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Showing drug card for Midazolam (DB00683)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:05:53
Primary Accession Number DB00683
Secondary Accession Number
  • APRD00680
Name Midazolam
Drug Type
  • Approved
  • Illicit
  • Small Molecule
Description A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. [PubChem] Midazolam is a schedule IV drug in the United States.
Synonyms
  1. Dea No. 2884
  2. Midazolam Base
  3. Midazolam Hcl
  4. Midazolamum [INN-Latin]
Brand Names
  1. Dormicum
  2. Versed
Brand Mixtures Not Available
Chemical IUPAC Name 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine
Chemical Formula C18H13ClFN3
Chemical Structure Structure
CAS Registry Number 59467-70-8
InChI Identifier InChI=1/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
InChI Key DDLIGBOFAVUZHB-UHFFFAOYAG
KEGG Drug D00550 Link Image
KEGG Compound C07524 Link Image
PubChem Compound 4192 Link Image
PubChem Substance 183492 Link Image
ChEBI ID Not Available
PharmGKB ID PA450496 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02240286 Link Image
RxList Link http://www.rxlist.com/cgi/generic2/versedsyr.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Midazolam Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 325.7670
Monoisotopic Molecular Weight 325.0782
State Solid
Melting Point 159 oC
Experimental Water Solubility 0.024 mg/mL [Thorsteinn Loftsson and Dagný Hreinsdóttir, 2006] Source: PhysProp
Predicted Water Solubility 9.87e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity Not Available Source: PhysProp
Predicted LogP 3.89 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.52 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
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 CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=C(C=CC(Cl)=C3)N12
Canonical SMILES CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=C(C=CC(Cl)=C3)N12
Drug Category
  • Adjuvants, Anesthesia
  • Anesthetics, Intravenous
  • Anti-anxiety Agents
  • GABA Modulators
  • Hypnotics and Sedatives
ATC Codes
AHFS Codes
  • 28:24.08
Indication For use in pediatric patients for sedation, anxiolysis, and amnesia prior to diagnostic, therapeutic, or endoscopic procedures or before induction of anesthesia.
Pharmacology Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepines, include sedative, anxiolytic, amnesic and hypnotic activities. Benzodiazepine pharmacologic effects appear to result from reversible interactions with the (gamma)-amino butyric acid (GABA) benzodiazepine receptor in the CNS, the major inhibitory neurotransmitter in the central nervous system. The action of midazolam is readily reversed by the benzodiazepine receptor antagonist, flumazenil.
Mechanism of Action It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Absorption Rapidly absorbed after oral administration (absolute bioavailability of the midazolam syrup in pediatric patients is about 36%, and intramuscular is greater than 90%).
Toxicity LD50=825 mg/kg (Orally in rats). Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs.
Protein Binding 97%
Biotransformation Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, (alpha)-hydroxymidazolam, and 4-hydroxymidazolam.
Half Life 2.2-6.8 hours
Dosage Forms
Form Route
Liquid Intravenous
Solution Intravenous
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Amprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Aprepitant Aprepitant increases the effect and toxicity of benzodiazepine
Atazanavir Atazanavir increases the effect and toxicity of benzodiazepine
Carbamazepine Carbamazepine reduces the effect of the benzodiazepine
Cimetidine Cimetidine increases the effect of benzodiazepine
Clarithromycin The macrolide increases the effect of benzodiazepine
Clozapine Increased risk of toxicity
Delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine
Diltiazem The calcium channel blocker increases the effect and toxicity of benzodiazepine
Docetaxel The agent increases the serum levels and toxicity of docetaxel
Efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine
Erythromycin The macrolide increases the effect of benzodiazepine
Ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fluconazole Fluconazole increases the effect of benzodiazepine
Fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Indinavir The protease inhibitor increases the effect of benzodiazepine
Itraconazole The imidazole increases the effect of benzodiazepine
Josamycin The macrolide increases the effect of benzodiazepine
Kava Kava increases the effect of benzodiazepine
Ketoconazole The imidazole increases the effect of benzodiazepine
Mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Nelfinavir The protease inhibitor increases the effect of benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Quinupristin This combination presents an increased risk of toxicity
Rifampin Rifampin increases the effect of benzodiazepine
Ritonavir The protease inhibitor increases the effect of benzodiazepine
Saquinavir The protease inhibitor increases the effect of benzodiazepine
St. John's Wort St. John's Wort could reduce the benzodiazepine effect
Telithromycin Telithromycin increases the effect/toxicity of the benzodiazepine
Verapamil The calcium channel blocker increases the effect and toxicity of benzodiazepine
Voriconazole The imidazole increases the effect of benzodiazepine
Food Interactions
  • Grapefruit juice slows the product's absorption and significantly increases its bioavailability.
Pathways Not Available
General References
  1. Isojarvi JI, Tokola RA: Benzodiazepines in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92. [PubMed Link Image]
  2. Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. [PubMed Link Image]
  3. Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed Link Image]
  4. Garratt JC, Gent JP, Feely M, Haigh JR: Can benzodiazepines be classified by characterising their anticonvulsant tolerance-inducing potential? Eur J Pharmacol. 1988 Jan 5;145(1):75-80. [PubMed Link Image]
  5. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [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. Cytochrome P450 3A5 (CYP3A5)
  2. Cytochrome P450 2E1 (CYP2E1)
  3. Cytochrome P450 3A4 (CYP3A4)
  4. Cytochrome P450 2C8 (CYP2C8)
  5. Cytochrome P450 2C9 (CYP2C9)
  6. Cytochrome P450 2D6 (CYP2D6)
  7. Cytochrome P450 2B6 (CYP2B6)
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. Gamma-aminobutyric-acid receptor subunit alpha-6
  6. Gamma-aminobutyric-acid receptor subunit alpha-1
  7. Gamma-aminobutyric-acid receptor subunit beta-1
  8. Gamma-aminobutyric-acid receptor subunit beta-3
  9. Gamma-aminobutyric-acid receptor subunit beta-2
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A5 (CYP3A5)
Enzyme 1 Gene Name CYP3A5
Enzyme 1 SwissProt ID P20815 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P20815|CP3A5_HUMAN Cytochrome P450 3A5 
MDLIPNLAVETWLLLAVSLVLLYLYGTRTHGLFKRLGIPGPTPLPLLGNVLSYRQGLWKF
DTECYKKYGKMWGTYEGQLPVLAITDPDVIRTVLVKECYSVFTNRRSLGPVGFMKSAISL
AEDEEWKRIRSLLSPTFTSGKLKEMFPIIAQYGDVLVRNLRREAEKGKPVTLKDIFGAYS
MDVITGTSFGVNIDSLNNPQDPFVESTKKFLKFGFLDPLFLSIILFPFLTPVFEALNVSL
FPKDTINFLSKSVNRMKKSRLNDKQKHRLDFLQLMIDSQNSKETESHKALSDLELAAQSI
IFIFAGYETTSSVLSFTLYELATHPDVQQKLQKEIDAVLPNKAPPTYDAVVQMEYLDMVV
NETLRLFPVAIRLERTCKKDVEINGVFIPKGSMVVIPTYALHHDPKYWTEPEEFRPERFS
KKKDSIDPYIYTPFGTGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLDTQG
LLQPEKPIVLKVDSRDGTLSGE
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 2E1 (CYP2E1)
Enzyme 2 Gene Name CYP2E1
Enzyme 2 SwissProt ID P05181 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P05181|CP2E1_HUMAN Cytochrome P450 2E1 (EC 1.14.14.1) 
MSALGVTVALLVWAAFLLLVSMWRQVHSSWNLPPGPFPLPIIGNLFQLELKNIPKSFTRL
AQRFGPVFTLYVGSQRMVVMHGYKAVKEALLDYKDEFSGRGDLPAFHAHRDRGIIFNNGP
TWKDIRRFSLTTLRNYGMGKQGNESRIQREAHFLLEALRKTQGQPFDPTFLIGCAPCNVI
ADILFRKHFDYNDEKFLRLMYLFNENFHLLSTPWLQLYNNFPSFLHYLPGSHRKVIKNVA
EVKEYVSERVKEHHQSLDPNCPRDLTDCLLVEMEKEKHSAERLYTMDGITVTVADLFFAG
TETTSTTLRYGLLILMKYPEIEEKLHEEIDRVIGPSRIPAIKDRQEMPYMDAVVHEIQRF
ITLVPSNLPHEATRDTIFRGYLIPKGTVVVPTLDSVLYDNQEFPDPEKFKPEHFLNENGK
FKYSDYFKPFSTGKRVCAGEGLARMELFLLLCAILQHFNLKPLVDPKDIDLSPIHIGFGC
IPPRYKLCVIPRS
Phase 1 Metabolizing Enzyme 3 [top]
Enzyme 3 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 3 Gene Name CYP3A4
Enzyme 3 SwissProt ID P08684 Link Image
Enzyme 3 SNPs SNPJam Report Link Image
Enzyme 3 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 4 [top]
Enzyme 4 Name Cytochrome P450 2C8 (CYP2C8)
Enzyme 4 Gene Name CYP2C8
Enzyme 4 SwissProt ID P10632 Link Image
Enzyme 4 SNPs SNPJam Report Link Image
Enzyme 4 Protein Sequence >sp|P10632|CP2C8_HUMAN Cytochrome P450 2C8 (EC 1.14.14.1) 
MEPFVVLVLCLSFMLLFSLWRQSCRRRKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKV
YGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRW
KEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICS
VVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALT
RSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTE
TTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSD
LVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFK
KSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLP
PSYQICFIPV
Phase 1 Metabolizing Enzyme 5 [top]
Enzyme 5 Name Cytochrome P450 2C9 (CYP2C9)
Enzyme 5 Gene Name CYP2C9
Enzyme 5 SwissProt ID P11712 Link Image
Enzyme 5 SNPs SNPJam Report Link Image
Enzyme 5 Protein Sequence >sp|P11712|CP2C9_HUMAN Cytochrome P450 2C9 (EC 1.14.13.80) 
MDSLVVLVLCLSCLLLLSLWRQSSGRGKLPPGPTPLPVIGNILQIGIKDISKSLTNLSKV
YGPVFTLYFGLKPIVVLHGYEAVKEALIDLGEEFSGRGIFPLAERANRGFGIVFSNGKKW
KEIRRFSLMTLRNFGMGKRSIEDRVQEEARCLVEELRKTKASPCDPTFILGCAPCNVICS
IIFHKRFDYKDQQFLNLMEKLNENIKILSSPWIQICNNFSPIIDYFPGTHNKLLKNVAFM
KSYILEKVKEHQESMDMNNPQDFIDCFLMKMEKEKHNQPSEFTIESLENTAVDLFGAGTE
TTSTTLRYALLLLLKHPEVTAKVQEEIERVIGRNRSPCMQDRSHMPYTDAVVHEVQRYID
LLPTSLPHAVTCDIKFRNYLIPKGTTILISLTSVLHDNKEFPNPEMFDPHHFLDEGGNFK
KSKYFMPFSAGKRICVGEALAGMELFLFLTSILQNFNLKSLVDPKNLDTTPVVNGFASVP
PFYQLCFIPV
Phase 1 Metabolizing Enzyme 6 [top]
Enzyme 6 Name Cytochrome P450 2D6 (CYP2D6)
Enzyme 6 Gene Name CYP2D6
Enzyme 6 SwissProt ID P10635 Link Image
Enzyme 6 SNPs SNPJam Report Link Image
Enzyme 6 Protein Sequence >sp|P10635|CP2D6_HUMAN Cytochrome P450 2D6 (EC 1.14.14.1) 
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGMTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Phase 1 Metabolizing Enzyme 7 [top]
Enzyme 7 Name Cytochrome P450 2B6 (CYP2B6)
Enzyme 7 Gene Name CYP2B6
Enzyme 7 SwissProt ID P20813 Link Image
Enzyme 7 SNPs SNPJam Report Link Image
Enzyme 7 Protein Sequence >sp|P20813|CP2B6_HUMAN Cytochrome P450 2B6 (EC 1.14.14.1) 
MELSVLLFLALLTGLLLLLVQRHPNTHDRLPPGPRPLPLLGNLLQMDRRGLLKSFLRFRE
KYGDVFTVHLGPRPVVMLCGVEAIREALVDKAEAFSGRGKIAMVDPFFRGYGVIFANGNR
WKVLRRFSVTTMRDFGMGKRSVEERIQEEAQCLIEELRKSKGALMDPTFLFQSITANIIC
SIVFGKRFHYQDQEFLKMLNLFYQTFSLISSVFGQLFELFSGFLKYFPGAHRQVYKNLQE
INAYIGHSVEKHRETLDPSAPKDLIDTYLLHMEKEKSNAHSEFSHQNLNLNTLSLFFAGT
ETTSTTLRYGFLLMLKYPHVAERVYREIEQVIGPHRPPELHDRAKMPYTEAVIYEIQRFS
DLLPMGVPHIVTQHTSFRGYIIPKDTEVFLILSTALHDPHYFEKPDAFNPDHFLDANGAL
KKTEAFIPFSLGKRICLGEGIARAELFLFFTTILQNFSMASPVAPEDIDLTPQECGVGKI
PPTYQIRFLPR
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 841
Target 5 Name Gamma-aminobutyric-acid receptor subunit alpha-6
Target 5 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-6 precursor
Target 5 Gene Name GABRA6
Target 5 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-6 precursor 
MASSLPWLCIILWLENALGKLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEI
VLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLPPAFGGTSKIDQY
SRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
Target 5 Number of Residues 460
Target 5 Molecular Weight 51035
Target 5 Theoretical pI 8.40
Target 5 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 5 General Function Involved in GABA-A receptor activity
Target 5 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 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • 1-19
Target 5 Transmembrane Regions
  • 243-264
  • 269-290
  • 301-324
  • 420-441
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 1470364 Link Image
Target 5 UniProtKB/Swiss-Prot ID Q16445 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name GBRA6_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 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 5 GenBank Gene ID
Target 5 GeneCard ID GABRA6 Link Image
Target 5 GenAtlas ID GABRA6 Link Image
Target 5 HGNC ID HGNC:4080 Link Image
Target 5 Chromosome Location 5
Target 5 Locus 5q34
Target 5 SNPs SNPJam Report Link Image
Target 5 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 5 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 6 [top]
Target 6 ID 872
Target 6 Name Gamma-aminobutyric-acid receptor subunit alpha-1
Target 6 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
Target 6 Gene Name GABRA1
Target 6 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-1 precursor 
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target 6 Number of Residues 463
Target 6 Molecular Weight 51802
Target 6 Theoretical pI 9.61
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
  • 1-27
Target 6 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 422-443
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 31631 Link Image
Target 6 UniProtKB/Swiss-Prot ID P14867 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name GBRA1_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 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 6 GenBank Gene ID
Target 6 GeneCard ID GABRA1 Link Image
Target 6 GenAtlas ID GABRA1 Link Image
Target 6 HGNC ID HGNC:4075 Link Image
Target 6 Chromosome Location 5
Target 6 Locus 5q34-q35
Target 6 SNPs SNPJam Report Link Image
Target 6 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 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 4098
Target 7 Name Gamma-aminobutyric-acid receptor subunit beta-1
Target 7 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-1 precursor
Target 7 Gene Name GABRB1
Target 7 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-1 
MWTVQNRESLGLLSFPVMITMVCCAHSTNEPSNMSYVKETVDRLLKGYDIRLRPDFGGPP
VDVGMRIDVASIDMVSEVNMDYTLTMYFQQSWKDKRLSYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWNGGEGAVTGVNKIELPQFSIVDYKMVSKKVEFTTGAYPRLSLSFRLK
RNIGYFILQTYMPSTLITILSWVSFWINYDASAARVALGITTVLTMTTISTHLRETLPKI
PYVKAIDIYLMGCFVFVFLALLEYAFVNYIFFGKGPQKKGASKQDQSANEKNKLEMNKVQ
VDAHGNILLSTLEIRNETSGSEVLTSVSDPKATMYSYDSASIQYRKPLSSREAYGRALDR
HGVPSKGRIRRRASQLKVKIPDLTDVNSIDKWSRMFFPITFSLFNVVYWLYYVH
Target 7 Number of Residues 481
Target 7 Molecular Weight 54235
Target 7 Theoretical pI 9.01
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
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 7 General Function Not Available
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
  • 1-25
Target 7 Transmembrane Regions
  • 246-267
  • 271-293
  • 305-327
  • 452-473
Target 7 Essentiality Non Essential
Target 7 GenBank ID Protein 31635 Link Image
Target 7 UniProtKB/Swiss-Prot ID P18505 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name GBRB1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
Target 7 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 7 GenBank Gene ID
Target 7 GeneCard ID GABRB1 Link Image
Target 7 GenAtlas ID GABRB1 Link Image
Target 7 HGNC ID HGNC:4081 Link Image
Target 7 Chromosome Location 4
Target 7 Locus 4p12
Target 7 SNPs SNPJam Report Link Image
Target 7 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 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 4099
Target 8 Name Gamma-aminobutyric-acid receptor subunit beta-3
Target 8 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-3 precursor
Target 8 Gene Name GABRB3
Target 8 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-3 
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
Target 8 Number of Residues 480
Target 8 Molecular Weight 54116
Target 8 Theoretical pI 9.41
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
  • 451-472
Target 8 Essentiality Non Essential
Target 8 GenBank ID Protein 182925 Link Image
Target 8 UniProtKB/Swiss-Prot ID P28472 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name GBRB3_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Membrane
Target 8 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 8 GenBank Gene ID
Target 8 GeneCard ID GABRB3 Link Image
Target 8 GenAtlas ID GABRB3 Link Image
Target 8 HGNC ID HGNC:4083 Link Image
Target 8 Chromosome Location 15
Target 8 Locus 15q11.2-q12
Target 8 SNPs SNPJam Report Link Image
Target 8 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 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 4100
Target 9 Name Gamma-aminobutyric-acid receptor subunit beta-2
Target 9 Synonyms
  1. GABA(A
  2. Gamma-aminobutyric-acid receptor subunit beta-2 precursor
Target 9 Gene Name GABRB2
Target 9 Protein Sequence >Gamma-aminobutyric-acid receptor subunit beta-2 
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
Target 9 Number of Residues 481
Target 9 Molecular Weight 54607
Target 9 Theoretical pI 9.66
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
  • 245-266
  • 270-292
  • 304-326
  • 452-473
Target 9 Essentiality Non Essential
Target 9 GenBank ID Protein 455946 Link Image
Target 9 UniProtKB/Swiss-Prot ID P47870 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name GBRB2_HUMAN Link Image
Target 9 PDB ID Not Available
Target 9 Cellular Location
  • Membrane
Target 9 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 9 GenBank Gene ID
Target 9 GeneCard ID GABRB2 Link Image
Target 9 GenAtlas ID GABRB2 Link Image
Target 9 HGNC ID HGNC:4082 Link Image
Target 9 Chromosome Location 5
Target 9 Locus 5q34
Target 9 SNPs SNPJam Report Link Image
Target 9 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 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]

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.