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Showing drug card for Olanzapine (DB00334)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:26
Primary Accession Number DB00334
Secondary Accession Number
  • APRD00138
Name Olanzapine
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description Olanzapine is an atypical antipsychotic, approved by the FDA in 1996. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper ends in 2011.
Synonyms
  1. olanzapine
Brand Names
  1. Olansek
  2. Symbyax
  3. Zydis
  4. Zyprexa
  5. Zyprexa Intramuscular
  6. Zyprexa Zydis
Brand Mixtures Not Available
Chemical IUPAC Name 2-methyl-4-(4-methylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine
Chemical Formula C17H20N4S
Chemical Structure Structure
CAS Registry Number 132539-06-1
InChI Identifier InChI=1/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,18H,7-10H2,1-2H3
InChI Key WXPNDRBBWZMPQG-UHFFFAOYAO
KEGG Drug D00454 Link Image
KEGG Compound C07322 Link Image
PubChem Compound 4585 Link Image
PubChem Substance 197059 Link Image
ChEBI ID Not Available
PharmGKB ID PA450688 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02247099 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/symbyax.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Olanzapine Link Image
FDA Label
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference J. K. Chakrabarti et al., U.S. Pat. 5,229,382 (1991)
Average Molecular Weight 312.4320
Monoisotopic Molecular Weight 312.1409
State Solid
Melting Point 195oC
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility 5.06e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 2 Source: PhysProp
Predicted LogP 2.65 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -2.79 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 CN1CCN(CC1)C1=C2C=C(C)SC2=NC2=CC=CC=C2N1
Canonical SMILES CN1CCN(CC1)C1=C2C=C(C)SC2=NC2=CC=CC=C2N1
Drug Category
  • Antiemetics
  • Antipsychotic Agents
  • Antipsychotics
  • Serotonin Uptake Inhibitors
ATC Codes
AHFS Codes
  • 28:16.08.04
Indication For the treatment of schizophrenia and manic depression (bipolar disorder).
Pharmacology Olanzapine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, olanzapine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Mechanism of Action Olanzapine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Olanzapine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Olanzapine does not appear to block dopamine within the tubero-infundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with olanzapine.
Absorption Well absorbed, with approximately 40% of the dose metabolized before reaching the systemic circulation.
Toxicity Symptoms of an overdose include tachycardia, agitation, dysarthria, decreased consciousness and coma. Death has been reported after an acute overdose of 0.45g, but also survival after an acute overdose of 1500g.
Protein Binding 93%
Biotransformation Hepatic
Half Life 21 to 54 hours
Dosage Forms
Form Route
Powder, for solution Intramuscular
Tablet Oral
Tablet, orally disintegrating Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Donepezil Possible antagonism of action
Fluvoxamine Fluvoxamine increases the effect and toxicity of olanzapine
Galantamine Possible antagonism of action
Ritonavir Ritonavir decreases the effect of olanzapine
Rivastigmine Possible antagonism of action
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.
Pathways Not Available
General References
  1. McGlashan TH, Zipursky RB, Perkins D, Addington J, Miller TJ, Woods SW, Hawkins KA, Hoffman R, Lindborg S, Tohen M, Breier A: The PRIME North America randomized double-blind clinical trial of olanzapine versus placebo in patients at risk of being prodromally symptomatic for psychosis. I. Study rationale and design. Schizophr Res. 2003 May 1;61(1):7-18. [PubMed Link Image]
  2. Jakovljevic M, Sagud M, Mihaljevic-Peles A: Olanzapine in the treatment-resistant, combat-related PTSD--a series of case reports. Acta Psychiatr Scand. 2003 May;107(5):394-6; discussion 396. [PubMed Link Image]
  3. de Haan L, van Amelsvoort T, Rosien K, Linszen D: Weight loss after switching from conventional olanzapine tablets to orally disintegrating olanzapine tablets. Psychopharmacology (Berl). 2004 Sep;175(3):389-90. [PubMed Link Image]
  4. Pollack MH, Simon NM, Zalta AK, Worthington JJ, Hoge EA, Mick E, Kinrys G, Oppenheimer J: Olanzapine augmentation of fluoxetine for refractory generalized anxiety disorder: a placebo controlled study. Biol Psychiatry. 2006 Feb 1;59(3):211-5. Epub 2005 Sep 1. [PubMed Link Image]
  5. Sepede G, De Berardis D, Gambi F, Campanella D, La Rovere R, D'Amico M, Cicconetti A, Penna L, Peca S, Carano A, Mancini E, Salerno RM, Ferro FM: Olanzapine augmentation in treatment-resistant panic disorder: a 12-week, fixed-dose, open-label trial. J Clin Psychopharmacol. 2006 Feb;26(1):45-9. [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 1A2 (CYP1A2)
Targets
  1. D(1A) dopamine receptor
  2. Muscarinic acetylcholine receptor M3
  3. Muscarinic acetylcholine receptor M1
  4. Muscarinic acetylcholine receptor M5
  5. D(4) dopamine receptor
  6. Muscarinic acetylcholine receptor M4
  7. Histamine H1 receptor
  8. 5-hydroxytryptamine 2A receptor
  9. 5-hydroxytryptamine 2C receptor
  10. Muscarinic acetylcholine receptor M2
  11. Alpha-1B adrenergic receptor
  12. D(3) dopamine receptor
  13. D(2) dopamine receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 1A2 (CYP1A2)
Enzyme 1 Gene Name CYP1A2
Enzyme 1 SwissProt ID P05177 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >P05177|CP1A2_HUMAN Cytochrome P450 1A2 - Homo sapiens (Human). 
MALSQSVPFSATELLLASAIFCLVFWVLKGLRPRVPKGLKSPPEPWGWPLLGHVLTLGKN
PHLALSRMSQRYGDVLQIRIGSTPVLVLSRLDTIRQALVRQGDDFKGRPDLYTSTLITDG
QSLTFSTDSGPVWAARRRLAQNALNTFSIASDPASSSSCYLEEHVSKEAKALISRLQELM
AGPGHFDPYNQVVVSVANVIGAMCFGQHFPESSDEMLSLVKNTHEFVETASSGNPLDFFP
ILRYLPNPALQRFKAFNQRFLWFLQKTVQEHYQDFDKNSVRDITGALFKHSKKGPRASGN
LIPQEKIVNLVNDIFGAGFDTVTTAISWSLMYLVTKPEIQRKIQKELDTVIGRERRPRLS
DRPQLPYLEAFILETFRHSSFLPFTIPHSTTRDTTLNGFYIPKKCCVFVNQWQVNHDPEL
WEDPSEFRPERFLTADGTAINKPLSEKMMLFGMGKRRCIGEVLAKWEIFLFLAILLQQLE
FSVPPGVKVDLTPIYGLTMKHARCEHVQARRFSIN
Drug Target 1 [top]
Target 1 ID 23
Target 1 Name D(1A) dopamine receptor
Target 1 Synonyms Not Available
Target 1 Gene Name DRD1
Target 1 Protein Sequence >D(1A) dopamine receptor 
MRTLNTSAMDGTGLVVERDFSVRILTACFLSLLILSTLLGNTLVCAAVIRFRHLRSKVTN
FFVISLAVSDLLVAVLVMPWKAVAEIAGFWPFGSFCNIWVAFDIMCSTASILNLCVISVD
RYWAISSPFRYERKMTPKAAFILISVAWTLSVLISFIPVQLSWHKAKPTSPSDGNATSLA
ETIDNCDSSLSRTYAISSSVISFYIPVAIMIVTYTRIYRIAQKQIRRIAALERAAVHAKN
CQTTTGNGKPVECSQPESSFKMSFKRETKVLKTLSVIMGVFVCCWLPFFILNCILPFCGS
GETQPFCIDSNTFDVFVWFGWANSSLNPIIYAFNADFRKAFSTLLGCYRLCPATNNAIET
VSINNNGAAMFSSHHEPRGSISKECNLVYLIPHAVGSSEDLKKEEAAGIARPLEKLSPAL
SVILDYDTDVSLEKIQPITQNGQHPT
Target 1 Number of Residues 453
Target 1 Molecular Weight 49294
Target 1 Theoretical pI 8.34
Target 1 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
dopamine receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in dopamine receptor activity
Target 1 Specific Function This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 24-49
  • 61-87
  • 97-119
  • 139-163
  • 193-218
  • 273-299
  • 313-337
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 30397 Link Image
Target 1 UniProtKB/Swiss-Prot ID P21728 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name DRD1_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Cell membrane
  • endoplasmic reticulum membrane
  • m
  • multi-pass membrane protein. Endoplasmic reticulum
Target 1 Gene Sequence >1341 bp 
ATGAGGACTCTGAACACCTCTGCCATGGACGGGACTGGGCTGGTGGTGGAGAGGGACTTC
TCTGTTCGTATCCTCACTGCCTGTTTCCTGTCGCTGCTCATCCTGTCCACGCTCCTGGGG
AACACGCTGGTCTGTGCTGCCGTTATCAGGTTCCGACACCTGCGGTCCAAGGTGACCAAC
TTCTTTGTCATCTCCTTGGCTGTGTCAGATCTCTTGGTGGCCGTCCTGGTCATGCCCTGG
AAGGCAGTGGCTGAGATTGCTGGCTTCTGGCCCTTTGGGTCCTTCTGTAACATCTGGGTG
GCCTTTGACATCATGTGCTCCACTGCATCCATCCTCAACCTCTGTGTGATCAGCGTGGAC
AGGTATTGGGCTATCTCCAGCCCTTTCCGGTATGAGAGAAAGATGACCCCCAAGGCAGCC
TTCATCCTGATCAGTGTGGCATGGACCTTGTCTGTACTCATCTCCTTCATCCCAGTGCAG
CTCAGCTGGCACAAGGCAAAACCCACAAGCCCCTCTGATGGAAATGCCACTTCCCTGGCT
GAGACCATAGACAACTGTGACTCCAGCCTCAGCAGGACATATGCCATCTCATCCTCTGTA
ATAAGCTTTTACATCCCTGTGGCCATCATGATTGTCACCTACACCAGGATCTACAGGATT
GCTCAGAAACAAATACGGCGCATTGCGGCCTTGGAGAGGGCAGCAGTCCACGCCAAGAAT
TGCCAGACCACCACAGGTAATGGAAAGCCTGTCGAATGTTCTCAACCGGAAAGTTCTTTT
AAGATGTCCTTCAAAAGAGAAACTAAAGTCCTGAAGACTCTGTCGGTGATCATGGGTGTG
TTTGTGTGCTGTTGGCTACCTTTCTTCATCTTGAACTGCATTTTGCCCTTCTGTGGGTCT
GGGGAGACGCAGCCCTTCTGCATTGATTCCAACACCTTTGACGTGTTTGTGTGGTTTGGG
TGGGCTAATTCATCCTTGAACCCCATCATTTATGCCTTTAATGCTGATTTTCGGAAGGCA
TTTTCAACCCTCTTAGGATGCTACAGACTTTGCCCTGCGACGAATAATGCCATAGAGACG
GTGAGTATCAATAACAATGGGGCCGCGATGTTTTCCAGCCATCATGAGCCACGAGGCTCC
ATCTCCAAGGAGTGCAATCTGGTTTACCTGATCCCACATGCTGTGGGCTCCTCTGAGGAC
CTGAAAAAGGAGGAGGCAGCTGGCATCGCCAGACCCTTGGAGAAGCTGTCCCCAGCCCTA
TCGGTCATATTGGACTATGACACTGACGTCTCTCTGGAGAAGATCCAACCCATCACACAA
AACGGTCAGCACCCAACCTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID DRD1 Link Image
Target 1 GenAtlas ID DRD1 Link Image
Target 1 HGNC ID HGNC:3020 Link Image
Target 1 Chromosome Location 5
Target 1 Locus 5q35.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Jin H, Xie Z, George SR, O'Dowd BF: Palmitoylation occurs at cysteine 347 and cysteine 351 of the dopamine D(1) receptor. Eur J Pharmacol. 1999 Dec 15;386(2-3):305-12. [PubMed Link Image]
  2. Sunahara RK, Niznik HB, Weiner DM, Stormann TM, Brann MR, Kennedy JL, Gelernter JE, Rozmahel R, Yang YL, Israel Y, et al.: Human dopamine D1 receptor encoded by an intronless gene on chromosome 5. Nature. 1990 Sep 6;347(6288):80-3. [PubMed Link Image]
  3. Dearry A, Gingrich JA, Falardeau P, Fremeau RT Jr, Bates MD, Caron MG: Molecular cloning and expression of the gene for a human D1 dopamine receptor. Nature. 1990 Sep 6;347(6288):72-6. [PubMed Link Image]
  4. Zhou QY, Grandy DK, Thambi L, Kushner JA, Van Tol HH, Cone R, Pribnow D, Salon J, Bunzow JR, Civelli O: Cloning and expression of human and rat D1 dopamine receptors. Nature. 1990 Sep 6;347(6288):76-80. [PubMed Link Image]
  5. Ohara K, Ulpian C, Seeman P, Sunahara RK, Van Tol HH, Niznik HB: Schizophrenia: dopamine D1 receptor sequence is normal, but has DNA polymorphisms. Neuropsychopharmacology. 1993 Feb;8(2):131-5. [PubMed Link Image]
Target 1 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 51
Target 2 Name Muscarinic acetylcholine receptor M3
Target 2 Synonyms Not Available
Target 2 Gene Name CHRM3
Target 2 Protein Sequence >Muscarinic acetylcholine receptor M3 
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI
SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR
TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF
YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM
KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE
TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR
MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN
PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL
Target 2 Number of Residues 599
Target 2 Molecular Weight 66129
Target 2 Theoretical pI 9.62
Target 2 GO Classification
Function
amine receptor activity
muscarinic acetylcholine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in rhodopsin-like receptor activity
Target 2 Specific Function The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 68-91
  • 105-125
  • 143-164
  • 185-207
  • 230-252
  • 493-513
  • 528-547
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 32324 Link Image
Target 2 UniProtKB/Swiss-Prot ID P20309 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name ACM3_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1773 bp 
ATGACCTTGCACAATAACAGTACAACCTCGCCTTTGTTTCCAAACATCAGCTCCTCCTGG
ATACACAGCCCCTCCGATGCAGGGCTGCCCCCGGGAACCGTCACTCATTTCGGCAGCTAC
AATGTTTCTCGAGCAGCTGGCAATTTCTCCTCTCCAGACGGTACCACCGATGACCCTCTG
GGAGGTCATACCGTCTGGCAAGTGGTCTTCATCGCTTTCTTAACGGGCATCCTGGCCTTG
GTGACCATCATCGGCAACATCCTGGTAATTGTGTCATTTAAGGTCAACAAGCAGCTGAAG
ACGGTCAACAACTACTTCCTCTTAAGCCTGGCCTGTGCCGATCTGATTATCGGGGTCATT
TCAATGAATCTGTTTACGACCTACATCATCATGAATCGATGGGCCTTAGGGAACTTGGCC
TGTGACCTCTGGCTTGCCATTGACTACGTAGCCAGCAATGCCTCTGTTATGAATCTTCTG
GTCATCAGCTTTGACAGATACTTTTCCATCACGAGGCCGCTCACGTACCGAGCCAAACGA
ACAACAAAGAGAGCCGGTGTGATGATCGGTCTGGCTTGGGTCATCTCCTTTGTCCTTTGG
GCTCCTGCCATCTTGTTCTGGCAATACTTTGTTGGAAAGAGAACTGTGCCTCCGGGAGAG
TGCTTCATTCAGTTCCTCAGTGAGCCCACCATTACTTTTGGCACAGCCATCGCTGCTTTT
TATATGCCTGTCACCATTATGACTATTTTATACTGGAGGATCTATAAGGAAACTGAAAAG
CGTACCAAAGAGCTTGCTGGCCTGCAAGCCTCTGGGACAGAGGCAGAGACAGAAAACTTT
GTCCACCCCACGGGCAGTTCTCGAAGCTGCAGCAGTTACGAACTTCAACAGCAAAGCATG
AAACGCTCCAACAGGAGGAAGTATGGCCGCTGCCACTTCTGGTTCACAACCAAGAGCTGG
AAACCCAGCTCCGAGCAGATGGACCAAGACCACAGCAGCAGTGACAGTTGGAACAACAAT
GATGCTGCTGCCTCCCTGGAGAACTCCGCCTCCTCCGACGAGGAGGACATTGGCTCCGAG
ACGAGAGCCATCTACTCCATCGTGCTCAAGCTTCCGGGTCACAGCACCATCCTCAACTCC
ACCAAGTTACCCTCATCGGACAACCTGCAGGTGCCTGAGGAGGAGCTGGGGATGGTGGAC
TTGGAGAGGAAAGCCGACAAGCTGCAGGCCCAGAAGAGCGTGGACGATGGAGGCAGTTTT
CCAAAAAGCTTCTCCAAGCTTCCCATCCAGCTAGAGTCAGCCGTGGACACAGCTAAGACT
TCTGACGTCAACTCCTCAGTGGGTAAGAGCACGGCCACTCTACCTCTGTCCTTCAAGGAA
GCCACTCTGGCCAAGAGGTTTGCTCTGAAGACCAGAAGTCAGATCACTAAGCGGAAAAGG
ATGTCCCTGGTCAAGGAGAAGAAAGCGGCCCAGACCCTCAGTGCGATCTTGCTTGCCTTC
ATCATCACTTGGACCCCATACAACATCATGGTTCTGGTGAACACCTTTTGTGACAGCTGC
ATACCCAAAACCTTTTGGAATCTGGGCTACTGGCTGTGCTACATCAACAGCACCGTGAAC
CCCGTGTGCTATGCTCTGTGCAACAAAACATTCAGAACCACTTTCAAGATGCTGCTGCTG
TGCCAGTGTGACAAAAAAAAGAGGCGCAAGCAGCAGTACCAGCAGAGACAGTCGGTCATT
TTTCACAAGCGCGCACCCGAGCAGGCCTTGTAG
Target 2 GenBank Gene ID
Target 2 GeneCard ID CHRM3 Link Image
Target 2 GenAtlas ID CHRM3 Link Image
Target 2 HGNC ID HGNC:1952 Link Image
Target 2 Chromosome Location 1
Target 2 Locus 1q43
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Speek M: Antisense promoter of human L1 retrotransposon drives transcription of adjacent cellular genes. Mol Cell Biol. 2001 Mar;21(6):1973-85. [PubMed Link Image]
  2. Bonner TI, Young AC, Brann MR, Buckley NJ: Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron. 1988 Jul;1(5):403-10. [PubMed Link Image]
  3. Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ: Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. [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 103
Target 3 Name Muscarinic acetylcholine receptor M1
Target 3 Synonyms Not Available
Target 3 Gene Name CHRM1
Target 3 Protein Sequence >Muscarinic acetylcholine receptor M1 
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
Target 3 Number of Residues 467
Target 3 Molecular Weight 51421
Target 3 Theoretical pI 9.67
Target 3 GO Classification
Function
amine receptor activity
muscarinic acetylcholine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Involved in rhodopsin-like receptor activity
Target 3 Specific Function The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 25-47
  • 62-82
  • 100-121
  • 142-164
  • 187-209
  • 367-387
  • 402-421
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 34451 Link Image
Target 3 UniProtKB/Swiss-Prot ID P11229 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name ACM1_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >1383 bp 
ATGAACACTTCAGCCCCACCTGCTGTCAGCCCCAACATCACCGTCCTGGCACCAGGAAAG
GGTCCCTGGCAAGTGGCCTTCATTGGGATCACCACGGGCCTCCTGTCGCTAGCCACAGTG
ACAGGCAACCTGCTGGTACTCATCTCTTTCAAGGTCAACACGGAGCTCAAGACAGTCAAT
AACTACTTCCTGCTGAGCCTGGCCTGTGCTGACCTCATCATCGGTACCTTCTCCATGAAC
CTCTATACCACGTACCTGCTCATGGGCCACTGGGCTCTGGGCACGCTGGCTTGTGACCTC
TGGCTGGCCCTGGACTATGTGGCCAGCAATGCCTCCGTCATGAATCTGCTGCTCATCAGC
TTTGACCGCTACTTCTCCGTGACTCGGCCCCTGAGCTACCGTGCCAAGCGCACACCCCGC
CGGGCAGCTCTGATGATCGGCCTGGCCTGGCTGGTTTCCTTTGTGCTCTGGGCCCCAGCC
ATCCTCTTCTGGCAGTACCTGGTAGGGGAGCGGACAGTGCTAGCTGGGCAGTGCTACATC
CAGTTCCTCTCCCAGCCCATCATCACCTTTGGCACAGCCATGGCTGCCTTCTACCTCCCT
GTCACAGTCATGTGCACGCTCTACTGGCGCATCTACCGGGAGACAGAGAACCGAGCACGG
GAGCTGGCAGCCCTTCAGGGCTCCGAGACGCCAGGCAAAGGGGGTGGCAGCAGCAGCAGC
TCAGAGAGGTCTCAGCCAGGGGCTGAGGGCTCACCAGAGACTCCTCCAGGCCGCTGCTGT
CGCTGCTGCCGGGCCCCCAGGCTGCTGCAGGCCTACAGCTGGAAGGAAGAAGAGGAAGAG
GACGAAGGCTCCATGGAGTCCCTCACATCCTCAGAGGGAGAGGAGCCTGGCTCCGAAGTG
GTGATCAAGATGCCAATGGTGGACCCCGAGGCACAGGCCCCCACCAAGCAGCCCCCACGG
AGCTCCCCAAATACAGTCAAGAGGCCGACTAAGAAAGGGCGTGATCGAGCTGGCAAGGGC
CAGAAGCCCCGTGGAAAGGAGCAGCTGGCCAAGCGGAAGACCTTCTCGCTGGTCAAGGAG
AAGAAGGCGGCTCGGACCCTGAGTGCCATCCTCCTGGCCTTCATCCTCACCTGGACACCG
TACAACATCATGGTGCTGGTGTCCACCTTCTGCAAGGACTGTGTTCCCGAGACCCTGTGG
GAGCTGGGCTACTGGCTGTGCTACGTCAACAGCACCATCAACCCCATGTGCTACGCACTC
TGCAACAAAGCCTTCCGGGACACCTTTCGCCTGCTGCTGCTTTGCCGCTGGGACAAGAGA
CGCTGGCGCAAGATCCCCAAGCGCCCTGGCTCCGTGCACCGCACTCCCTCCCGCCAATGC
TGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID CHRM1 Link Image
Target 3 GenAtlas ID CHRM1 Link Image
Target 3 HGNC ID HGNC:1950 Link Image
Target 3 Chromosome Location 11
Target 3 Locus 11q13
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Arden JR, Nagata O, Shockley MS, Philip M, Lameh J, Sadee W: Mutational analysis of third cytoplasmic loop domains in G-protein coupling of the HM1 muscarinic receptor. Biochem Biophys Res Commun. 1992 Nov 16;188(3):1111-5. [PubMed Link Image]
  2. Chapman CG, Browne MJ: Isolation of the human ml (Hml) muscarinic acetylcholine receptor gene by PCR amplification. Nucleic Acids Res. 1990 Apr 25;18(8):2191. [PubMed Link Image]
  3. Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ: Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. [PubMed Link Image]
  4. Allard WJ, Sigal IS, Dixon RA: Sequence of the gene encoding the human M1 muscarinic acetylcholine receptor. Nucleic Acids Res. 1987 Dec 23;15(24):10604. [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 274
Target 4 Name Muscarinic acetylcholine receptor M5
Target 4 Synonyms Not Available
Target 4 Gene Name CHRM5
Target 4 Protein Sequence >Muscarinic acetylcholine receptor M5 
MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQ
LKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMN
LLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPL
DECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAE
KRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQL
TTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPN
YLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNP
NPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLG
YWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP
Target 4 Number of Residues 540
Target 4 Molecular Weight 60074
Target 4 Theoretical pI 9.64
Target 4 GO Classification
Function
amine receptor activity
muscarinic acetylcholine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Involved in rhodopsin-like receptor activity
Target 4 Specific Function The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 30-53
  • 67-87
  • 105-126
  • 147-169
  • 192-214
  • 444-464
  • 479-498
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 177988 Link Image
Target 4 UniProtKB/Swiss-Prot ID P08912 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name ACM5_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1599 bp 
ATGGAAGGGGATTCTTACCACAATGCAACCACCGTCAATGGCACCCCAGTAAATCACCAG
CCTTTGGAACGCCACAGGTTGTGGGAAGTCATCACCATTGCAGCTGTGACTGCTGTGGTA
AGCCTGATCACCATTGTGGGCAATGTCTTGGTCATGATCTCCTTCAAAGTCAACAGCCAG
CTCAAGACAGTTAACAACTATTACCTGCTCAGCTTAGCCTGTGCAGATCTCATCATTGGA
ATCTTCTCCATGAACCTCTACACCACCTACATCCTCATGGGACGCTGGGCTCTCGGGAGT
CTGGCTTGTGACCTTTGGCTTGCACTGGACTACGTGGCCAGCAACGCTTCTGTCATGAAC
CTTCTGGTGATCAGTTTTGACCGTTACTTTTCCATCACAAGACCCTTGACATATCGGGCC
AAGCGTACTCCGAAAAGGGCTGGCATCATGATTGGCTTGGCCTGGCTGATCTCCTTCATC
CTCTGGGCCCCAGCAATCCTCTGCTGGCAGTACTTGGTTGGGAAGCGGACAGTTCCACTG
GATGAGTGCCAGATCCAGTTTCTCTCTGAGCCCACCATCACTTTTGGCACTGCCATTGCT
GCCTTCTACATCCCTGTTTCTGTCATGACCATCCTCTACTGTCGAATCTACCGGGAAACA
GAGAAGCGAACCAAGGACCTGGCTGACCTCCAGGGTTCTGACTCTGTGACCAAAGCTGAG
AAGAGAAAGCCAGCTCATAGGGCTCTGTTCAGATCCTGCTTGCGCTGTCCTCGACCCACC
CTGGCCCAGCGGGAAAGGAACCAGGCCTCCTGGTCATCCTCCCGCAGGAGCACCTCCACC
ACTGGGAAGCCATCCCAAGCCACTGGCCCAAGCGCCAATTGGGCCAAAGCTGAGCAGCTC
ACCACCTGTAGCAGCTACCCTTCCTCAGAGGATGAGGACAAGCCCGCCACTGACCCTGTC
CTCCAAGTGGTCTACAAGAGTCAGGGTAAGGAAAGCCCAGGGGAAGAATTCAGTGCTGAA
GAGACTGAGGAAACTTTTGTGAAAGCTGAAACTGAAAAAAGTGACTATGACACCCCAAAC
TACCTTCTGTCTCCAGCAGCTGCTCATAGACCCAAGAGTCAGAAATGTGTGGCCTATAAG
TTCCGATTGGTGGTAAAAGCTGACGGGAACCAGGAGACCAACAATGGCTGTCACAAGGTG
AAAATCATGCCCTGCCCCTTCCCAGTGGCCAAGGAACCTTCAACGAAAGGCCTCAATCCC
AACCCCAGCCATCAAATGACCAAACGAAAGAGAGTGGTCCTAGTCAAAGAGAGGAAAGCA
GCCCAGACACTGAGTGCCATTCTCCTGGCCTTCATCATCACATGGACCCCGTATAACATC
ATGGTCCTGGTTTCTACCTTCTGTGACAAGTGTGTCCCAGTCACCCTGTGGCACTTGGGC
TATTGGTTGTGCTATGTCAATAGCACTGTCAACCCCATCTGCTATGCCCTCTGCAACAGA
ACCTTCAGGAAGACCTTTAAGATGCTGCTTCTCTGCCGATGGAAAAAGAAAAAAGTGGAA
GAGAAGTTGTACTGGCAGGGGAACAGCAAGCTACCCTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID CHRM5 Link Image
Target 4 GenAtlas ID CHRM5 Link Image
Target 4 HGNC ID HGNC:1954 Link Image
Target 4 Chromosome Location 15
Target 4 Locus 15q26
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Bonner TI, Young AC, Brann MR, Buckley NJ: Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron. 1988 Jul;1(5):403-10. [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 432
Target 5 Name D(4) dopamine receptor
Target 5 Synonyms
  1. D(2C) dopamine receptor
  2. Dopamine D4 receptor
Target 5 Gene Name DRD4
Target 5 Protein Sequence >D(4) dopamine receptor 
MGNRSTADADGLLAGRGPAAGASAGASAGLAGQGAAALVGGVLLIGAVLAGNSLVCVSVA
TERALQTPTNSFIVSLAAADLLLALLVLPLFVYSEVQGGAWLLSPRLCDALMAMDVMLCT
ASIFNLCAISVDRFVAVAVPLRYNRQGGSRRQLLLIGATWLLSAAVAAPVLCGLNDVRGR
DPAVCRLEDRDYVVYSSVCSFFLPCPLMLLLYWATFRGLQRWEVARRAKLHGRAPRRPSG
PGPPSPTPPAPRLPQDPCGPDCAPPAPGLPRGPCGPDCAPAAPGLPPDPCGPDCAPPAPG
LPQDPCGPDCAPPAPGLPRGPCGPDCAPPAPGLPQDPCGPDCAPPAPGLPPDPCGSNCAP
PDAVRAAALPPQTPPQTRRRRRAKITGRERKAMRVLPVVVGAFLLCWTPFFVVHITQALC
PACSVPPRLVSAVTWLGYVNSALNPVIYTVFNAEFRNVFRKALRACC
Target 5 Number of Residues 474
Target 5 Molecular Weight 48361
Target 5 Theoretical pI 8.37
Target 5 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
dopamine receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 5 General Function Cell cycle control, cell division, chromosome partitioning
Target 5 Specific Function This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 38-60
  • 71-93
  • 110-131
  • 152-175
  • 192-213
  • 395-417
  • 427-449
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 291946 Link Image
Target 5 UniProtKB/Swiss-Prot ID P21917 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name DRD4_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >1404 bp 
ATGGGGAACCGCAGCACCGCGGACGCGGACGGGCTGCTGGCTGGGCGCGGGCCGGCCGCG
GGGGCATCTGCGGGGGCATCTGCGGGGCTGGCTGGGCAGGGCGCGGCGGCGCTGGTGGGG
GGCGTGCTGCTCATCGGCGCGGTGCTCGCGGGGAACTCGCTCGTGTGCGTGAGCGTGGCC
ACCGAGCGCGCCCTGCAGACGCCCACCAACTCCTTCATCGTGAGCCTGGCGGCCGCCGAC
CTCCTCCTCGCTCTCCTGGTGCTGCCGCTCTTCGTCTACTCCGAGGTCCAGGGTGGCGCG
TGGCTGCTGAGCCCCCGCCTGTGCGACGCCCTCATGGCCATGGACGTCATGCTGTGCACC
GCCTCCATCTTCAACCTGTGCGCCATCAGCGTGGACAGGTTCGTGGCCGTGGCCGTGCCG
CTGCGCTACAACCGGCAGGGTGGGAGCCGCCGGCAGCTGCTGCTCATCGGCGCCACGTGG
CTGCTGTCCGCGGCGGTGGCGGCGCCCGTACTGTGCGGCCTCAACGACGTGCGCGGCCGC
GACCCCGCCGTGTGCCGCCTGGAGGACCGCGACTACGTGGTCTACTCGTCCGTGTGCTCC
TTCTTCCTACCCTGCCCGCTCATGCTGCTGCTCTACTGGGCCACGTTCCGCGGCCTGCAG
CGCTGGGAGGTGGCACGTCGCGCCAAGCTGCACGGCCGCGCGCCCCGCCGACCCAGCGGC
CCTGGCCCGCCTTCCCCCACGCCACCCGCGCCCCGCCTCCCCCAGGACCCCTGCGGCCCC
GACTGTGCGCCCCCCGCGCCCGGCCTTCCCCGGGGTCCCTGCGGCCCCGACTGTGCGCCC
GCCGCGCCCGGCCTCCCCCCGGACCCCTGCGGCCCCGACTGTGCGCCCCCCGCGCCCGGC
CTCCCCCAGGACCCCTGCGGCCCCGACTGTGCGCCCCCCGCGCCCGGCCTTCCCCGGGGT
CCCTGCGGCCCCGACTGTGCGCCCCCCGCGCCCGGCCTCCCCCAGGACCCCTGCGGCCCC
GACTGTGCGCCCCCCGCGCCCGGCCTCCCCCCGGACCCCTGCGGCTCCAACTGTGCTCCC
CCCGACGCCGTCAGAGCCGCCGCGCTCCCACCCCAGACTCCACCGCAGACCCGCAGGAGG
CGGCGTGCCAAGATCACCGGCCGGGAGCGCAAGGCCATGAGGGTCCTGCCGGTGGTGGTC
GGGGCCTTCCTGCTGTGCTGGACGCCCTTCTTCGTGGTGCACATCACGCAGGCGCTGTGT
CCTGCCTGCTCCGTGCCCCCGCGGCTGGTCAGCGCCGTCACCTGGCTGGGCTACGTCAAC
AGCGCCCTCAACCCCGTCATCTACACTGTCTTCAACGCCGAGTTCCGCAACGTCTTCCGC
AAGGCCCTGCGTGCCTGCTGCTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID DRD4 Link Image
Target 5 GenAtlas ID DRD4 Link Image
Target 5 HGNC ID HGNC:3025 Link Image
Target 5 Chromosome Location 11
Target 5 Locus 11p15.5
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Van Tol HH, Wu CM, Guan HC, Ohara K, Bunzow JR, Civelli O, Kennedy J, Seeman P, Niznik HB, Jovanovic V: Multiple dopamine D4 receptor variants in the human population. Nature. 1992 Jul 9;358(6382):149-52. [PubMed Link Image]
  2. Livingstone CD, Strange PG, Naylor LH: Molecular modelling of D2-like dopamine receptors. Biochem J. 1992 Oct 1;287 ( Pt 1):277-82. [PubMed Link Image]
  3. Van Tol HH, Bunzow JR, Guan HC, Sunahara RK, Seeman P, Niznik HB, Civelli O: Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature. 1991 Apr 18;350(6319):610-4. [PubMed Link Image]
  4. Seeman P, Ulpian C, Chouinard G, Van Tol HH, Dwosh H, Lieberman JA, Siminovitch K, Liu IS, Waye J, Voruganti P, et al.: Dopamine D4 receptor variant, D4GLYCINE194, in Africans, but not in Caucasians: no association with schizophrenia. Am J Med Genet. 1994 Dec 15;54(4):384-90. [PubMed Link Image]
Target 5 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. Hutchison KE, Ray L, Sandman E, Rutter MC, Peters A, Davidson D, Swift R: The effect of olanzapine on craving and alcohol consumption. Neuropsychopharmacology. 2006 Jun;31(6):1310-7. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 450
Target 6 Name Muscarinic acetylcholine receptor M4
Target 6 Synonyms Not Available
Target 6 Gene Name CHRM4
Target 6 Protein Sequence >Muscarinic acetylcholine receptor M4 
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVN
RQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASV
MNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTV
PDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAK
TLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGS
ATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIV
PATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMV
LVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
Target 6 Number of Residues 486
Target 6 Molecular Weight 53050
Target 6 Theoretical pI 10.34
Target 6 GO Classification
Function
amine receptor activity
muscarinic acetylcholine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 6 General Function Involved in rhodopsin-like receptor activity
Target 6 Specific Function The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 32-54
  • 69-89
  • 107-128
  • 149-171
  • 194-216
  • 402-422
  • 437-456
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 61970253 Link Image
Target 6 UniProtKB/Swiss-Prot ID P08173 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name ACM4_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >1440 bp 
ATGGCCAACTTCACACCTGTCAATGGCAGCTCGGGCAATCAGTCCGTGCGCCTGGTCACG
TCATCATCCCACAATCGCTATGAGACGGTGGAAATGGTCTTCATTGCCACAGTGACAGGC
TCCCTGAGCCTGGTGACTGTCGTGGGCAACATCCTGGTGATGCTGTCCATCAAGGTCAAC
AGGCAGCTGCAGACAGTCAACAACTACTTCCTCTTCAGCCTGGCGTGTGCTGATCTCATC
ATAGGCGCCTTCTCCATGAACCTCTACACCGTGTACATCATCAAGGGCTACTGGCCCCTG
GGCGCCGTGGTCTGCGACCTGTGGCTGGCCCTGGACTACGTGGTGAGCAACGCCTCCGTC
ATGAACCTTCTCATCATCAGCTTTGACCGCTACTTCTGCGTCACCAAGCCTCTCACCTAC
CCTGCCCGGCGCACCACCAAGATGGCAGGCCTCATGATTGCTGCTGCCTGGGTACTGTCC
TTCGTGCTCTGGGCGCCTGCCATCTTGTTCTGGCAGTTTGTGGTGGGTAAGCGGACGGTG
CCCGACAACCAGTGCTTCATCCAGTTCCTGTCCAACCCAGCAGTGACCTTTGGCACAGCC
ATTGCTGCCTTCTACCTGCCTGTGGTCATCATGACGGTGCTGTACATCCACATCTCCCTG
GCCAGTCGCAGCCGAGTCCACAAGCACCGGCCCGAGGGCCCGAAGGAGAAGAAAGCCAAG
ACGCTGGCCTTCCTCAAGAGCCCACTAATGAAGCAGAGCGTCAAGAAGCCCCCGCCCGGG
GAGGCCGCCCGGGAGGAGCTGCGCAATGGCAAGCTGGAGGAGGCCCCCCCGCCAGCGCTG
CCACCGCCACCGCGCCCCGTGGCTGATAAGGACACTTCCAATGAGTCCAGCTCAGGCAGT
GCCACCCAGAACACCAAGGAACGCCCAGCCACAGAGCTGTCCACCACAGAGGCCACCACG
CCCGCCATGCCCGCCCCTCCCCTGCAGCCGCGGGCCCTCAACCCAGCCTCCAGATGGTCC
AAGATCCAGATTGTGACGAAGCAGACAGGCAATGAGTGTGTGACAGCCATTGAGATTGTG
CCTGCCACGCCGGCTGGCATGCGCCCTGCGGCCAACGTGGCCCGCAAGTTCGCCAGCATC
GCTCGCAACCAGGTGCGCAAGAAGCGGCAGATGGCGGCCCGGGAGCGCAAAGTGACACGA
ACGATCTTTGCCATTCTGCTAGCCTTCATCCTCACCTGGACGCCCTACAACGTCATGGTC
CTGGTGAACACCTTCTGCCAGAGCTGCATCCCTGACACGGTGTGGTCCATTGGCTACTGG
CTCTGCTACGTCAACAGCACCATCAACCCTGCCTGCTATGCTCTGTGCAACGCCACCTTT
AAAAAGACCTTCCGGCACCTGCTGCTGTGCCAGTATCGGAACATCGGCACTGCCAGGTAG
Target 6 GenBank Gene ID
Target 6 GeneCard ID CHRM4 Link Image
Target 6 GenAtlas ID CHRM4 Link Image
Target 6 HGNC ID HGNC:1953 Link Image
Target 6 Chromosome Location 11
Target 6 Locus 11p12-p11.2
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Bonner TI, Buckley NJ, Young AC, Brann MR: Identification of a family of muscarinic acetylcholine receptor genes. Science. 1987 Jul 31;237(4814):527-32. [PubMed Link Image]
  2. Bonner TI, Young AC, Brann MR, Buckley NJ: Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron. 1988 Jul;1(5):403-10. [PubMed Link Image]
  3. Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ: Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. [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 492
Target 7 Name Histamine H1 receptor
Target 7 Synonyms Not Available
Target 7 Gene Name HRH1
Target 7 Protein Sequence >Histamine H1 receptor 
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Target 7 Number of Residues 495
Target 7 Molecular Weight 55785
Target 7 Theoretical pI 9.58
Target 7 GO Classification
Function
amine receptor activity
histamine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 7 General Function Involved in rhodopsin-like receptor activity
Target 7 Specific Function In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • 30-49
  • 64-83
  • 102-123
  • 146-165
  • 190-210
  • 419-438
  • 451-470
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 510296 Link Image
Target 7 UniProtKB/Swiss-Prot ID P35367 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name HRH1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 Gene Sequence >1464 bp 
ATGAGCCTCCCCAATTCCTCCTGCCTCTTAGAAGACAAGATGTGTGAGGGCAACAAGACC
ACTATGGCCAGCCCCCAGCTGATGCCCCTGGTGGTGGTCCTGAGCACTATCTGCTTGGTC
ACAGTAGGGCTCAACCTGCTGGTGCTGTATGCCGTACGGAGTGAGCGGAAGCTCCACACT
GTGGGGAACCTGTACATCGTCAGCCTCTCGGTGGCGGACTTGATCGTGGGTGCCGTCGTC
ATGCCTATGAACATCCTCTACCTGCTCATGTCCAAGTGGTCACTGGGCCGTCCTCTCTGC
CTCTTTTGGCTTTCCATGGACTATGTGGCCAGCACAGCGTCCATTTTCAGTGTCTTCATC
CTGTGCATTGATCGCTACCGCTCTGTCCAGCAGCCCCTCAGGTACCTTAAGTATCGTACC
AAGACCCGAGCCTCGGCCACCATTCTGGGGGCCTGGTTTCTCTCTTTTCTGTGGGTTATT
CCCATTCTAGGCTGGAATCACTTCATGCAGCAGACCTCGGTGCGCCGAGAGGACAAGTGT
GAGACAGACTTCTATGATGTCACCTGGTTCAAGGTCATGACTGCCATCATCAACTTCTAC
CTGCCCACCTTGCTCATGCTCTGGTTCTATGCCAAGATCTACAAGGCCGTACGACAACAC
TGCCAGCACCGGGAGCTCATCAATAGGTCCCTCCCTTCCTTCTCAGAAATTAAGCTGAGG
CCAGAGAACCCCAAGGGGGATGCCAAGAAACCAGGGAAGGAGTCTCCCTGGGAGGTTCTG
AAAAGGAAGCCAAAAGATGCTGGTGGTGGATCTGTCTTGAAGTCACCATCCCAAACCCCC
AAGGAGATGAAATCCCCAGTTGTCTTCAGCCAAGAGGATGATAGAGAAGTAGACAAACTC
TACTGCTTTCCACTTGATATTGTGCACATGCAGGCTGCGGCAGAGGGGAGTAGCAGGGAC
TATGTAGCCGTCAACCGGAGCCATGGCCAGCTCAAGACAGATGAGCAGGGCCTGAACACA
CATGGGGCCAGCGAGATATCAGAGGATCAGATGTTAGGTGATAGCCAATCCTTCTCTCGA
ACGGACTCAGATACCACCACAGAGACAGCACCAGGCAAAGGCAAATTGAGGAGTGGGTCT
AACACAGGCCTGGATTACATCAAGTTTACTTGGAAGAGGCTCCGCTCGCATTCAAGACAG
TATGTATCTGGGTTGCACATGAACCGCGAAAGGAAGGCCGCCAAACAGTTGGGTTTTATC
ATGGCAGCCTTCATCCTCTGCTGGATCCCTTATTTCATCTTCTTCATGGTCATTGCCTTC
TGCAAGAACTGTTGCAATGAACATTTGCACATGTTCACCATCTGGCTGGGCTACATCAAC
TCCACACTGAACCCCCTCATCTACCCCTTGTGCAATGAGAACTTCAAGAAGACATTCAAG
AGAATTCTGCATATTCGCTCCTAA
Target 7 GenBank Gene ID
Target 7 GeneCard ID HRH1 Link Image
Target 7 GenAtlas ID HRH1 Link Image
Target 7 HGNC ID HGNC:5182 Link Image
Target 7 Chromosome Location 3
Target 7 Locus 3p25
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Fukui H, Fujimoto K, Mizuguchi H, Sakamoto K, Horio Y, Takai S, Yamada K, Ito S: Molecular cloning of the human histamine H1 receptor gene. Biochem Biophys Res Commun. 1994 Jun 15;201(2):894-901. [PubMed Link Image]
  2. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH: Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem Biophys Res Commun. 1993 Dec 30;197(3):1601-8. [PubMed Link Image]
Target 7 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. Poyurovsky M, Pashinian A, Levi A, Weizman R, Weizman A: The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. [PubMed Link Image]
  3. Altschuler EL, Kast RE: Using histamine (H1) antagonists, in particular atypical antipsychotics, to treat anemia of chronic disease via interleukin-6 suppression. Med Hypotheses. 2005;65(1):65-7. [PubMed Link Image]
  4. Rasmussen K, Benvenga MJ, Bymaster FP, Calligaro DO, Cohen IR, Falcone JF, Hemrick-Luecke SK, Martin FM, Moore NA, Nisenbaum LK, Schaus JM, Sundquist SJ, Tupper DE, Wiernicki TR, Nelson DL: Preclinical pharmacology of FMPD [6-fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-th ia-4,9-diaza-benzo[f]azulene]: a potential novel antipsychotic with lower histamine H1 receptor affinity than olanzapine. J Pharmacol Exp Ther. 2005 Dec;315(3):1265-77. Epub 2005 Sep 1. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 502
Target 8 Name 5-hydroxytryptamine 2A receptor
Target 8 Synonyms
  1. 5- HT-2
  2. 5-HT-2A
  3. Serotonin receptor 2A
Target 8 Gene Name HTR2A
Target 8 Protein Sequence >5-hydroxytryptamine 2A receptor 
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
Target 8 Number of Residues 478
Target 8 Molecular Weight 52604
Target 8 Theoretical pI 7.72
Target 8 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 8 General Function Involved in rhodopsin-like receptor activity
Target 8 Specific Function This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • 76-99
  • 111-132
  • 148-171
  • 192-215
  • 234-254
  • 325-346
  • 363-384
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 36431 Link Image
Target 8 UniProtKB/Swiss-Prot ID P28223 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name 5HT2A_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Cell membrane
  • multi-pass membrane protein. Localizes to the post-synaptic thickening of axo-dendrit
Target 8 Gene Sequence >1416 bp 
ATGGATATTCTTTGTGAAGAAAATACTTCTTTGAGCTCAACTACGAACTCCCTAATGCAA
TTAAATGATGACACCAGGCTCTACAGTAATGACTTTAACTCTGGAGAAGCTAACACTTCT
GATGCATTTAACTGGACAGTCGACTCTGAAAATCGAACCAACCTTTCCTGTGAAGGGTGC
CTCTCACCGTCGTGTCTCTCCTTACTTCATCTCCAGGAAAAAAACTGGTCTGCTTTACTG
ACAGCCGTAGTGATTATTCTAACTATTGCTGGAAACATACTCGTCATCATGGCAGTGTCC
CTAGAGAAAAAGCTGCAGAATGCCACCAACTATTTCCTGATGTCACTTGCCATAGCTGAT
ATGCTGCTGGGTTTCCTTGTCATGCCCGTGTCCATGTTAACCATCCTGTATGGGTACCGG
TGGCCTCTGCCGAGCAAGCTTTGTGCAGTCTGGATTTACCTGGACGTGCTCTTCTCCACG
GCCTCCATCATGCACCTCTGCGCCATCTCGCTGGACCGCTACGTCGCCATCCAGAATCCC
ATCCACCACAGCCGCTTCAACTCCAGAACTAAGGCATTTCTGAAAATCATTGCTGTTTGG
ACCATATCAGTAGGTATATCCATGCCAATACCAGTCTTTGGGCTACAGGACGATTCGAAG
GTCTTTAAGGAGGGGAGTTGCTTACTCGCCGATGATAACTTTGTCCTGATCGGCTCTTTT
GTGTCATTTTTCATTCCCTTAACCATCATGGTGATCACCTACTTTCTAACTATCAAGTCA
CTCCAGAAAGAAGCTACTTTGTGTGTAAGTGATCTTGGCACACGGGCCAAATTAGCTTCT
TTCAGCTTCCTCCCTCAGAGTTCTTTGTCTTCAGAAAAGCTCTTCCAGCGGTCGATCCAT
AGGGAGCCAGGGTCCTACACAGGCAGGAGGACTATGCAGTCCATCAGCAATGAGCAAAAG
GCATGCAAGGTGCTGGGCATCGTCTTCTTCCTGTTTGTGGTGATGTGGTGCCCTTTCTTC
ATCACAAACATCATGGCCGTCATCTGCAAAGAGTCCTGCAATGAGGATGTCATTGGGGCC
CTGCTCAATGTGTTTGTTTGGATCGGTTATCTCTCTTCAGCAGTCAACCCACTAGTCTAC
ACACTGTTCAACAAGACCTATAGGTCAGCCTTTTCACGGTATATTCAGTGTCAGTACAAG
GAAAACAAAAAACCATTGCAGTTAATTTTAGTGAACACAATACCGGCTTTGGCCTACAAG
TCTAGCCAACTTCAAATGGGACAAAAAAAGAATTCAAAGCAAGATGCCAAGACAACAGAT
AATGACTGCTCAATGGTTGCTCTAGGAAAGCAGCATTCTGAAGAGGCTTCTAAAGACAAT
AGCGACGGAGTGAATGAAAAGGTGAGCTGTGTGTGA
Target 8 GenBank Gene ID
Target 8 GeneCard ID HTR2A Link Image
Target 8 GenAtlas ID HTR2A Link Image
Target 8 HGNC ID HGNC:5293 Link Image
Target 8 Chromosome Location 13
Target 8 Locus 13q14-q21
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Marshall SE, Bird TG, Hart K, Welsh KI: Unified approach to the analysis of genetic variation in serotonergic pathways. Am J Med Genet. 1999 Dec 15;88(6):621-7. [PubMed Link Image]
  3. Becamel C, Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, Lubbert H, Ullmer C: Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem. 2001 Apr 20;276(16):12974-82. Epub 2001 Jan 9. [PubMed Link Image]
  4. Chen K, Yang W, Grimsby J, Shih JC: The human 5-HT2 receptor is encoded by a multiple intron-exon gene. Brain Res Mol Brain Res. 1992 Jun;14(1-2):20-6. [PubMed Link Image]
  5. Stam NJ, Van Huizen F, Van Alebeek C, Brands J, Dijkema R, Tonnaer JA, Olijve W: Genomic organization, coding sequence and functional expression of human 5-HT2 and 5-HT1A receptor genes. Eur J Pharmacol. 1992 Oct 1;227(2):153-62. [PubMed Link Image]
  6. Saltzman AG, Morse B, Whitman MM, Ivanshchenko Y, Jaye M, Felder S: Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1469-78. [PubMed Link Image]
  7. Cook EH Jr, Fletcher KE, Wainwright M, Marks N, Yan SY, Leventhal BL: Primary structure of the human platelet serotonin 5-HT2A receptor: identify with frontal cortex serotonin 5-HT2A receptor. J Neurochem. 1994 Aug;63(2):465-9. [PubMed Link Image]
  8. Erdmann J, Shimron-Abarbanell D, Rietschel M, Albus M, Maier W, Korner J, Bondy B, Chen K, Shih JC, Knapp M, Propping P, Nothen MM: Systematic screening for mutations in the human serotonin-2A (5-HT2A) receptor gene: identification of two naturally occurring receptor variants and association analysis in schizophrenia. Hum Genet. 1996 May;97(5):614-9. [PubMed Link Image]
Target 8 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. McDonald LM, Moran PM, Vythelingum GN, Joseph MH, Stephenson JD, Gray JA: Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning. Psychopharmacology (Berl). 2003 Sep;169(3-4):321-31. Epub 2002 Aug 9. [PubMed Link Image]
  3. Moresco RM, Cavallaro R, Messa C, Bravi D, Gobbo C, Galli L, Lucignani G, Colombo C, Rizzo G, Velona I, Smeraldi E, Fazio F: Cerebral D2 and 5-HT2 receptor occupancy in Schizophrenic patients treated with olanzapine or clozapine. J Psychopharmacol. 2004 Sep;18(3):355-65. [PubMed Link Image]
  4. Sharpley AL, Attenburrow ME, Hafizi S, Cowen PJ: Olanzapine increases slow wave sleep and sleep continuity in SSRI-resistant depressed patients. J Clin Psychiatry. 2005 Apr;66(4):450-4. [PubMed Link Image]
  5. Yatham LN, Goldstein JM, Vieta E, Bowden CL, Grunze H, Post RM, Suppes T, Calabrese JR: Atypical antipsychotics in bipolar depression: potential mechanisms of action. J Clin Psychiatry. 2005;66 Suppl 5:40-8. [PubMed Link Image]
  6. Padin JF, Rodriguez MA, Dominguez E, Dopeso-Reyes IG, Buceta M, Cano E, Sotelo E, Brea J, Caruncho HJ, Isabel Cadavid M, Castro M, Isabel Loza M: Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells. Neuropharmacology. 2006 Sep;51(4):923-32. Epub 2006 Aug 14. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 590
Target 9 Name 5-hydroxytryptamine 2C receptor
Target 9 Synonyms
  1. 5- HT2C
  2. 5-HT-2C
  3. 5-HTR2C
  4. 5HT-1C
  5. Serotonin receptor 2C
Target 9 Gene Name HTR2C
Target 9 Protein Sequence >5-hydroxytryptamine 2C receptor 
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Target 9 Number of Residues 465
Target 9 Molecular Weight 51822
Target 9 Theoretical pI 9.11
Target 9 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 9 General Function Involved in rhodopsin-like receptor activity
Target 9 Specific Function This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system
Target 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Pfam Domain Function
Target 9 Signals
  • None
Target 9 Transmembrane Regions
  • 53-78
  • 90-110
  • 128-150
  • 171-193
  • 214-235
  • 312-333
  • 349-371
Target 9 Essentiality Non-Essential
Target 9 GenBank ID Protein 338028 Link Image
Target 9 UniProtKB/Swiss-Prot ID P28335 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name 5HT2C_HUMAN Link Image
Target 9 PDB ID Not Available
Target 9 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 9 Gene Sequence >1377 bp 
ATGGTGAACCTGAGGAATGCGGTGCATTCATTCCTTGTGCACCTAATTGGCCTATTGGTT
TGGCAATGTGATATTTCTGTGAGCCCAGTAGCAGCTATAGTAACTGACATTTTCAATACC
TCCGATGGTGGACGCTTCAAATTCCCAGACGGGGTACAAAACTGGCCAGCACTTTCAATC
GTCATCATAATAATCATGACAATAGGTGGCAACATCCTTGTGATCATGGCAGTAAGCATG
GAAAAGAAACTGCACAATGCCACCAATTACTTCTTAATGTCCCTAGCCATTGCTGATATG
CTAGTGGGACTACTTGTCATGCCCCTGTCTCTCCTGGCAATCCTTTATGATTATGTCTGG
CCACTACCTAGATATTTGTGCCCCGTCTGGATTTCTTTAGATGTTTTATTTTCAACAGCG
TCCATCATGCACCTCTGCGCTATATCGCTGGATCGGTATGTAGCAATACGTAATCCTATT
GAGCATAGCCGTTTCAATTCGCGGACTAAGGCCATCATGAAGATTGCTATTGTTTGGGCA
ATTTCTATAGGTGTATCAGTTCCTATCCCTGTGATTGGACTGAGGGACGAAGAAAAGGTG
TTCGTGAACAACACGACGTGCGTGCTCAACGACCCAAATTTCGTTCTTATTGGGTCCTTC
GTAGCTTTCTTCATACCGCTGACGATTATGGTGATTACGTATTGCCTGACCATCTACGTT
CTGCGCCGACAAGCTTTGATGTTACTGCACGGCCACACCGAGGAACCGCCTGGACTAAGT
CTGGATTTCCTGAAGTGCTGCAAGAGGAATACGGCCGAGGAAGAGAACTCTGCAAACCCT
AACCAAGACCAGAACGCACGCCGAAGAAAGAAGAAGGAGAGACGTCCTAGGGGCACCATG
CAGGCTATCAACAATGAAAGAAAAGCTTCGAAAGTCCTTGGGATTGTTTTCTTTGTGTTT
CTGATCATGTGGTGCCCATTTTTCATTACCAATATTCTGTCTGTTCTTTGTGAGAAGTCC
TGTAACCAAAAGCTCATGGAAAAGCTTCTGAATGTGTTTGTTTGGATTGGCTATGTTTGT
TCAGGAATCAATCCTCTGGTGTATACTCTGTTCAACAAAATTTACCGAAGGGCATTCTCC
AACTATTTGCGTTGCAATTATAAGGTAGAGAAAAAGCCTCCTGTCAGGCAGATTCCAAGA
GTTGCCGCCACTGCTTTGTCTGGGAGGGAGCTTAATGTTAACATTTATCGGCATACCAAT
GAACCGGTGATCGAGAAAGCCAGTGACAATGAGCCCGGTATAGAGATGCAAGTTGAGAAT
TTAGAGTTACCAGTAAATCCCTCCAGTGTGGTTAGCGAAAGGATTAGCAGTGTGTGA
Target 9 GenBank Gene ID
Target 9 GeneCard ID HTR2C Link Image
Target 9 GenAtlas ID HTR2C Link Image
Target 9 HGNC ID HGNC:5295 Link Image
Target 9 Chromosome Location X
Target 9 Locus Xq24
Target 9 SNPs SNPJam Report Link Image
Target 9 General References
  1. Samochowiec J, Smolka M, Winterer G, Rommelspacher H, Schmidt LG, Sander T: Association analysis between a Cys23Ser substitution polymorphism of the human 5-HT2c receptor gene and neuronal hyperexcitability. Am J Med Genet. 1999 Apr 16;88(2):126-30. [PubMed Link Image]
  2. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  3. Marshall SE, Bird TG, Hart K, Welsh KI: Unified approach to the analysis of genetic variation in serotonergic pathways. Am J Med Genet. 1999 Dec 15;88(6):621-7. [PubMed Link Image]
  4. Becamel C, Figge A, Poliak S, Dumuis A, Peles E, Bockaert J, Lubbert H, Ullmer C: Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem. 2001 Apr 20;276(16):12974-82. Epub 2001 Jan 9. [PubMed Link Image]
  5. Saltzman AG, Morse B, Whitman MM, Ivanshchenko Y, Jaye M, Felder S: Cloning of the human serotonin 5-HT2 and 5-HT1C receptor subtypes. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1469-78. [PubMed Link Image]
  6. Lappalainen J, Zhang L, Dean M, Oz M, Ozaki N, Yu DH, Virkkunen M, Weight F, Linnoila M, Goldman D: Identification, expression, and pharmacology of a Cys23-Ser23 substitution in the human 5-HT2c receptor gene (HTR2C). Genomics. 1995 May 20;27(2):274-9. [PubMed Link Image]
  7. Stam NJ, Vanderheyden P, van Alebeek C, Klomp J, de Boer T, van Delft AM, Olijve W: Genomic organisation and functional expression of the gene encoding the human serotonin 5-HT2C receptor. Eur J Pharmacol. 1994 Nov 15;269(3):339-48. [PubMed Link Image]
  8. Xie E, Zhu L, Zhao L, Chang LS: The human serotonin 5-HT2C receptor: complete cDNA, genomic structure, and alternatively spliced variant. Genomics. 1996 Aug 1;35(3):551-61. [PubMed Link Image]
  9. Niswender CM, Sanders-Bush E, Emeson RB: Identification and characterization of RNA editing events within the 5-HT2C receptor. Ann N Y Acad Sci. 1998 Dec 15;861:38-48. [PubMed Link Image]
Target 9 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. Zhang JY, Kowal DM, Nawoschik SP, Lou Z, Dunlop J: Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms. Biochem Pharmacol. 2006 Feb 14;71(4):521-9. Epub 2005 Dec 5. [PubMed Link Image]
  3. Wood MD, Scott C, Clarke K, Cato KJ, Patel N, Heath J, Worby A, Gordon L, Campbell L, Riley G, Davies CH, Gribble A, Jones DN: Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006 Aug;5(4):445-52. [PubMed Link Image]
  4. Hertel P: Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action. Synapse. 2006 Dec 1;60(7):543-52. [PubMed Link Image]
  5. Theisen FM, Haberhausen M, Firnges MA, Gregory P, Reinders JH, Remschmidt H, Hebebrand J, Antel J: No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. Epub 2006 Sep 19. [PubMed Link Image]
  6. Overstreet DH, Knapp DJ, Breese GR: Drug challenges reveal differences in mediation of stress facilitation of voluntary alcohol drinking and withdrawal-induced anxiety in alcohol-preferring P rats. Alcohol Clin Exp Res. 2007 Sep;31(9):1473-81. Epub 2007 Jul 11. [PubMed Link Image]
Drug Target 10 [top]
Target 10 ID 617
Target 10 Name Muscarinic acetylcholine receptor M2
Target 10 Synonyms Not Available
Target 10 Gene Name CHRM2
Target 10 Protein Sequence >Muscarinic acetylcholine receptor M2 
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNY
FLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFD
RYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQF
FSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRI
VKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDE
ITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNI
VARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT
VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
Target 10 Number of Residues 473
Target 10 Molecular Weight 51716
Target 10 Theoretical pI 9.08
Target 10 GO Classification
Function
amine receptor activity
muscarinic acetylcholine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 10 General Function Involved in rhodopsin-like receptor activity
Target 10 Specific Function The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition
Target 10 Pathways Not Available
Target 10 Reactions Not Available
Target 10 Pfam Domain Function
Target 10 Signals
  • None
Target 10 Transmembrane Regions
  • 23-45
  • 60-80
  • 98-119
  • 140-162
  • 185-207
  • 389-409
  • 424-443
Target 10 Essentiality Non-Essential
Target 10 GenBank ID Protein 177990 Link Image
Target 10 UniProtKB/Swiss-Prot ID P08172 Link Image
Target 10 UniProtKB/Swiss-Prot Entry Name ACM2_HUMAN Link Image
Target 10 PDB ID Not Available
Target 10 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 10 Gene Sequence >1401 bp 
ATGAATAACTCAACAAACTCCTCTAACAATAGCCTGGCTCTTACAAGTCCTTATAAGACA
TTTGAAGTGGTGTTTATTGTCCTGGTGGCTGGATCCCTCAGTTTGGTGACCATTATCGGG
AACATCCTAGTCATGGTTTCCATTAAAGTCAACCGCCACCTCCAGACCGTCAACAATTAC
TTTTTATTCAGCTTGGCCTGTGCTGACCTTATCATAGGTGTTTTCTCCATGAACTTGTAC
ACCCTCTACACTGTGATTGGTTACTGGCCTTTGGGACCTGTGGTGTGTGACCTTTGGCTA
GCCCTGGACTATGTGGTCAGCAATGCCTCAGTTATGAATCTGCTCATCATCAGCTTTGAC
AGGTACTTCTGTGTCACAAAACCTCTGACCTACCCAGTCAAGCGGACCACAAAAATGGCA
GGTATGATGATTGCAGCTGCCTGGGTCCTCTCTTTCATCCTCTGGGCTCCAGCCATTCTC
TTCTGGCAGTTCATTGTAGGGGTGAGAACTGTGGAGGATGGGGAGTGCTACATTCAGTTT
TTTTCCAATGCTGCTGTCACCTTTGGTACGGCTATTGCAGCCTTCTATTTGCCAGTGATC
ATCATGACTGTGCTATATTGGCACATATCCCGAGCCAGCAAGAGCAGGATAAAGAAGGAC
AAGAAGGAGCCTGTTGCCAACCAAGACCCCGTTTCTCCAAGTCTGGTACAAGGAAGGATA
GTGAAGCCAAACAATAACAACATGCCCAGCAGTGACGATGGCCTGGAGCACAACAAAATC
CAGAATGGCAAAGCCCCCAGGGATCCTGTGACTGAAAACTGTGTTCAGGGAGAGGAGAAG
GAGAGCTCCAATGACTCCACCTCAGTCAGTGCTGTTGCCTCTAATATGAGAGATGATGAA
ATAACCCAGGATGAAAACACAGTTTCCACTTCCCTGGGCCATTCCAAAGATGAGAACTCT
AAGCAAACATGCATCAGAATTGGCACCAAGACCCCAAAAAGTGACTCATGTACCCCAACT
AATACCACCGTGGAGGTAGTGGGGTCTTCAGGTCAGAATGGAGATGAAAAGCAGAATATT
GTAGCCCGCAAGATTGTGAAGATGACTAAGCAGCCTGCAAAAAAGAAGCCTCCTCCTTCC
CGGGAAAAGAAAGTCACCAGGACAATCTTGGCTATTCTGTTGGCTTTCATCATCACTTGG
GCCCCATACAATGTCATGGTGCTCATTAACACCTTTTGTGCACCTTGCATCCCCAACACT
GTGTGGACAATTGGTTACTGGCTTTGTTACATCAACAGCACTATCAACCCTGCCTGCTAT
GCACTTTGCAATGCCACCTTCAAGAAGACCTTTAAACACCTTCTCATGTGTCATTATAAG
AACATAGGCGCTACAAGGTAA
Target 10 GenBank Gene ID
Target 10 GeneCard ID CHRM2 Link Image
Target 10 GenAtlas ID CHRM2 Link Image
Target 10 HGNC ID HGNC:1951 Link Image
Target 10 Chromosome Location 7
Target 10 Locus 7q31-q35
Target 10 SNPs SNPJam Report Link Image
Target 10 General References
  1. Bonner TI, Buckley NJ, Young AC, Brann MR: Identification of a family of muscarinic acetylcholine receptor genes. Science. 1987 Jul 31;237(4814):527-32. [PubMed Link Image]
  2. Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ: Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. [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]
Drug Target 11 [top]
Target 11 ID 632
Target 11 Name Alpha-1B adrenergic receptor
Target 11 Synonyms
  1. Alpha 1B- adrenoreceptor
  2. Alpha 1B-adrenoceptor
Target 11 Gene Name ADRA1B
Target 11 Protein Sequence >Alpha-1B adrenergic receptor 
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
Target 11 Number of Residues 528
Target 11 Molecular Weight 56837
Target 11 Theoretical pI 9.79
Target 11 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
adrenoceptor activity
alpha-adrenergic receptor activity
alpha1-adrenergic receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 11 General Function Involved in alpha1-adrenergic receptor activity
Target 11 Specific Function This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
Target 11 Pathways Not Available
Target 11 Reactions Not Available
Target 11 Pfam Domain Function
Target 11 Signals
  • None
Target 11 Transmembrane Regions
  • 46-70
  • 84-105
  • 116-141
  • 162-182
  • 202-224
  • 296-319
  • 327-340
Target 11 Essentiality Non-Essential
Target 11 GenBank ID Protein Not Available
Target 11 UniProtKB/Swiss-Prot ID P35368 Link Image
Target 11 UniProtKB/Swiss-Prot Entry Name ADA1B_HUMAN Link Image
Target 11 PDB ID Not Available
Target 11 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 11 Gene Sequence Not Available
Target 11 GenBank Gene ID
Target 11 GeneCard ID ADRA1B Link Image
Target 11 GenAtlas ID ADRA1B Link Image
Target 11 HGNC ID HGNC:278 Link Image
Target 11 Chromosome Location 5
Target 11 Locus 5q23-q32
Target 11 SNPs SNPJam Report Link Image
Target 11 General References
  1. Ramarao CS, Denker JM, Perez DM, Gaivin RJ, Riek RP, Graham RM: Genomic organization and expression of the human alpha 1B-adrenergic receptor. J Biol Chem. 1992 Oct 25;267(30):21936-45. [PubMed Link Image]
  2. Schwinn DA, Johnston GI, Page SO, Mosley MJ, Wilson KH, Worman NP, Campbell S, Fidock MD, Furness LM, Parry-Smith DJ, et al.: Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. [PubMed Link Image]
  3. Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA, et al.: The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol. 1994 Apr;45(4):703-8. [PubMed Link Image]
Target 11 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
Drug Target 12 [top]
Target 12 ID 638
Target 12 Name D(3) dopamine receptor
Target 12 Synonyms Not Available
Target 12 Gene Name DRD3
Target 12 Protein Sequence >D(3) dopamine receptor 
MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN
LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV
CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ
QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK
LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV
SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC
Target 12 Number of Residues 406
Target 12 Molecular Weight 44225
Target 12 Theoretical pI 9.07
Target 12 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
dopamine receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 12 General Function Involved in dopamine receptor activity
Target 12 Specific Function This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 12 Pathways Not Available
Target 12 Reactions Not Available
Target 12 Pfam Domain Function
Target 12 Signals
  • None
Target 12 Transmembrane Regions
  • 33-55
  • 67-92
  • 105-126
  • 150-172
  • 186-209
  • 330-351
  • 367-388
Target 12 Essentiality Non-Essential
Target 12 GenBank ID Protein 927342 Link Image
Target 12 UniProtKB/Swiss-Prot ID P35462 Link Image
Target 12 UniProtKB/Swiss-Prot Entry Name DRD3_HUMAN Link Image
Target 12 PDB ID Not Available
Target 12 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 12 Gene Sequence >1203 bp 
ATGGCATCTCTGAGTCAGCTGAGTAGCCACCTGAACTACACCTGTGGGGCAGAGAACTCC
ACAGGTGCCAGCCAGGCCCGCCCACATGCCTACTATGCCCTCTCCTACTGCGCGCTCATC
CTGGCCATCGTCTTCGGCAATGGCCTGGTGTGCATGGCTGTGCTGAAGGAGCGGGCCCTG
CAGACTACCACCAACTACTTAGTAGTGAGCCTGGCTGTGGCAGACTTGCTGGTGGCCACC
TTGGTGATGCCCTGGGTGGTATACCTGGAGGTGACAGGTGGAGTCTGGAATTTCAGCCGC
ATTTGCTGTGATGTTTTTGTCACCCTGGATGTCATGATGTGTACAGCCAGCATCCTTAAT
CTCTGTGCCATCAGCATAGACAGGTACACTGCAGTGGTCATGCCCGTTCACTACCAGCAT
GGCACGGGACAGAGCTCCTGTCGGCGCGTGGCCCTCATGATCACGGCCGTCTGGGTACTG
GCCTTTGCTGTGTCCTGCCCTCTTCTGTTTGGCTTTAATACCACAGGGGACCCCACTGTC
TGCTCCATCTCCAACCCTGATTTTGTCATCTACTCTTCAGTGGTGTCCTTCTACCTGCCC
TTTGGAGTGACTGTCCTTGTCTATGCCAGAATCTATGTGGTGCTGAAACAAAGGAGACGG
AAAAGGATCCTCACTCGACAGAACAGTCAGTGCAACAGTGTCAGGCCTGGCTTCCCCCAA
CAAACCCTCTCTCCTGACCCGGCACATCTGGAGCTGAAGCGTTACTACAGCATCTGCCAG
GACACTGCCTTGGGTGGACCAGGCTTCCAAGAAAGAGGAGGAGAGTTGAAAAGAGAGGAG
AAGACTCGGAATTCCCTGAGTCCCACCATAGCGCCCAAGCTCAGCTTAGAAGTTCGAAAA
CTCAGCAATGGCAGATTATCGACATCTTTGAAGCTGGGGCCCCTGCAACCTCGGGGAGTG
CCACTTCGGGAGAAGAAGGCAACCCAAATGGTGGCCATTGTGCTTGGGGCCTTCATTGTC
TGCTGGCTGCCCTTCTTCTTGACCCATGTTCTCAATACCCACTGCCAGACATGCCACGTG
TCCCCAGAGCTTTACAGTGCCACGACATGGCTGGGCTACGTGAATAGCGCCCTCAACCCT
GTGATCTATACCACCTTCAATATCGAGTTCCGGAAAGCCTTCCTCAAGATCCTGTCTTGC
TGA
Target 12 GenBank Gene ID
Target 12 GeneCard ID DRD3 Link Image
Target 12 GenAtlas ID DRD3 Link Image
Target 12 HGNC ID HGNC:3024 Link Image
Target 12 Chromosome Location 3
Target 12 Locus 3q13.3
Target 12 SNPs SNPJam Report Link Image
Target 12 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Giros B, Martres MP, Sokoloff P, Schwartz JC: [Gene cloning of human dopaminergic D3 receptor and identification of its chromosome] C R Acad Sci III. 1990;311(13):501-8. [PubMed Link Image]
  3. Liu K, Bergson C, Levenson R, Schmauss C: On the origin of mRNA encoding the truncated dopamine D3-type receptor D3nf and detection of D3nf-like immunoreactivity in human brain. J Biol Chem. 1994 Nov 18;269(46):29220-6. [PubMed Link Image]
  4. Schmauss C, Haroutunian V, Davis KL, Davidson M: Selective loss of dopamine D3-type receptor mRNA expression in parietal and motor cortices of patients with chronic schizophrenia. Proc Natl Acad Sci U S A. 1993 Oct 1;90(19):8942-6. [PubMed Link Image]
  5. Chen CH, Liu MY, Wei FC, Koong FJ, Hwu HG, Hsiao KJ: Further evidence of no association between Ser9Gly polymorphism of dopamine D3 receptor gene and schizophrenia. Am J Med Genet. 1997 Feb 21;74(1):40-3. [PubMed Link Image]
Target 12 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
Drug Target 13 [top]
Target 13 ID 831
Target 13 Name D(2) dopamine receptor
Target 13 Synonyms
  1. Dopamine D2 receptor
Target 13 Gene Name DRD2
Target 13 Protein Sequence >D(2) dopamine receptor 
MDPLNLSWYDDDLERQNWSRPFNGSDGKADRPHYNYYATLLTLLIAVIVFGNVLVCMAVS
REKALQTTTNYLIVSLAVADLLVATLVMPWVVYLEVVGEWKFSRIHCDIFVTLDVMMCTA
SILNLCAISIDRYTAVAMPMLYNTRYSSKRRVTVMISIVWVLSFTISCPLLFGLNNADQN
ECIIANPAFVVYSSIVSFYVPFIVTLLVYIKIYIVLRRRRKRVNTKRSSRAFRAHLRAPL
KGNCTHPEDMKLCTVIMKSNGSFPVNRRRVEAARRAQELEMEMLSSTSPPERTRYSPIPP
SHHQLTLPDPSHHGLHSTPDSPAKPEKNGHAKDHPKIAKIFEIQTMPNGKTRTSLKTMSR
RKLSQQKEKKATQMLAIVLGVFIICWLPFFITHILNIHCDCNIPPVLYSAFTWLGYVNSA
VNPIIYTTFNIEFRKAFLKILHC
Target 13 Number of Residues 450
Target 13 Molecular Weight 50620
Target 13 Theoretical pI 9.85
Target 13 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
dopamine receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 13 General Function Involved in dopamine receptor activity
Target 13 Specific Function This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 13 Pathways Not Available
Target 13 Reactions Not Available
Target 13 Pfam Domain Function
Target 13 Signals
  • None
Target 13 Transmembrane Regions
  • 38-60
  • 72-97
  • 109-130
  • 152-174
  • 187-210
  • 374-397
  • 406-429
Target 13 Essentiality Non-Essential
Target 13 GenBank ID Protein 181432 Link Image
Target 13 UniProtKB/Swiss-Prot ID P14416 Link Image
Target 13 UniProtKB/Swiss-Prot Entry Name DRD2_HUMAN Link Image
Target 13 PDB ID Not Available
Target 13 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 13 Gene Sequence >1332 bp 
ATGGATCCACTGAATCTGTCCTGGTATGATGATGATCTGGAGAGGCAGAACTGGAGCCGG
CCCTTCAACGGGTCAGACGGGAAGGCGGACAGACCCCACTACAACTACTATGCCACACTG
CTCACCCTGCTCATCGCTGTCATCGTCTTCGGCAACGTGCTGGTGTGCATGGCTGTGTCC
CGCGAGAAGGCGCTGCAGACCACCACCAACTACCTGATCGTCAGCCTCGCAGTGGCCGAC
CTCCTCGTCGCCACACTGGTCATGCCATGGGTTGTCTACCTGGAGGTGGTAGGTGAGTGG
AAATTCAGCAGGATTCACTGTGACATCTTCGTCACTCTGGACGTCATGATGTGCACGGCG
AGCATCCTGAACTTGTGTGCCATCAGCATCGACAGGTACACAGCTGTGGCCATGCCCATG
CTGTACAATACGCGCTACAGCTCCAAGCGCCGGGTCACCGTCATGATCTCCATCGTCTGG
GTCCTGTCCTTCACCATCTCCTGCCCACTCCTCTTCGGACTCAATAACGCAGACCAGAAC
GAGTGCATCATTGCCAACCCGGCCTTCGTGGTCTACTCCTCCATCGTCTCCTTCTACGTG
CCCTTCATTGTCACCCTGCTGGTCTACATCAAGATCTACATTGTCCTCCGCAGACGCCGC
AAGCGAGTCAACACCAAACGCAGCAGCCGAGCTTTCAGGGCCCACCTGAGGGCTCCACTA
AAGGGCAACTGTACTCACCCCGAGGACATGAAACTCTGCACCGTTATCATGAAGTCTAAT
GGGAGTTTCCCAGTGAACAGGCGGAGAGTGGAGGCTGCCCGGCGAGCCCAGGAGCTGGAG
ATGGAGATGCTCTCCAGCACCAGCCCACCCGAGAGGACCCGGTACAGCCCCATCCCACCC
AGCCACCACCAGCTGACTCTCCCCGACCCGTCCCACCACGGTCTCCACAGCACTCCTGAC
AGCCCCGCCAAACCAGAGAAGAATGGGCATGCCAAAGACCACCCCAAGATTGCCAAGATC
TTTGAGATCCAGACCATGCCCAATGGCAAAACCCGGACCTCCCTCAAGACCATGAGCCGT
AGAAAGCTCTCCCAGCAGAAGGAGAAGAAAGCCACTCAGATGCTCGCCATTGTTCTCGGC
GTGTTCATCATCTGCTGGCTGCCCTTCTTCATCACACACATCCTGAACATACACTGTGAC
TGCAACATCCCGCCTGTCCTGTACAGCGCCTTCACGTGGCTGGGCTATGTCAACAGCGCC
GTGAACCCCATCATCTACACCACCTTCAACATTGAGTTCCGCAAGGCCTTCCTGAAGATC
CTTCACTGCTGA
Target 13 GenBank Gene ID
Target 13 GeneCard ID DRD2 Link Image
Target 13 GenAtlas ID DRD2 Link Image
Target 13 HGNC ID HGNC:3023 Link Image
Target 13 Chromosome Location 11
Target 13 Locus 11q23
Target 13 SNPs SNPJam Report Link Image
Target 13 General References
  1. Klein C, Brin MF, Kramer P, Sena-Esteves M, de Leon D, Doheny D, Bressman S, Fahn S, Breakefield XO, Ozelius LJ: Association of a missense change in the D2 dopamine receptor with myoclonus dystonia. Proc Natl Acad Sci U S A. 1999 Apr 27;96(9):5173-6. [PubMed Link Image]
  2. Seeman P, Nam D, Ulpian C, Liu IS, Tallerico T: New dopamine receptor, D2(Longer), with unique TG splice site, in human brain. Brain Res Mol Brain Res. 2000 Mar 10;76(1):132-41. [PubMed Link Image]
  3. Araki K, Kuwano R, Morii K, Hayashi S, Minoshima S, Shimizu N, Katagiri T, Usui H, Kumanishi T, Takahashi Y: Structure and expression of human and rat D2 dopamine receptor genes. Neurochem Int. 1992 Jul;21(1):91-8. [PubMed Link Image]
  4. Dearry A, Falardeau P, Shores C, Caron MG: D2 dopamine receptors in the human retina: cloning of cDNA and localization of mRNA. Cell Mol Neurobiol. 1991 Oct;11(5):437-53. [PubMed Link Image]
  5. Stormann TM, Gdula DC, Weiner DM, Brann MR: Molecular cloning and expression of a dopamine D2 receptor from human retina. Mol Pharmacol. 1990 Jan;37(1):1-6. [PubMed Link Image]
  6. Robakis NK, Mohamadi M, Fu DY, Sambamurti K, Refolo LM: Human retina D2 receptor cDNAs have multiple polyadenylation sites and differ from a pituitary clone at the 5' non-coding region. Nucleic Acids Res. 1990 Mar 11;18(5):1299. [PubMed Link Image]
  7. Selbie LA, Hayes G, Shine J: DNA homology screening: isolation and characterization of the human D2A dopamine receptor subtype. Adv Second Messenger Phosphoprotein Res. 1990;24:9-14. [PubMed Link Image]
  8. Dal Toso R, Sommer B, Ewert M, Herb A, Pritchett DB, Bach A, Shivers BD, Seeburg PH: The dopamine D2 receptor: two molecular forms generated by alternative splicing. EMBO J. 1989 Dec 20;8(13):4025-34. [PubMed Link Image]
  9. Grandy DK, Marchionni MA, Makam H, Stofko RE, Alfano M, Frothingham L, Fischer JB, Burke-Howie KJ, Bunzow JR, Server AC, et al.: Cloning of the cDNA and gene for a human D2 dopamine receptor. Proc Natl Acad Sci U S A. 1989 Dec;86(24):9762-6. [PubMed Link Image]
  10. Selbie LA, Hayes G, Shine J: The major dopamine D2 receptor: molecular analysis of the human D2A subtype. DNA. 1989 Nov;8(9):683-9. [PubMed Link Image]
  11. 7902708 Itokawa M, Arinami T, Futamura N, Hamaguchi H, Toru M: A structural polymorphism of human dopamine D2 receptor, D2(Ser311-->Cys). Biochem Biophys Res Commun. 1993 Nov 15;196(3):1369-75.
  12. 8471125 Seeman P, Ohara K, Ulpian C, Seeman MV, Jellinger K, Van Tol HH, Niznik HB: Schizophrenia: normal sequence in the dopamine D2 receptor region that couples to G-proteins. DNA polymorphisms in D2. Neuropsychopharmacology. 1993 Feb;8(2):137-42.
Target 13 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. [PubMed Link Image]
  3. Lencz T, Robinson DG, Xu K, Ekholm J, Sevy S, Gunduz-Bruce H, Woerner MG, Kane JM, Goldman D, Malhotra AK: DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients. Am J Psychiatry. 2006 Mar;163(3):529-31. [PubMed Link Image]
  4. Naiker DV, Catts SV, Catts VS, Bedi KS, Bryan-Lluka LJ: Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. Epub 2006 May 11. [PubMed Link Image]
  5. Thacker SK, Perna MK, Ward JJ, Schaefer TL, Williams MT, Kostrzewa RM, Brown RW: The effects of adulthood olanzapine treatment on cognitive performance and neurotrophic factor content in male and female rats neonatally treated with quinpirole. Eur J Neurosci. 2006 Oct;24(7):2075-83. [PubMed Link Image]
  6. Jordan S, Regardie K, Johnson JL, Chen R, Kambayashi J, McQuade R, Kitagawa H, Tadori Y, Kikuchi T: In vitro functional characteristics of dopamine D2 receptor partial agonists in second and third messenger-based assays of cloned human dopamine D2Long receptor signalling. J Psychopharmacol. 2007 Aug;21(6):620-7. Epub 2006 Nov 8. [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.