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Showing drug card for Lorazepam (DB00186)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:04:55
Primary Accession Number DB00186
Secondary Accession Number
  • APRD00116
Name Lorazepam
Drug Type
  • Approved
  • Small Molecule
Description A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. [PubChem]
Synonyms
  1. (+/-)-Lorazepam
  2. L-Lorazepam Acetate
  3. O-Chlorooxazepam
  4. O-Chloroxazepam
Brand Names
  1. Almazine
  2. Alzapam
  3. Anxiedin
  4. Aplacassee
  5. Ativan
  6. Bonatranquan
  7. Delormetazepam
  8. Emotival
  9. Idalprem
  10. Lorabenz
  11. Lorax
  12. Loraz
  13. Lorazepam Intensol
  14. Lorsilan
  15. Pro Dorm
  16. Psicopax
  17. Punktyl
  18. Quait
  19. Securit
  20. Sedatival
  21. Sedazin
  22. Somagerol
  23. Tavor
  24. Temesta
  25. Wypax
Brand Mixtures Not Available
Chemical IUPAC Name 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one
Chemical Formula C15H10Cl2N2O2
Chemical Structure Structure
CAS Registry Number 846-49-1
InChI Identifier InChI=1/C15H10Cl2N2O2/c16-8-5-6-12-10(7-8)13(19-15(21)14(20)18-12)9-3-1-2-4-11(9)17/h1-7,15,21H,(H,18,20)/f/h18H
InChI Key DIWRORZWFLOCLC-GPQMBLKYCT
KEGG Drug D00365 Link Image
KEGG Compound Not Available
PubChem Compound 3958 Link Image
PubChem Substance 156663 Link Image
ChEBI ID Not Available
PharmGKB ID Not Available
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02243278 Link Image
RxList Link http://www.rxlist.com/cgi/generic/loraz.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Lorazepam Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Childress, Gluckman, J. Pharm. Sci. 53, 577 (1964)
Average Molecular Weight 321.1580
Monoisotopic Molecular Weight 320.0119
State Solid
Melting Point 166-168oC
Experimental Water Solubility 0.08 mg/mL Source: PhysProp
Predicted Water Solubility 1.76e-02 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3.5 Source: PhysProp
Predicted LogP 2.98 Calculated using ALOGPS
Experimental LogS -3.6 [ADME Research, USCD]
Predicted LogS -4.26 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 13
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES O[C@@H]1N=C(C2=CC=CC=C2Cl)C2=C(NC1=O)C=CC(Cl)=C2
Canonical SMILES OC1N=C(C2=CC=CC=C2Cl)C2=C(NC1=O)C=CC(Cl)=C2
Drug Category
  • Anti-anxiety Agents
  • Anticonvulsants
  • Antiemetics
  • Benzodiazepines
  • GABA Modulators
  • Hypnotics and Sedatives
ATC Codes
AHFS Codes
  • 28:24.08
Indication For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms
Pharmacology Lorazepam, a benzodiazepine not transformed to active metabolites, is used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia.
Mechanism of Action Lorazepam binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
Absorption Readily absorbed with an absolute bioavailability of 90%.
Toxicity Somnolence, confusion, and coma, LD50=3178mg/kg (orally in mice).
Protein Binding 85%
Biotransformation Hepatic
Half Life 12 hours
Dosage Forms
Form Route
Liquid Intravenous
Tablet Oral
Tablet Sublingual
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Clozapine Increased risk of toxicity
Ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Kava Kava increases the effect of the benzodiazepine
Mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Take with food.
Pathways Not Available
General References
  1. Heisterkamp DV, Cohen PJ: The effect of intravenous premedication with lorazepam (ativan), pentobarbitone or diazepam on recall. Br J Anaesth. 1975 Jan;47(1):79-81. [PubMed Link Image]
  2. Milligan DW, Howard MR, Judd A: Premedication with lorazepam before bone marrow biopsy. J Clin Pathol. 1987 Jun;40(6):696-8. [PubMed Link Image]
  3. Lader M: Short-term versus long-term benzodiazepine therapy. Curr Med Res Opin. 1984;8 Suppl 4:120-6. [PubMed Link Image]
  4. Kemper N, Poser W, Poser S: [Benzodiazepine dependence: addiction potential of the benzodiazepines is greater than previously assumed (author's transl)] Dtsch Med Wochenschr. 1980 Dec 5;105(49):1707-12. [PubMed Link Image]
  5. Maltais F, Laberge F, Laviolette M: A randomized, double-blind, placebo-controlled study of lorazepam as premedication for bronchoscopy. Chest. 1996 May;109(5):1195-8. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
  8. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. UDP-glucuronic acid
  2. Monoamine oxidase type A (MAO-A)
Targets
  1. Gamma-aminobutyric-acid receptor subunit alpha-2
  2. Gamma-aminobutyric-acid receptor subunit alpha-5
  3. Gamma-aminobutyric-acid receptor subunit alpha-4
  4. Gamma-aminobutyric-acid receptor subunit alpha-3
  5. Translocator protein
  6. Gamma-aminobutyric-acid receptor subunit alpha-6
  7. Gamma-aminobutyric-acid receptor subunit alpha-1
  8. Gamma-aminobutyric-acid receptor subunit beta-1
  9. Gamma-aminobutyric-acid receptor subunit beta-3
  10. Gamma-aminobutyric-acid receptor subunit beta-2
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name UDP-glucuronic acid
Enzyme 1 Gene Name SLC35D1
Enzyme 1 SwissProt ID Q9NTN3 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|Q9NTN3|S35D1_HUMAN UDP-glucuronic acid
MAEVHRRQHARVKGEAPAKSSTLRDEEELGMASAETLTVFLKLLAAGFYGVSSFLIVVVN
KSVLTNYRFPSSLCVGLGQMVATVAVLWVGKALRVVKFPDLDRNVPRKTFPLPLLYFGNQ
ITGLFSTKKLNLPMFTVLRRFSILFTMFAEGVLLKKTFSWGIKMTVFAMIIGAFVAASSD
LAFDLEGYAFILINDVLTAANGAYVKQKLDSKELGKYGLLYYNALFMILPTLAIAYFTGD
AQKAVEFEGWADTLFLLQFTLSCVMGFILMYATVLCTQYNSALTTTIVGCIKNILITYIG
MVFGGDYIFTWTNFIGLNISIAGSLVYSYITFTEEQLSKQSEANNKLDIKGKGAV
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Monoamine oxidase type A (MAO-A)
Enzyme 2 Gene Name MAOA
Enzyme 2 SwissProt ID P21397 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P21397|AOFA_HUMAN Amine oxidase [flavin-containing]
MENQEKASIAGHMFDVVVIGGGISGLSAAKLLTEYGVSVLVLEARDRVGGRTYTIRNEHV
DYVDVGGAYVGPTQNRILRLSKELGIETYKVNVSERLVQYVKGKTYPFRGAFPPVWNPIA
YLDYNNLWRTIDNMGKEIPTDAPWEAQHADKWDKMTMKELIDKICWTKTARRFAYLFVNI
NVTSEPHEVSALWFLWYVKQCGGTTRIFSVTNGGQERKFVGGSGQVSERIMDLLGDQVKL
NHPVTHVDQSSDNIIIETLNHEHYECKYVINAIPPTLTAKIHFRPELPAERNQLIQRLPM
GAVIKCMMYYKEAFWKKKDYCGCMIIEDEDAPISITLDDTKPDGSLPAIMGFILARKADR
LAKLHKEIRKKKICELYAKVLGSQEALHPVHYEEKNWCEEQYSGGCYTAYFPPGIMTQYG
RVIRQPVGRIFFAGTETATKWSGYMEGAVEAGERAAREVLNGLGKVTEKDIWVQEPESKD
VPAVEITHTFWERNLPSVSGLLKIIGFSTSVTALGFVLYKYKLLPRS
Drug Target 1 [top]
Target 1 ID 423
Target 1 Name Gamma-aminobutyric-acid receptor subunit alpha-2
Target 1 Synonyms
  1. GABA(A) receptor subunit alpha-2
  2. Gamma-aminobutyric-acid receptor subunit alpha-2 precursor
Target 1 Gene Name GABRA2
Target 1 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-2 precursor
MKTKLNIYNIEFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWTWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
Target 1 Number of Residues 458
Target 1 Molecular Weight 51340
Target 1 Theoretical pI 9.41
Target 1 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 1 General Function Involved in GABA-A receptor activity
Target 1 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 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-28
Target 1 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 420-441
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 386422 Link Image
Target 1 UniProtKB/Swiss-Prot ID P47869 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name GBRA2_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1356 bp
ATGAAGACAAAATTGAACATCTACAACATCGAGTTCCTGCTTTTTGTTTTCTTGGTGTGG
GACCCTGCCAGGTTGGTGCTGGCTAACATCCAAGAAGATGAGGCTAAAAATAACATTACC
ATCTTTACGAGAATTCTTGACAGACTTCTGGATGGTTACGATAATCGGCTTAGACCAGGA
CTGGGAGACAGTATTACTGAAGTCTTCACTAACATCTACGTGACCAGTTTTGGCCCTGTC
TCAGATACAGATATGGAATATACAATTGATGTTTTCTTTCGACAAAAATGGAAAGATGAA
CGTTTAAAATTTAAAGGTCCTATGAATATCCTTCGACTAAACAATTTAATGGCTAGCAAA
ATCTGGACTCCAGATACCTTTTTTCACAATGGGAAGAAATCAGTAGCTCATAATATGACA
ATGCCAAATAAGTTGCTTCGAATTCAGGATGATGGGACTCTGCTGTATACCATGAGGCTT
ACAGTTCAAGCTGAATGCCCAATGCACTTGGAGGATTTCCCAATGGATGCTCATTCATGT
CCTCTGAAATTTGGCAGCTATGCATATACAACTTCAGAGGTCACTTATATTTGGACTTAC
AATGCATCTGATTCAGTACAGGTTGCTCCTGATGGCTCTAGGTTAAATCAATATGACCTG
CTGGGCCAATCAATCGGAAAGGAGACAATTAAATCCAGTACAGGTGAATATACTGTAATG
ACAGCTCATTTCCACCTGAAAAGAAAAATTGGGTATTTTGTGATTCAAACCTATCTGCCT
TGCATCATGACTGTCATTCTCTCCCAAGTTTCATTCTGGCTTAACAGAGAATCTGTGCCT
GCAAGAACTGTGTTTGGAGTAACAACTGTCCTAACAATGACAACTCTAAGCATCAGTGCT
CGGAATTCTCTCCCCAAAGTGGCTTATGCAACTGCCATGGACTGGTTTATTGCTGTTTGT
TATGCATTTGTGTTCTCTGCCCTAATTGAATTTGCAACTGTTAATTACTTCACCAAAAGA
GGATGGACTTGGGATGGGAAGAGTGTAGTAAATGACAAGAAAAAAGAAAAGGCTTCCGTT
ATGATACAGAACAACGCTTATGCAGTGGCTGTTGCCAATTATGCCCCGAATCTTTCAAAA
GATCCAGTTCTCTCCACCATCTCCAAGAGTGCAACCACGCCAGAACCCAACAAGAAGCCA
GAAAACAAGCCAGCTGAAGCAAAGAAAACTTTCAACAGTGTTAGCAAAATTGACAGAATG
TCCAGAATAGTTTTTCCAGTTTTGTTTGGTACCTTTAATTTAGTTTACTGGGCTACATAT
TTAAACAGAGAACCTGTATTAGGGGTCAGTCCTTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID GABRA2 Link Image
Target 1 GenAtlas ID GABRA2 Link Image
Target 1 HGNC ID HGNC:4076 Link Image
Target 1 Chromosome Location 4
Target 1 Locus 4p12
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Hadingham KL, Wingrove P, Le Bourdelles B, Palmer KJ, Ragan CI, Whiting PJ: Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol. 1993 Jun;43(6):970-5. [PubMed Link Image]
Target 1 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 523
Target 2 Name Gamma-aminobutyric-acid receptor subunit alpha-5
Target 2 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-5 precursor
Target 2 Gene Name GABRA5
Target 2 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-5 precursor
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN
SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
Target 2 Number of Residues 469
Target 2 Molecular Weight 52147
Target 2 Theoretical pI 9.56
Target 2 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 2 General Function Involved in GABA-A receptor activity
Target 2 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 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-31
Target 2 Transmembrane Regions
  • 260-281
  • 286-307
  • 319-341
  • 428-449
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 182916 Link Image
Target 2 UniProtKB/Swiss-Prot ID P31644 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name GBRA5_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1389 bp
ATGGACAATGGAATGTTCTCTGGTTTTATCATGATCAAAAACCTCCTTCTCTTTTGTATT
TCCATGAACTTATCCAGTCACTTTGGCTTTTCACAGATGCCAACCAGTTCAGTGAAAGAT
GAGACCAATGACAACATCACGATATTTACCAGGATCTTGGATGGGCTCTTGGATGGCTAC
GACAACAGACTTCGGCCCGGGCTGGGAGAGCGCATCACTCAGGTGAGGACCGACATCTAC
GTCACCAGCTTCGGCCCGGTGTCCGACACGGAAATGGAGTACACCATAGACGTGTTTTTC
CGACAAAGCTGGAAAGATGAAAGGCTTCGGTTTAAGGGGCCCATGCAGCGCCTCCCTCTC
AACAACCTCCTTGCCAGCAAGATCTGGACCCCAGACACGTTCTTCCACAACGGGAAGAAG
TCCATCGCTCACAACATGACCACGCCCAACAAGCTGCTGCGGCTGGAGGACGACGGCACC
CTGCTCTACACCATGCGCTTGACCATCTCTGCAGAGTGCCCCATGCAGCTTGAGGACTTC
CCGATGGATGCGCACGCTTGCCCTCTGAAATTTGGCAGCTATGCGTACCCTAATTCTGAA
GTCGTTTACGTCTGGACCAACGGCTCCACCAAGTCGGTGGTGGTGGCGGAAGATGGCTCC
AGACTGAACCAGTACCACCTGATGGGGCAGACGGTGGGCACTGAGAACATCAGCACCAGC
ACAGGCGAATACACAATCATGACAGCTCACTTCCACCTGAAAAGGAAGATTGGCTACTTT
GTCATCCAGACCTACCTTCCCTGCATAATGACCGTGATCTTATCACAGGTGTCCTTTTGG
CTGAACCGGGAATCAGTCCCAGCCAGGACAGTTTTTGGGGTCACCACGGTGCTGACCATG
ACGACCCTCAGCATCAGCGCCAGGAACTCTCTGCCCAAAGTGGCCTACGCCACCGCCATG
GACTGGTTCATAGCTGTGTGCTATGCCTTCGTCTTCTCGGCGCTGATAGAGTTTGCCACG
GTCAATTACTTTACCAAGAGAGGCTGGGCCTGGGATGGCAAAAAAGCCTTGGAAGCAGCC
AAGATCAAGAAAAAGCGTGAAGTCATACTAAATAAGTCAACAAACGCTTTTACAACTGGG
AAGATGTCTCACCCCCCAAACATTCCGAAGGAACAGACCCCAGCAGGGACGTCGAATACA
ACCTCAGTCTCAGTAAAACCCTCTGAAGAGAAGACTTCTGAAAGCAAAAAGACTTACAAC
AGTATCAGCAAAATTGACAAAATGTCCCGAATCGTATTCCCAGTCTTGTTCGGCACTTTC
AACTTAGTTTACTGGGCAACGTATTTGAATAGGGAGCCGGTGATAAAAGGAGCCGCCTCT
CCAAAATAA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GABRA5 Link Image
Target 2 GenAtlas ID GABRA5 Link Image
Target 2 HGNC ID HGNC:4079 Link Image
Target 2 Chromosome Location 15
Target 2 Locus 15q11.2-q12
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Wingrove P, Hadingham K, Wafford K, Kemp JA, Ragan CI, Whiting P: Cloning and expression of a cDNA encoding the human GABA-A receptor alpha 5 subunit. Biochem Soc Trans. 1992 Feb;20(1):18S. [PubMed Link Image]
  2. Knoll JH, Sinnett D, Wagstaff J, Glatt K, Wilcox AS, Whiting PM, Wingrove P, Sikela JM, Lalande M: FISH ordering of reference markers and of the gene for the alpha 5 subunit of the gamma-aminobutyric acid receptor (GABRA5) within the Angelman and Prader-Willi syndrome chromosomal regions. Hum Mol Genet. 1993 Feb;2(2):183-9. [PubMed Link Image]
  3. Kim Y, Glatt H, Xie W, Sinnett D, Lalande M: Human gamma-aminobutyric acid-type A receptor alpha5 subunit gene (GABRA5): characterization and structural organization of the 5' flanking region. Genomics. 1997 Jun 15;42(3):378-87. [PubMed Link Image]
Target 2 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 530
Target 3 Name Gamma-aminobutyric-acid receptor subunit alpha-4
Target 3 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-4 precursor
Target 3 Gene Name GABRA4
Target 3 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-4 precursor
MVSAKKVPAIALSAGVSFALLRFLCLAVCLNESPGQNQKEEKLCTENFTRILDSLLDGYD
NRLRPGFGGPVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWIDKRLKYDGPIEILRLN
NMMVTKVWTPDTFFRNGKKSVSHNMTAPNKLFRIMRNGTILYTMRLTISAECPMRLVDFP
MDGHACPLKFGSYAYPKSEMIYTWTKGPEKSVEVPKESSSLVQYDLIGQTVSSETIKSIT
GEYIVMTVYFHLRRKMGYFMIQTYIPCIMTVILSQVSFWINKESVPARTVFGITTVLTMT
TLSISARHSLPKVSYLTAMDWFIAVCFAFVFSALIEFAAVNYFTNIQMEKAKRKTSKPPQ
EVPAAPVQREKHPEAPLQDTNANLNMRKRTNALVHSESDVGNRTEVGNHSSKSSTVVQES
SKGTPRSYLASSPNPFSRANAAETISAARALPSASPTSIRTGHMPRKASVGSASTRHVFG
SRLQRIKTTVNTIGATGKLSATPPPSAPPPSGSGTSKIDKYARILFPVTFGAFNMVYWVV
YLSKDTMEKSESLM
Target 3 Number of Residues 563
Target 3 Molecular Weight 61641
Target 3 Theoretical pI 10.00
Target 3 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 3 General Function Involved in GABA-A receptor activity
Target 3 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 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • 1-35
Target 3 Transmembrane Regions
  • 259-280
  • 285-306
  • 318-340
  • 524-543
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 905393 Link Image
Target 3 UniProtKB/Swiss-Prot ID P48169 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name GBRA4_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1665 bp
ATGGTTTCTGCCAAGAAGGTACCCGCGATCGCTCTGTCCGCCGGGGTCAGTTTCGCCCTC
CTGCGCTTCCTGTGCCTGGCGGTTTGTTTAAACGAATCCCCAGGACAGAACCAAAAGGAG
GAGAAATTGTGCACAGAAAATTTCACCCGCATCCTGGACAGTTTGCTCGATGGTTATGAC
AACAGGCTGCGTCCTGGATTTGGGGGTCCTGTTACAGAAGTGAAAACTGACATATATGTC
ACCAGCTTTGGACCTGTTTCTGATGTTGAAATGGAATACACAATGGATGTGTTCTTCAGG
CAGACATGGATTGACAAAAGATTAAAATATGACGGCCCCATTGAAATTTTGAGATTGAAC
AATATGATGGTAACGAAAGTGTGGACCCCTGATACTTTCTTCAGGAATGGAAAGAAATCT
GTCTCACATAATATGACAGCTCCAAATAAGCTTTTTAGAATTATGAGAAATGGTACTATT
TTATACACAATGAGACTCACCATAAGTGCGGAGTGTCCCATGAGATTGGTGGATTTTCCC
ATGGATGGTCATGCATGCCCTTTGAAATTCGGGAGTTATGCCTATCCAAAGAGTGAGATG
ATCTATACCTGGACAAAAGGTCCTGAGAAATCAGTTGAAGTTCCGAAGGAGTCTTCCAGC
TTAGTTCAATATGATTTGATTGGGCAAACCGTATCAAGTGAAACCATCAAATCAATTACG
GGCGAATATATTGTTATGACGGTTTACTTCCACCTCAGACGGAAGATGGGTTATTTTATG
ATTCAGACCTATATTCCGTGCATTATGACAGTGATTCTTTCTCAAGTTTCATTTTGGATA
AATAAAGAATCAGTTCCCGCTAGGACTGTATTTGGAATAACAACTGTCCTCACCATGACC
ACACTAAGCATCAGTGCACGACATTCTTTGCCCAAAGTGTCCTACTTGACCGCCATGGAC
TGGTTCATAGCTGTCTGCTTTGCTTTTGTATTTTCGGCCCTTATCGAGTTTGCTGCTGTC
AACTATTTCACCAATATTCAAATGGAAAAAGCCAAAAGAAAGACATCAAAGCCCCCTCAG
GAAGTTCCCGCTGCTCCAGTGCAGAGAGAGAAGCATCCTGAAGCCCCTCTGCAGGATACA
AATGCCAATTTGAACATGAGAAAAAGAACAAATGCTTTGGTTCACTCTGAATCTGATGTT
GGCAACAGAACTGAGGTGGGAAACCATTCAAGCAAATCTTCCACAGTTGTTCAAGAATCT
TCTAAAGGCACACCTCGGTCTTACTTAGCTTCCAGTCCAAACCCATTCAGCCGTGCAAAT
GCAGCTGAAACCATATCTGCAGCAAGAGCACTTCCATCTGCTTCTCCTACTTCTATCCGA
ACTGGACATATGCCTCGAAAGGCTTCAGTTGGATCTGCTTCTACTCGTCACGTGTTTGGA
TCAAGACTGCAGAGGATAAAGACCACAGTTAATACCATAGGGGCTACTGGGAAGTTGTCA
GCTACTCCTCCTCCATCGGCTCCACCACCTTCTGGATCTGGCACAAGTAAAATAGACAAA
TATGCCCGTATTCTCTTTCCAGTCACATTTGGGGCATTTAACATGGTTTATTGGGTTGTT
TATTTATCTAAGGACACTATGGAGAAATCAGAAAGTCTAATGTAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID GABRA4 Link Image
Target 3 GenAtlas ID GABRA4 Link Image
Target 3 HGNC ID HGNC:4078 Link Image
Target 3 Chromosome Location 4
Target 3 Locus 4p12
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. McLean PJ, Farb DH, Russek SJ: Mapping of the alpha 4 subunit gene (GABRA4) to human chromosome 4 defines an alpha 2-alpha 4-beta 1-gamma 1 gene cluster: further evidence that modern GABAA receptor gene clusters are derived from an ancestral cluster. Genomics. 1995 Apr 10;26(3):580-6. [PubMed Link Image]
  2. Yang W, Drewe JA, Lan NC: Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a unique diazepam-insensitive binding site. Eur J Pharmacol. 1995 Nov 30;291(3):319-25. [PubMed Link Image]
Target 3 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 580
Target 4 Name Gamma-aminobutyric-acid receptor subunit alpha-3
Target 4 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-3 precursor
Target 4 Gene Name GABRA3
Target 4 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-3 precursor
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
Target 4 Number of Residues 500
Target 4 Molecular Weight 55165
Target 4 Theoretical pI 8.93
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
  • 1-28
Target 4 Transmembrane Regions
  • 277-298
  • 304-325
  • 338-359
  • 458-479
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 386424 Link Image
Target 4 UniProtKB/Swiss-Prot ID P34903 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name GBRA3_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1479 bp
ATGATAATCACACAAACAAGTCACTGTTACATGACCAGCCTTGGGATTCTTTTCCTGATT
AATATTCTCCCTGGAACCACTGGTCAAGGGGAATCAAGACGACAAGAACCCGGGGACTTT
GTGAAGCAGGACATTGGCGGGCTGTCTCCTAAGCATGCCCCAGATATTCCTGATGACAGC
ACTGACAACATCACTATCTTCACCAGAATCTTGGATCGTCTTCTGGACGGCTATGACAAC
CGGCTGCGACCTGGGCTTGGAGATGCAGTGACTGAAGTGAAGACTGACATCTACGTGACC
AGTTTTGGCCCTGTGTCAGACACTGACATGGAGTACACTATTGATGTATTTTTTCGGCAG
ACATGGCATGATGAAAGACTGAAATTTGATGGCCCCATGAAGATCCTTCCACTGAACAAT
CTCCTGGCTAGTAAGATCTGGACACCGGACACCTTCTTCCACAATGGCAAGAAATCAGTG
GCTCATAACATGACCACGCCCAACAAGCTGCTCAGATTGGTGGACAACGGAACCCTCCTC
TATACAATGAGGTTAACAATTCATGCTGAGTGTCCCATGCATTTGGAAGATTTTCCCATG
GATGTGCATGCCTGCCCACTGAAGTTTGGAAGCTATGCCTATACAACAGCTGAAGTGGTT
TATTCTTGGACTCTCGGAAAGAACAAATCCGTGGAAGTGGCACAGGATGGTTCTCGCTTG
AACCAGTATGACCTTTTGGGCCATGTTGTTGGGACAGAGATAATCCGGTCTAGTACAGGA
GAATATGTCGTCATGACAACCCACTTCCATCTCAAGCGAAAAATTGGCTACTTTGTGATC
CAGACCTACTTGCCATGTATCATGACTGTCATTCTGTCACAAGTGTCGTTCTGGCTCAAC
AGAGAGTCTGTTCCTGCCCGTACAGTCTTTGGTGTCACCACTGTGCTTACCATGACCACC
TTGAGTATCAGTGCCAGAAATTCCTTACCTAAAGTGGCATATGCGACGGCCATGGACTGG
TTCATAGCCGTCTGTTATGCCTTTGTATTTTCTGCACTGATTGAATTTGCCACTGTCAAC
TATTTCACCAAGCGGAGTTGGGCTTGGGAAGGCAAGAAGGTGCCAGAGGCCCTGGAGATG
AAGAAGAAAACACCAGCAGCCCCAGCAAAGAAAACCAGCACTACCTTCAACATCGTGGGG
ACCACCTATCCCATCAACCTGGCCAAGGACACTGAATTTTCCACCATCTCCAAGGGCGCT
GCTCCCAGTGCCTCCTCAACCCCAACAATCATTGCTTCACCCAAGGCCACCTACGTGCAG
GACAGCCCGACTGAGACCAAGACCTACAACAGTGTCAGCAAGGTTGACAAAATTTCCCGC
ATCATCTTTCCTGTGCTCTTTGCCATATTCAATCTGGTCTATTGGGCCACATATGTCAAC
CGGGAGTCAGCTATCAAGGGCATGATCCGCAAACAGTAG
Target 4 GenBank Gene ID
Target 4 GeneCard ID GABRA3 Link Image
Target 4 GenAtlas ID GABRA3 Link Image
Target 4 HGNC ID HGNC:4077 Link Image
Target 4 Chromosome Location X
Target 4 Locus Xq28
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Amir R, Dahle EJ, Toriolo D, Zoghbi HY: Candidate gene analysis in Rett syndrome and the identification of 21 SNPs in Xq. Am J Med Genet. 2000 Jan 3;90(1):69-71. [PubMed Link Image]
  2. Hadingham KL, Wingrove P, Le Bourdelles B, Palmer KJ, Ragan CI, Whiting PJ: Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol. 1993 Jun;43(6):970-5. [PubMed Link Image]
Target 4 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 811
Target 5 Name Translocator protein
Target 5 Synonyms
  1. Mitochondrial benzodiazepine receptor
  2. PBR
  3. PKBS
  4. Peripheral-type benzodiazepine receptor
Target 5 Gene Name BZRP
Target 5 Protein Sequence >Peripheral-type benzodiazepine receptor
MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM
GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA
ATTVAWYQVSPLAARLLYPYLAWLAFATTLNYCVWRDNHGWHGGRRLPE
Target 5 Number of Residues 171
Target 5 Molecular Weight 18779
Target 5 Theoretical pI 9.33
Target 5 GO Classification
Function
Not Available
Process
Not Available
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 5 General Function Signal transduction mechanisms
Target 5 Specific Function Responsible for the manifestation of peripheral-type benzodiazepine recognition sites and is most likely to comprise binding domains for benzodiazepines and isoquinoline carboxamides. May play a role in the transport of porphyrins and heme
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 6-26
  • 47-67
  • 80-100
  • 106-126
  • 135-155
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 306883 Link Image
Target 5 UniProtKB/Swiss-Prot ID P30536 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name BZRP_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Mitochondrion
  • mitochondrial membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >510 bp
ATGGCCCCGCCCTGGGTGCCCGCCATGGGCTTCACGCTGGCGCCCAGCCTGGGGTGCTTC
GTGGGCTCCCGCTTTGTCCACGGCGAGGGTCTCCGCTGGTACGCCGGCCTGCAGAAGCCC
TCGTGGCACCCGCCCCACTGGGTGCTGGGCCCTGTCTGGGGCACGCTCTACTCAGCCATG
GGGTACGGCTCCTACCTGGTCTGGAAAGAGCTGGGAGGCTTCACAGAGAAGGCTGTGGTT
CCCCTGGGCCTCTACACTGGGCAGCTGGCCCTGAACTGGGCATGGCCCCCCATCTTCTTT
GGTGCCCGACAAATGGGCTGGGCCTTGGTGGATCTCCTGCTGGTCAGTGGGGCGGCGGCN
GCCACTACCGTGGCCTGGTACCAGGTGAGCCCGCTGGCCGCCCGCCTGCTCTACCCCTAC
CTGGCCTGGCTGGCCTTCGCGACCACACTCAACTACTGCGTATGGCGGGACAACCATGGC
TGGCATGGGGGACGGCGGCTGCCAGAGTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID TSPO Link Image
Target 5 GenAtlas ID TSPO Link Image
Target 5 HGNC ID HGNC:1158 Link Image
Target 5 Chromosome Location 22
Target 5 Locus 22q13.31
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Dunham I, Shimizu N, Roe BA, Chissoe S, Hunt AR, Collins JE, Bruskiewich R, Beare DM, Clamp M, Smink LJ, Ainscough R, Almeida JP, Babbage A, Bagguley C, Bailey J, Barlow K, Bates KN, Beasley O, Bird CP, Blakey S, Bridgeman AM, Buck D, Burgess J, Burrill WD, O'Brien KP, et al.: The DNA sequence of human chromosome 22. Nature. 1999 Dec 2;402(6761):489-95. [PubMed Link Image]
  2. Kurumaji A, Nomoto H, Yoshikawa T, Okubo Y, Toru M: An association study between two missense variations of the benzodiazepine receptor (peripheral) gene and schizophrenia in a Japanese sample. J Neural Transm. 2000;107(4):491-500. [PubMed Link Image]
  3. Kurumaji A, Nomoto H, Yamada K, Yoshikawa T, Toru M: No association of two missense variations of the benzodiazepine receptor (peripheral) gene and mood disorders in a Japanese sample. Am J Med Genet. 2001 Mar 8;105(2):172-5. [PubMed Link Image]
  4. Riond J, Mattei MG, Kaghad M, Dumont X, Guillemot JC, Le Fur G, Caput D, Ferrara P: Molecular cloning and chromosomal localization of a human peripheral-type benzodiazepine receptor. Eur J Biochem. 1991 Jan 30;195(2):305-11. [PubMed Link Image]
  5. Yakovlev AG, Ruffo M, Jurka J, Krueger KE: Comparison of repetitive elements in the third intron of human and rodent mitochondrial benzodiazepine receptor-encoding genes. Gene. 1995 Apr 3;155(2):201-5. [PubMed Link Image]
  6. Galiegue S, Jbilo O, Combes T, Bribes E, Carayon P, Le Fur G, Casellas P: Cloning and characterization of PRAX-1. A new protein that specifically interacts with the peripheral benzodiazepine receptor. J Biol Chem. 1999 Jan 29;274(5):2938-52. [PubMed Link Image]
Target 5 Drug References
  1. Uusi-Oukari M, Korpi ER: Specific alterations in the cerebellar GABA(A) receptors of an alcohol-sensitive ANT rat line. Alcohol Clin Exp Res. 1991 Mar;15(2):241-8. [PubMed Link Image]
  2. Miller EI, Wylie FM, Oliver JS: Detection of benzodiazepines in hair using ELISA and LC-ESI-MS-MS. J Anal Toxicol. 2006 Sep;30(7):441-8. [PubMed Link Image]
  3. Park CH, Carboni E, Wood PL, Gee KW: Characterization of peripheral benzodiazepine type sites in a cultured murine BV-2 microglial cell line. Glia. 1996 Jan;16(1):65-70. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 841
Target 6 Name Gamma-aminobutyric-acid receptor subunit alpha-6
Target 6 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-6 precursor
Target 6 Gene Name GABRA6
Target 6 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-6 precursor
MASSLPWLCIILWLENALGKLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEI
VLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLPPAFGGTSKIDQY
SRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
Target 6 Number of Residues 460
Target 6 Molecular Weight 51035
Target 6 Theoretical pI 8.40
Target 6 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 6 General Function Involved in GABA-A receptor activity
Target 6 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 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • 1-19
Target 6 Transmembrane Regions
  • 243-264
  • 269-290
  • 301-324
  • 420-441
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 1470364 Link Image
Target 6 UniProtKB/Swiss-Prot ID Q16445 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name GBRA6_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >1362 bp
ATGGCGTCATCTCTGCCCTGGCTGTGCATTATTCTGTGGCTAGAAAATGCCCTAGGGAAA
CTCGAAGTTGAAGGCAACTTCTACTCAGAAAACGTCAGTCGGATCCTGGACAACTTGCTT
GAAGGCTATGACAATCGGCTGCGGCCGGGATTTGGAGGTGCTGTCACTGAAGTCAAAACA
GACATTTATGTGACCAGTTTTGGGCCCGTGTCAGATGTGGAGATGGAGTATACGATGGAT
GTTTTTTTTCGCCAGACCTGGACTGATGAGAGGTTGAAGTTTGGGGGGCCAACTGAGATT
CTGAGTCTGAATAATTTGATGGTCAGTAAAATCTGGACGCCTGACACCTTTTTCAGAAAT
GGTAAAAAGTCCATTGCTCACAACATGACAACTCCTAATAAACTCTTCAGAATAATGCAG
AATGGAACCATTTTATACACCATGAGGCTTACCATCAATGCTGACTGTCCCATGAGGCTG
GTTAACTTTCCTATGGATGGGCATGCTTGTCCACTCAAGTTTGGGAGCTATGCTTATCCC
AAAAGTGAAATCATATATACGTGGAAAAAAGGACCACTTTACTCAGTAGAAGTCCCAGAA
GAATCTTCAAGCCTTCTCCAGTATGATCTGATTGGACAAACAGTATCTAGTGAGACAATT
AAATCTAACACAGGTGAATACGTTATAATGACAGTTTACTTCCACTTGCAAAGGAAGATG
GGCTACTTCATGATACAGATATACACTCCTTGCATTATGACAGTCATTCTTTCCCAGGTG
TCTTTCTGGATTAATAAGGAGTCCGTCCCAGCAAGAACTGTTTTTGGGATCACCACTGTT
TTAACTATGACCACTTTGAGCATCAGTGCCCGGCACTCTTTGCCAAAAGTGTCATATGCC
ACTGCCATGGATTGGTTCATAGCTGTTTGCTTTGCATTCGTCTTCTCTGCTCTTATCGAG
TTCGCAGCTGTCAACTACTTTACCAATCTTCAGACACAGAAGGCGAAAAGGAAGGCACAG
TTTGCAGCCCCACCCACAGTGACAATATCAAAAGCTACTGAACCTTTGGAAGCTGAGATT
GTTTTGCATCCTGACTCCAAATATCATCTGAAGAAAAGGATCACTTCTCTGTCTTTGCCA
ATAGTTTCATCTTCCGAGGCCAATAAAGTGCTCACGAGAGCGCCCATCTTACAATCAACA
CCTGTCACACCCCCACCACTCCCGCCAGCCTTTGGAGGCACCAGTAAAATAGACCAGTAT
TCTCGAATTCTCTTCCCAGTTGCATTTGCAGGATTCAACCTTGTGTACTGGGTAGTTTAT
CTTTCCAAAGATACAATGGAAGTGAGTAGCAGTGTTGAATAG
Target 6 GenBank Gene ID
Target 6 GeneCard ID GABRA6 Link Image
Target 6 GenAtlas ID GABRA6 Link Image
Target 6 HGNC ID HGNC:4080 Link Image
Target 6 Chromosome Location 5
Target 6 Locus 5q34
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [PubMed Link Image]
Target 6 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 872
Target 7 Name Gamma-aminobutyric-acid receptor subunit alpha-1
Target 7 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
Target 7 Gene Name GABRA1
Target 7 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target 7 Number of Residues 463
Target 7 Molecular Weight 51802
Target 7 Theoretical pI 9.61
Target 7 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 7 General Function Involved in GABA-A receptor activity
Target 7 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 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • 1-27
Target 7 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 422-443
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 31631 Link Image
Target 7 UniProtKB/Swiss-Prot ID P14867 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name GBRA1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 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 7 GenBank Gene ID
Target 7 GeneCard ID GABRA1 Link Image
Target 7 GenAtlas ID GABRA1 Link Image
Target 7 HGNC ID HGNC:4075 Link Image
Target 7 Chromosome Location 5
Target 7 Locus 5q34-q35
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. 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 Link Image]
  2. 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 Link Image]
  3. 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 Link Image]
Target 7 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 4098
Target 8 Name Gamma-aminobutyric-acid receptor subunit beta-1
Target 8 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-1 precursor
Target 8 Gene Name GABRB1
Target 8 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-1
MWTVQNRESLGLLSFPVMITMVCCAHSTNEPSNMSYVKETVDRLLKGYDIRLRPDFGGPP
VDVGMRIDVASIDMVSEVNMDYTLTMYFQQSWKDKRLSYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWNGGEGAVTGVNKIELPQFSIVDYKMVSKKVEFTTGAYPRLSLSFRLK
RNIGYFILQTYMPSTLITILSWVSFWINYDASAARVALGITTVLTMTTISTHLRETLPKI
PYVKAIDIYLMGCFVFVFLALLEYAFVNYIFFGKGPQKKGASKQDQSANEKNKLEMNKVQ
VDAHGNILLSTLEIRNETSGSEVLTSVSDPKATMYSYDSASIQYRKPLSSREAYGRALDR
HGVPSKGRIRRRASQLKVKIPDLTDVNSIDKWSRMFFPITFSLFNVVYWLYYVH
Target 8 Number of Residues 481
Target 8 Molecular Weight 54235
Target 8 Theoretical pI 9.01
Target 8 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
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 8 General Function Not Available
Target 8 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 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • 1-25
Target 8 Transmembrane Regions
  • 246-267
  • 271-293
  • 305-327
  • 452-473
Target 8 Essentiality Non Essential
Target 8 GenBank ID Protein 31635 Link Image
Target 8 UniProtKB/Swiss-Prot ID P18505 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name GBRB1_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Membrane
Target 8 Gene Sequence >1425 bp
ATGTGGACAGTACAAAATCGAGAGAGTCTGGGGCTTCTCTCTTTCCCTGTGATGATTACC
ATGGTCTGTTGTGCACACAGCACCAATGAACCCAGCAACATGCCATACGTGAAAGAGACA
GTGGACAGATTGCTCAAAGGATATGACATTCGCTTGCGGCCGGACTTCGGAGGGCCCCCC
GTCGACGTTGGGATGCGGATCGATGTCGCCAGCATAGACATGGTCTCCGAAGTGAATATG
GATTATACACTCACCATGTATTTCCAGCAGTCTTGGAAAGACAAAAGGCTTTCTTATTCT
GGAATCCCACTGAACCTCACCCTAGACAATAGGGTAGCTGACCAACTCTGGGTACCAGAC
ACCTACTTTCTGAATGACAAGAAATCATTTGTGCATGGGGTCACAGTGAAAAATCGAATG
ATTCGACTGCATCCTGATGGAACAGTTCTCTATGGACTCCGAATCACAACCACAGCTGCA
TGTATGATGGATCTTCGAAGATATCCACTGGATGAGCAGAACTGCACCCTGGAGATCGAA
AGTTATGGCTATACCACTGATGACATTGAATTTTACTGGAATGGAGGAGAAGGGGCAGTC
ACTGGTGTTAATAAAATCGAACTTCCTCAATTTTCAATTGTTGACTACAAGATGGTGTCT
AAGAAGGTGGAGTTCACAACAGGAGCGTATCCACGACTGTCACTAAGTTTTCGTCTAAAG
AGAAACATTGGTTACTTCATTTTGCAAACCTACATGCCTTCTACACTGATTACAATTCTG
TCCTGGGTGTCTTTTTGGATCAACTATGATGCATCTGCAGCCAGAGTCGCACTAGGAATC
ACGACGGTGCTTACAATGACAACCATCAGCACCCACCTCAGGGAGACCCTGCCAAAGATC
CCTTATGTCAAAGCGATTGATATTTATCTGATGGGTTGCTTTGTGTTTGTGTTCCTGGCT
CTGCTGGAGTATGCCTTTGTAAATTACATCTTCTTTGGGAAAGGCCCTCAGAAAAAGGGA
GCTAGCAAACAAGACCAGAGTGCCAATGAGAAGAATAAACTGGAGATGAATAAAGTCCAG
GTCGACGCCCACGGTAACATTCTCCTCAGCACCCTGGAAATCCGGAATGAGACGAGTGGC
TCGGAAGTGCTCACGAGCGTGAGCGACCCCAAGGCCACCATGTACTCCTATGACAGCGCC
AGCATCCAGTACCGCAAGCCCCTGAGCAGCCGCGAGGCCTACGGGCGCGCCCTGGACCGG
CACGGGGTACCCAGCAAGGGGCGCATCCGCAGGCGTGCCTCCCAGCTCAAAGTCAAGATC
CCCGACTTGACTGATGTGAATTCCATAGACAAGTGGTCCCGAATGTTTTTCCCCATCACC
TTTTCTCTTTTTAATGTCGTCTATTGGCTTTACTATGTACACTGA
Target 8 GenBank Gene ID
Target 8 GeneCard ID GABRB1 Link Image
Target 8 GenAtlas ID GABRB1 Link Image
Target 8 HGNC ID HGNC:4081 Link Image
Target 8 Chromosome Location 4
Target 8 Locus 4p12
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Kirkness EF, Kusiak JW, Fleming JT, Menninger J, Gocayne JD, Ward DC, Venter JC: Isolation, characterization, and localization of human genomic DNA encoding the beta 1 subunit of the GABAA receptor (GABRB1). Genomics. 1991 Aug;10(4):985-95. [PubMed Link Image]
  2. Garrett KM, Saito N, Duman RS, Abel MS, Ashton RA, Fujimori S, Beer B, Tallman JF, Vitek MP, Blume AJ: Differential expression of gamma-aminobutyric acidA receptor subunits. Mol Pharmacol. 1990 May;37(5):652-7. [PubMed Link Image]
  3. 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 Link Image]
  4. Coon H, Sobell J, Heston L, Sommer S, Hoff M, Holik J, Umar F, Robertson M, Reimherr F, Wender P, et al.: Search for mutations in the beta 1 GABAA receptor subunit gene in patients with schizophrenia. Am J Med Genet. 1994 Mar 15;54(1):12-20. [PubMed Link Image]
Target 8 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 4099
Target 9 Name Gamma-aminobutyric-acid receptor subunit beta-3
Target 9 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-3 precursor
Target 9 Gene Name GABRB3
Target 9 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-3
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
Target 9 Number of Residues 480
Target 9 Molecular Weight 54116
Target 9 Theoretical pI 9.41
Target 9 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
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 9 General Function Not Available
Target 9 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 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Pfam Domain Function
Target 9 Signals
  • 1-25
Target 9 Transmembrane Regions
  • 246-267
  • 271-293
  • 305-327
  • 451-472
Target 9 Essentiality Non Essential
Target 9 GenBank ID Protein 182925 Link Image
Target 9 UniProtKB/Swiss-Prot ID P28472 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name GBRB3_HUMAN Link Image
Target 9 PDB ID Not Available
Target 9 Cellular Location
  • Membrane
Target 9 Gene Sequence >1422 bp
ATGTGGGGCCTTGCGGGAGGAAGGCTTTTCGGCATCTTCTCGGCCCCGGTGCTGGTGGCT
GTGGTGTGCTGCGCCCAGAGTGTGAACGATCCCGGGAACATGTCCTTTGTGAAGGAGACG
GTGGACAAGCTGTTGAAAGGCTACGACATTCGCCTAAGACCCGACTTCGGGGGTCCCCCG
GTCTGCGTGGGGATGAACATCGACATCGCCAGCATCGACATGGTTTCCGAAGTCAACATG
GATTATACCTTAACCATGTATTTTCAACAATATTGGAGAGATAAAAGGCTCGCCTATTCT
GGGATCCCTCTCAACCTCACGCTTGACAATCGAGTGGCTGACCAGCTATGGGTGCCCGAC
ACATATTTCTTAAATGACAAAAAGTCATTTGTGCATGGAGTGACAGTGAAAAACCGCATG
ATCCGTCTTCACCCTGATGGGACAGTGCTGTATGGGCTCAGAATCACCACGACAGCAGCA
TGCATGATGGACCTCAGGAGATACCCCCTGGACGAGCAGAACTGCACTCTGGAAATTGAA
AGCTATGGCTACACCACGGATGACATTGAGTTTTACTGGCGAGGCGGGGACAAGGCTGTT
ACCGGAGTGGAAAGGATTGAGCTCCCGCAGTTCTCCATCGTGGAGCACCGTCTGGTCTCG
AGGAATGTTGTCTTCGCCACAGGTGCCTATCCTCGACTGTCACTGAGCTTTCGGTTGAAG
AGGAACATTGGATACTTCATTCTTCAGACTTATATGCCCTCTATACTGATAACGATTCTG
TCGTGGGTGTCCTTCTGGATCAATTATGATGCATCTGCTGCTAGAGTTGCCCTCGGGATC
ACAACTGTGCTGACAATGACAACCATCAACACCCACCTTCGGGAGACCTTGCCCAAAATC
CCCTATGTCAAAGCCATTGACATGTACCTTATGGGCTGCTTCGTCTTTGTGTTCCTGGCC
CTTCTGGAGTATGCCTTTGTCAACTACATTTTCTTTGGAAGAGGCCCTCAAAGGCAGAAG
AAGCTTGCAGAAAAGACAGCCAAGGCAAAGAATGACCGTTCAAAGAGCGAAAGCAACCGG
GTGGATGCTCATGGAAATATTCTGTTGACATCGCTGGAAGTTCACAATGAAATGAATGAG
GTCTCAGGCGGCATTGGCGATACCAGGAATTCAGCAATATCCTTTGACAACTCAGGAATC
CAGTACAGGAAACAGAGCATGCCTCGAGAAGGGCATGGGCGATTCCTGGGGGACAGAAGC
CTCCCGCACAAGAAGACCCATCTACGGAGGAGGTCTTCACAGCTCAAAATTAAAATACCT
GATCTAACCGATGTGAATGCCATAGACAGATGGTCCAGGATCGTGTTTCCATTCACTTTT
TCTCTTTTCAACTTAGTTTACTGGCTGTACTATGTTAACTGA
Target 9 GenBank Gene ID
Target 9 GeneCard ID GABRB3 Link Image
Target 9 GenAtlas ID GABRB3 Link Image
Target 9 HGNC ID HGNC:4083 Link Image
Target 9 Chromosome Location 15
Target 9 Locus 15q11.2-q12
Target 9 SNPs SNPJam Report Link Image
Target 9 General References
  1. Wagstaff J, Chaillet JR, Lalande M: The GABAA receptor beta 3 subunit gene: characterization of a human cDNA from chromosome 15q11q13 and mapping to a region of conserved synteny on mouse chromosome 7. Genomics. 1991 Dec;11(4):1071-8. [PubMed Link Image]
  2. Kirkness EF, Fraser CM: A strong promoter element is located between alternative exons of a gene encoding the human gamma-aminobutyric acid-type A receptor beta 3 subunit (GABRB3). J Biol Chem. 1993 Feb 25;268(6):4420-8. [PubMed Link Image]
Target 9 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 10 [top]
Target 10 ID 4100
Target 10 Name Gamma-aminobutyric-acid receptor subunit beta-2
Target 10 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-2 precursor
Target 10 Gene Name GABRB2
Target 10 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-2
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
Target 10 Number of Residues 481
Target 10 Molecular Weight 54607
Target 10 Theoretical pI 9.66
Target 10 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
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 10 General Function Not Available
Target 10 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 10 Pathways Not Available
Target 10 Reactions Not Available
Target 10 Pfam Domain Function
Target 10 Signals
  • 1-25
Target 10 Transmembrane Regions
  • 245-266
  • 270-292
  • 304-326
  • 452-473
Target 10 Essentiality Non Essential
Target 10 GenBank ID Protein 455946 Link Image
Target 10 UniProtKB/Swiss-Prot ID P47870 Link Image
Target 10 UniProtKB/Swiss-Prot Entry Name GBRB2_HUMAN Link Image
Target 10 PDB ID Not Available
Target 10 Cellular Location
  • Membrane
Target 10 Gene Sequence >1425 bp
ATGTGGAGAGTGCGGAAAAGGGGCTACTTTGGGATTTGGTCCTTCCCCTTAATAATCGCC
GCTGTCTGTGCGCAGAGTGTCAATGACCCTAGTAATATGTCGCTGGTTAAAGAGACGGTG
GATAGACTCCTGAAAGGCTATGACATTCGTCTGAGACCAGATTTTGGAGGTCCCCCCGTG
GCTGTGGGGATGAACATTGACATTGCCAGCATCGATATGGTTTCTGAAGTCAATATGGAT
TATACCTTGACAATGTACTTTCAACAAGCCTGGAGAGATAAGAGGCTGTCCTATAATGTA
ATACCTTTAAACTTGACTCTGGACAACAGAGTGGCAGACCAGCTCTGGGTGCCTGATACC
TATTTCCTGAACGATAAGAAGTCATTTGTGCACGGAGTGACTGTTAAGAACCGCATGATT
CGCCTGCATCCTGATGGCACCGTCCTTTATGGACTCAGAATCACAACCACAGCTGCCTGC
ATGATGGACCTAAGGAGGTACCCACTGGATGAACAAAACTGCACCTTGGAAATTGAGAGC
TATGGATACACAACTGATGACATTGAGTTTTACTGGCGTGGCGATGATAATGCAGTAACA
GGAGTAACGAAAATTGAACTTCCACAGTTCTCTATTGTAGATTACAAACTTATCACCAAG
AAGGTTGTTTTTTCCACAGGTTCCTATCCCAGGTTATCCCTCAGCTTTAAGCTTAAGAGA
AACATTGGCTACTTTATCCTGCAAACATACATGCCTTCCATCCTGATTACCATCCTCTCC
TGGGTCTCCTTCTGGATTAATTACGATGCTTCAGCTGCAAGGGTGGCATTAGGAATCACA
ACTGTCCTCACAATGACCACAATCAACACCCACCTCCGGGAAACTCTCCCTAAAATCCCC
TATGTGAAGGCCATTGACATGTACCTGATGGGGTGCTTTGTCTTCGTTTTCATGGCCCTT
CTGGAATATGCCCTAGTCAACTACATCTTCTTTGGGAGGGGGCCCCAACGCCAAAAGAAA
GCAGCTGAGAAGGCTGCCAGTGCCAACAATGAGAAGATGCGCCTGGATGTCAACAAGATG
GACCCCCATGAGAACATCTTACTGAGCACTCTCGAGATAAAAAATGAAATGGCCACATCT
GAGGCTGTGATGGGACTTGGAGACCCCAGAAGCACAATGCTAGCCTATGATGCCTCCAGC
ATCCAGTATCGGAAAGCTGGGTTGCCCAGGCATAGTTTTGGCCGAAATGCTCTGGAACGA
CATGTGGCGCAAAAGAAAAGTCGCCTGAGGAGACGCGCCTCCCAACTGAAAATCACCATC
CCTGACTTGACTGATGTGAATGCCATAGATCGGTGGTCCCGCATATTCTTCCCAGTGGTT
TTTTCCTTCTTCAACATCGTCTATTGGCTTTATTATGTGAACTAA
Target 10 GenBank Gene ID
Target 10 GeneCard ID GABRB2 Link Image
Target 10 GenAtlas ID GABRB2 Link Image
Target 10 HGNC ID HGNC:4082 Link Image
Target 10 Chromosome Location 5
Target 10 Locus 5q34
Target 10 SNPs SNPJam Report Link Image
Target 10 General References
  1. McKinley DD, Lennon DJ, Carter DB: Cloning, sequence analysis and expression of two forms of mRNA coding for the human beta 2 subunit of the GABAA receptor. Brain Res Mol Brain Res. 1995 Jan;28(1):175-9. [PubMed Link Image]
  2. Hadingham KL, Wingrove PB, Wafford KA, Bain C, Kemp JA, Palmer KJ, Wilson AW, Wilcox AS, Sikela JM, Ragan CI, et al.: Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors. Mol Pharmacol. 1993 Dec;44(6):1211-8. [PubMed Link Image]
Target 10 Drug References
  1. 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 Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.