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Showing drug card for Atropine (DB00572)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:08
Primary Accession Number DB00572
Secondary Accession Number
  • APRD00807
  • EXPT02427
Name Atropine
Drug Type
  • Approved
  • Small Molecule
Description An alkaloid, originally from Atropa belladonna, but found in other plants, mainly solanaceae. [PubChem]
Synonyms
  1. Atropin [German]
  2. Atropina [Italian]
  3. Atropine Sulfate
  4. DL-Hyoscyamine
  5. DL-Tropyl tropate
Brand Names
  1. Atnaa
  2. Atropair
  3. Atropen
  4. Atropin
  5. Atropin-flexiolen
  6. Atropine Care
  7. Atropine Sulfate Ansyr Plastic Syringe
  8. Atropine Sulfate S.O.P.
  9. Atropinol
  10. Atropisol
  11. Atrosulf
  12. Equipin
  13. Eyesules
  14. Homapin-10
  15. Homapin-5
  16. I-Tropine
  17. Isopto Atropine
  18. Isopto-atropine
  19. Minims Atropine
  20. Ocu-Tropine
  21. Tropine tropate
  22. Troyl tropate
Brand Mixtures
  1. Diban Cap (Atropine Sulfate + Attapulgite (Activated) + Hyoscyamine Sulfate + Opium + Pectin + Scopolamine Hydrobromide)
  2. Donnagel Liq (Atropine Sulfate + Hyoscyamine Sulfate + Kaolin + Pectin + Scopolamine Hydrobromide)
  3. Donnatal Elixir (Atropine Sulfate + Hyoscyamine Sulfate + Phenobarbital + Scopolamine Hydrobromide)
  4. Donnatal Extentabs (Atropine Sulfate + Hyoscyamine Sulfate + Phenobarbital + Scopolamine Hydrobromide)
  5. Donnatal Extentabs Srt (Atropine Sulfate + Hyoscyamine Sulfate + Phenobarbital + Scopolamine Hydrobromide)
  6. Donnatal Tab (Atropine Sulfate + Hyoscyamine Sulfate + Phenobarbital + Scopolamine Hydrobromide)
  7. Spascupreel Injeel Liq (Aconite + Atropine Sulfate + Chamomile + Citrullus Colocynthis + Copper Sulfate + Gelsemium Sempervirens + Magnesium Phosphate Dibasic + Mushroom + Passion Flower)
  8. Spascupreel Tablets (Aconitum + Agaricus + Atropine Sulfate + Chamomile + Citrullus Colocynthis + Copper Sulfate + Gelsemium Sempervirens + Magnesium Phosphate Dibasic + Passion Flower)
Chemical IUPAC Name [(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3-hydroxy-2-phenylpropanoate
Chemical Formula C17H23NO3
Chemical Structure Structure
CAS Registry Number 51-55-8
InChI Identifier InChI=1/C17H23NO3/c1-18-13-7-8-14(18)10-15(9-13)21-17(20)16(11-19)12-5-3-2-4-6-12/h2-6,13-16,19H,7-11H2,1H3/t13-,14+,15?,16?
InChI Key RKUNBYITZUJHSG-PJPHBNEVBA
KEGG Drug D00113 Link Image
KEGG Compound C01479 Link Image
PubChem Compound 174174 Link Image
PubChem Substance 4651 Link Image
ChEBI ID 16684 Link Image
PharmGKB ID PA448505 Link Image
HET ID OIN Link Image
GenBank ID Not Available
Drug ID Number [DIN] 00715492 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/atropen.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Atropine Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 289.3694
Monoisotopic Molecular Weight 289.1678
State Solid
Melting Point 118.5 oC
Experimental Water Solubility Highly soluble (2200 mg/L) Source: PhysProp
Predicted Water Solubility 2.52e+00 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 1.8 Source: PhysProp
Predicted LogP 2.19 Calculated using ALOGPS
Experimental LogS -2.12 [ADME Research, USCD]
Predicted LogS -2.06 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 9.43
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 1TH6 Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES CN1[C@H]2CC[C@@H]1C[C@H](C2)OC(=O)[C@@H](CO)C1=CC=CC=C1
Canonical SMILES CN1C2CCC1CC(C2)OC(=O)C(CO)C1=CC=CC=C1
Drug Category
  • Adjuvants, Anesthesia
  • Anti-Arrhythmia Agents
  • Bronchodilator Agents
  • Muscarinic Antagonists
  • Mydriatics
  • Parasympatholytics
ATC Codes
AHFS Codes
  • 12:08.08
  • 52:24.00
  • 92:02.00*
Indication For the treatment of poisoning by susceptible organophosphorous nerve agents having cholinesterase activity as well as organophosphorous or carbamate insecticides.
Pharmacology Atropine, a naturally occurring belladonna alkaloid, is a racemic mixture of equal parts of d- and l-hyoscyamine, whose activity is due almost entirely to the levo isomer of the drug. Atropine is commonly classified as an anticholinergic or antiparasympathetic (parasympatholytic) drug. More precisely, however, it is termed an antimuscarinic agent since it antagonizes the muscarine-like actions of acetylcholine and other choline esters. Adequate doses of atropine abolish various types of reflex vagal cardiac slowing or asystole. The drug also prevents or abolishes bradycardia or asystole produced by injection of choline esters, anticholinesterase agents or other parasympathomimetic drugs, and cardiac arrest produced by stimulation of the vagus. Atropine may also lessen the degree of partial heart block when vagal activity is an etiologic factor. Atropine in clinical doses counteracts the peripheral dilatation and abrupt decrease in blood pressure produced by choline esters. However, when given by itself, atropine does not exert a striking or uniform effect on blood vessels or blood pressure.
Mechanism of Action Generally, atropine lowers the "rest and digest" activity of all muscles and glands regulated by the parasympathetic nervous system. This occurs because atropine is a competitive inhibitor of the muscarinic acetylcholine receptors (acetylcholine is the neurotransmitter used by the parasympathetic nervous system).
Absorption Atropine is rapidly and well absorbed after intramuscular administration. Atropine disappears rapidly from the blood and is distributed throughout the various body tissues and fluids.
Toxicity Oral, mouse: LD50 = 75 mg/kg. Symptoms of overdose includes widespread paralysis of parasympathetically innervated organs. Dry mucous membranes, widely dilated and nonresponsive pupils, tachycardia, fever and cutaneous flush are especially prominent, as are mental and neurological symptoms. In instances of severe intoxication, respiratory depression, coma, circulatory collapse and death may occur.
Protein Binding The protein binding of atropine is 14 to 22% in plasma.
Biotransformation Much of the drug is destroyed by enzymatic hydrolysis, particularly in the liver. From 13 to 50% is excreted unchanged in the urine.
Half Life 3.0 ± 0.9 hours in adults. The half-life of atropine is slightly shorter (approximately 20 minutes) in females than males.
Dosage Forms
Form Route
Liquid Ophthalmic
Liquid Oral
Ointment Ophthalmic
Solution Intramuscular
Solution Intravenous
Solution Ophthalmic
Solution / drops Oral
Tablet Oral
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions
  • Avoid alcohol.
  • Take with food.
Pathways Not Available
General References
  1. Wikipedia Link Image
  2. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cholinesterase
Targets
  1. Muscarinic acetylcholine receptor M3
  2. Muscarinic acetylcholine receptor M1
  3. Muscarinic acetylcholine receptor M5
  4. Muscarinic acetylcholine receptor M4
  5. Acetylcholinesterase
  6. Muscarinic acetylcholine receptor M2
  7. Phospholipase A2 VRV-PL-VIIIa
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cholinesterase
Enzyme 1 Gene Name BCHE
Enzyme 1 SwissProt ID P06276 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >Cholinesterase 
MHSKVTIICIRFLFWFLLLCMLIGKSHTEDDIIIATKNGKVRGMNLTVFGGTVTAFLGIP
YAQPPLGRLRFKKPQSLTKWSDIWNATKYANSCCQNIDQSFPGFHGSEMWNPNTDLSEDC
LYLNVWIPAPKPKNATVLIWIYGGGFQTGTSSLHVYDGKFLARVERVIVVSMNYRVGALG
FLALPGNPEAPGNMGLFDQQLALQWVQKNIAAFGGNPKSVTLFGESAGAASVSLHLLSPG
SHSLFTRAILQSGSFNAPWAVTSLYEARNRTLNLAKLTGCSRENETEIIKCLRNKDPQEI
LLNEAFVVPYGTPLSVNFGPTVDGDFLTDMPDILLELGQFKKTQILVGVNKDEGTAFLVY
GAPGFSKDNNSIITRKEFQEGLKIFFPGVSEFGKESILFHYTDWVDDQRPENYREALGDV
VGDYNFICPALEFTKKFSEWGNNAFFYYFEHRSSKLPWPEWMGVMHGYEIEFVFGLPLER
RDNYTKAEEILSRSIVKRWANFAKYGNPNETQNNSTSWPVFKSTEQKYLTLNTESTRIMT
KLRAQQCRFWTSFFPKVLEMTGNIDEAEWEWKAGFHRWNNYMMDWKNQFNDYTSKKESCV
GL
Drug Target 1 [top]
Target 1 ID 51
Target 1 Name Muscarinic acetylcholine receptor M3
Target 1 Synonyms Not Available
Target 1 Gene Name CHRM3
Target 1 Protein Sequence >Muscarinic acetylcholine receptor M3 
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI
SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR
TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF
YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM
KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE
TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR
MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN
PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL
Target 1 Number of Residues 599
Target 1 Molecular Weight 66129
Target 1 Theoretical pI 9.62
Target 1 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 1 General Function Involved in rhodopsin-like receptor activity
Target 1 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 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 68-91
  • 105-125
  • 143-164
  • 185-207
  • 230-252
  • 493-513
  • 528-547
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 32324 Link Image
Target 1 UniProtKB/Swiss-Prot ID P20309 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name ACM3_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 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 1 GenBank Gene ID
Target 1 GeneCard ID CHRM3 Link Image
Target 1 GenAtlas ID CHRM3 Link Image
Target 1 HGNC ID HGNC:1952 Link Image
Target 1 Chromosome Location 1
Target 1 Locus 1q43
Target 1 SNPs SNPJam Report Link Image
Target 1 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 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 103
Target 2 Name Muscarinic acetylcholine receptor M1
Target 2 Synonyms Not Available
Target 2 Gene Name CHRM1
Target 2 Protein Sequence >Muscarinic acetylcholine receptor M1 
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
Target 2 Number of Residues 467
Target 2 Molecular Weight 51421
Target 2 Theoretical pI 9.67
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
  • 25-47
  • 62-82
  • 100-121
  • 142-164
  • 187-209
  • 367-387
  • 402-421
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 34451 Link Image
Target 2 UniProtKB/Swiss-Prot ID P11229 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name ACM1_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 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 2 GenBank Gene ID
Target 2 GeneCard ID CHRM1 Link Image
Target 2 GenAtlas ID CHRM1 Link Image
Target 2 HGNC ID HGNC:1950 Link Image
Target 2 Chromosome Location 11
Target 2 Locus 11q13
Target 2 SNPs SNPJam Report Link Image
Target 2 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 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 274
Target 3 Name Muscarinic acetylcholine receptor M5
Target 3 Synonyms Not Available
Target 3 Gene Name CHRM5
Target 3 Protein Sequence >Muscarinic acetylcholine receptor M5 
MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQ
LKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMN
LLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPL
DECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAE
KRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQL
TTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPN
YLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNP
NPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLG
YWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP
Target 3 Number of Residues 540
Target 3 Molecular Weight 60074
Target 3 Theoretical pI 9.64
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
  • 30-53
  • 67-87
  • 105-126
  • 147-169
  • 192-214
  • 444-464
  • 479-498
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 177988 Link Image
Target 3 UniProtKB/Swiss-Prot ID P08912 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name ACM5_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 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 3 GenBank Gene ID
Target 3 GeneCard ID CHRM5 Link Image
Target 3 GenAtlas ID CHRM5 Link Image
Target 3 HGNC ID HGNC:1954 Link Image
Target 3 Chromosome Location 15
Target 3 Locus 15q26
Target 3 SNPs SNPJam Report Link Image
Target 3 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 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 450
Target 4 Name Muscarinic acetylcholine receptor M4
Target 4 Synonyms Not Available
Target 4 Gene Name CHRM4
Target 4 Protein Sequence >Muscarinic acetylcholine receptor M4 
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVN
RQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASV
MNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTV
PDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAK
TLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGS
ATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIV
PATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMV
LVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
Target 4 Number of Residues 486
Target 4 Molecular Weight 53050
Target 4 Theoretical pI 10.34
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 inhibition of adenylate cyclase
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 32-54
  • 69-89
  • 107-128
  • 149-171
  • 194-216
  • 402-422
  • 437-456
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 61970253 Link Image
Target 4 UniProtKB/Swiss-Prot ID P08173 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name ACM4_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 4 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 4 GenBank Gene ID
Target 4 GeneCard ID CHRM4 Link Image
Target 4 GenAtlas ID CHRM4 Link Image
Target 4 HGNC ID HGNC:1953 Link Image
Target 4 Chromosome Location 11
Target 4 Locus 11p12-p11.2
Target 4 SNPs SNPJam Report Link Image
Target 4 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 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 474
Target 5 Name Acetylcholinesterase
Target 5 Synonyms
  1. AChE
  2. Acetylcholinesterase precursor
  3. EC 3.1.1.7
Target 5 Gene Name ACHE
Target 5 Protein Sequence >Acetylcholinesterase precursor 
MRPPQCLLHTPSLASPLLLLLLWLLGGGVGAEGREDAELLVTVRGGRLRGIRLKTPGGPV
SAFLGIPFAEPPMGPRRFLPPEPKQPWSGVVDATTFQSVCYQYVDTLYPGFEGTEMWNPN
RELSEDCLYLNVWTPYPRPTSPTPVLVWIYGGGFYSGASSLDVYDGRFLVQAERTVLVSM
NYRVGAFGFLALPGSREAPGNVGLLDQRLALQWVQENVAAFGGDPTSVTLFGESAGAASV
GMHLLSPPSRGLFHRAVLQSGAPNGPWATVGMGEARRRATQLAHLVGCPPGGTGGNDTEL
VACLRTRPAQVLVNHEWHVLPQESVFRFSFVPVVDGDFLSDTPEALINAGDFHGLQVLVG
VVKDEGSYFLVYGAPGFSKDNESLISRAEFLAGVRVGVPQVSDLAAEAVVLHYTDWLHPE
DPARLREALSDVVGDHNVVCPVAQLAGRLAAQGARVYAYVFEHRASTLSWPLWMGVPHGY
EIEFIFGIPLDPSRNYTAEEKIFAQRLMRYWANFARTGDPNEPRDPKAPQWPPYTAGAQQ
YVSLDLRPLEVRRGLRAQACAFWNRFLPKLLSATDTLDEAERQWKAEFHRWSSYMVHWKN
QFDHYSKQDRCSDL
Target 5 Number of Residues 624
Target 5 Molecular Weight 67797
Target 5 Theoretical pI 6.24
Target 5 GO Classification
Function
catalytic activity
hydrolase activity
hydrolase activity, acting on ester bonds
carboxylic ester hydrolase activity
cholinesterase activity
Process
Not Available
Component
Not Available
Target 5 General Function Lipid transport and metabolism
Target 5 Specific Function Rapidly hydrolyzes choline released into the synapse
Target 5 Pathways
Name SMPDB Link KEGG Link
Glycerophospholipid metabolism map00564 Link Image
Target 5 Reactions
  • acetylcholine + H2O = choline + acetate
Target 5 Pfam Domain Function
Target 5 Signals
  • 1-31
Target 5 Transmembrane Regions
  • None
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 177975 Link Image
Target 5 UniProtKB/Swiss-Prot ID P22303 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name ACES_HUMAN Link Image
Target 5 PDB ID 1F8U Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Cytoplasmic
Target 5 Gene Sequence >1845 bp 
ATGAGGCCCCCGCAGTGTCTGCTGCACACGCCTTCCCTGGCTTCCCCACTCCTTCTCCTC
CTCCTCTGGCTCCTGGGTGGAGGAGTGGGGGCTGAGGGCCGGGAGGATGCAGAGCTGCTG
GTGACGGTGCGTGGGGGCCGGCTGCGGGGCATTCGCCTGAAGACCCCCGGGGGCCCTGTC
TCTGCTTTCCTGGGCATCCCCTTTGCGGAGCCACCCATGGGACCCCGTCGCTTTCTGCCA
CCGGAGCCCAAGCAGCCTTGGTCAGGGGTGGTAGACGCTACAACCTTCCAGAGTGTCTGC
TACCAATATGTGGACACCCTATACCCAGGTTTTGAGGGCACCGAGATGTGGAACCCCAAC
CGTGAGCTGAGCGAGGACTGCCTGTACCTCAACGTGTGGACACCATACCCCCGGCCTACA
TCCCCCACCCCTGTCCTCGTCTGGATCTATGGGGGTGGCTTCTACAGTGGGGCCTCCTCC
TTGGACGTGTACGATGGCCGCTTCTTGGTACAGGCCGAGAGGACTGTGCTGGTGTCCATG
AACTACCGGGTGGGAGCCTTTGGCTTCCTGGCCCTGCCGGGGAGCCGAGAGGCCCCGGGC
AATGTGGGTCTCCTGGATCAGAGGCTGGCCCTGCAGTGGGTGCAGGAGAACGTGGCAGCC
TTCGGGGGTGACCCGACATCAGTGACGCTGTTTGGGGAGAGCGCGGGAGCCGCCTCGGTG
GGCATGCACCTGCTGTCCCCGCCCAGCCGGGGCCTGTTCCACAGGGCCGTGCTGCAGAGC
GGTGCCCCCAATGGACCCTGGGCCACGGTGGGCATGGGAGAGGCCCGTCGCAGGGCCACG
CAGCTGGCCCACCTTGTGGGCTGTCCTCCAGGCGGCACTGGTGGGAATGACACAGAGCTG
GTAGCCTGCCTTCGGACACGACCAGCGCAGGTCCTGGTGAACCACGAATGGCACGTGCTG
CCTCAAGAAAGCGTCTTCCGGTTCTCCTTCGTGCCTGTGGTAGATGGAGACTTCCTCAGT
GACACCCCAGAGGCCCTCATCAACGCGGGAGACTTCCACGGCCTGCAGGTGCTGGTGGGT
GTGGTGAAGGATGAGGGCTCGTATTTTCTGGTTTACGGGGCCCCAGGCTTCAGCAAAGAC
AACGAGTCTCTCATCAGCCGGGCCGAGTTCCTGGCCGGGGTGCGGGTCGGGGTTCCCCAG
GTAAGTGACCTGGCAGCCGAGGCTGTGGTCCTGCATTACACAGACTGGCTGCATCCCGAG
GACCCGGCACGCCTGAGGGAGGCCCTGAGCGATGTGGTGGGCGACCACAATGTCGTGTGC
CCCGTGGCCCAGCTGGCTGGGCGACTGGCTGCCCAGGGTGCCCGGGTCTACGCCTACGTC
TTTGAACACCGTGCTTCCACGCTCTCCTGGCCCCTGTGGATGGGGGTGCCCCACGGCTAC
GAGATCGAGTTCATCTTTGGGATCCCCCTGGACCCCTCTCGAAACTACACGGCAGAGGAG
AAAATCTTCGCCCAGCGACTGATGCGATACTGGGCCAACTTTGCCCGCACAGGGGATCCC
AATGAGCCCCGAGACCCCAAGGCCCCACAATGGCCCCCGTACACGGCGGGGGCTCAGCAG
TACGTTAGTCTGGACCTGCGGCCGCTGGAGGTGCGGCGGGGGCTGCGCGCCCAGGCCTGC
GCCTTCTGGAACCGCTTCCTCCCCAAATTGCTCAGCGCCACCGACACGCTCGACGAGGCG
GAGCGCCAGTGGAAGGCCGAGTTCCACCGCTGGAGCTCCTACATGGTGCACTGGAAGAAC
CAGTTCGACCACTACAGCAAGCAGGATCGCTGCTCAGACCTGTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID ACHE Link Image
Target 5 GenAtlas ID ACHE Link Image
Target 5 HGNC ID HGNC:108 Link Image
Target 5 Chromosome Location 7
Target 5 Locus 7q22
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Kryger G, Harel M, Giles K, Toker L, Velan B, Lazar A, Kronman C, Barak D, Ariel N, Shafferman A, Silman I, Sussman JL: Structures of recombinant native and E202Q mutant human acetylcholinesterase complexed with the snake-venom toxin fasciculin-II. Acta Crystallogr D Biol Crystallogr. 2000 Nov;56(Pt 11):1385-94. [PubMed Link Image]
  2. Wilson MD, Riemer C, Martindale DW, Schnupf P, Boright AP, Cheung TL, Hardy DM, Schwartz S, Scherer SW, Tsui LC, Miller W, Koop BF: Comparative analysis of the gene-dense ACHE/TFR2 region on human chromosome 7q22 with the orthologous region on mouse chromosome 5. Nucleic Acids Res. 2001 Mar 15;29(6):1352-65. [PubMed Link Image]
  3. Hillier LW, Fulton RS, Fulton LA, Graves TA, Pepin KH, Wagner-McPherson C, Layman D, Maas J, Jaeger S, Walker R, Wylie K, Sekhon M, Becker MC, O'Laughlin MD, Schaller ME, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Cordes M, Du H, Sun H, Edwards J, Bradshaw-Cordum H, Ali J, Andrews S, Isak A, Vanbrunt A, Nguyen C, Du F, Lamar B, Courtney L, Kalicki J, Ozersky P, Bielicki L, Scott K, Holmes A, Harkins R, Harris A, Strong CM, Hou S, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Leonard S, Rohlfing T, Rock SM, Tin-Wollam AM, Abbott A, Minx P, Maupin R, Strowmatt C, Latreille P, Miller N, Johnson D, Murray J, Woessner JP, Wendl MC, Yang SP, Schultz BR, Wallis JW, Spieth J, Bieri TA, Nelson JO, Berkowicz N, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Bedell JA, Mardis ER, Clifton SW, Chissoe SL, Marra MA, Raymond C, Haugen E, Gillett W, Zhou Y, James R, Phelps K, Iadanoto S, Bubb K, Simms E, Levy R, Clendenning J, Kaul R, Kent WJ, Furey TS, Baertsch RA, Brent MR, Keibler E, Flicek P, Bork P, Suyama M, Bailey JA, Portnoy ME, Torrents D, Chinwalla AT, Gish WR, Eddy SR, McPherson JD, Olson MV, Eichler EE, Green ED, Waterston RH, Wilson RK: The DNA sequence of human chromosome 7. Nature. 2003 Jul 10;424(6945):157-64. [PubMed Link Image]
  4. Shafferman A, Kronman C, Flashner Y, Leitner M, Grosfeld H, Ordentlich A, Gozes Y, Cohen S, Ariel N, Barak D, et al.: Mutagenesis of human acetylcholinesterase. Identification of residues involved in catalytic activity and in polypeptide folding. J Biol Chem. 1992 Sep 5;267(25):17640-8. [PubMed Link Image]
  5. Velan B, Grosfeld H, Kronman C, Leitner M, Gozes Y, Lazar A, Flashner Y, Marcus D, Cohen S, Shafferman A: The effect of elimination of intersubunit disulfide bonds on the activity, assembly, and secretion of recombinant human acetylcholinesterase. Expression of acetylcholinesterase Cys-580----Ala mutant. J Biol Chem. 1991 Dec 15;266(35):23977-84. [PubMed Link Image]
  6. Soreq H, Ben-Aziz R, Prody CA, Seidman S, Gnatt A, Neville L, Lieman-Hurwitz J, Lev-Lehman E, Ginzberg D, Lipidot-Lifson Y, et al.: Molecular cloning and construction of the coding region for human acetylcholinesterase reveals a G + C-rich attenuating structure. Proc Natl Acad Sci U S A. 1990 Dec;87(24):9688-92. [PubMed Link Image]
  7. Chhajlani V, Derr D, Earles B, Schmell E, August T: Purification and partial amino acid sequence analysis of human erythrocyte acetylcholinesterase. FEBS Lett. 1989 Apr 24;247(2):279-82. [PubMed Link Image]
  8. Karpel R, Ben Aziz-Aloya R, Sternfeld M, Ehrlich G, Ginzberg D, Tarroni P, Clementi F, Zakut H, Soreq H: Expression of three alternative acetylcholinesterase messenger RNAs in human tumor cell lines of different tissue origins. Exp Cell Res. 1994 Feb;210(2):268-77. [PubMed Link Image]
  9. Bartels CF, Zelinski T, Lockridge O: Mutation at codon 322 in the human acetylcholinesterase (ACHE) gene accounts for YT blood group polymorphism. Am J Hum Genet. 1993 May;52(5):928-36. [PubMed Link Image]
  10. Felder CE, Botti SA, Lifson S, Silman I, Sussman JL: External and internal electrostatic potentials of cholinesterase models. J Mol Graph Model. 1997 Oct;15(5):318-27, 335-7. [PubMed Link Image]
Target 5 Drug References
  1. Sogorb-Sanchez MA, Vilanova-Gisbert E, Carrera-Gonzalez V: [Perspectives in the treatments of poisonings by organophosphorus insecticides and warfare nerve agents] Rev Neurol. 2004 Oct 16-31;39(8):739-47. [PubMed Link Image]
  2. Pajoumand A, Shadnia S, Rezaie A, Abdi M, Abdollahi M: Benefits of magnesium sulfate in the management of acute human poisoning by organophosphorus insecticides. Hum Exp Toxicol. 2004 Dec;23(12):565-9. [PubMed Link Image]
  3. Li W, Pi R, Chan HH, Fu H, Lee NT, Tsang HW, Pu Y, Chang DC, Li C, Luo J, Xiong K, Li Z, Xue H, Carlier PR, Pang Y, Tsim KW, Li M, Han Y: Novel dimeric acetylcholinesterase inhibitor bis7-tacrine, but not donepezil, prevents glutamate-induced neuronal apoptosis by blocking N-methyl-D-aspartate receptors. J Biol Chem. 2005 May 6;280(18):18179-88. Epub 2005 Feb 14. [PubMed Link Image]
  4. Bartosova L, Kuca K, Jun D, Kunesova G: Bispyridinium oximes as antidotal treatment of cyclosarin poisoning-in vitro and in vivo testing. Int J Toxicol. 2005 Nov-Dec;24(6):399-402. [PubMed Link Image]
  5. Kuca K, Cabal J, Jun D, Kassa J, Bartosova L, Kunesova G, Dohnal V: Strategy for the development of new acetylcholinesterase reactivators - antidotes used for treatment of nerve agent poisonings. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005 Dec;149(2):429-31. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 617
Target 6 Name Muscarinic acetylcholine receptor M2
Target 6 Synonyms Not Available
Target 6 Gene Name CHRM2
Target 6 Protein Sequence >Muscarinic acetylcholine receptor M2 
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNY
FLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFD
RYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQF
FSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRI
VKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDE
ITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNI
VARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT
VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
Target 6 Number of Residues 473
Target 6 Molecular Weight 51716
Target 6 Theoretical pI 9.08
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 adenylate cyclase inhibition
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 23-45
  • 60-80
  • 98-119
  • 140-162
  • 185-207
  • 389-409
  • 424-443
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 177990 Link Image
Target 6 UniProtKB/Swiss-Prot ID P08172 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name ACM2_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 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 6 GenBank Gene ID
Target 6 GeneCard ID CHRM2 Link Image
Target 6 GenAtlas ID CHRM2 Link Image
Target 6 HGNC ID HGNC:1951 Link Image
Target 6 Chromosome Location 7
Target 6 Locus 7q31-q35
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. 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. May LT, Lin Y, Sexton PM, Christopoulos A: Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators. J Pharmacol Exp Ther. 2005 Jan;312(1):382-90. Epub 2004 Aug 27. [PubMed Link Image]
  2. Nelson CP, Nahorski SR, Challiss RA: Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor. J Pharmacol Exp Ther. 2006 Jan;316(1):279-88. Epub 2005 Sep 27. [PubMed Link Image]
  3. Roman S, Badia A, Camps P, Munoz-Torrero D, Clos MV: Nicotinic-receptor potentiator drugs, huprine X and galantamine, increase ACh release by blocking AChE activity but not acting on nicotinic receptors. Brain Res. 2005 Nov 9;1061(2):73-9. Epub 2005 Oct 24. [PubMed Link Image]
  4. Minaba M, Ichiyama S, Kojima K, Ozaki M, Kato Y: Activation of nematode G protein GOA-1 by the human muscarinic acetylcholine receptor M2 subtype. Functional coupling of G-protein-coupled receptor and G protein originated from evolutionarily distant animals. FEBS J. 2006 Dec;273(24):5508-16. Epub 2006 Nov 3. [PubMed Link Image]
  5. Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 2394
Target 7 Name Phospholipase A2 VRV-PL-VIIIa
Target 7 Synonyms
  1. DPLA2
  2. EC 3.1.1.4
  3. Phosphatidylcholine 2- acylhydrolase
Target 7 Gene Name Not Available
Target 7 Protein Sequence >Phospholipase A2 VRV-PL-VIIIa 
SLLEFGKMILEETGKLAIPSYSSYGCYCGWGGKGTPKDATDRCCFVHDCCYGNLPDCNPK
SDRYKYKRVNGAIVCEKGTSCENRICECDKAAAICFRQNLNTYSKKYMLYPDFLCKGELK
C
Target 7 Number of Residues 123
Target 7 Molecular Weight 13611
Target 7 Theoretical pI 8.06
Target 7 GO Classification
Function
binding
ion binding
cation binding
calcium ion binding
catalytic activity
hydrolase activity
hydrolase activity, acting on ester bonds
carboxylic ester hydrolase activity
lipase activity
phospholipase activity
phospholipase A2 activity
Process
physiological process
metabolism
primary metabolism
lipid metabolism
lipid catabolism
Component
Not Available
Target 7 General Function Involved in phospholipase A2 activity
Target 7 Specific Function PA2 catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides. This toxin shows neurotoxic symptoms and damages vital organs such as lung, liver and kidney. Displays edema-inducing activities when injected into the foot pads of mice and induces necrosis of muscle cells when injected into the thigh muscle
Target 7 Pathways
Name SMPDB Link KEGG Link
Glycerophospholipid metabolism map00564 Link Image
Target 7 Reactions
  • phosphatidylcholine + H2O = 1-acylglycerophosphocholine + a carboxylate
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • None
Target 7 Essentiality Essential
Target 7 GenBank ID Protein Not Available
Target 7 UniProtKB/Swiss-Prot ID P59071 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name PA28_DABRP Link Image
Target 7 PDB ID 1Y38 Link Image
Target 7 PDB File Show
Target 7 3D Structure
Target 7 Cellular Location
  • Secreted protein
Target 7 Gene Sequence Not Available
Target 7 GenBank Gene ID
Target 7 GeneCard ID Not Available
Target 7 GenAtlas ID Not Available
Target 7 HGNC ID Not Available
Target 7 Chromosome Location Not Available
Target 7 Locus Not Available
Target 7 SNPs Not Available
Target 7 General References
  1. Kasturi S, Gowda TV: Purification and characterization of a major phospholipase A2 from Russell's viper (Vipera russelli) venom. Toxicon. 1989;27(2):229-37. [PubMed Link Image]
  2. Gowda VT, Schmidt J, Middlebrook JL: Primary sequence determination of the most basic myonecrotic phospholipase A2 from the venom of Vipera russelli. Toxicon. 1994 Jun;32(6):665-73. [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]

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.