 5%
- Ethyl Alcohol & Water, 50%
- Ethyl Alcohol & Water, 60%
- Ethyl Alcohol & Water, 70%
- Ethyl Alcohol & Water, 80%
- Ethyl Alcohol & Water, 95%
- Ethyl Alcohol & Water, 96%
- Glycinol
- Jaysol
- Jaysol S
- Methylated Spirit Mineralised
- Pyro
- Reagent Alcohol
- Spirit
- Synasol
- Tecsol
- Tecsol C
- Thanol
- Thiofaco M-50
|
| Brand Mixtures |
Not Available |
| Chemical IUPAC Name |
ethanol |
| Chemical Formula |
C2H6O |
| Chemical Structure |
 |
| CAS Registry Number |
64-17-5 |
| InChI Identifier |
InChI=1/C2H6O/c1-2-3/h3H,2H2,1H3 |
| InChI Key |
LFQSCWFLJHTTHZ-UHFFFAOYAB |
| KEGG Drug |
D00068  |
| KEGG Compound |
C00469  |
| PubChem Compound |
702  |
| PubChem Substance |
3752  |
| ChEBI ID |
16236  |
| PharmGKB ID |
PA451989  |
| HET ID |
168  |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
00724947  |
| RxList Link |
http://www.rxlist.com/cgi/generic/dhydalco.htm  |
| PDRhealth Link |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Ethanol  |
| FDA Label |
Not Available |
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
Not Available |
| Average Molecular Weight |
46.0684 |
| Monoisotopic Molecular Weight |
46.0419 |
| State |
Liquid |
| Melting Point |
-114.1 oC |
| Experimental Water Solubility |
Miscible in water
Source: PhysProp
|
| Predicted Water Solubility |
5.79e+02 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
-0.1
Source: PhysProp
|
| Predicted LogP |
-0.40
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
1.10
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| pKa/Isoelectric Point |
15.9 |
| Mass Spectrum |
Not Available
|
| MOL File |
Show | Download  |
| SDF File |
Show | Download  |
| PDB File |
Show | Download  |
| 2D Structure |
|
| 3D Structure |
|
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
CCO |
| Canonical SMILES |
CCO |
| Drug Category |
- Anti-Infective Agents, Local
- Central Nervous System Depressants
- Disinfectants
- Solvents
|
| ATC Codes |
|
| AHFS Codes |
- 84:04.92
- 92:00.00
- 92:02.00*
|
| Indication |
For therapeutic neurolysis of nerves or ganglia for the relief of intractable chronic pain in such conditions as inoperable cancer and trigeminal neuralgia (tic douloureux), in patients for whom neurosurgical procedures are contraindicated. |
| Pharmacology |
Alcohol produces injury to cells by dehydration and precipitation of the cytoplasm or protoplasm. This accounts for its bacteriocidal and antifungal action. When alcohol is injected in close proximity to nerve tissues, it produces neuritis and nerve degeneration (neurolysis). Ninety to 98% of ethanol that enters the body is completely oxidized. Ethanol is also used as a cosolvent to dissolve many insoluble drugs and to serve as a mild sedative in some medicinal formulations. |
| Mechanism of Action |
The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes. |
| Absorption |
Rapidly absorbed. |
| Toxicity |
Oral, rat LD50: 5628 mg/kg. Symptoms and effects of overdose include nausea, vomiting, CNS depression, acute respiratory failure or death and with chronic use, severe health problems, such as liver and brain damage. |
| Protein Binding |
Not Available |
| Biotransformation |
Hepatic. Metabolized by cytochrome P450 enzyme CYP2E1. |
| Half Life |
Not Available |
| Dosage Forms |
| Form |
Route |
| Aerosol |
Topical |
| Gel |
Topical |
| Liquid |
Intramuscular |
| Liquid |
Intravenous |
| Liquid |
Oral |
| Liquid |
Topical |
| Lotion |
Topical |
| Solution |
Topical |
| Solution / drops |
Oral |
| Spray |
Topical |
|
| Patient Information |
Not Available |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
Not Available
|
| Food Interactions |
Not Available
|
| Pathways |
Not Available
|
| General References |
- Barceloux DG, Bond GR, Krenzelok EP, Cooper H, Vale JA: American Academy of Clinical Toxicology practice guidelines on the treatment of methanol poisoning. J Toxicol Clin Toxicol. 2002;40(4):415-46. [PubMed
]
- Hingson R, Winter M: Epidemiology and consequences of drinking and driving. Alcohol Res Health. 2003;27(1):63-78. [PubMed
]
- Chastain G: Alcohol, neurotransmitter systems, and behavior. J Gen Psychol. 2006 Oct;133(4):329-35. [PubMed
]
- Snyder R, Kalf GF: A perspective on benzene leukemogenesis. Crit Rev Toxicol. 1994;24(3):177-209. [PubMed
]
- McDonnell G, Russell AD: Antiseptics and disinfectants: activity, action, and resistance. Clin Microbiol Rev. 1999 Jan;12(1):147-79. [PubMed
]
- Wikipedia

- RxList

|
| Organisms Affected |
|
| Phase 1 Metabolizing Enzymes |
- Cytochrome P450 2E1 (CYP2E1)
|
| Targets |
- Glycine receptor subunit alpha-1
- Glutamate [NMDA] receptor subunit 3A
- Glycine receptor subunit alpha-2
- Gamma-aminobutyric-acid receptor subunit alpha-1
|
|
Drug Target 1
[top]
|
| Target 1 ID |
482 |
| Target 1 Name |
Glycine receptor subunit alpha-1 |
| Target 1 Synonyms |
- Glycine receptor 48 kDa subunit
- Glycine receptor strychnine-binding subunit
- Glycine receptor subunit alpha-1 precursor
|
| Target 1 Gene Name |
GLRA1 |
| Target 1 Protein Sequence |
>Glycine receptor subunit alpha-1 precursor
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
|
| Target 1 Number of Residues |
464 |
| Target 1 Molecular Weight |
52625 |
| Target 1 Theoretical pI |
9.04 |
| Target 1 GO Classification |
|
Function
|
neurotransmitter receptor activity
anion channel activity
chloride channel activity
glycine-gated chloride channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity |
|
Process
|
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport |
|
Component
|
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 1 General Function |
Involved in GABA-A receptor activity |
| Target 1 Specific Function |
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing) |
| Target 1 Pathways |
Not Available
|
| Target 1 Reactions |
Not Available |
| Target 1 Pfam Domain Function |
|
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 248-274
- 281-298
- 313-336
- 429-446
|
| Target 1 Essentiality |
Non-Essential |
| Target 1 GenBank ID Protein |
31851  |
| Target 1 UniProtKB/Swiss-Prot ID |
P23415  |
| Target 1 UniProtKB/Swiss-Prot Entry Name |
GLRA1_HUMAN  |
| Target 1 PDB ID |
Not Available |
| Target 1 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 1 Gene Sequence |
>1350 bp
ATGTACAGCTTCAATACTCTTCGACTCTACCTTTCGGGAGCCATTGTATTCTTCAGCCTT
GCTGCTTCTAAGGAGGCTGAAGCTGCTCGCTCCGCAACCAAGCCTATGTCACCCTCGGAT
TTCCTGGATAAGCTAATGGGGAGAACCTCCGGATATGATGCCAGGATCAGGCCCAATTTT
AAAGGTCCCCCAGTGAACGTGAGCTGCAACATTTTCATCAACAGCTTTGGTTCCATTGCT
GAGACAACCATGGACTATAGGGTCAACATCTTCCTGCGGCAGCAATGGAACGACCCCCGC
CTGGCCTATAATGAATACCCTGACGACTCTCTGGACCTGGACCCATCCATGCTGGACTCC
ATCTGGAAACCTGACCTGTTCTTTGCCAACGAGAAGGGGGCCCACTTCCATGAGATCACC
ACAGACAACAAATTGCTAAGGATCTCCCGGAATGGGAATGTCCTCTACAGCATCAGAATC
ACCCTGACACTGGCCTGCCCCATGGACTTGAAGAATTTCCCCATGGATGTCCAGACATGT
ATCATGCAACTGGAAAGCTTTGGATATACGATGAATGACCTCATCTTTGAGTGGCAGGAA
CAGGGAGCCGTGCAGGTAGCAGATGGACTAACTCTGCCCCAGTTTATCTTGAAGGAAGAG
AAGGACTTGAGATACTGCACCAAGCACTACAACACAGGTAAATTCACCTGCATTGAGGCC
CGGTTCCACCTGGAGCGGCAGATGGGTTACTACCTGATTCAGATGTATATTCCCAGCCTG
CTCATTGTCATCCTCTCATGGATCTCCTTCTGGATCAACATGGATGCTGCACCTGCTCGT
GTGGGCCTAGGCATCACCACTGTGCTCACCATGACCACCCAGAGCTCCGGCTCTCGAGCA
TCTCTGCCCAAGGTGTCCTATGTGAAAGCCATTGACATTTGGATGGCAGTTTGCCTGCTC
TTTGTGTTCTCAGCCCTATTAGAATATGCTGCCGTTAACTTTGTGTCTCGGCAACATAAG
GAGCTGCTCCGATTCAGGAGGAAGCGGAGACATCACAAGGAGGATGAAGCTGGAGAAGGC
CGCTTTAACTTCTCTGCCTATGGGATGGGCCCAGCCTGTCTACAGGCCAAGGATGGCATC
TCAGTCAAGGGCGCCAACAACAGTAACACCACCAACCCCCCTCCTGCACCATCTAAGTCC
CCAGAGGAGATGCGAAAACTCTTCATCCAGAGGGCCAAGAAGATCGACAAAATATCCCGC
ATTGGCTTCCCCATGGCCTTCCTCATTTTCAACATGTTCTACTGGATCATCTACAAGATT
GTCCGTAGAGAGGACGTCCACAACCAGTGA
|
| Target 1 GenBank Gene ID |
|
| Target 1 GeneCard ID |
GLRA1  |
| Target 1 GenAtlas ID |
GLRA1  |
| Target 1 HGNC ID |
HGNC:4326  |
| Target 1 Chromosome Location |
5 |
| Target 1 Locus |
5q32 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 General References |
- Vergouwe MN, Tijssen MA, Peters AC, Wielaard R, Frants RR: Hyperekplexia phenotype due to compound heterozygosity for GLRA1 gene mutations. Ann Neurol. 1999 Oct;46(4):634-8. [PubMed
]
- Grenningloh G, Schmieden V, Schofield PR, Seeburg PH, Siddique T, Mohandas TK, Becker CM, Betz H: Alpha subunit variants of the human glycine receptor: primary structures, functional expression and chromosomal localization of the corresponding genes. EMBO J. 1990 Mar;9(3):771-6. [PubMed
]
- Shiang R, Ryan SG, Zhu YZ, Fielder TJ, Allen RJ, Fryer A, Yamashita S, O'Connell P, Wasmuth JJ: Mutational analysis of familial and sporadic hyperekplexia. Ann Neurol. 1995 Jul;38(1):85-91. [PubMed
]
- Rees MI, Andrew M, Jawad S, Owen MJ: Evidence for recessive as well as dominant forms of startle disease (hyperekplexia) caused by mutations in the alpha 1 subunit of the inhibitory glycine receptor. Hum Mol Genet. 1994 Dec;3(12):2175-9. [PubMed
]
- Langosch D, Laube B, Rundstrom N, Schmieden V, Bormann J, Betz H: Decreased agonist affinity and chloride conductance of mutant glycine receptors associated with human hereditary hyperekplexia. EMBO J. 1994 Sep 15;13(18):4223-8. [PubMed
]
- Schorderet DF, Pescia G, Bernasconi A, Regli F: An additional family with Startle disease and a G1192A mutation at the alpha 1 subunit of the inhibitory glycine receptor gene. Hum Mol Genet. 1994 Jul;3(7):1201. [PubMed
]
- Shiang R, Ryan SG, Zhu YZ, Hahn AF, O'Connell P, Wasmuth JJ: Mutations in the alpha 1 subunit of the inhibitory glycine receptor cause the dominant neurologic disorder, hyperekplexia. Nat Genet. 1993 Dec;5(4):351-8. [PubMed
]
- Milani N, Dalpra L, del Prete A, Zanini R, Larizza L: A novel mutation (Gln266-->His) in the alpha 1 subunit of the inhibitory glycine-receptor gene (GLRA1) in hereditary hyperekplexia. Am J Hum Genet. 1996 Feb;58(2):420-2. [PubMed
]
- Elmslie FV, Hutchings SM, Spencer V, Curtis A, Covanis T, Gardiner RM, Rees M: Analysis of GLRA1 in hereditary and sporadic hyperekplexia: a novel mutation in a family cosegregating for hyperekplexia and spastic paraparesis. J Med Genet. 1996 May;33(5):435-6. [PubMed
]
- Seri M, Bolino A, Galietta LJ, Lerone M, Silengo M, Romeo G: Startle disease in an Italian family by mutation (K276E): The alpha-subunit of the inhibiting glycine receptor. Hum Mutat. 1997;9(2):185-7. [PubMed
]
- 9920650 Saul B, Kuner T, Sobetzko D, Brune W, Hanefeld F, Meinck HM, Becker CM: Novel GLRA1 missense mutation (P250T) in dominant hyperekplexia defines an intracellular determinant of glycine receptor channel gating. J Neurosci. 1999 Feb 1;19(3):869-77.
|
| Target 1 Drug References |
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|
|
Drug Target 2
[top]
|
| Target 2 ID |
706 |
| Target 2 Name |
Glutamate [NMDA] receptor subunit 3A |
| Target 2 Synonyms |
- Glutamate receptor subunit 3A precursor
- N-methyl-D-aspartate receptor subtype NR3A
- NMDAR-L
|
| Target 2 Gene Name |
GRIN3A |
| Target 2 Protein Sequence |
>Glutamate [NMDA] receptor subunit 3A precursor
MRRLSLWWLLSRVCLLLPPPCALVLAGVPSSSSHPQPCQILKRIGHAVRVGAVHLQPWTT
APRAASRAPDDSRAGAQRDEPEPGTRRSPAPSPGARWLGSTLHGRGPPGSRKPGEGARAE
ALWPRDALLFAVDNLNRVEGLLPYNLSLEVVMAIEAGLGDLPLLPFSSPSSPWSSDPFSF
LQSVCHTVVVQGVSALLAFPQSQGEMMELDLVSLVLHIPVISIVRHEFPRESQNPLHLQL
SLENSLSSDADVTVSILTMNNWYNFSLLLCQEDWNITDFLLLTQNNSKFHLGSIINITAN
LPSTQDLLSFLQIQLESIKNSTPTVVMFGCDMESIRRIFEITTQFGVMPPELRWVLGDSQ
NMEELRTEGLPLGLIAHGKTTQSVFEHYVQDAMELVARAVATATMIQPELALIPSTMNCM
EVETTNLTSGQYLSRFLANTTFRGLSGSIRVKGSTIVSSENNFFIWNLQHDPMGKPMWTR
LGSWQGRKIVMDYGIWPEQAQRHKTHFQHPSKLHLRVVTLIEHPFVFTREVDDEGLCPAG
QLCLDPMTNDSSTLDSLFSSLHSSNDTVPIKFKKCCYGYCIDLLEKIAEDMNFDFDLYIV
GDGKYGAWKNGHWTGLVGDLLRGTAHMAVTSFSINTARSQVIDFTSPFFSTSLGILVRTR
DTAAPIGAFMWPLHWTMWLGIFVALHITAVFLTLYEWKSPFGLTPKGRNRSKVFSFSSAL
NICYALLFGRTVAIKPPKCWTGRFLMNLWAIFCMFCLSTYTANLAAVMVGEKIYEELSGI
HDPKLHHPSQGFRFGTVRESSAEDYVRQSFPEMHEYMRRYNVPATPDGVEYLKNNPEKLD
AFIMDKALLDYEVSIDADCKLLTVGKPFAIEGYGIGLPPNSPLTANISELISQYKSHGFM
DMLHDKWYRVVPCGKRSFAVTETLQMGIKHFSGLFVLLCIGFGLSILTTIGEHIVYRLLL
PRIKNKSKLQYWLHTSQRLHRAINTSFIEEKQQHFKTKRVEKRSNVGPRQLTVWNTSNLS
HDNRRKYIFSDEEGQNQLGIRIHQDIPLPPRRRELPALRTTNGKADSLNVSRNSVMQELS
ELEKQIQVIRQELQLAVSRKTELEEYQRTSRTCES
|
| Target 2 Number of Residues |
1133 |
| Target 2 Molecular Weight |
125597 |
| Target 2 Theoretical pI |
7.81 |
| Target 2 GO Classification |
|
Function
|
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity |
|
Process
|
physiological process
cellular physiological process
transport
ion transport |
|
Component
|
cell
membrane |
|
| Target 2 General Function |
Involved in ionotropic glutamate receptor activity |
| Target 2 Specific Function |
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism |
| Target 2 Pathways |
Not Available
|
| Target 2 Reactions |
Not Available |
| Target 2 Pfam Domain Function |
|
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
|
| Target 2 Essentiality |
Non-Essential |
| Target 2 GenBank ID Protein |
20372905  |
| Target 2 UniProtKB/Swiss-Prot ID |
Q8TCU5  |
| Target 2 UniProtKB/Swiss-Prot Entry Name |
NMD3A_HUMAN  |
| Target 2 PDB ID |
Not Available |
| Target 2 Cellular Location |
- Cell membrane
- multi-pass membrane protein. Enriched in post-synaptic plasma membrane and post-synap
|
| Target 2 Gene Sequence |
>3348 bp
ATGAGGAGACTGAGTTTGTGGTGGCTGCTGAGCAGGGTCTGTCTGCTGTTGCCGCCGCCC
TGCGCACTGGTGCTGGCCGGGGTGCCCAGCTCCTCCTCGCACCCGCAGCCCTGCCAGATC
CTCAAGCGCATCGGGCACGCGGTGAGGGTGGGCGCGGTGCACTTGCAGCCCTGGACCACC
GCCCCCCGCGCGGCCAGCCGCGCTCCGGACGACAGCCGAGCAGGAGCCCAGAGGGATGAG
CCGGAGCCAGGGACTAGGCGGTCCCCGGCGCCCTCGCCGGGCGCACGCTGGTTGGGGAGC
ACCCTGCATGGCCGGGGGCCGCCGGGCTCCCGTAAGCCCGGGGAGGGCGCCAGGGCGGAG
GCCCTGTGGCCACGGGACGCCCTCCTATTTGCCGTGGACAACCTGAACCGCGTGGAAGGG
CTGCTACCCTACAACCTGTCTTTGGAAGTAGTGATGGCCATCGAGGCAGGCCTGGGCGAT
CTGCCACTTTTGCCCTTCTCCTCCCCTAGTTCGCCATGGAGCAGTGACCCTTTCTCCTTC
CTGCAAAGTGTGTGCCATACCGTGGTGGTGCAAGGGGTGTCGGCGCTGCTCGCCTTCCCC
CAGAGCCAGGGCGAAATGATGGAGCTCGACTTGGTCAGCTTAGTCCTGCACATTCCAGTG
ATCAGCATCGTGCGCCACGAGTTTCCGCGGGAGAGTCAGAATCCCCTTCACCTACAACTG
AGTTTAGAAAATTCATTAAGTTCTGATGCTGATGTCACTGTCTCAATCCTGACCATGAAC
AACTGGTACAATTTTAGCTTGTTGCTGTGCCAGGAAGACTGGAACATCACCGACTTCCTC
CTCCTTACCCAGAATAATTCCAAGTTCCACCTTGGTTCTATCATCAACATCACCGCTAAC
CTCCCCTCCACCCAGGACCTCTTGAGCTTCCTACAGATCCAGCTTGAGAGTATTAAGAAC
AGCACACCCACAGTGGTGATGTTTGGCTGCGACATGGAAAGTATCCGGCGGATTTTCGAA
ATTACAACCCAGTTTGGGGTCATGCCCCCTGAACTTCGTTGGGTGCTGGGAGATTCCCAG
AATATGGAGGAACTGAGGACAGAGGGTCTGCCCTTAGGACTCATTGCTCATGGAAAAACA
ACACAGTCTGTCTTTGAGCACTACGTACAAGATGCTATGGAGCTGGTCGCAAGAGCTGTA
GCCACAGCCACCATGATCCAACCAGAACTTGCTCTCATTCCCAGCACGATGAACTGCATG
GAGGTGGAAACTACAAATCTCACTTCAGGACAATATTTATCAAGGTTTCTAGCCAATACC
ACTTTCAGAGGCCTCAGTGGTTCCATCAGAGTAAAAGGTTCCACCATCGTCAGCTCAGAA
AACAACTTTTTCATCTGGAATCTTCAACATGACCCCATGGGAAAGCCAATGTGGACCCGC
TTGGGCAGCTGGCAGGGGAGAAAGATTGTCATGGACTATGGAATATGGCCAGAGCAGGCC
CAGAGACACAAAACCCACTTCCAACATCCAAGTAAGCTACACTTGAGAGTGGTTACCCTG
ATTGAGCATCCTTTTGTCTTCACAAGGGAGGTAGATGATGAAGGCTTGTGCCCTGCTGGC
CAACTCTGTCTAGACCCCATGACTAATGACTCTTCCACACTGGACAGCCTTTTTAGCAGC
CTCCATAGCAGTAATGATACAGTGCCCATTAAATTCAAGAAGTGCTGCTATGGATATTGC
ATTGATCTGCTGGAAAAGATAGCAGAAGACATGAACTTTGACTTCGACCTCTATATTGTA
GGGGATGGAAAGTATGGAGCCTGGAAAAATGGGCACTGGACTGGGCTAGTGGGTGATCTC
CTGAGAGGGACTGCCCACATGGCAGTCACTTCCTTTAGCATCAATACTGCACGGAGCCAG
GTGATAGATTTCACCAGCCCTTTCTTCTCCACCAGCTTGGGCATCTTAGTGAGGACCCGA
GATACAGCAGCTCCCATTGGAGCCTTCATGTGGCCACTCCACTGGACAATGTGGCTGGGG
ATTTTTGTGGCTCTGCACATCACTGCCGTCTTCCTCACTCTGTATGAATGGAAGAGTCCA
TTTGGTTTGACTCCCAAGGGGCGAAATAGAAGTAAAGTCTTCTCCTTTTCTTCAGCCTTG
AACATCTGTTATGCCCTCTTGTTTGGCAGAACAGTGGCCATCAAACCTCCAAAATGTTGG
ACTGGAAGGTTTCTAATGAACCTTTGGGCCATTTTCTGTATGTTTTGCCTTTCCACATAC
ACGGCAAACTTGGCTGCTGTCATGGTAGGTGAGAAGATCTATGAAGAGCTTTCTGGAATA
CATGACCCCAAGTTACATCATCCTTCCCAAGGATTCCGCTTTGGAACTGTCCGAGAAAGC
AGTGCTGAAGATTATGTGAGACAAAGTTTCCCAGAGATGCATGAATATATGAGAAGGTAC
AATGTTCCAGCCACCCCTGATGGAGTGGAGTATCTGAAGAACAATCCAGAGAAACTAGAC
GCCTTCATCATGGACAAAGCCCTTCTGGATTATGAAGTGTCAATAGATGCTGACTGCAAA
CTTCTCACTGTGGGGAAGCCATTTGCCATAGAAGGATACGGCATTGGCCTCCCACCCAAC
TCTCCATTGACCGCCAACATATCCGAGCTAATCAGTCAATACAAGTCACATGGGTTTATG
GATATGCTCCATGACAAGTGGTACAGGGTGGTTCCCTGTGGCAAGAGAAGTTTTGCTGTC
ACGGAGACTTTGCAAATGGGCATCAAACACTTCTCTGGGCTCTTTGTGCTGCTGTGCATT
GGATTTGGTCTGTCCATTTTGACCACCATTGGTGAGCACATAGTATACAGGCTGCTGCTA
CCACGAATCAAAAACAAATCCAAGCTGCAATACTGGCTCCACACCAGCCAGAGATTACAC
AGAGCAATAAATACATCATTTATAGAGGAAAAGCAGCAGCATTTCAAGACCAAACGTGTG
GAAAAGAGGTCTAATGTGGGACCCCGTCAGCTTACCGTATGGAATACTTCCAATCTGAGT
CATGACAACCGACGGAAATACATCTTTAGTGATGAGGAAGGACAAAACCAGCTGGGCATC
CGGATCCACCAGGACATCCCCCTCCCTCCAAGGAGAAGAGAGCTCCCTGCCTTGCGGACC
ACCAATGGGAAAGCAGACTCCCTAAATGTATCTCGGAACTCAGTGATGCAGGAACTCTCA
GAGCTCGAGAAGCAGATTCAGGTGATCCGTCAGGAGCTGCAGCTGGCTGTGAGCAGGAAA
ACGGAGCTGGAGGAGTATCAAAGGACAAGTCGGACTTGTGAGTCCTAG
|
| Target 2 GenBank Gene ID |
|
| Target 2 GeneCard ID |
GRIN3A  |
| Target 2 GenAtlas ID |
GRIN3A  |
| Target 2 HGNC ID |
HGNC:16767  |
| Target 2 Chromosome Location |
9 |
| Target 2 Locus |
9q31.1 |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 General References |
- Andersson O, Stenqvist A, Attersand A, von Euler G: Nucleotide sequence, genomic organization, and chromosomal localization of genes encoding the human NMDA receptor subunits NR3A and NR3B. Genomics. 2001 Dec;78(3):178-84. [PubMed
]
- Nagase T, Kikuno R, Ohara O: Prediction of the coding sequences of unidentified human genes. XXII. The complete sequences of 50 new cDNA clones which code for large proteins. DNA Res. 2001 Dec 31;8(6):319-27. [PubMed
]
- Eriksson M, Nilsson A, Froelich-Fabre S, Akesson E, Dunker J, Seiger A, Folkesson R, Benedikz E, Sundstrom E: Cloning and expression of the human N-methyl-D-aspartate receptor subunit NR3A. Neurosci Lett. 2002 Mar 22;321(3):177-81. [PubMed
]
|
| Target 2 Drug References |
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|
|
Drug Target 3
[top]
|
| Target 3 ID |
820 |
| Target 3 Name |
Glycine receptor subunit alpha-2 |
| Target 3 Synonyms |
- Glycine receptor subunit alpha-2 precursor
|
| Target 3 Gene Name |
GLRA2 |
| Target 3 Protein Sequence |
>Glycine receptor subunit alpha-2 precursor
MNRQLVNILTALFAFFLETNHFRTAFCKDHDSRSGKQPSQTLSPSDFLDKLMGRTSGYDA
RIRPNFKGPPVNVTCNIFINSFGSVTETTMDYRVNIFLRQQWNDSRLAYSEYPDDSLDLD
PSMLDSIWKPDLFFANEKGANFHDVTTDNKLLRISKNGKVLYSIRLTLTLSCPMDLKNFP
MDVQTCTMQLESFGYTMNDLIFEWLSDGPVQVAEGLTLPQFILKEEKELGYCTKHYNTGK
FTCIEVKFHLERQMGYYLIQMYIPSLLIVILSWVSFWINMDAAPARVALGITTVLTMTTQ
SSGSRASLPKVSYVKAIDIWMAVCLLFVFAALLEYAAVNFVSRQHKEFLRLRRRQKRQNK
EEDVTRESRFNFSGYGMGHCLQVKDGTAVKATPANPLPQPPKDGDAIKKKFVDRAKRIDT
ISRAAFPLAFLIFNIFYWITYKIIRHEDVHKK
|
| Target 3 Number of Residues |
459 |
| Target 3 Molecular Weight |
52003 |
| Target 3 Theoretical pI |
9.20 |
| Target 3 GO Classification |
|
Function
|
neurotransmitter receptor activity
anion channel activity
chloride channel activity
glycine-gated chloride channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity |
|
Process
|
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport |
|
Component
|
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 3 General Function |
Involved in GABA-A receptor activity |
| Target 3 Specific Function |
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing) |
| Target 3 Pathways |
Not Available
|
| Target 3 Reactions |
Not Available |
| Target 3 Pfam Domain Function |
|
| Target 3 Signals |
|
| Target 3 Transmembrane Regions |
- 254-280
- 287-304
- 319-342
- 424-441
|
| Target 3 Essentiality |
Non-Essential |
| Target 3 GenBank ID Protein |
31849  |
| Target 3 UniProtKB/Swiss-Prot ID |
P23416  |
| Target 3 UniProtKB/Swiss-Prot Entry Name |
GLRA2_HUMAN  |
| Target 3 PDB ID |
Not Available |
| Target 3 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 3 Gene Sequence |
>1359 bp
ATGAACCGGCAGCTAGTGAACATTTTGACAGCCTTGTTTGCATTTTTCTTAGAGACAAAC
CACTTCAGGACGGCTTTCTGCAAAGACCATGACTCCAGGTCTGGAAAACAACCTTCACAG
ACCCTATCTCCTTCAGATTTCTTGGACAAGTTAATGGGAAGGACATCAGGATATGATGCA
AGAATCAGGCCAAATTTTAAAGGTCCTCCAGTAAACGTTACTTGCAATATTTTTATCAAC
AGTTTTGGATCAGTCACAGAAACGACCATGGACTACCGAGTGAATATTTTTCTGAGACAA
CAGTGGAATGATTCACGGCTGGCGTACAGTGAGTACCCAGATGACTCCCTGGACTTGGAC
CCATCCATGCTAGACTCCATTTGGAAACCAGATTTGTTCTTTGCCAATGAGAAGGGTGCC
AACTTCCACGATGTCACCACTGACAACAAATTGCTACGGATTTCGAAAAATGGCAAAGTG
CTCTACAGTATCAGACTCACCTTGACCTTATCCTGTCCCATGGACTTGAAGAACTTTCCG
ATGGATGTCCAGACCTGTACAATGCAGCTGGAGAGTTTTGGGTACACGATGAATGACCTG
ATATTTGAGTGGTTAAGTGATGGTCCAGTGCAAGTTGCTGAAGGATTGACCCTGCCCCAG
TTTATTTTGAAAGAAGAGAAGGAACTTGGCTACTGTACAAAGCACTACAACACTGGAAAG
TTTACCTGCATTGAGGTCAAGTTTCACCTGGAACGCCAAATGGGATATTATTTGATCCAG
ATGTACATCCCAAGCCTGCTTATAGTAATTTTGTCCTGGGTTTCCTTTTGGATAAATATG
GATGCAGCCCCTGCCAGGGTCGCACTGGGCATCACCACAGTCTTAACGATGACCACCCAG
AGTTCAGGCTCCAGGGCATCTCTGCCAAAGGTCTCCTATGTAAAAGCGATTGACATCTGG
ATGGCGGTGTGCCTTCTGTTTGTGTTTGCTGCCTTACTGGAATACGCAGCGGTGAACTTC
GTCTCCAGGCAACACAAGGAGTTCCTGCGCCTCCGAAGAAGACAGAAGAGGCAGAATAAG
GAAGAAGACGTTACTCGTGAAAGTCGTTTTAATTTTAGCGGTTATGGGATGGGTCACTGC
CTCCAAGTGAAAGATGGAACAGCTGTCAAGGCCACACCTGCCAACCCACTCCCACAACCG
CCAAAAGATGGAGATGCTATCAAGAAGAAGTTTGTGGACCGGGCAAAAAGGATTGACACG
ATATCTCGAGCTGCCTTCCCATTGGCCTTCCTCATTTTCAACATCTTTTACTGGATCACA
TACAAGATCATTCGGCATGAAGATGTCCACAAGAAATAG
|
| Target 3 GenBank Gene ID |
|
| Target 3 GeneCard ID |
GLRA2  |
| Target 3 GenAtlas ID |
GLRA2  |
| Target 3 HGNC ID |
HGNC:4327  |
| Target 3 Chromosome Location |
X |
| Target 3 Locus |
Xp22.1-p21.3 |
| Target 3 SNPs |
SNPJam Report  |
| Target 3 General References |
- Grenningloh G, Schmieden V, Schofield PR, Seeburg PH, Siddique T, Mohandas TK, Becker CM, Betz H: Alpha subunit variants of the human glycine receptor: primary structures, functional expression and chromosomal localization of the corresponding genes. EMBO J. 1990 Mar;9(3):771-6. [PubMed
]
- Monani U, Burghes AH: Structure of the human alpha 2 subunit gene of the glycine receptor--use of vectorette and Alu-exon PCR. Genome Res. 1996 Dec;6(12):1200-6. [PubMed
]
- Cummings CJ, Dahle EJ, Zoghbi HY: Analysis of the genomic structure of the human glycine receptor alpha2 subunit gene and exclusion of this gene as a candidate for Rett syndrome. Am J Med Genet. 1998 Jun 30;78(2):176-8. [PubMed
]
|
| Target 3 Drug References |
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|
|
Drug Target 4
[top]
|
| Target 4 ID |
872 |
| Target 4 Name |
Gamma-aminobutyric-acid receptor subunit alpha-1 |
| Target 4 Synonyms |
- Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
|
| Target 4 Gene Name |
GABRA1 |
| Target 4 Protein Sequence |
>Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
|
| Target 4 Number of Residues |
463 |
| Target 4 Molecular Weight |
51802 |
| Target 4 Theoretical pI |
9.61 |
| Target 4 GO Classification |
|
Function
|
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity |
|
Process
|
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport |
|
Component
|
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 4 General Function |
Involved in GABA-A receptor activity |
| Target 4 Specific Function |
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel |
| Target 4 Pathways |
Not Available
|
| Target 4 Reactions |
Not Available |
| Target 4 Pfam Domain Function |
|
| Target 4 Signals |
|
| Target 4 Transmembrane Regions |
- 252-273
- 279-300
- 313-334
- 422-443
|
| Target 4 Essentiality |
Non-Essential |
| Target 4 GenBank ID Protein |
31631  |
| Target 4 UniProtKB/Swiss-Prot ID |
P14867  |
| Target 4 UniProtKB/Swiss-Prot Entry Name |
GBRA1_HUMAN  |
| Target 4 PDB ID |
Not Available |
| Target 4 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 4 Gene Sequence |
>1371 bp
ATGAGGAAAAGTCCAGGTCTGTCTGACTGTCTTTGGGCCTGGATCCTCCTTCTGAGCACA
CTGACTGGAAGAAGCTATGGACAGCCGTCATTACAAGATGAACTTAAAGACAATACCACT
GTCTTCACCAGGATTTTGGACAGACTCCTAGATGGTTATGACAATCGCCTGAGACCAGGA
TTGGGAGAGCGTGTAACCGAAGTGAAGACTGATATCTTCGTCACCAGTTTCGGACCCGTT
TCAGACCATGATATGGAATATACAATAGATGTATTTTTCCGTCAAAGCTGGAAGGATGAA
AGGTTAAAATTTAAAGGACCTATGACAGTCCTCCGGTTAAATAACCTAATGGCAAGTAAA
ATCTGGACTCCGGACACATTTTTCCACAATGGAAAGAAGTCAGTGGCCCACAACATGACC
ATGCCCAACAAACTCCTGCGGATCACAGAGGATGGCACCTTGCTGTACACCATGAGGCTG
ACAGTGAGAGCTGAATGTCCGATGCATTTGGAGGACTTCCCTATGGATGCCCATGCTTGC
CCACTAAAATTTGGAAGTTATGCTTATACAAGAGCAGAAGTTGTTTATGAATGGACCAGA
GAGCCAGCACGCTCAGTGGTTGTAGCAGAAGATGGATCACGTCTAAACCAGTATGACCTT
CTTGGACAAACAGTAGACTCTGGAATTGTCCAGTCAAGTACAGGAGAATATGTTGTTATG
ACCACTCATTTCCACTTGAAGAGAAAGATTGGCTACTTTGTTATTCAAACATACCTGCCA
TGCATAATGACAGTGATTCTCTCACAAGTCTCCTTCTGGCTCAACAGAGAGTCTGTACCA
GCAAGAACTGTCTTTGGAGTAACAACTGTGCTCACCATGACAACATTGAGCATCAGTGCC
AGAAACTCCCTCCCTAAGGTGGCTTATGCAACAGCTATGGATTGGTTTATTGCCGTGTGC
TATGCCTTTGTGTTCTCAGCTCTGATTGAGTTTGCCACAGTAAACTATTTCACTAAGAGA
GGTTATGCATGGGATGGCAAAAGTGTGGTTCCAGAAAAGCCAAAGAAAGTAAAGGATCCT
CTTATTAAGAAAAACAACACTTACGCTCCAACAGCAACCAGCTACACCCCTAATTTGGCC
AGGGGCGACCCGGGCTTAGCCACCATTGCTAAAAGTGCAACCATAGAACCTAAAGAGGTC
AAGCCCGAAACAAAACCACCAGAACCCAAGAAAACCTTTAACAGTGTCAGCAAAATTGAC
CGACTGTCAAGAATAGCCTTCCCGCTGCTATTTGGAATCTTTAACTTAGTCTACTGGGCT
ACGTATTTAAACAGAGAGCCTCAGCTAAAAGCCCCCACACCACATCAATAG
|
| Target 4 GenBank Gene ID |
|
| Target 4 GeneCard ID |
GABRA1  |
| Target 4 GenAtlas ID |
GABRA1  |
| Target 4 HGNC ID |
HGNC:4075  |
| Target 4 Chromosome Location |
5 |
| Target 4 Locus |
5q34-q35 |
| Target 4 SNPs |
SNPJam Report  |
| Target 4 General References |
- Cossette P, Liu L, Brisebois K, Dong H, Lortie A, Vanasse M, Saint-Hilaire JM, Carmant L, Verner A, Lu WY, Wang YT, Rouleau GA: Mutation of GABRA1 in an autosomal dominant form of juvenile myoclonic epilepsy. Nat Genet. 2002 Jun;31(2):184-9. Epub 2002 May 6. [PubMed
]
- Schofield PR, Pritchett DB, Sontheimer H, Kettenmann H, Seeburg PH: Sequence and expression of human GABAA receptor alpha 1 and beta 1 subunits. FEBS Lett. 1989 Feb 27;244(2):361-4. [PubMed
]
- Garrett KM, Duman RS, Saito N, Blume AJ, Vitek MP, Tallman JF: Isolation of a cDNA clone for the alpha subunit of the human GABA-A receptor. Biochem Biophys Res Commun. 1988 Oct 31;156(2):1039-45. [PubMed
]
|
| Target 4 Drug References |
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed
]
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed
]
|