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Showing drug card for Loperamide (DB00836)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:07:26
Primary Accession Number DB00836
Secondary Accession Number
  • APRD00275
Name Loperamide
Drug Type
  • Approved
  • Small Molecule
Description One of the long-acting synthetic antidiarrheals; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally. [PubChem]
Synonyms Not Available
Brand Names
  1. Apo-Loperamide
  2. Diarr-Eze
  3. Imodium
  4. Imodium A-D
  5. Imodium A-D Caplets
  6. Ioperamide
  7. Kaopectate II
  8. Loperacap
  9. Loperamida [INN-Spanish]
  10. Loperamide HCL
  11. Loperamidum [INN-Latin]
  12. Maalox Anti-Diarrheal
  13. Nu-Loperamide
  14. PMS-Loperamide
  15. Pepto Diarrhea Control
  16. Rho-Loperamide
Brand Mixtures Not Available
Chemical IUPAC Name 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-di(phenyl)butanamide
Chemical Formula C29H33ClN2O2
Chemical Structure Structure
CAS Registry Number 53179-11-6
InChI Identifier InChI=1/C29H33ClN2O2/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23/h3-16,34H,17-22H2,1-2H3
InChI Key RDOIQAHITMMDAJ-UHFFFAOYAJ
KEGG Drug Not Available
KEGG Compound C07080 Link Image
PubChem Compound 3955 Link Image
PubChem Substance 9291 Link Image
ChEBI ID Not Available
PharmGKB ID PA450262 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02240415 Link Image
RxList Link http://www.rxlist.com/cgi/generic3/loperamide.htm Link Image
PDRhealth Link http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/imo1206.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Loperamide Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 477.0380
Monoisotopic Molecular Weight 476.2231
State Solid
Melting Point 228 oC
Experimental Water Solubility Slight Source: PhysProp
Predicted Water Solubility 8.60e-04 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 5.5 Source: PhysProp
Predicted LogP 4.44 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -5.74 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 CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1
Canonical SMILES CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1
Drug Category
  • Antidiarrheals
ATC Codes
AHFS Codes
  • 56:08.00
Indication For the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease or gastroenteritis. Also used for reducing the volume of discharge from ileostomies.
Pharmacology Loperamide is a synthetic anti-diarrheal indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide is also indicated for reducing the volume of discharge from ileostomies. In man, Loperamide prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Loperamide is an opioid receptor agonist and acts on the mu opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids. It works specifically by decreasing the activity of the myenteric plexus which decreases the motility of the circular and longitudinal smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.
Mechanism of Action In vitro and animal studies show that Loperamide acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide inhibits peristaltic activity by a direct effect on the circular and longitudinal muscles of the intestinal wall. It is a non-selective calcium channel blocker and binds to opioid mu-receptors. Evidence also suggests that at higher concentrations it binds to NMDA receptors and to calmodulin.
Absorption Not significantly absorbed from the gut
Toxicity Oral, mouse: LD50 = 105 mg/kg. Symptoms of overdose include constipation, drowsiness, lethargy, and nausea.
Protein Binding 97%
Biotransformation Hepatic
Half Life 9.1 to 14.4 hours (average 10.8 hours)
Dosage Forms
Form Route
Solution Oral
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions
  • Take without regard to meals. Increase liquid intake.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
  4. PDRhealth Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
Targets
  1. Voltage-dependent P/Q-type calcium channel subunit alpha-1A
  2. Glutamate [NMDA] receptor subunit epsilon-4
  3. Glutamate [NMDA] receptor subunit epsilon-2
  4. Calmodulin
  5. Delta-type opioid receptor
  6. Glutamate [NMDA] receptor subunit epsilon-3
  7. Glutamate [NMDA] receptor subunit epsilon-1
  8. Mu-type opioid receptor
  9. Corticotropin-lipotropin
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Drug Target 1 [top]
Target 1 ID 392
Target 1 Name Voltage-dependent P/Q-type calcium channel subunit alpha-1A
Target 1 Synonyms
  1. BI
  2. Brain calcium channel I
  3. Calcium channel, L type, alpha-1 polypeptide isoform 4
  4. Voltage- gated calcium channel subunit alpha Cav2.1
Target 1 Gene Name CACNA1A
Target 1 Protein Sequence >Voltage-dependent P/Q-type calcium channel subunit alpha-1A 
MARFGDEMPARYGGGGSGAAAGVVVGSGGGRGAGGSRQGGQPGAQRMYKQSMAQRARTMA
LYNPIPVRQNCLTVNRSLFLFSEDNVVRKYAKKITEWPPFEYMILATIIANCIVLALEQH
LPDDDKTPMSERLDDTEPYFIGIFCFEAGIKIIALGFAFHKGSYLRNGWNVMDFVVVLTG
ILATVGTEFDLRTLRAVRVLRPLKLVSGIPSLQVVLKSIMKAMIPLLQIGLLLFFAILIF
AIIGLEFYMGKFHTTCFEEGTDDIQGESPAPCGTEEPARTCPNGTKCQPYWEGPNNGITQ
FDNILFAVLTVFQCITMEGWTDLLYNSNDASGNTWNWLYFIPLIIIGSFFMLNLVLGVLS
GEFAKERERVENRRAFLKLRRQQQIERELNGYMEWISKAEEVILAEDETDGEQRHPFDGA
LRRTTIKKSKTDLLNPEEAEDQLADIASVGSPFARASIKSAKLENSTFFHKKERRMRFYI
RRMVKTQAFYWTVLSLVALNTLCVAIVHYNQPEWLSDFLYYAEFIFLGLFMSEMFIKMYG
LGTRPYFHSSFNCFDCGVIIGSIFEVIWAVIKPGTSFGISVLRALRLLRIFKVTKYWASL
RNLVVSLLNSMKSIISLLFLLFLFIVVFALLGMQLFGGQFNFDEGTPPTNFDTFPAAIMT
VFQILTGEDWNEVMYDGIKSQGGVQGGMVFSIYFIVLTLFGNYTLLNVFLAIAVDNLANA
QELTKDEQEEEEAANQKLALQKAKEVAEVSPLSAANMSIAVKEQQKNQKPAKSVWEQRTS
EMRKQNLLASREALYNEMDPDERWKAAYTRHLRPDMKTHLDRPLVVDPQENRNNNTNKSR
AAEPTVDQRLGQQRAEDFLRKQARYHDRARDPSGSAGLDARRPWAGSQEAELSREGPYGR
ESDHHAREGSLEQPGFWEGEAERGKAGDPHRRHVHRQGGSRESRSGSPRTGADGEHRRHR
AHRRPGEEGPEDKAERRARHREGSRPARGGEGEGEGPDGGERRRRHRHGAPATYEGDARR
EDKERRHRRRKENQGSGVPVSGPNLSTTRPIQQDLGRQDPPLAEDIDNMKNNKLATAESA
APHGSLGHAGLPQSPAKMGNSTDPGPMLAIPAMATNPQNAASRRTPNNPGNPSNPGPPKT
PENSLIVTNPSGTQTNSAKTARKPDHTTVDIPPACPPPLNHTVVQVNKNANPDPLPKKEE
EKKEEEEDDRGEDGPKPMPPYSSMFILSTTNPLRRLCHYILNLRYFEMCILMVIAMSSIA
LAAEDPVQPNAPRNNVLRYFDYVFTGVFTFEMVIKMIDLGLVLHQGAYFRDLWNILDFIV
VSGALVAFAFTGNSKGKDINTIKSLRVLRVLRPLKTIKRLPKLKAVFDCVVNSLKNVFNI
LIVYMLFMFIFAVVAVQLFKGKFFHCTDESKEFEKDCRGKYLLYEKNEVKARDREWKKYE
FHYDNVLWALLTLFTVSTGEGWPQVLKHSVDATFENQGPSPGYRMEMSIFYVVYFVVFPF
FFVNIFVALIIITFQEQGDKMMEEYSLEKNERACIDFAISAKPLTRHMPQNKQSFQYRMW
QFVVSPPFEYTIMAMIALNTIVLMMKFYGASVAYENALRVFNIVFTSLFSLECVLKVMAF
GILNYFRDAWNIFDFVTVLGSITDILVTEFGNNFINLSFLRLFRAARLIKLLRQGYTIRI
LLWTFVQSFKALPYVCLLIAMLFFIYAIIGMQVFGNIGIDVEDEDSDEDEFQITEHNNFR
TFFQALMLLFRSATGEAWHNIMLSCLSGKPCDKNSGILTRECGNEFAYFYFVSFIFLCSF
LMLNLFVAVIMDNFEYLTRDSSILGPHHLDEYVRVWAEYDPAAWGRMPYLDMYQMLRHMS
PPLGLGKKCPARVAYKRLLRMDLPVADDNTVHFNSTLMALIRTALDIKIAKGGADKQQMD
AELRKEMMAIWPNLSQKTLDLLVTPHKSTDLTVGKIYAAMMIMEYYRQSKAKKLQAMREE
QDRTPLMFQRMEPPSPTQEGGPGQNALPSTQLDPGGALMAHESGLKESPSWVTQRAQEMF
QKTGTWSPEQGPPTDMPNSQPNSQSVEMREMGRDGYSDSEHYLPMEGQGRAASMPRLPAE
NQRRRGRPRGNNLSTISDTSPMKRSASVLGPKARRLDDYSLERVPPEENQRHHQRRRDRS
HRASERSLGRYTDVDTGLGTDLSMTTQSGDLPSKERDQERGRPKDRKHRQHHHHHHHHHH
PPPPDKDRYAQERPDHGRARARDQRWSRSPSEGREHMAHRQGSSSVSGSPAPSTSGTSTP
RRGRRQLPQTPSTPRPHVSYSPVIRKAGGSGPPQQQQQQQQQQQAVARPGRAATSGPRRY
PGPTAEPLAGDRPPTGGHSSGRSPRMERRVPGPARSESPRACRHGGARWPASGPHVSEGP
PGPRHHGYYRGSDYDEADGPGSGGGEEAMAGAYDAPPPVRHASSGATGRSPRTPRASGPA
CASPSRHGRRLPNGYYPAHGLARPRGPGSRKGLHEPYSESDDDWC
Target 1 Number of Residues 2546
Target 1 Molecular Weight 282368
Target 1 Theoretical pI 9.10
Target 1 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
voltage-gated ion channel activity
voltage-gated calcium channel activity
Process
physiological process
cellular physiological process
transport
ion transport
cation transport
di-, tri-valent inorganic cation transport
calcium ion transport
Component
intrinsic to membrane
integral to membrane
cell
membrane
protein complex
voltage-gated calcium channel complex
Target 1 General Function Involved in voltage-gated calcium channel activity
Target 1 Specific Function Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1A gives rise to P and/or Q-type calcium currents. P/Q-type calcium channels belong to the "high-voltage activated" (HVA) group and are blocked by the funnel toxin (Ftx) and by the omega-agatoxin- IVA (omega-Aga-IVA). They are however insensitive to dihydropyridines (DHP), and omega-conotoxin-GVIA (omega-CTx-GVIA)
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 99-117
  • 136-155
  • 168-185
  • 191-209
  • 229-248
  • 336-360
  • 488-506
  • 522-541
  • 550-568
  • 579-597
  • 617-636
  • 690-714
  • 1243-1261
  • 1278-1297
  • 1310-1328
  • 1340-1358
  • 1378-1397
  • 1485-1509
  • 1565-1593
  • 1599-1618
  • 1627-1645
  • 1653-1671
  • 1691-1710
  • 1783-1807
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 2213913 Link Image
Target 1 UniProtKB/Swiss-Prot ID O00555 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name CAC1A_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >7533 bp 
ATGGCCCGCTTCGGAGACGAGATGCCGGCCCGCTACGGGGGAGGAGGCTCCGGGGCAGCC
GCCGGGGTGGTCGTGGGCAGCGGAGGCGGGCGAGGAGCCGGGGGCAGCCGGCAGGGCGGG
CAGCCCGGGGCGCAAAGGATGTACAAGCAGTCAATGGCGCAGAGAGCGCGGACCATGGCA
CTCTACAACCCCATCCCCGTCCGACAGAACTGCCTCACGGTTAACCGGTCTCTCTTCCTC
TTCAGCGAAGACAACGTGGTGAGAAAATACGCCAAAAAGATCACCGAATGGCCTCCCTTT
GAATATATGATTTTAGCCACCATCATAGCGAATTGCATCGTCCTCGCACTGGAGCAGCAT
CTGCCTGATGATGACAAGACCCCGATGTCTGAACGGCTGGATGACACAGAACCATACTTC
ATTGGAATTTTTTGTTTCGAGGCTGGAATTAAAATCATTGCCCTTGGGTTTGCCTTCCAC
AAAGGCTCCTACTTGAGGAATGGCTGGAATGTCATGGACTTTGTGGTGGTGCTAACGGGC
ATCTTGGCGACAGTTGGGACGGAGTTTGACCTACGGACGCTGAGGGCAGTTCGAGTGCTG
CGGCCGCTCAAGCTGGTGTCTGGAATCCCAAGTTTACAAGTCGTCCTGAAGTCGATCATG
AAGGCGATGATCCCTTTGCTGCAGATCGGCCTCCTCCTATTTTTTGCAATCCTTATTTTT
GCAATCATAGGGTTAGAATTTTATATGGGAAAATTTCATACCACCTGCTTTGAAGAGGGG
ACAGATGACATTCAGGGTGAGTCTCCGGCTCCATGTGGGACAGAAGAGCCCGCCCGCACC
TGCCCCAATGGGACCAAATGTCAGCCCTACTGGGAAGGGCCCAACAACGGGATCACTCAG
TTCGACAACATCCTGTTTGCAGTGCTGACTGTTTTCCAGTGCATAACCATGGAAGGGTGG
ACTGATCTCCTCTACAATAGCAACGATGCCTCAGGGAACACTTGGAACTGGTTGTACTTC
ATCCCCCTCATCATCATCGGCTCCTTTTTTATGCTGAACCTTGTGCTGGGTGTGCTGTCA
GGGGAGTTTGCCAAAGAAAGGGAACGGGTGGAGAACCGGCGGGCTTTTCTGAAGCTGAGG
CGGCAACAACAGATTGAACGTGAGCTCAATGGGTACATGGAATGGATCTCAAAAGCAGAA
GAGGTGATCCTCGCCGAGGATGAAACTGACGGGGAGCAGAGGCATCCCTTTGATGGAGCT
CTGCGGAGAACCACCATAAAGAAAAGCAAGACAGATTTGCTCAACCCCGAAGAGGCTGAG
GATCAGCTGGCTGATATAGCCTCTGTGGGTTCTCCCTTCGCCCGAGCCAGCATTAAAAGT
GCCAAGCTGGAGAACTCGACCTTTTTTCACAAAAAGGAGAGGAGGATGCGTTTCTACATC
CGCCGCATGGTCAAAACTCAGGCCTTCTACTGGACTGTACTCAGTTTGGTAGCTCTCAAC
ACGCTGTGTGTTGCTATTGTTCACTACAACCAGCCCGAGTGGCTCTCCGACTTCCTTTAC
TATGCAGAATTCATTTTCTTAGGACTCTTTATGTCCGAAATGTTTATAAAAATGTACGGG
CTTGGGACGCGGCCTTACTTCCACTCTTCCTTCAACTGCTTTGACTGTGGGGTTATCATT
GGGAGCATCTTCGAGGTCATCTGGGCTGTCATAAAACCTGGCACATCCTTTGGAATCAGC
GTGTTACGAGCCCTCAGGTTATTGCGTATTTTCAAAGTCACAAAGTACTGGGCATCTCTC
AGAAACCTGGTCGTCTCTCTCCTCAACTCCATGAAGTCCATCATCAGCCTGTTGTTTCTC
CTTTTCCTGTTCATTGTCGTCTTCGCCCTTTTGGGAATGCAACTCTTCGGCGGCCAGTTT
AATTTCGATGAAGGGACTCCTCCCACCAACTTCGATACTTTTCCAGCAGCAATAATGACG
GTGTTTCAGATCCTGACGGGCGAAGACTGGAACGAGGTCATGTACGACGGGATCAAGTCT
CAGGGGGGCGTGCAGGGCGGCATGGTGTTCTCCATCTATTTCATTGTACTGACGCTCTTT
GGGAACTACACCCTCCTGAATGTGTTCTTGGCCATCGCTGTGGACAATCTGGCCAACGCC
CAGGAGCTCACCAAGGTGGAGGCGGACGAGCAAGAGGAAGAAGAAGCAGCGAACCAGAAA
CTTGCCCTACAGAAAGCCAAGGAGGTGGCAGAAGTGAGTCCTCTGTCCGCGGCCAACATG
TCTATAGCTGTGAAAGAGCAACAGAAGAATCAAAAGCCAGCCAAGTCCGTGTGGGAGCAG
CGGACCAGTGAGATGCGAAAGCAGAACTTGCTGGCCAGCCGGGAGGCCCTGTATAACGAA
ATGGACCCGGACGAGCGCTGGAAGGCTGCCTACACGCGGCACCTGCGGCCAGACATGAAG
ACGCACTTGGACCGGCCGCTGGTGGTGGACCCGCAGGAGAACCGCAACAACAACACCAAC
AAGAGCCGGGCGGCCGAGCCCACCGTGGACCAGCGCCTCGGCCAGCAGCGCGCCGAGGAC
TTCCTCAGGAAACAGGCCCGCTACCACGATCGGGCCCGGGACCCCAGCGGCTCGGCGGGC
CTGGACGCACGGAGGCCCTGGGCGGGAAGCCAGGAGGCCGAGCTGAGCCGGGAGGGACCC
TACGGCCGCGAGTCGGACCACCACGCCCGGGAGGGCAGCCTGGAGCAACCCGGGTTCTGG
GAGGGCGAGGCCGAGCGAGGCAAGGCCGGGGACCCCCACCGGAGGCACGTGCACCGGCAG
GGGGGCAGCAGGGAGAGCCGCAGCGGGTCCCCGCGCACGGGCGCGGACGGGGAGCATCGA
CGTCATCGCGCGCACCGCAGGCCCGGGGAGGAGGGTCCGGAGGACAAGGCGGAGCGGAGG
GCGCGGCACCGCGAGGGCAGCCGGCCGGCCCGGGGCGGCGAGGGCGAGGGCGAGGGCCCC
GACGGGGGCGAGCGCAGGAGAAGGCACCGGCATGGCGCTCCAGCCACGTACGAGGGGGAC
GCGCGGAGGGAGGACAAGGAGCGGAGGCATCGGAGGAGGAAAGAGAACCAGGGCTCCGGG
GTCCCTGTGTCGGGCCCCAACCTGTCAACCACCCGGCCAATCCAGCAGGACCTGGGCCGC
CAAGACCCACCCCTGGCAGAGGATATTGACAACATGAAGAACAACAAGCTGGCCACCGCG
GAGTCGGCCGCTCCCCACGGCAGCCTTGGCCACGCCGGCCTGCCCCAGAGCCCAGCCAAG
ATGGGAAACAGCACCGACCCCGGCCCCATGCTGGCCATCCCTGCCATGGCCACCAACCCC
CAGAACGCCGCCAGCCGCCGGACGCCCAACAACCCGGGGAACCCATCCAATCCCGGCCCC
CCCAAGACCCCCGAGAATAGCCTTATCGTCACCAACCCCAGCGGCACCCAGACCAATTCA
GCTAAGACTGCCAGGAAACCCGACCACACCACAGTGGACATCCCCCCAGCCTGCCCACCC
CCCCTCAACCACACCGTCGTACAAGTGAACAAAAACGCCAACCCAGACCCACTGCCAAAA
AAAGAGGAAGAGAAGAAGGAGGAGGAGGAAGACGACCGTGGGGAAGACGGCCCTAAGCCA
ATGCCTCCCTATAGCTCCATGTTCATCCTGTCCACGACCAACCCCCTTCGCCGCCTGTGC
CATTACATCCTGAACCTGCGCTACTTTGAGATGTGCATCCTCATGGTCATTGCCATGAGC
AGCATCGCCCTGGCCGCCGAGGACCCTGTGCAGCCCAACGCACCTCGGAACAACGTGCTG
CGATACTTTGACTACGTTTTTACAGGCGTCTTCACCTTTGAGATGGTGATCAAGATGATT
GACCTGGGGCTCGTCCTGCATCAGGGTGCCTACTTCCGTGACCTCTGGAATATTCTCGAC
TTCATAGTGGTCAGTGGGGCCCTGGTAGCCTTTGCCTTCACTGGCAATAGCAAAGGAAAA
GACATCAACACGATTAAATCCCTCCGAGTCCTCCGGGTGCTACGACCTCTTAAAACCATC
AAGCGGCTGCCAAAGCTCAAGGCTGTGTTTGACTGTGTGGTGAACTCACTTAAAAACGTC
TTCAACATCCTCATCGTCTACATGCTATTCATGTTCATCTTCGCCGTGGTGGCTGTGCAG
CTCTTCAAGGGGAAATTCTTCCACTGCACTGACGAGTCCAAAGAGTTTGAGAAAGATTGT
CGAGGCAAATACCTCCTCTACGAGAAGAATGAGGTGAAGGCGCGAGACCGGGAGTGGAAG
AAGTATGAATTCCATTACGACAATGTGCTGTGGGCTCTGCTGACCCTCTTCACCGTGTCC
ACGGGAGAAGGCTGGCCACAGGTCCTCAAGCATTCGGTGGACGCCACCTTTGAGAACCAG
GGCCCCAGCCCCGGGTACCGCATGGAGATGTCCATTTTCTACGTCGTCTACTTTGTGGTG
TTCCCCTTCTTCTTTGTCAATATCTTTGTGGCCTTGATCATCATCACCTTCCAGGAGCAA
GGGGACAAGATGATGGAGGAATACAGCCTGGAGAAAAATGAGAGGGCCTGCATTGATTTC
GCCATCAGCGCCAAGCCGCTGACCCGACACATGCCGCAGAACAAGCAGAGCTTCCAGTAC
CGCATGTGGCAGTTCGTGGTGTCTCCGCCTTTCGAGTACACGATCATGGCCATGATCGCC
CTCAACACCATCGTGCTTATGATGAAGTTCTATGGGGCTTCTGTTGCTTATGAAAATGCC
CTGCGGGTGTTCAACATCGTCTTCACCTCCCTCTTCTCTCTGGAATGTGTGCTGAAAGTC
ATGGCTTTTGGGATTCTGAATTATTTCCGCGATGCCTGGAACATCTTCGACTTTGTGACT
GTTCTGGGCAGCATCACCGATATCCTCGTGACTGAGTTTGGGAATCCGAATAACTTCATC
AACCTGAGCTTTCTCCGCCTCTTCCGAGCTGCCCGGCTCATCAAACTTCTCCGTCAGGGT
TACACCATCCGCATTCTTCTCTGGACCTTTGTGCAGTCCTTCAAGGCCCTGCCTTATGTC
TGTCTGCTGATCGCCATGCTCTTCTTCATCTATGCCATCATTGGGATGCAGGTGTTTGGT
AACATTGGCATCGACGTGGAGGACGAGGACAGTGATGAAGATGAGTTCCAAATCACTGAG
CACAATAACTTCCGGACCTTCTTCCAGGCCCTCATGCTTCTCTTCCGGAGTGCCACCGGG
GAAGCTTGGCACAACATCATGCTTTCCTGCCTCAGCGGGAAACCGTGTGATAAGAACTCT
GGCATCCTGACTCGAGAGTGTGGCAATGAATTTGCTTATTTTTACTTTGTTTCCTTCATC
TTCCTCTGCTCGTTTCTGATGCTGAATCTCTTTGTCGCCGTCATCATGGACAACTTTGAG
TACCTCACCCGAGACTCCTCCATCCTGGGCCCCCACCACCTGGATGAGTACGTGCGTGTC
TGGGCCGAGTATGACCCCGCAGCTTGGGGCCGCATGCCTTACCTGGACATGTATCAGATG
CTGAGACACATGTCTCCGCCCCTGGGTCTGGGGAAGAAGTGTCCGGCCAGAGTGGCTTAC
AAGCGGCTTCTGCGGATGGACCTGCCCGTCGCAGATGACAACACCGTCCACTTCAATTCC
ACCCTCATGGCTCTGATCCGCACAGCCCTGGACATCAAGATTGCCAAGGGAGGAGCCGAC
AAACAGCAGATGGACGCTGAGCTGCGGAAGGAGATGATGGCGATTTGGCCCAATCTGTCC
CAGAAGACGCTAGACCTGCTGGTCACACCTCACAAGTCCACGGACCTCACCGTGGGGAAG
ATCTACGCAGCCATGATGATCATGGAGTACTACCGGCAGAGCAAGGCCAAGAAGCTGCAG
GCCATGCGCGAGGAGCAGGACCGGACACCCCTCATGTTCCAGCGCATGGAGCCCCCGTCC
CCAACGCAGGAAGGGGGACCTGGCCAGAACGCCCTCCCCTCCACCCAGCTGGACCCAGGA
GGAGCCCTGATGGCTCACGAAAGCGGCCTCAAGGAGAGCCCGTCCTGGGTGACCCAGCGT
GCCCAGGAGATGTTCCAGAAGACGGGCACATGGAGTCCGGAACAAGGCCCCCCTACCGAC
ATGCCCAACAGCCAGCCTAACTCTCAGTCCGTGGAGATGCGAGAGATGGGCAGAGATGGC
TACTCCGACAGCGAGCACTACCTCCCCATGGAAGGCCAGGGCCGGGCTGCCTCCATGCCC
CGCCTCCCTGCAGAGAACCAGAGGAGAAGGGGCCGGCCACGTGGGAATAACCTCAGTACC
ATCTCAGACACCAGCCCCATGAAGCGTTCAGCCTCCGTGCTGGGCCCCAAGGCCCGACGC
CTGGACGATTACTCGCTGGAGCGGGTCCCGCCCGAGGAGAACCAGCGGCACCACCAGCGG
CGCCGCGACCGCAGCCACCGCGCCTCTGAGCGCTCCCTGGGCCGCTACACCGATGTGGAC
ACAGGCTTGGGGACAGACCTGAGCATGACCACCCAATCCGGGGACCTGCCGTCGAAGGAG
CGGGACCAGGAGCGGGGCCGGCCCAAGGATCGGAAGCATCGACAGCACCACCACCACCAC
CACCACCACCACCATCCCCCGCCCCCCGACAAGGACCGCTATGCCCAGGAACGGCCGGAC
CACGGCCGGGCACGGGCTCGGGACCAGCGCTGGTCCCGCTCGCCCAGCGAGGGCCGAGAG
CACATGGCGCACCGGCAGGGCAGTAGTTCCGTAAGTGGAAGCCCAGCCCCCTCAACATCT
GGTACCAGCACTCCGCGGCGGGGCCGCCGCCAGCTCCCCCAGACCCCCTCCACCCCCCGG
CCACACGTGTCCTATTCCCCTGTGATCCGTAAGGCCGGCGGCTCGGGGCCCCCGCAGCAG
CAGCAGCAGCAGCAGCAGCAGCAGCAGGCGGTGGCCAGGCCGGGCCGGGCGGCCACCAGC
GGCCCTCGGAGGTACCCAGGCCCCACGGCCGAGCCTCTGGCCGGAGATCGGCCGCCCACG
GGGGGCCACAGCAGCGGCCGCTCGCCCAGGATGGAGAGGCGGGTCCCAGGCCCGGCCCGG
AGCGAGTCCCCCAGGGCCTGTCGACACGGCGGGGCCCGGTGGCCGGCATCTGGCCCGCAC
GTGTCCGAGGGGCCCCCGGGTCCCCGGCACCATGGCTACTACCGGGGCTCCGACTACGAC
GAGGCCGATGGCCCGGGCAGCGGGGGCGGCGAGGAGGCCATGGCCGGGGCCTACGACGCG
CCACCCCCCGTACGACACGCGTCCTCGGGCGCCACCGGGCGCTCGCCCAGGACTCCCCGG
GCCTCGGGCCCGGCCTGCGCCTCGCCTTCTCGGCACGGCCGGCGACTCCCCAACGGCTAC
TACCCGGCGCACGGACTGGCCAGGCCCCGCGGGCCGGGCTCCAGGAAGGGCCTGCACGAA
CCCTACAGCGAGAGTGACGATGATTGGTGCTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID CACNA1A Link Image
Target 1 GenAtlas ID CACNA1A Link Image
Target 1 HGNC ID HGNC:1388 Link Image
Target 1 Chromosome Location 19
Target 1 Locus 19p13.2-p13.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Hans M, Urrutia A, Deal C, Brust PF, Stauderman K, Ellis SB, Harpold MM, Johnson EC, Williams ME: Structural elements in domain IV that influence biophysical and pharmacological properties of human alpha1A-containing high-voltage-activated calcium channels. Biophys J. 1999 Mar;76(3):1384-400. [PubMed Link Image]
  2. Barry EL, Viglione MP, Kim YI, Froehner SC: Expression and antibody inhibition of P-type calcium channels in human small-cell lung carcinoma cells. J Neurosci. 1995 Jan;15(1 Pt 1):274-83. [PubMed Link Image]
  3. Margolis RL, Breschel TS, Li SH, Kidwai AS, Antonarakis SE, McInnis MG, Ross CA: Characterization of cDNA clones containing CCA trinucleotide repeats derived from human brain. Somat Cell Mol Genet. 1995 Jul;21(4):279-84. [PubMed Link Image]
  4. Ophoff RA, Terwindt GM, Vergouwe MN, van Eijk R, Oefner PJ, Hoffman SM, Lamerdin JE, Mohrenweiser HW, Bulman DE, Ferrari M, Haan J, Lindhout D, van Ommen GJ, Hofker MH, Ferrari MD, Frants RR: Familial hemiplegic migraine and episodic ataxia type-2 are caused by mutations in the Ca2+ channel gene CACNL1A4. Cell. 1996 Nov 1;87(3):543-52. [PubMed Link Image]
  5. Zhuchenko O, Bailey J, Bonnen P, Ashizawa T, Stockton DW, Amos C, Dobyns WB, Subramony SH, Zoghbi HY, Lee CC: Autosomal dominant cerebellar ataxia (SCA6) associated with small polyglutamine expansions in the alpha 1A-voltage-dependent calcium channel. Nat Genet. 1997 Jan;15(1):62-9. [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 439
Target 2 Name Glutamate [NMDA] receptor subunit epsilon-4
Target 2 Synonyms
  1. EB11
  2. Glutamate receptor subunit epsilon-4 precursor
  3. N-methyl D- aspartate receptor subtype 2D
  4. NMDAR2D
  5. NR2D
Target 2 Gene Name GRIN2D
Target 2 Protein Sequence >Glutamate [NMDA] receptor subunit epsilon 4 precursor 
MRGAGGPRGPRGPAKMLLLLALACASPFPEEAPGPGGAGGPGGGLGGARPLNVALVFSGP
AYAAEAARLGPAVAAAVRSPGLDVRPVALVLNGSDPRSLVLQLCDLLSGLRVHGVVFEDD
SRAPAVAPILDFLSAQTSLPIVAVHGGAALVLTPKEKGSTFLQLGSSTEQQLQVIFEVLE
EYDWTSFVAVTTRAPGHRAFLSYIEVLTDGSLVGWEHRGALTLDPGAGEAVLSAQLRSVS
AQIRLLFCAREEAEPVFRAAEEAGLTGSGYVWFMVGPQLAGGGGSGAPGEPPLLPGGAPL
PAGLFAVRSAGWRDDLARRVAAGVAVVARGAQALLRDYGFLPELGHDCRAQNRTHRGESL
HRYFMNITWDNRDYSFNEDGFLVNPSLVVISLTRDRTWEVVGSWEQQTLRLKYPLWSRYG
RFLQPVDDTQHLTVATLEERPFVIVEPADPISGTCIRDSVPCRSQLNRTHSPPPDAPRPE
KRCCKGFCIDILKRLAHTIGFSYDLYLVTNGKHGKKIDGVWNGMIGEVFYQRADMAIGSL
TINEERSEIVDFSVPFVETGISVMVARSNGTVSPSAFLEPYSPAVWVMMFVMCLTVVAVT
VFIFEYLSPVGYNRSLATGKRPGGSTFTIGKSIWLLWALVFNNSVPVENPRGTTSKIMVL
VWAFFAVIFLASYTANLAAFMIQEEYVDTVSGLSDRKFQRPQEQYPPLKFGTVPNGSTEK
NIRSNYPDMHSYMVRYNQPRVEEALTQLKAGKLDAFIYDAAVLNYMARKDEGCKLVTIGS
GKVFATTGYGIALHKGSRWKRPIDLALLQFLGDDEIEMLERLWLSGICHNDKIEVMSSKL
DIDNMAGVFYMLLVAMGLSLLVFAWEHLVYWRLRHCLGPTHRMDFLLAFSRGMYSCCSAE
AAPPPAKPPPPPQPLPSPAYPAPGPAPGPAPFVPRERASVDRWRRTKGAGPPGGAGLADG
FHRYYGPIEPQGLGLGLGEARAAPRGAAGRPLSPPAAQPPQKPPASYFAIVRDKEPAEPP
AGAFPGFPSPPAPPAAAATAVGPPLCRLAFEDESPPAPARWPRSDPESQPLLGPGAGGAG
GTGGAGGGAPAAPPPCCAAPPPCPYLDLEPSPSDSEDSESLGGASLGGLDPWWFADFPYP
YAERLGPPPGRYWSVDKLGGWRAGSWDYLPPRSGPAAWHCRHCASLELLPPPRHLSCSHD
GLDGGWWAPPPPPWAAGPLPRRRARCGCPRSHPHRPRASHRTPAAAAPHHHRHRRAAGGW
DLPPPAPTSRSLEDLSSCPRAAPARRLTGPSRHARRCPHAAHWGPPLPTASHRRHRGGDL
GTRRGSAHFSSLESEV
Target 2 Number of Residues 1358
Target 2 Molecular Weight 143561
Target 2 Theoretical pI 8.27
Target 2 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 2 General Function Secondary metabolites biosynthesis, transport and catabolism
Target 2 Specific Function NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-27
Target 2 Transmembrane Regions
  • 584-604
  • 627-647
  • 657-677
  • 845-865
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 2444026 Link Image
Target 2 UniProtKB/Swiss-Prot ID O15399 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name NMDE4_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >4011 bp 
ATGCGCGGCGCCGGTGGCCCCCGCGGCCCTCGGGGCCCCGCTAAGATGCTGCTGCTGCTG
GCGCTGGCCTGCGCCAGCCCGTTCCCGGAGGAGGCGCCGGGGCCGGGCGGGGCCGGTGGG
CCCGGCGGCGGCCTCGGCGGGGCGCGGCCGCTCAACGTGGCGCTCGTGTTCTCGGGGCCC
GCGTACGCGGCCGAGGCGGCACGCCTGGGCCCGGCCGTGGCGGCGGCGGTGCGCAGCCCG
GGCCTAGACGTGCGGCCCGTGGCGCTGGTGCTCAACGGCTCGGACCCGCGCAGCCTCGTG
CTGCAGCTCTGCGACCTGCTGTCGGGGTTGCGCGTGCACGGCGTGGTCTTCGAAGACGAC
TCGCGCGCGCCCGCCGTCGCGCCCATCCTCGACTTCCTGTCGGCGCAGACCTCGCTGCCC
ATCGTGGCCGTGCACGGCGGCGCCGCGCTCGTGCTCACGCCCAAGGAGAAGGGCTCCACC
TTCCTGCAGCTGGGCTCTTCCACCGAGCAACAGCTTCAGGTCATCTTTGAGGTGCTGGAG
GAGTATGACTGGACGTCCTTTGTAGCCGTGACCACTCGTGCCCCTGGCCACCGGGCCTTC
CTGTCCTACATTGAGGTGCTGACTGACGGTAGTCTGGTGGGCTGGGAGCACCGCGGAGCG
CTGACGCTGGACCCTGGGGCGGGCGAGGCCGTGCTCAGTGCCCAGCTCCGCAGTGTCAGC
GCGCAGATCCGCCTGCTCTTCTGCGCCCGAGAGGAGGCCGAGCCCGTGTTCCGCGCAGCT
GAGGAGGCTGGCCTCACTGGATCTGGCTACGTCTGGTTCATGGTGGGGCCCCAGCTGGCT
GGAGGCGGGGGCTCTGGGGCCCCTGGTGAGCCCCCTCTTCTGCCAGGAGGCGCCCCCCTG
CCTGCCGGGCTGTTTGCAGTGCGCTCGGCTGGCTGGCGGGATGACCTGGCTCGGCGAGTG
GCAGCTGGCGTGGCCGTAGTGGCCAGAGGTGCCCAGGCCCTGCTGCGTGATTATGGTTTC
CTTCCTGAGCTCGGCCACGACTGTCGCGCCCAGAACCGCACCCACCGCGGCGAGAGTCTG
CATAGGTACTTCATGAACATCACGTGGGATAACCGGGATTACTCCTTCAATGAGGACGGC
TTCCTAGTGAACCCCTCCCTGGTGGTCATCTCCCTCACCAGAGACAGGACGTGGGAGGTG
GTGGGCAGCTGGGAGCAGCAGACGCTCCGCCTCAAGTACCCGCTGTGGTCCCGCTATGGT
CGCTTCCTGCAGCCAGTGGACGACACGCAGCACCTCACGGTGGCCACGCTGGAGGAAAGG
CCGTTTGTCATCGTGGAGCCTGCAGACCCTATCAGCGGCACCTGCATCCGAGACTCCGTC
CCCTGCCGGAGCCAGCTCAACCGAACCCACAGCCCTCCACCGGATGCCCCCCGCCCGGAA
AAGCGCTGCTGCAAGGGTTTCTGCATCGACATTCTGAAGCGGCTGGCGCATACCATCGGC
TTCAGCTACGACCTCTACCTGGTCACCAATGGCAAGCACGGAAAGAAGATCGATGGCGTC
TGGAACGGCATGATCGGGGAGGTGTTCTACCAGCGCGCAGACATGGCCATCGGCTCCCTC
ACCATCAACGAGGAGCGCTCCGAGATCGTGGACTTCTCCGTCCCCTTCGTGGAGACCGGC
ATCAGCGTCATGGTGGCGCGCAGCAATGGCACGGTGTCCCCCTCGGCCTTCCTCGAGCCC
TACAGCCCCGCCGTGTGGGTGATGATGTTCGTCATGTGCCTCACTGTGGTCGCCGTCACT
GTTTTCATCTTCGAGTACCTCAGTCCTGTTGGTTACAACCGCAGCCTGGCCACGGGCAAG
CGCCCTGGCGGTTCAACCTTCACCATTGGGAAATCCATCTGGCTGCTCTGGGCCCTGGTG
TTCAATAATTCGGTGCCCGTGGAGAACCCCCGGGGAACCACCAGCAAAATCATGGTGCTG
GTGTGGGCCTTCTTCGCCGTCATCTTCCTCGCCAGCTACACAGCCAACCTGGCCGCCTTC
ATGATCCAGGAGGAGTACGTGGATACTGTGTCTGGGCTCAGTGACCGCAAGTTCCAGAGG
CCCCAGGAGCAGTACCCGCCCCTGAAGTTTGGGACCGTGCCCAACGGCTCCACGGAGAAG
AACATCCGCAGCAACTATCCCGACATGCACAGCTACATGGTGCGCTACAACCAGCCCCGC
GTAGAGGAAGCGCTCACTCAGCTCAAGGCAGGGAAGCTGGACGCCTTCATCTACGATGCT
GCAGTGCTCAATTACATGGCCCGCAAGGACGAGGGCTGCAAGCTTGTCACCATCGGCTCC
GGCAAGGTCTTCGCCACGACAGGCTATGGCATCGCCCTGCACAAGGGCTCCCGCTGGAAG
CGGCCCATCGACCTGGCGTTGCTGCAGTTCCTGGGGGATGATGAGATCGAGATGCTGGAG
CGGCTGTGGCTCTCTGGGATCTGCCACAATGACAAAATCGAGGTGATGAGCAGCAAGCTG
GACATCGACAACATGGCGGGCGTCTTCTACATGCTCCTGGTGGCCATGGGCCTGTCCCTG
CTGGTCTTCGCCTGGGAGCACCTGGTGTACTGGCGCCTGCGGCACTGCCTGGGGCCCACC
CACCGCATGGACTTCCTGCTGGCCTTCTCCAGGGGCATGTACAGCTGCTGCAGCGCTGAG
GCCGCCCCACCGCCCGCCAAGCCCCCGCCGCCGCCACAGCCCCTGCCCAGCCCCGCGTAC
CCCGCGCCGGGGCCGGCTCCCGGGCCCGCACCTTTCGTGCCCCGCGAGCGCGCCTCAGTG
GACCGCTGGCGCCGGACCAAGGGCGCGGGGCCGCCGGGGGGCGCGGGCCTGGCCGACGGC
TTCCACCGCTACTACGGCCCCATCGAGCCGCAGGGCCTAGGCCTCGGCCTGGGCGAAGCG
CGCGCGGCACCGCGGGGCGCAGCCGGGCGCCCGCTGTCCCCGCCGGCCGCTCAGCCCCCG
CAGAAGCCGCCGGCCTCCTATTTCGCCATCGTACGCGACAAGGAGCCAGCCGAGCCCCCC
GCCGGCGCCTTCCCCGGCTTCCCGTCGCCGCCCGCGCCCCCCGCCGCCGCGGCCACCGCC
GTCGGGCCGCCACTCTGCCGCTTGGCCTTCGAGGACGAGAGCCCGCCGGCGCCCGCGCGG
TGGCCGCGCTCGGACCCCGAGAGCCAACCCCTGCTGGGGCCAGGCGCGGGCGGCGCGGGG
GGCACGGGGGGCGCAGGCGGAGGAGCCCCGGCCGCTCCGCCCCCGTGCTGCGCCGCGCCG
CCCCCGTGCCCTTACCTCGATCTCGAGCCGTCGCCGTCGGACTCGGAGGACTCGGAGAGC
CTGGGCGGCGCGTCGCTGGGCGGCCTGGATCCCTGGTGGTTCGCCGACTTCCCTTACCCG
TATGCCGAGCGCCTCGGGCCGCCGCCCGGCCGCTACTGGTCGGTCGACAAGCTCGGGGGC
TGGCGCGCCGGGAGCTGGGACTACCTGCCCCCGCGCAGCGGTCCGGCCGCCTGGCACTGT
CGGCACTGCGCCAGCCTGGAGCTGCTGCCGCCGCCGCGCCATCTCAGCTGCTCGCACGAT
GGCCTGGACGGCGGCTGGTGGGCGCCACCGCCTCCACCCTGGGCCGCCGGGCCCCTGCCC
CGACGCCGGGCCCGCTGCGGGTGCCCGCGGTCGCACCCGCACCGCCCGCGGGCCTCGCAC
CGCACGCCCGCCGCTGCCGCGCCCCACCACCACAGGCACCGGCGCGCCGCTGGGGGCTGG
GACCTCCCGCCGCCCGCGCCCACCTCGCGCTCGCTCGAGGACCTCAGCTCGTGCCCTCGC
GCCGCCCCTGCGCGCAGGCTTACCGGGCCCTCCCGCCACGCTCGCAGGTGTCCGCACGCC
GCGCACTGGGGGCCGCCGCTGCCCACAGCTTCCCACCGGAGACACCGGGGCGGGGACCTG
GGCACCCGCAGGGGCTCGGCGCACTTCTCTAGCCTCGAGTCCGAGGTATGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GRIN2D Link Image
Target 2 GenAtlas ID GRIN2D Link Image
Target 2 HGNC ID HGNC:4588 Link Image
Target 2 Chromosome Location 19
Target 2 Locus 19q13.1-qter
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Hess SD, Daggett LP, Deal C, Lu CC, Johnson EC, Velicelebi G: Functional characterization of human N-methyl-D-aspartate subtype 1A/2D receptors. J Neurochem. 1998 Mar;70(3):1269-79. [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 464
Target 3 Name Glutamate [NMDA] receptor subunit epsilon-2
Target 3 Synonyms
  1. Glutamate receptor subunit epsilon-2 precursor
  2. N-methyl D- aspartate receptor subtype 2B
  3. N-methyl-D-aspartate receptor subunit 3
  4. NMDAR2B
  5. NR2B
  6. NR3
  7. hNR3
Target 3 Gene Name GRIN2B
Target 3 Protein Sequence >Glutamate [NMDA] receptor subunit epsilon 2 precursor 
MKPRAECCSPKFWLVLAVLAVSGSRARSQKSPPSIGIAVILVGTSDEVAIKDAHEKDDFH
HLSVVPRVELVAMNETDPKSIITRICDLMSDRKIQGVVFADDTDQEAIAQILDFISAQTL
TPILGIHGGSSMIMADKDESSMFFQFGPSIEQQASVMLNIMEEYDWYIFSIVTTYFPGYQ
DFVNKIRSTIENSFVGWELEEVLLLDMSLDDGDSKIQNQLKKLQSPIILLYCTKEEATYI
FEVANSVGLTGYGYTWIVPSLVAGDTDTVPAEFPTGLISVSYDEWDYGLPARVRDGIAII
TTAASDMLSEHSFIPEPKSSCYNTHEKRIYQSNMLNRYLINVTFEGRNLSFSEDGYQMHP
KLVIILLNKERKWERVGKWKDKSLQMKYYVWPRMCPETEEQEDDHLSIVTLEEAPFVIVE
SVDPLSGTCMRNTVPCQKRIVTENKTDEEPGYIKKCCKGFCIDILKKISKSVKFTYDLYL
VTNGKHGKKINGTWNGMIGEVVMKRAYMAVGSLTINEERSEVVDFSVPFIETGISVMVSR
SNGTVSPSAFLEPFSADVWVMMFVMLLIVSAVAVFVFEYFSPVGYNRCLADGREPGGPSF
TIGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEYV
DQVSGLSDKKFQRPNDFSPPFRFGTVPNGSTERNIRNNYAEMHAYMGKFNQRGVDDALLS
LKTGKLDAFIYDAAVLNYMAGRDEGCKLVTIGSGKVFASTGYGIAIQKDSGWKRQVDLAI
LQLFGDGEMEELEALWLTGICHNEKNEVMSSQLDIDNMAGVFYMLGAAMALSLITFICEH
LFYWQFRHCFMGVCSGKPGMVFSISRGIYSCIHGVAIEERQSVMNSPTATMNNTHSNILR
LLRTAKNMANLSGVNGSPQSALDFIRRESSVYDISEHRRSFTHSDCKSYNNPPCEENLFS
DYISEVERTFGNLQLKDSNVYQDHYHHHHRPHSIGSASSIDGLYDCDNPPFTTQSRSISK
KPLDIGLPSSKHSQLSDLYGKFSFKSDRYSGHDDLIRSDVSDISTHTVTYGNIEGNAAKR
RKQQYKDSLKKRPASAKSRREFDEIELAYRRRPPRSPDHKRYFRDKEGLRDFYLDQFRTK
ENSPHWEHVDLTDIYKERSDDFKRDSVSGGGPCTNRSHIKHGTGDKHGVVSGVPAPWEKN
LTNVEWEDRSGGNFCRSCPSKLHNYSTTVTGQNSGRQACIRCEACKKAGNLYDISEDNSL
QELDQPAAPVAVTSNASTTKYPQSPTNSKAQKKNRNKLRRQHSYDTFVDLQKEEAALAPR
SVSLKDKGRFMDGSPYAHMFEMSAGESTFANNKSSVPTAGHHHHNNPGGGYMLSKSLYPD
RVTQNPFIPTFGDDQCLLHGSKSYFFRQPTVAGASKARPDFRALVTNKPVVSALHGAVPA
RFQKDICIGNQSNPCVPNNKNPRAFNGSSNGHVYEKLSSIESDV
Target 3 Number of Residues 1508
Target 3 Molecular Weight 166369
Target 3 Theoretical pI 6.92
Target 3 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 3 General Function Involved in ionotropic glutamate receptor activity
Target 3 Specific Function NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • 1-26
Target 3 Transmembrane Regions
  • 558-578
  • 635-655
  • 818-838
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 1899202 Link Image
Target 3 UniProtKB/Swiss-Prot ID Q13224 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name NMDE2_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >4455 bp 
ATGAAGCCCAGAGCGGAGTGCTGTTCTCCCAAGTTCTGGTTGGTGTTGGCCGTCCTGGCC
GTGTCAGGCAGCAGAGCTCGTTCTCAGAAGAGCCCCCCCAGCATTGGCATTGCTGTCATC
CTCGTGGGCACTTCCGACGAGGTGGCCATCAAGGATGCCCACGAGAAAGATGATTTCCAC
CATCTCTCCGTGGTACCCCGGGTGGAACTGGTAGCCATGAATGAGACCGACCCAAAGAGC
ATCATCACCCGCATCTGTGATCTCATGTCTGACCGGAAGATCCAGGGGGTGGTGTTTGCT
GATGACACAGACCAGGAAGCCATCGCCCAGATCCTCGATTTCATTTCAGCACAGACTCTC
ACCCCGATCCTGGGCATCCACGGGGGCTCCTCTATGATAATGGCAGATAAGGATGAATCC
TCCATGTTCTTCCAGTTTGGCCCATCAATTGAACAGCAAGCTTCCGTAATGCTCAACATC
ATGGAAGAATATGACTGGTACATCTTTTCTATCGTCACCACCTATTTCCCTGGCTACCAG
GACTTTGTAAACAAGATCCGCAGCACCATTGAGAATAGCTTTGTGGGCTGGGAGCTAGAG
GAGGTCCTCCTACTGGACATGTCCCTGGACGATGGAGATTCTAAGATCCAGAATCAGCTC
AAGAAACTTCAAAGCCCCATCATTCTTCTTTACTGTACCAAGGAAGAAGCCACCTACATC
TTTGAAGTGGCCAACTCAGTAGGGCTGACTGGCTATGGCTACACGTGGATCGTGCCCAGT
CTGGTGGCAGGGGATACAGACACAGTGCCTGCGGAGTTCCCCACTGGGCTCATCTCTGTA
TCATATGATGAATGGGACTATGGCCTCCCCGCCAGAGTGAGAGATGGAATTGCCATAATC
ACCACTGCTGCTTCTGACATGCTGTCTGAGCACAGCTTCATCCCTGAGCCCAAAAGCAGT
TGTTACAACACCCACGAGAAGAGAATCTACCAGTCCAATATGCTAAATAGGTATCTGATC
AATGTCACTTTTGAGGGGAGGAATTTGTCCTTCAGTGAAGATGGCTACCAGATGCACCCG
AAACTGGTGATAATTCTTCTGAACAAGGAGAGGAAGTGGGAAAGGGTGGGGAAGTGGAAA
GACAAGTCCCTGCAGATGAAGTACTATGTGTGGCCCCGAATGTGTCCAGAGACTGAAGAG
CAGGAGGATGACCATCTGAGCATTGTGACCCTGGAGGAGGCACCATTTGTCATTGTGGAA
AGTGTGGACCCTCTGAGTGGAACCTGCATGAGGAACACAGTCCCCTGCCAAAAACGCATA
GTCACTGAGAATAAAACAGACGAGGAGCCGGGTTACATCAAAAAATGCTGCAAGGGGTTC
TGTATTGACATCCTTAAGAAAATTTCTAAATCTGTGAAGTTCACCTATGACCTTTACCTG
GTTACCAATGGCAAGCATGGGAAGAAAATCAATGGAACCTGGAATGGTATGATTGGAGAG
GTGGTCATGAAGAGGGCCTACATGGCAGTGGGCTCACTCACCATCAATGAGGAACGATCG
GAGGTGGTCGACTTCTCTGTGCCCTTCATAGAGACAGGCATCAGTGTCATGGTGTCACGC
AGCAATGGGACTGTCTCACCTTCTGCCTTCTTAGAGCCATTCAGCGCTGACGTATGGGTG
ATGATGTTTGTGATGCTGCTCATCGTCTCAGCCGTGGCTGTCTTTGTCTTTGAGTACTTC
AGCCCTGTGGGTTATAACAGGTGCCTCGCTGATGGCAGAGAGCCTGGTGGACCCTCTTTC
ACCATCGGCAAAGCTATTTGGTTGCTCTGGGGTCTGGTGTTTAACAACTCCGTACCTGTG
CAGAACCCAAAGGGGACCACCTCCAAGATCATGGTGTCAGTGTGGGCCTTCTTTGCTGTC
ATCTTCCTGGCCAGCTACACTGCCAACTTAGCTGCCTTCATGATCCAAGAGGAATATGTG
GACCAGGTTTCTGGCCTGAGCGACAAAAAGTTCCAGAGACCTAATGACTTCTCACCCCCT
TTCCGCTTTGGGACCGTGCCCAACGGCAGCACAGAGAGAAATATTCGCAATAACTATGCA
GAAATGCATGCCTACATGGGAAAGTTCAACCAGAGGGGTGTAGATGATGCATTGCTCTCC
CTGAAAACAGGGAAACTGGATGCCTTCATCTATGATGCAGCAGTGCTGAACTATATGGCA
GGCAGAGATGAAGGCTGCAAGCTGGTGACCATTGGCAGTGGGAAGGTCTTTGCTTCCACT
GGCTATGGCATTGCCATCCAAAAAGATTCTGGGTGGAAGCGCCAGGTGGACCTTGCTATC
CTGCAGCTCTTTGGAGATGGGGAGATGGAAGAACTGGAAGCTCTCTGGCTCACTGGCATT
TGTCACAATGAGAAGAATGAGGTCATGAGCAGCCAGCTGGACATTGACAACATGGCAGGG
GTCTTCTACATGTTGGGGGCGGCCATGGCTCTCAGCCTCATCACCTTCATCTGCGAACAC
CTTTTCTATTGGCAGTTCCGACATTGCTTTATGGGTGTCTGTTCTGGCAAGCCTGGCATG
GTCTTCTCCATCAGCAGAGGTATCTACAGCTGCATCCATGGGGTGGCGATCGAGGAGCGC
CAGTCTGTAATGAACTCCCCCACCGCAACCATGAACAACACACACTCCAACATCCTGCGC
CTGCTGCGCACGGCCAAGAACATGGCTAACCTGTCTGGTGTGAATGGCTCACCGCAGAGC
GCCCTGGACTTCATCCGACGGGAGTCATCCGTCTATGACATCTCAGAGCACCGCCGCAGC
TTCACGCATTCTGACTGCAAATCCTACAACAACCCGCCCTGTGAGGAGAACCTCTTCAGT
GACTACATCAGTGAGGTAGAGAGAACGTTCGGGAACCTGCAGCTGAAGGACAGCAACGTG
TACCAAGATCACTACCACCATCACCACCGGCCCCATAGTATTGGCAGTGCCAGCTCCATC
GATGGGCTCTACGACTGTGACAACCCACCCTTCACCACCCAGTCCAGGTCCATCAGCAAG
AAGCCCCTGGACATCGGCCTCCCCTCCTCCAAGCACAGCCAGCTCAGTGACCTGTACGGC
AAATTCTCCTTCAAGAGCGACCGCTACAGTGGCCACGACGACTTGATCCGCTCCGATGTC
TCTGACATCTCAACCCACACCGTCACCTATGGGAACATCGAGGGCAATGCCGCCAAGAGG
CGTAAGCAGCAATATAAGGACAGCCTGAAGAAGCGGCCTGCCTCGGCCAAGTCCCGCAGG
GAGTTTGACGAGATCGAGCTGGCCTACCGTCGCCGACCGCCCCGCTCCCCTGACCACAAG
CGCTACTTCAGGGACAAGGAAGGGCTACGGGACTTCTACCTGGACCAGTTCCGAACAAAG
GAGAACTCACCCCACTGGGAGCACGTAGACCTGACCGACATCTACAAGGAGCGGAGTGAT
GACTTTAAGCGCGACTCCATCAGCGGAGGAGGGCCCTGTACCAACAGGTCTCACATCAAG
CACGGGACGGGCGACAAACACGGCGTGGTCAGCGGGGTACCTGCACCTTGGGAGAAGAAC
CTGACCAACGTGGAGTGGGAGGACCGGTCCGGGGGCAACTTCTGCCGCAGCTGTCCCTCC
AAGCTGCACAACTACTCCACGACGGTGACGGGTCAGAACTCGGGCAGGCAGGCGTGCATC
CGGTGTGAGGCTTGCAAGAAAGCAGGCAACCTGTATGACATCAGTGAGGACAACTCCCTG
CAGGAACTGGACCAGCCGGCTGCCCCAGTGGCGGTGACGTCAAACGCCTCCACCACTAAG
TACCCTCAGAGCCCGACTAATTCCAAGGCCCAGAAGAAGAACCGGAACAAACTGCGCCGG
CAGCACTCCTACGACACCTTCGTGGACCTGCAGAAGGAAGAAGCCGCCCTGGCCCCGCGC
AGCGTAAGCCTGAAAGACAAGGGCCGATTCATGGATGGGAGCCCCTACGCCCACATGTTT
GAGATGTCAGCTGGCGAGAGCACCTTTGCCAACAACAAGTCCTCAGTGCCCACTGCCGGA
CATCACCACCACAACAACCCCGGCGGCGGGTACATGCTCAGCAAGTCGCTCTACCCTGAC
CGGGTCACGCAAAACCCTTTCATCCCCACTTTTGGGGACGACCAGTGCTTGCTCCATGGC
AGCAAATCCTACTTCTTCAGGCAGCCCACGGTGGCGGGGGCGTCGAAAGCCAGGCCGGAC
TTCCGGGCCCTTGTCACCAACAAGCCGGTGGTCTCGGCCCTTCATGGGGCCGTGCCAGCC
CGTTTCCAGAAGGACATCTGTATAGGGAACCAGTCCAACCCCTGTGTGCCTAACAACAAA
AACCCCAGGGCTTTCAATGGCTCCAGCAATGGGCATGTTTATGAGAAACTTTCTAGTATT
GAGTCTGATGTCTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID GRIN2B Link Image
Target 3 GenAtlas ID GRIN2B Link Image
Target 3 HGNC ID HGNC:4586 Link Image
Target 3 Chromosome Location 12
Target 3 Locus 12p12
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Mandich P, Schito AM, Bellone E, Antonacci R, Finelli P, Rocchi M, Ajmar F: Mapping of the human NMDAR2B receptor subunit gene (GRIN2B) to chromosome 12p12. Genomics. 1994 Jul 1;22(1):216-8. [PubMed Link Image]
  2. Adams SL, Foldes RL, Kamboj RK: Human N-methyl-D-aspartate receptor modulatory subunit hNR3: cloning and sequencing of the cDNA and primary structure of the protein. Biochim Biophys Acta. 1995 Jan 2;1260(1):105-8. [PubMed Link Image]
  3. Hess SD, Daggett LP, Crona J, Deal C, Lu CC, Urrutia A, Chavez-Noriega L, Ellis SB, Johnson EC, Velicelebi G: Cloning and functional characterization of human heteromeric N-methyl-D-aspartate receptors. J Pharmacol Exp Ther. 1996 Aug;278(2):808-16. [PubMed Link Image]
  4. Schito AM, Pizzuti A, Di Maria E, Schenone A, Ratti A, Defferrari R, Bellone E, Mancardi GL, Ajmar F, Mandich P: mRNA distribution in adult human brain of GRIN2B, a N-methyl-D-aspartate (NMDA) receptor subunit. Neurosci Lett. 1997 Dec 12;239(1):49-53. [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 465
Target 4 Name Calmodulin
Target 4 Synonyms
  1. CaM
Target 4 Gene Name CALM1
Target 4 Protein Sequence >Calmodulin 
ADQLTEEQIAEFKEAFSLFDKDGDGTITTKELGTVMRSLGQNPTEAELQDMINEVDADGN
GTIDFPEFLTMMARKMKDTDSEEEIREAFRVFDKDGNGYISAAELRHVMTNLGEKLTDEE
VDEMIREADIDGDGQVNYEEFVQMMTAK
Target 4 Number of Residues 150
Target 4 Molecular Weight 16707
Target 4 Theoretical pI 3.84
Target 4 GO Classification
Function
binding
ion binding
cation binding
calcium ion binding
Process
Not Available
Component
Not Available
Target 4 General Function Involved in calcium ion binding
Target 4 Specific Function Calmodulin mediates the control of a large number of enzymes and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • None
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 179888 Link Image
Target 4 UniProtKB/Swiss-Prot ID P62158 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name CALM_HUMAN Link Image
Target 4 PDB ID 1IQ5 Link Image
Target 4 PDB File Show
Target 4 3D Structure
Target 4 Cellular Location Not Available
Target 4 Gene Sequence >450 bp 
ATGGCTGACCAGCTGACTGAGGAGCAGATTGCAGAGTTCAAGGAGGCCTTCTCCCTCTTT
GACAAGGATGGAGATGGCACTATCACCACCAAGGAGTTGGGGACAGTGATGAGATCCCTG
GGACAGAACCCCACTGAAGCAGAGCTGCAGGATATGATCAATGAGGTGGATGCAGATGGG
AACGGGACCATTGACTTCCCGGAGTTCCTGACCATGATGGCCAGAAAGATGAAGGACACA
GACAGTGAGGAGGAGATCCGAGAGGCGTTCCGTGTCTTTGACAAGGATGGGAATGGCTAC
ATCAGCGCCGCAGAGCTGCGTCACGTAATGACGAACCTGGGGGAGAAGCTGACCGATGAG
GAGGTGGATGAGATGATCAGGGAGGCTGACATCGATGGAGATGGCCAGGTCAATTATGAA
GAGTTTGTACAGATGATGACTGCAAAGTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID CALM1 Link Image
Target 4 GenAtlas ID CALM1 Link Image
Target 4 HGNC ID HGNC:1442 Link Image
Target 4 Chromosome Location 14
Target 4 Locus 14q24-q31
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Drum CL, Yan SZ, Bard J, Shen YQ, Lu D, Soelaiman S, Grabarek Z, Bohm A, Tang WJ: Structural basis for the activation of anthrax adenylyl cyclase exotoxin by calmodulin. Nature. 2002 Jan 24;415(6870):396-402. [PubMed Link Image]
  2. Heilig R, Eckenberg R, Petit JL, Fonknechten N, Da Silva C, Cattolico L, Levy M, Barbe V, de Berardinis V, Ureta-Vidal A, Pelletier E, Vico V, Anthouard V, Rowen L, Madan A, Qin S, Sun H, Du H, Pepin K, Artiguenave F, Robert C, Cruaud C, Bruls T, Jaillon O, Friedlander L, Samson G, Brottier P, Cure S, Segurens B, Aniere F, Samain S, Crespeau H, Abbasi N, Aiach N, Boscus D, Dickhoff R, Dors M, Dubois I, Friedman C, Gouyvenoux M, James R, Madan A, Mairey-Estrada B, Mangenot S, Martins N, Menard M, Oztas S, Ratcliffe A, Shaffer T, Trask B, Vacherie B, Bellemere C, Belser C, Besnard-Gonnet M, Bartol-Mavel D, Boutard M, Briez-Silla S, Combette S, Dufosse-Laurent V, Ferron C, Lechaplais C, Louesse C, Muselet D, Magdelenat G, Pateau E, Petit E, Sirvain-Trukniewicz P, Trybou A, Vega-Czarny N, Bataille E, Bluet E, Bordelais I, Dubois M, Dumont C, Guerin T, Haffray S, Hammadi R, Muanga J, Pellouin V, Robert D, Wunderle E, Gauguet G, Roy A, Sainte-Marthe L, Verdier J, Verdier-Discala C, Hillier L, Fulton L, McPherson J, Matsuda F, Wilson R, Scarpelli C, Gyapay G, Wincker P, Saurin W, Quetier F, Waterston R, Hood L, Weissenbach J: The DNA sequence and analysis of human chromosome 14. Nature. 2003 Feb 6;421(6923):601-7. Epub 2003 Jan 1. [PubMed Link Image]
  3. Koller M, Schnyder B, Strehler EE: Structural organization of the human CaMIII calmodulin gene. Biochim Biophys Acta. 1990 Oct 23;1087(2):180-9. [PubMed Link Image]
  4. SenGupta B, Friedberg F, Detera-Wadleigh SD: Molecular analysis of human and rat calmodulin complementary DNA clones. Evidence for additional active genes in these species. J Biol Chem. 1987 Dec 5;262(34):16663-70. [PubMed Link Image]
  5. Fischer R, Koller M, Flura M, Mathews S, Strehler-Page MA, Krebs J, Penniston JT, Carafoli E, Strehler EE: Multiple divergent mRNAs code for a single human calmodulin. J Biol Chem. 1988 Nov 15;263(32):17055-62. [PubMed Link Image]
  6. Wawrzynczak EJ, Perham RN: Isolation and nucleotide sequence of a cDNA encoding human calmodulin. Biochem Int. 1984 Aug;9(2):177-85. [PubMed Link Image]
  7. Sasagawa T, Ericsson LH, Walsh KA, Schreiber WE, Fischer EH, Titani K: Complete amino acid sequence of human brain calmodulin. Biochemistry. 1982 May 11;21(10):2565-9. [PubMed Link Image]
  8. Rhyner JA, Ottiger M, Wicki R, Greenwood TM, Strehler EE: Structure of the human CALM1 calmodulin gene and identification of two CALM1-related pseudogenes CALM1P1 and CALM1P2. Eur J Biochem. 1994 Oct 1;225(1):71-82. [PubMed Link Image]
  9. Toutenhoofd SL, Foletti D, Wicki R, Rhyner JA, Garcia F, Tolon R, Strehler EE: Characterization of the human CALM2 calmodulin gene and comparison of the transcriptional activity of CALM1, CALM2 and CALM3. Cell Calcium. 1998 May;23(5):323-38. [PubMed Link Image]
Target 4 Drug References
  1. Daly JW, Harper J: Loperamide: novel effects on capacitative calcium influx. Cell Mol Life Sci. 2000 Jan 20;57(1):149-57. [PubMed Link Image]
  2. Suzuki T, Sakai H, Ikari A, Takeguchi N: Inhibition of thromboxane A(2)-induced Cl(-) secretion by antidiarrhea drug loperamide in isolated rat colon. J Pharmacol Exp Ther. 2000 Oct;295(1):233-8. [PubMed Link Image]
  3. Mellstrand T: Loperamide--an opiate receptor agonist with gastrointestinal motility effects. Scand J Gastroenterol Suppl. 1987;130:65-6. [PubMed Link Image]
  4. Stoll R, Ruppin H, Domschke W: Calmodulin-mediated effects of loperamide on chloride transport by brush border membrane vesicles from human ileum. Gastroenterology. 1988 Jul;95(1):69-76. [PubMed Link Image]
  5. Diener M, Knobloch SF, Rummel W: Action of loperamide on neuronally mediated and Ca2+- or cAMP-mediated secretion in rat colon. Eur J Pharmacol. 1988 Aug 2;152(3):217-25. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 467
Target 5 Name Delta-type opioid receptor
Target 5 Synonyms
  1. DOR-1
Target 5 Gene Name OPRD1
Target 5 Protein Sequence >Delta-type opioid receptor 
MEPAPSAGAELQPPLFANASDAYPSAFPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC
TPSDGPGGGAAA
Target 5 Number of Residues 378
Target 5 Molecular Weight 40413
Target 5 Theoretical pI 9.17
Target 5 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
peptide receptor activity, G-protein coupled
opioid receptor activity
delta-opioid 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 Involved in delta-opioid receptor activity
Target 5 Specific Function Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • 46-75
  • 85-102
  • 125-144
  • 175-190
  • 216-238
  • 262-284
  • 294-310
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 27545517 Link Image
Target 5 UniProtKB/Swiss-Prot ID P41143 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name OPRD_HUMAN Link Image
Target 5 PDB ID Not Available
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >1119 bp 
ATGGAACCGGCCCCCTCCGCCGGCGCCGAGCTGCAGCCCCCGCTCTTCGCCAACGCCTCG
GACGCCTACCCTAGCGCCTTCCCCAGCGCTGGCGCCAATGCGTCGGGGCCGCCAGGCGCG
CGGAGCGCCTCGTCCCTCGCCCTGGCAATCGCCATCACCGCGCTCTACTCGGCCGTGTGC
GCCGTGGGGCTGCTGGGCAACGTGCTTGTCATGTTCGGCATCGTCCGGTACACTAAGATG
AAGACGGCCACCAACATCTACATCTTCAACCTGGCCTTAGCCGATGCGCTGGCCACCAGC
ACGCTGCCTTTCCAGAGTGCCAAGTACCTGATGGAGACGTGGCCCTTCGGCGAGCTGCTC
TGCAAGGCTGTGCTCTCCATCGACTACTACAATATGTTCACCAGCATCTTCACGCTCACC
ATGATGAGTGTTGACCGCTACATCGCTGTCTGCCACCCTGTCAAGGCCCTGGACTTCCGC
ACGCCTGCCAAGGCCAAGCTGATCAACATCTGTATCTGGGTCCTGGCCTCAGGCGTTGGC
GTGCCCATCATGGTCATGGCTGTGACCCGTCCCCGGGACGGGGCAGTGGTGTGCATGCTC
CAGTTCCCCAGCCCCAGCTGGTACTGGGACACGGTGACCAAGATCTGCGTGTTCCTCTTC
GCCTTCGTGGTGCCCATCCTCATCATCACCGTGTGCTATGGCCTCATGCTGCTGCGCCTG
CGCAGTGTGCGCCTGCTGTCGGGCTCCAAGGAGAAGGACCGCAGCCTGCGGCGCATCACG
CGCATGGTGCTGGTGGTTGTGGGCGCCTTCGTGGTGTGTTGGGCGCCCATCCACATCTTC
GTCATCGTCTGGACGCTGGTGGACATCGACCGGCGCGACCCGCTGGTGGTGGCTGCGCTG
CACCTGTGCATCGCGCTGGGCTACGCCAATAGCAGCCTCAACCCCGTGCTCTACGCTTTC
CTCGACGAGAACTTCAAGCGCTGCTTCCGCCAGCTCTGCCGCAAGCCCTGCGGCCGCCCA
GACCCCAGCAGCTTCAGCCGCGCCCGCGAAGCCACGGCCCGCGAGCGTGTCACCGCCTGC
ACCCCGTCCGATGGTCCCGGCGGTGGCGCTGCCGCCTGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID OPRD1 Link Image
Target 5 GenAtlas ID OPRD1 Link Image
Target 5 HGNC ID HGNC:8153 Link Image
Target 5 Chromosome Location 1
Target 5 Locus 1p36.1-p34.3
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Gelernter J, Kranzler HR: Variant detection at the delta opioid receptor (OPRD1) locus and population genetics of a novel variant affecting protein sequence. Hum Genet. 2000 Jul;107(1):86-8. [PubMed Link Image]
  2. Simonin F, Befort K, Gaveriaux-Ruff C, Matthes H, Nappey V, Lannes B, Micheletti G, Kieffer B: The human delta-opioid receptor: genomic organization, cDNA cloning, functional expression, and distribution in human brain. Mol Pharmacol. 1994 Dec;46(6):1015-21. [PubMed Link Image]
  3. Knapp RJ, Malatynska E, Fang L, Li X, Babin E, Nguyen M, Santoro G, Varga EV, Hruby VJ, Roeske WR, et al.: Identification of a human delta opioid receptor: cloning and expression. Life Sci. 1994;54(25):PL463-9. [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]
Drug Target 6 [top]
Target 6 ID 505
Target 6 Name Glutamate [NMDA] receptor subunit epsilon-3
Target 6 Synonyms
  1. Glutamate receptor subunit epsilon-3 precursor
  2. N-methyl D- aspartate receptor subtype 2C
  3. NMDAR2C
  4. NR2C
Target 6 Gene Name GRIN2C
Target 6 Protein Sequence >Glutamate [NMDA] receptor subunit epsilon 3 precursor 
MGGALGPALLLTSLFGAWAGLGPGQGEQGMTVAVVFSSSGPPQAQFRARLTPQSFLDLPL
EIQPLTVGVNTTNPSSLLTQICGLLGAAHVHGIVFEDNVDTEAVAQILDFISSQTHVPIL
SISGGSAVVLTPKEPGSAFLQLGVSLEQQLQVLFKVLEEYDWSAFAVITSLHPGHALFLE
GVRAVADASHVSWRLLDVVTLELGPGGPRARTQRLLRQLDAPVFVAYCSREEAEVLFAEA
AQAGLVGPGHVWLVPNLALGSTDAPPATFPVGLISVVTESWRLSLRQKVRDGVAILALGA
HSYWRQHGTLPAPAGDCRVHPGPVSPAREAFYRHLLNVTWEGRDFSFSPGGYLVQPTMVV
IALNRHRLWEMVGRWEHGVLYMKYPVWPRYSASLQPVVDSRHLTVATLEERPFVIVESPD
PGTGGCVPNTVPCRRQSNHTFSSGDVAPYTKLCCKGFCIDILKKLARVVKFSYDLYLVTN
GKHGKRVRGVWNGMIGEVYYKRADMAIGSLTINEERSEIVDFSVPFVETGISVMVARSNG
TVSPSAFLEPYSPAVWVMMFVMCLTVVAITVFMFEYFSPVSYNQNLTRGKKSGGPAFTIG
KSVWLLWALVFNNSVPIENPRGTTSKIMVLVWAFFAVIFLASYTANLAAFMIQEQYIDTV
SGLSDKKFQRPQDQYPPFRFGTVPNGSTERNIRSNYRDMHTHMVKFNQRSVEDALTSLKM
GKLDAFIYDAAVLNYMAGKDEGCKLVTIGSGKVFATTGYGIAMQKDSHWKRAIDLALLQF
LGDGETQKLETVWLSGICQNEKNEVMSSKLDIDNMAGVFYMLLVAMGLALLVFAWEHLVY
WKLRHSVPNSSQLDFLLAFSRGIYSCFSGVQSLASPPRQASPDLTASSAQASVLKMLQAA
RDMVTTAGVSSSLDRATRTIENWGGGRRAPPPSPCPTPRSGPSPCLPTPDPPPEPSPTGW
GPPDGGRAALVRRAPQPPGRPPTPGPPLSDVSRVSRRPAWEARWPVRTGHCGRHLSASER
PLSPARCHYSSFPRADRSGRPFLPLFPELEDLPLLGKEQLARREALLHAAWARGSRPRHA
SLPSSVAEAFARPSSLPAGCTGPACARPDGHSACRRLAQAQSMCLPIYREACQEGEQAGA
PAWQHRQHVCLHAHAHLPFCWGAVCPHLPPCASHGSWLSGAWGPLGHRGRTLGLGTGYRD
SGGLDEISRVARGTQGFPGPCTWRRISSLESEV
Target 6 Number of Residues 1253
Target 6 Molecular Weight 134241
Target 6 Theoretical pI 8.61
Target 6 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 6 General Function Involved in ionotropic glutamate receptor activity
Target 6 Specific Function NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • 1-19
Target 6 Transmembrane Regions
  • 554-574
  • 597-617
  • 627-647
  • 815-835
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 1196449 Link Image
Target 6 UniProtKB/Swiss-Prot ID Q14957 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name NMDE3_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >3702 bp 
ATGGGTGGGGCCCTGGGGCCGGCCCTGTTGCTCACCTCGCTCTTCGGTGCCTGGGCAGGG
CTGGGTCCGGGGCAGGGCGAGCAGGGCATGACGGTGGCCGTGGTGTTTAGCAGCTCAGGG
CCGCCCCAGGCCCAGTTCCGTGCCCGCCTCACCCCCCAGAGCTTCCTGGACCTACCCCTG
GAGATCCAGCCGCTCACAGTTGGGGTCAACACCACCAACCCCAGCAGCCTCCTCACCCAG
ATCTGCGGCCTCCTGGGTGCTGCCCACGTCCACGGCATTGTCTTTGAGGACAACGTGGAC
ACCGAGGCGGTGGCCCAGATCCTTGACTTCATCTCCTCCCAGACCCATGTGCCCATCCTC
AGCATCAGCGGAGGCTCTGCTGTGGTCCTCACCCCCAAGGAGCCGGGCTCCGCCTTCCTG
CAGCTGGGCGTGTCCCTGGAGCAGCAGCTGCAGGTGCTGTTCAAGGTGCTGGAAGAGTAC
GACTGGAGCGCCTTCGCCGTCATCACCAGCCTGCACCCGGGCCACGCGCTCTTCCTGGAG
GGCGTGCGCGCCGTCGCCGACGCCAGCCACGTGAGTTGGCGGCTGCTGGACGTGGTCACG
CTGGAGCTGGGCCCGGGAGGGCCGCGCGCGCGCACGCAGCGCCTGCTGCGCCAGCTCGAC
GCGCCCGTGTTTGTGGCCTACTGCTCGCGCGAGGAGGCCGAGGTGCTCTTCGCCGAGGCG
GCGCAGGCCGGTCTGGTGGGGCCCGGCCACGTGTGGTTGGTGCCCAACCTGGCGCTGGGC
AGCACCGATGCGCCCCCCGCCACCTTCCCCGTGGGCCTCATCAGCGTCGTCACCGAGAGC
TGGCGCCTCAGCCTGCGCCAGAAGGTGCGCGACGGCGTGGCCATTCTGGCCCTGGGCGCC
CACAGCTACTGGCGCCAGCATGGAACCCTGCCAGCCCCGGCCGGGGACTGCCGTGTTCAC
CCTGGGCCCGTCAGCCCTGCCCGGGAGGCCTTCTACAGGCACCTACTGAATGTCACCTGG
GAGGGCCGAGACTTCTCCTTCAGCCCTGGTGGGTACCTGGTCCAGCCCACCATGGTGGTG
ATCGCCCTCAACCGGCACCGCCTCTGGGAGATGGTGGGGCGCTGGGAGCATGGCGTCCTA
TACATGAAGTACCCCGTGTGGCCTCGCTACAGTGCCTCTCTGCAGCCTGTGGTGGACAGT
CGGCACCTGACGGTGGCCACGCTGGAAGAGCGGCCCTTTGTCATCGTGGAGAGCCCTGAC
CCTGGCACAGGAGGCTGTGTCCCCAACACCGTGCCCTGCCGCAGGCAGAGCAACCACACC
TTCAGCAGCGGGGACGTGGCCCCCTACACCAAGCTCTGCTGTAAGGGATTCTGCATCGAC
ATCCTCAAGAAGCTGGCCAGAGTGGTCAAATTCTCCTACGACCTGTACCTGGTGACCAAC
GGCAAGCATGGCAAGCGGGTGCGCGGCGTATGGAACGGCATGATTGGGGAGGTGTACTAC
AAGCGGGCAGACATGGCCATCGGCTCCCTCACCATCAATGAGGAACGCTCCGAGATCGTA
GACTTCTCTGTACCCTTTGTGGAGACGGGCATCAGTGTGATGGTGGCTCGCAGCAATGGC
ACCGTCTCCCCCTCGGCCTTCTTGGAGCCATATAGCCCTGCAGTGTGGGTGATGATGTTT
GTCATGTGCCTCACTGTGGTGGCCATCACCGTCTTCATGTTCGAGTACTTCAGCCCTGTC
AGCTACAACCAGAACCTCACCAGAGGCAAGAAGTCCGGGGGCCCAGCTTTCACTATCGGC
AAGTCCGTGTGGCTGCTGTGGGCGCTGGTCTTCAACAACTCAGTGCCCATCGAGAACCCG
CGGGGCACCACCAGCAAGATCATGGTTCTGGTCTGGGCCTTCTTTGCTGTCATCTTCCTC
GCCAGCTACACGGCCAACCTGGCCGCCTTCATGATCCAAGAGCAATACATCGACACTGTG
TCGGGCCTCAGTGACAAGAAGTTTCAGCGGCCTCAAGATCAGTACCCACCTTTCCGCTTC
GGCACGGTGCCCAACGGCAGCACGGAGCGGAACATCCGCAGTAACTACCGTGACATGCAC
ACCCACATGGTCAAGTTCAACCAGCGCTCGGTGGAGGACGCGCTCACCAGCCTCAAGATG
GGGAAGCTGGATGCCTTCATCTATGATGCTGCTGTCCTCAACTACATGGCAGGCAAGGAC
GAGGGCTGCAAGCTGGTCACCATTGGGTCTGGCAAGGTCTTTGCTACCACTGGCTACGGC
ATCGCCATGCAGAAGGACTCCCACTGGAAGCGGGCCATAGACCTGGCGCTCTTGCAGTTC
CTGGGGGACGGAGAGACACAGAAACTGGAGACAGTGTGGCTCTCAGGGATCTGCCAGAAT
GAGAAGAACGAGGTGATGAGCAGCAAGCTGGACATCGACAACATGGCAGGCGTCTTCTAC
ATGCTGCTGGTGGCCATGGGGCTGGCCCTGCTGGTCTTCGCCTGGGAGCACCTGGTCTAC
TGGAAGCTGCGCCACTCGGTGCCCAACTCATCCCAGCTGGACTTCCTGCTGGCTTTCAGC
AGGGGCATCTACAGCTGCTTCAGCGGGGTGCAGAGCCTCGCCAGCCCACCGCGGCAGGCC
AGCCCGGACCTCACGGCCAGCTCGGCCCAGGCCAGCGTGCTCAAGATGCTGCAGGCAGCC
CGCGACATGGTGACCACGGCGGGCGTAAGCAGCTCCCTGGACCGCGCCACTCGCACCATC
GAGAATTGGGGTGGCGGCCGCCGTGCGCCCCCACCGTCCCCCTGCCCGACCCCGCGGTCT
GGCCCCAGCCCATGCCTGCCCACCCCCGACCCGCCCCCAGAGCCGAGCCCCACGGGCTGG
GGACCGCCAGACGGGGGTCGCGCGGCGCTTGTGCGCAGGGCTCCGCAGCCCCCGGGCCGC
CCCCCGACGCCGGGGCCGCCCCTGTCCGACGTCTCCCGAGTGTCGCGCCGCCCAGCCTGG
GAGGCGCGGTGGCCGGTGCGGACCGGGCACTGCGGGAGGCACCTCTCGGCCTCCGAGCGG
CCCCTGTCGCCCGCGCGCTGTCACTACAGCTCCTTTCCTCGAGCCGACCGATCCGGCCGC
CCCTTCCTCCCGCTCTTCCCGGAGCTGGAGGACCTGCCGCTGCTCGGTAAGGAGCAGCTG
GCCCGGCGGGAGGCCCTGCTGCACGCGGCCTGGGCCCGGGGCTCGCGCCCGCGTCACGCT
TCCCTGCCCAGCTCCGTGGCCGAGGCCTTCGCTCGGCCCAGCTCGCTGCCCGCTGGGTGC
ACCGGCCCCGCCTGCGCCCGCCCCGACGGCCACTCGGCCTGCAGGCGCTTGGCGCAGGCG
CAGTCGATGTGCTTGCCGATCTACCGGGAGGCCTGCCAGGAGGGCGAGCAGGCAGGGGCC
CCCGCCTGGCAGCACAGACAGCACGTCTGCCTGCACGCCCACGCCCACCTGCCATTTTGC
TGGGGGGCTGTCTGTCCTCACCTTCCACCCTGTGCCAGCCACGGCTCCTGGCTCTCCGGG
GCCTGGGGGCCTCTGGGGCACAGGGGCAGGACTCTGGGGCTGGGCACAGGCTACAGAGAC
AGTGGGGGACTGGACGAGATCAGCAGGGTAGCCCGTGGGACGCAAGGCTTCCCGGGACCC
TGCACCTGGAGACGGATCTCCAGTCTGGAGTCAGAAGTGTGA
Target 6 GenBank Gene ID
Target 6 GeneCard ID GRIN2C Link Image
Target 6 GenAtlas ID GRIN2C Link Image
Target 6 HGNC ID HGNC:4587 Link Image
Target 6 Chromosome Location 17
Target 6 Locus 17q25
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Lin YJ, Bovetto S, Carver JM, Giordano T: Cloning of the cDNA for the human NMDA receptor NR2C subunit and its expression in the central nervous system and periphery. Brain Res Mol Brain Res. 1996 Dec 31;43(1-2):57-64. [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 837
Target 7 Name Glutamate [NMDA] receptor subunit epsilon-1
Target 7 Synonyms
  1. Glutamate receptor subunit epsilon-1 precursor
  2. N-methyl D- aspartate receptor subtype 2A
  3. NMDAR2A
  4. NR2A
  5. hNR2A
Target 7 Gene Name GRIN2A
Target 7 Protein Sequence >Glutamate [NMDA] receptor subunit epsilon 1 precursor 
MGRVGYWTLLVLPALLVWRGPAPSAAAEKGPPALNIAVMLGHSHDVTERELRTLWGPEQA
AGLPLDVNVVALLMNRTDPKSLITHVCDLMSGARIHGLVFGDDTDQEAVAQMLDFISSHT
FVPILGIHGGASMIMADKDPTSTFFQFGASIQQQATVMLKIMQDYDWHVFSLVTTIFPGY
REFISFVKTTVDNSFVGWDMQNVITLDTSFEDAKTQVQLKKIHSSVILLYCSKDEAVLIL
SEARSLGLTGYDFFWIVPSLVSGNTELIPKEFPSGLISVSYDDWDYSLEARVRDGIGILT
TAASSMLEKFSYIPEAKASCYGQMERPEVPMHTLHPFMVNVTWDGKDLSFTEEGYQVHPR
LVVIVLNKDREWEKVGKWENHTLSLRHAVWPRYKSFSDCEPDDNHLSIVTLEEAPFVIVE
DIDPLTETCVRNTVPCRKFVKINNSTNEGMNVKKCCKGFCIDILKKLSRTVKFTYDLYLV
TNGKHGKKVNNVWNGMIGEVVYQRAVMAVGSLTINEERSEVVDFSVPFVETGISVMVSRS
NGTVSPSAFLEPFSASVWVMMFVMLLIVSAIAVFVFEYFSPVGYNRNLAKGKAPHGPSFT
IGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEFVD
QVTGLSDKKFQRPHDYSPPFRFGTVPNGSTERNIRNNYPYMHQYMTKFNQKGVEDALVSL
KTGKLDAFIYDAAVLNYKAGRDEGCKLVTIGSGYIFATTGYGIALQKGSPWKRQIDLALL
QFVGDGEMEELETLWLTGICHNEKNEVMSSQLDIDNMAGVFYMLAAAMALSLITFIWEHL
FYWKLRFCFTGVCSDRPGLLFSISRGIYSCIHGVHIEEKKKSPDFNLTGSQSNMLKLLRS
AKNISSMSNMNSSRMDSPKRAADFIQRGSLIMDMVSDKGNLMYSDNRSFQGKESIFGDNM
NELQTFVANRQKDNLNNYVFQGQHPLTLNESNPNTVEVAVSTESKANSRPRQLWKKSVDS
IRQDSLSQNPVSQRDEATAENRTHSLKSPRYLPEEMAHSDISETSNRATCHREPDNSKNH
KTKDNFKRSVASKYPKDCSEVERTYLKTKSSSPRDKIYTIDGEKEPGFHLDPPQFVENVT
LPENVDFPDPYQDPSENFRKGDSTLPMNRNPLHNEEGLSNNDQYKLYSKHFTLKDKGSPH
SETSERYRQNSTHCRSCLSNMPTYSGHFTMRSPFKCDACLRMGNLYDIDEDQMLQETGNP
ATGEQVYQQDWAQNNALQLQKNKLRISRQHSYDNIVDKPRELDLSRPSRSISLKDRERLL
EGNFYGSLFSVPSSKLSGKKSSLFPQGLEDSKRSKSLLPDHTSDNPFLHSHRDDQRLVIG
RCPSDPYKHSLPSQAVNDSYLRSSLRSTASYCSRDSRGHNDVYISEHVMPYAANKNNMYS
TPRVLNSCSNRRVYKKMPSIESDV
Target 7 Number of Residues 1488
Target 7 Molecular Weight 165284
Target 7 Theoretical pI 7.11
Target 7 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 7 General Function Involved in ionotropic glutamate receptor activity
Target 7 Specific Function NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • 1-22
Target 7 Transmembrane Regions
  • 556-576
  • 593-613
  • 634-654
  • 817-837
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 558749 Link Image
Target 7 UniProtKB/Swiss-Prot ID Q12879 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name NMDE1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 Gene Sequence >4395 bp 
ATGGGCAGAGTGGGCTATTGGACCCTGCTGGTGCTGCCGGCCCTTCTGGTCTGGCGCGGT
CCGGCGCCGAGCGCGGCGGCGGAGAAGGGTCCCCCCGCGCTAAATATTGCGGTGATGCTG
GGTCACAGCCACGACGTGACAGAGCGCGAACTTCGAACACTGTGGGGCCCCGAGCAGGCG
GCGGGGCTGCCCCTGGACGTGAACGTGGTAGCTCTGCTGATGAACCGCACCGACCCCAAG
AGCCTCATCACGCACGTGTGCGACCTCATGTCCGGGGCACGCATCCACGGCCTCGTGTTT
GGGGACGACACGGACCAGGAGGCCGTAGCCCAGATGCTGGATTTTATCTCCTCCCACACC
TTCGTCCCCATCTTGGGCATTCATGGGGGCGCATCTATGATCATGGCTGACAAGGATCCG
ACGTCTACCTTCTTCCAGTTTGGAGCGTCCATCCAGCAGCAAGCCACGGTCATGCTGAAG
ATCATGCAGGATTATGACTGGCATGTCTTCTCCCTGGTGACCACTATCTTCCCTGGCTAC
AGGGAATTCATCAGCTTCGTCAAGACCACAGTGGACAACAGCTTTGTGGGCTGGGACATG
CAGAATGTGATCACACTGGACACTTCCTTTGAGGATGCAAAGACACAAGTCCAGCTGAAG
AAGATCCACTCTTCTGTCATCTTGCTCTACTGTTCCAAAGACGAGGCTGTTCTCATTCTG
AGTGAGGCCCGCTCCCTTGGCCTCACCGGGTATGATTTCTTCTGGATTGTCCCCAGCTTG
GTCTCTGGGAACACGGAGCTCATCCCAAAAGAGTTTCCATCGGGACTCATTTCTGTCTCC
TACGATGACTGGGACTACAGCCTGGAGGCGAGAGTGAGGGACGGCATTGGCATCCTAACC
ACCGCTGCATCTTCTATGCTGGAGAAGTTCTCCTACATCCCCGAGGCCAAGGCCAGCTGC
TACGGGCAGATGGAGAGGCCAGAGGTCCCGATGCACACCTTGCACCCATTTATGGTCAAT
GTTACATGGGATGGCAAAGACTTATCCTTCACTGAGGAAGGCTACCAGGTGCACCCCAGG
CTGGTGGTGATTGTGCTGAACAAAGACCGGGAATGGGAAAAGGTGGGCAAGTGGGAGAAC
CATACGCTGAGCCTGAGGCACGCCGTGTGGCCCAGGTACAAGTCCTTCTCCGACTGTGAG
CCGGATGACAACCATCTCAGCATCGTCACCCTGGAGGAGGCCCCATTCGTCATCGTGGAA
GACATAGACCCCCTAACCGAGACGTGTGTGAGGAACACCGTGCCATGTCGGAAGTTCGTC
AAAATCAACAATTCAACCAATGAGGGGATGAATGTGAAGAAATGCTGCAAGGGGTTCTGC
ATTGATATTCTGAAGAAGCTTTCCAGAACTGTGAAGTTTACTTACGACCTCTATCTGGTG
ACCAATGGGAAGCATGGCAAGAAAGTTAACAATGTGTGGAATGGAATGATCGGTGAAGTG
GTCTATCAACGGGCAGTCATGGCAGTTGGCTCGCTCACCATCAATGAGGAACGTTCTGAA
GTGGTGGACTTCTCTGTGCCCTTTGTGGAAACGGGAATCAGTGTCATGGTTTCAAGAAGT
AATGGCACCGTCTCACCTTCTGCTTTTCTAGAACCATTCAGCGCCTCTGTCTGGGTGATG
ATGTTTGTGATGCTGCTCATTGTTTCTGCCATAGCTGTTTTTGTCTTTGAATACTTCAGC
CCTGTTGGATACAACAGAAACTTAGCCAAAGGGAAAGCACCCCATGGGCCTTCTTTTACA
ATTGGAAAAGCTATATGGCTTCTTTGGGGCCTGGTGTTCAATAACTCCGTGCCTGTCCAG
AATCCTAAAGGGACCACCAGCAAGATCATGGTATCTGTATGGGCCTTCTTCGCTGTCATA
TTCCTGGCTAGCTACACAGCCAATCTGGCTGCCTTCATGATCCAAGAGGAATTTGTGGAC
CAAGTGACCGGCCTCAGTGACAAAAAGTTTCAGAGACCTCATGACTATTCCCCACCTTTT
CGATTTGGGACAGTGCCTAATGGAAGCACGGAGAGAAACATTCGGAATAACTATCCCTAC
ATGCATCAGTACATGACCAAATTTAATCAGAAAGGAGTAGAGGACGCCTTGGTCAGCCTG
AAAACGGGGAAGCTGGACGCTTTCATCTACGATGCCGCAGTCTTGAATTACAAGGCTGGG
AGGGATGAAGGCTGCAAGCTGGTGACCATCGGGAGTGGGTACATCTTTGCCACCACCGGT
TATGGAATTGCCCTTCAGAAAGGCTCTCCTTGGAAGAGGCAGATCGACCTGGCCTTGCTT
CAGTTTGTGGGTGATGGTGAGATGGAGGAGCTGGAGACCCTGTGGCTCACTGGGATCTGC
CACAACGAGAAGAACGAGGTGATGAGCAGCCAGCTGGACATTGACAACATGGCGGGCGTA
TTCTACATGCTGGCTGCCGCCATGGCCCTTAGCCTCATCACCTTCATCTGGGAGCACCTC
TTCTACTGGAAGCTGCGCTTCTGTTTCACGGGCGTGTGCTCCGACCGGCCTGGGTTGCTC
TTCTCCATCAGCAGGGGCATCTACAGCTGCATTCATGGAGTGCACATTGAAGAAAAGAAG
AAGTCTCCAGACTTCAATCTGACGGGATCCCAGAGCAACATGTTAAAACTCCTCCGGTCA
GCCAAAAACATTTCCAGCATGTCCAACATGAACTCCTCAAGAATGGACTCACCCAAAAGA
GCTGCTGACTTCATCCAAAGAGGTTCCCTCATCATGGACATGGTTTCAGATAAGGGGAAT
TTGATGTACTCAGACAACAGGTCCTTTCAGGGGAAAGAGAGCATTTTTGGAGACAACATG
AACGAACTCCAAACATTTGTGGCCAACCGGCAGAAGGATAACCTCAATAACTATGTATTC
CAGGGACAACATCCTCTTACTCTCAATGAGTCCAACCCTAACACGGTGGAGGTGGCCGTG
AGCACAGAATCCAAAGCGAACTCTAGACCCCGGCAGCTGTGGAAGAAATCCGTAGATTCC
ATACGCCAGGATTCACTATCCCAGAATCCAGTCTCCCAGAGGGATGAGGCAACAGCAGAG
AATAGGACCCACTCCCTAAAGAGCCCTAGGTATCTTCCAGAAGAGATGGCCCACTCTGAC
ATTTCAGAAACGTCAAATCGGGCCACGTGCCACAGGGAACCTGACAACAGTAAGAACCAC
AAAACCAAGGACAACTTTAAAAGGTCAGTGGCCTCCAAATACCCCAAGGACTGTAGTGAG
GTCGAGCGCACCTACCTGAAAACCAAATCAAGCTCCCCTAGAGACAAGATCTACACTATA
GATGGTGAGAAGGAGCCTGGTTTCCACTTAGATCCACCCCAGTTTGTTGAAAATGTGACC
CTGCCCGAGAACGTGGACTTCCCGGACCCCTACCAGGATCCCAGTGAAAACTTCCGCAAG
GGGGACTCCACGCTGCCAATGAACCGGAACCCCTTGCATAATGAAGAGGGGCTTTCCAAC
AACGACCAGTATAAACTCTACTCCAAGCACTTCACCTTGAAAGACAAGGGTTCCCCGCAC
AGTGAGACCAGCGAGCGATACCGGCAGAACTCCACGCACTGCAGAAGCTGCCTTTCCAAC
ATGCCCACCTATTCAGGCCACTTCACCATGAGGTCCCCCTTCAAGTGCGATGCCTGCCTG
CGGATGGGGAATCTCTATGACATCGATGAAGACCAGATGCTTCAGGAGACAGGTAACCCA
GCCACCGGGGAGCAGGTCTACCAGCAGGACTGGGCACAGAACAATGCCCTTCAATTACAA
AAGAACAAGCTAAGGATTAGCCGTCAGCATTCCTACGATAACATTGTCGACAAACCTAGG
GAGCTAGACCTTAGCAGGCCCTCCCGGAGCATAAGCCTCAAGGACAGGGAACGGCTTCTG
GAGGGAAATTTTTACGGCAGCCTGTTTAGTGTCCCCTCAAGCAAACTCTCGGGGAAAAAA
AGCTCCCTTTTCCCCCAAGGTCTGGAGGACAGCAAGAGGAGCAAGTCTCTCTTGCCAGAC
CACACCTCCGATAACCCTTTCCTCCACTCCCACAGGGATGACCAACGCTTGGTTATTGGG
AGATGCCCCTCGGACCCTTACAAACACTCGTTGCCATCCCAGGCGGTGAATGACAGCTAT
CTTCGGTCGTCCTTGAGGTCAACGGCATCGTACTGTTCCAGGGACAGTCGGGGCCACAAT
GATGTGTATATTTCGGAGCATGTTATGCCTTATGCTGCAAATAAGAATAATATGTACTCT
ACCCCCAGGGTTTTAAATTCCTGCAGCAATAGACGCGTGTACAAGAAAATGCCTAGTATC
GAATCTGATGTTTAA
Target 7 GenBank Gene ID
Target 7 GeneCard ID GRIN2A Link Image
Target 7 GenAtlas ID GRIN2A Link Image
Target 7 HGNC ID HGNC:4585 Link Image
Target 7 Chromosome Location 16
Target 7 Locus 16p13.2
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Foldes RL, Adams SL, Fantaske RP, Kamboj RK: Human N-methyl-D-aspartate receptor modulatory subunit hNR2A: cloning and sequencing of the cDNA and primary structure of the protein. Biochim Biophys Acta. 1994 Aug 11;1223(1):155-9. [PubMed Link Image]
  2. Hess SD, Daggett LP, Crona J, Deal C, Lu CC, Urrutia A, Chavez-Noriega L, Ellis SB, Johnson EC, Velicelebi G: Cloning and functional characterization of human heteromeric N-methyl-D-aspartate receptors. J Pharmacol Exp Ther. 1996 Aug;278(2):808-16. [PubMed Link Image]
Target 7 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 847
Target 8 Name Mu-type opioid receptor
Target 8 Synonyms
  1. MOR-1
Target 8 Gene Name OPRM1
Target 8 Protein Sequence >Mu-type opioid receptor 
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Target 8 Number of Residues 406
Target 8 Molecular Weight 44780
Target 8 Theoretical pI 8.29
Target 8 GO Classification
Function
peptide receptor activity, G-protein coupled
opioid receptor activity
mu-opioid 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 8 General Function Involved in rhodopsin-like receptor activity
Target 8 Specific Function Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • 67-96
  • 106-123
  • 146-165
  • 196-211
  • 237-259
  • 283-305
  • 314-330
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 452073 Link Image
Target 8 UniProtKB/Swiss-Prot ID P35372 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name OPRM_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 8 Gene Sequence >1203 bp 
ATGGACAGCAGCGCTGCCCCCACGAACGCCAGCAATTGCACTGATGCCTTGGCGTACTCA
AGTTGCTCCCCAGCACCCAGCCCCGGTTCCTGGGTCAACTTGTCCCACTTAGATGGCAAC
CTGTCCGACCCATGCGGTCCGAACCGCACCAACCTGGGCGGGAGAGACAGCCTGTGCCCT
CCGACCGGCAGTCCCTCCATGATCACGGCCATCACGATCATGGCCCTCTACTCCATCGTG
TGCGTGGTGGGGCTCTTCGGAAACTTCCTGGTCATGTATGTGATTGTCAGATACACCAAG
ATGAAGACTGCCACCAACATCTACATTTTCAACCTTGCTCTGGCAGATGCCTTAGCCACC
AGTACCCTGCCCTTCCAGAGTGTGAATTACCTAATGGGAACATGGCCATTTGGAACCATC
CTTTGCAAGATAGTGATCTCCATAGATTACTATAACATGTTCACCAGCATATTCACCCTC
TGCACCATGAGTGTTGATCGATACATTGCAGTCTGCCACCCTGTCAAGGCCTTAGATTTC
CGTACTCCCCGAAATGCCAAAATTATCAATGTCTGCAACTGGATCCTCTCTTCAGCCATT
GGTCTTCCTGTAATGTTCATGGCTACAACAAAATACAGGCAAGGTTCCATAGATTGTACA
CTAACATTCTCTCATCCAACCTGGTACTGGGAAAACCTCGTGAAGATCTGTGTTTTCATC
TTCGCCTTCATTATGCCAGTGCTCATCATTACCGTGTGCTATGGACTGATGATCTTGCGC
CTCAAGAGTGTCCGCATGCTCTCTGGCTCCAAAGAAAAGGACAGGAATCTTCGAAGGATC
ACCAGGATGGTGCTGGTGGTGGTGGCTGTGTTCATCGTCTGCTGGACTCCCATTCACATT
TACGTCATCATTAAAGCCTTGGTTACAATCCCAGAAACTACGTTCCAGACTGTTTCTTGG
CACTTCTGCATTGCTCTAGGTTACACAAACAGCTGCCTCAACCCAGTCCTTTATGCATTT
CTGGATGAAAACTTCAAACGATGCTTCAGAGAGTTCTGTATCCCAACCTCTTCCAACATT
GAGCAACAAAACTCCACTCGAATTCGTCAGAACACTAGAGACCACCCCTCCACGGCCAAT
ACAGTGGATAGAACTAATCATCAGCTAGAAAATCTGGAAGCAGAAACTGCTCCGTTGCCC
TAA
Target 8 GenBank Gene ID
Target 8 GeneCard ID OPRM1 Link Image
Target 8 GenAtlas ID OPRM1 Link Image
Target 8 HGNC ID HGNC:8156 Link Image
Target 8 Chromosome Location 6
Target 8 Locus 6q24-q25
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Uhl GR, Sora I, Wang Z: The mu opiate receptor as a candidate gene for pain: polymorphisms, variations in expression, nociception, and opiate responses. Proc Natl Acad Sci U S A. 1999 Jul 6;96(14):7752-5. [PubMed Link Image]
  2. Chuang TK, Killam KF Jr, Chuang LF, Kung HF, Sheng WS, Chao CC, Yu L, Chuang RY: Mu opioid receptor gene expression in immune cells. Biochem Biophys Res Commun. 1995 Nov 22;216(3):922-30. [PubMed Link Image]
  3. Mestek A, Hurley JH, Bye LS, Campbell AD, Chen Y, Tian M, Liu J, Schulman H, Yu L: The human mu opioid receptor: modulation of functional desensitization by calcium/calmodulin-dependent protein kinase and protein kinase C. J Neurosci. 1995 Mar;15(3 Pt 2):2396-406. [PubMed Link Image]
  4. Wang JB, Johnson PS, Persico AM, Hawkins AL, Griffin CA, Uhl GR: Human mu opiate receptor. cDNA and genomic clones, pharmacologic characterization and chromosomal assignment. FEBS Lett. 1994 Jan 31;338(2):217-22. [PubMed Link Image]
  5. Bare LA, Mansson E, Yang D: Expression of two variants of the human mu opioid receptor mRNA in SK-N-SH cells and human brain. FEBS Lett. 1994 Nov 7;354(2):213-6. [PubMed Link Image]
  6. Bergen AW, Kokoszka J, Peterson R, Long JC, Virkkunen M, Linnoila M, Goldman D: Mu opioid receptor gene variants: lack of association with alcohol dependence. Mol Psychiatry. 1997 Oct-Nov;2(6):490-4. [PubMed Link Image]
  7. Bond C, LaForge KS, Tian M, Melia D, Zhang S, Borg L, Gong J, Schluger J, Strong JA, Leal SM, Tischfield JA, Kreek MJ, Yu L: Single-nucleotide polymorphism in the human mu opioid receptor gene alters beta-endorphin binding and activity: possible implications for opiate addiction. Proc Natl Acad Sci U S A. 1998 Aug 4;95(16):9608-13. [PubMed Link Image]
Target 8 Drug References
  1. DeHaven-Hudkins DL, Burgos LC, Cassel JA, Daubert JD, DeHaven RN, Mansson E, Nagasaka H, Yu G, Yaksh T: Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. [PubMed Link Image]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  3. Tan-No K, Niijima F, Nakagawasai O, Sato T, Satoh S, Tadano T: Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci. 2003 Nov;20(3):357-63. [PubMed Link Image]
  4. Roge J, Baumer P, Berard H, Schwartz JC, Lecomte JM: The enkephalinase inhibitor, acetorphan, in acute diarrhoea. A double-blind, controlled clinical trial versus loperamide. Scand J Gastroenterol. 1993 Apr;28(4):352-4. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 1262
Target 9 Name Corticotropin-lipotropin
Target 9 Synonyms
  1. Corticotropin-lipotropin precursor
  2. POMC
  3. Pro-opiomelanocortin
Target 9 Gene Name POMC
Target 9 Protein Sequence >Corticotropin-lipotropin precursor 
MPRSCCSRSGALLLALLLQASMEVRGWCLESSQCQDLTTESNLLECIRACKPDLSAETPM
FPGNGDEQPLTENPRKYVMGHFRWDRFGRRNSSSSGSSGAGQKREDVSAGEDCGPLPEGG
PEPRSDGAKPGPREGKRSYSMEHFRWGKPVGKKRRPVKVYPNGAEDESAEAFPLEFKREL
TGQRLREGDGPDGPADDGAGAQADLEHSLLVAAEKKDEGPYRMEHFRWGSPPKDKRYGGF
MTSEKSQTPLVTLFKNAIIKNAYKKGE
Target 9 Number of Residues 271
Target 9 Molecular Weight 29424
Target 9 Theoretical pI 7.75
Target 9 GO Classification
Function
signal transducer activity
receptor binding
hormone activity
Process
Not Available
Component
extracellular region
Target 9 General Function Involved in hormone activity
Target 9 Specific Function Beta-endorphin and Met-enkephalin are endogenous opiates
Target 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Pfam Domain Function
Target 9 Signals
  • 1-26
Target 9 Transmembrane Regions
  • None
Target 9 Essentiality Non-Essential
Target 9 GenBank ID Protein 190188 Link Image
Target 9 UniProtKB/Swiss-Prot ID P01189 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name COLI_HUMAN Link Image
Target 9 PDB ID Not Available
Target 9 Cellular Location Not Available
Target 9 Gene Sequence >789 bp 
TGCAGCCGCTCGGGGGCCCTGTTGCTGGCCTTGCTGCTTCAGGCCTCCATGGAAGTGCGT
GGCTGGTGCCTGGAGAGCAGCCAGTGTCAGGACCTCACCACGGAAAGCAACCTGCTGGAG
TGCATCCGGGCCTGCAAGCCCGACCTCTCGGCCGAGACTCCCATGTTCCCGGGAAATGGC
GACGAGCAGCCTCTGACCGAGAACCCCCGGAAGTACGTCATGGGCCACTTCCGCTGGGAC
CGATTCGGCCGCCGCAACAGCAGCAGCAGCGGCAGCAGCGGCGCAGGGCAGAAGCGCGAG
GACGTCTCAGCGGGCGAAGACTGCGGCCCGCTGCCTGAGGGCGGCCCCGAGCCCCGCAGC
GATGGTGCCAAGCCGGGCCCGCGCGAGGGCAAGCGCTCCTACTCCATGGAGCACTTCCGC
TGGGGCAAGCCGGTGGGCAAGAAGCGGCGCCCAGTGAAGGTGTACCCTAACGGCGCCGAG
GACGAGTCGGCCGAGGCCTTCCCCCTGGAGTTCAAGAGGGAGCTGACTGGCCAGCGACTC
CGGGAGGGAGATGGCCCCGACGGCCCTGCCGATGACGGCGCAGGGGCCCAGGCCGACCTG
GAGCACAGCCTGCTGGTGGCGGCCGAGAAGAAGGACGAGGGCCCCTACAGGATGGAGCAC
TTCCGCTGGGGCAGCCCGCCCAAGGACAAGCGCTACGGCGGTTTCATGACCTCCGAGAAG
AGCCAGACGCCCCTGGTGACGCTGTTCAAAAACGCCATCATCAAGAACGCCTACAAGAAG
GGCGAGTGA
Target 9 GenBank Gene ID
Target 9 GeneCard ID POMC Link Image
Target 9 GenAtlas ID POMC Link Image
Target 9 HGNC ID HGNC:9201 Link Image
Target 9 Chromosome Location 2
Target 9 Locus 2p23.3
Target 9 SNPs SNPJam Report Link Image
Target 9 General References
  1. Echwald SM, Sorensen TI, Andersen T, Tybjaerg-Hansen A, Clausen JO, Pedersen O: Mutational analysis of the proopiomelanocortin gene in Caucasians with early onset obesity. Int J Obes Relat Metab Disord. 1999 Mar;23(3):293-8. [PubMed Link Image]
  2. Miraglia del Giudice E, Cirillo G, Santoro N, D'Urso L, Carbone MT, Di Toro R, Perrone L: Molecular screening of the proopiomelanocortin (POMC ) gene in Italian obese children: report of three new mutations. Int J Obes Relat Metab Disord. 2001 Jan;25(1):61-7. [PubMed Link Image]
  3. Li CH, Chung D: Primary structure of human beta-lipotropin. Nature. 1976 Apr 15;260(5552):622-4. [PubMed Link Image]
  4. Dragon N, Seidah NG, Lis M, Routhier R, Chretien M: Primary structure and morphine-like activity of human beta-endorphin. Can J Biochem. 1977 Jun;55(6):666-70. [PubMed Link Image]
  5. Bovenberg RA, Burbach JP, Wiegant VM, Veeneman GH, van Boom JH, Baas PD, Jansz HS, de Wied D: gamma-Endorphin and schizophrenia: amino acid composition of gamma-endorphin and nucleotide sequence of gamma-endorphin cDNA from pituitary glands of schizophrenic patients. Brain Res. 1986 Jun 18;376(1):29-37. [PubMed Link Image]
  6. Fenger M, Johnsen AH: Alpha-amidated peptides derived from pro-opiomelanocortin in normal human pituitary. Biochem J. 1988 Mar 15;250(3):781-8. [PubMed Link Image]
  7. Golovin SIa, Karginov VA, Bondar' AA, Beklemishev AB, Chekhranova MK: [Synthesis, cloning and primary structure of DNA complementary to mRNA for human pituitary pro-opiomelanocortin] Bioorg Khim. 1987 Apr;13(4):562-4. [PubMed Link Image]
  8. Riniker B, Sieber P, Rittel W, Zuber H: Revised amino-acid sequences for porcine and human adrenocorticotrophic hormone. Nat New Biol. 1972 Jan 26;235(56):114-5. [PubMed Link Image]
  9. Sieber P, Rittel W, Riniker B: [Synthesis of the human adrenal cortex hormone ( h ACTH) with a revised amino acid sequence] Helv Chim Acta. 1972;55(4):1243-66. [PubMed Link Image]
  10. Yamashiro D, Li CH: Adrenocorticotropins. 44. Total synthesis of the human hormone by the solid-phase method. J Am Chem Soc. 1973 Feb 21;95(4):1310-5. [PubMed Link Image]
  11. 4352834 Bennett HP, Lowry PJ, McMartin C: Confirmation of the 1-20 amino acid sequence of human adrenocorticotrophin. Biochem J. 1973 May;133(1):11-3.
  12. 6254047 Chang AC, Cochet M, Cohen SN: Structural organization of human genomic DNA encoding the pro-opiomelanocortin peptide. Proc Natl Acad Sci U S A. 1980 Aug;77(8):4890-4.
  13. 6267033 Seidah NG, Rochemont J, Hamelin J, Lis M, Chretien M: Primary structure of the major human pituitary pro-opiomelanocortin NH2-terminal glycopeptide. Evidence for an aldosterone-stimulating activity. J Biol Chem. 1981 Aug 10;256(15):7977-84.
  14. 6272808 Seidah NG, Rochemont J, Hamelin J, Benjannet S, Chretien M: The missing fragment of the pro-sequence of human pro-opiomelanocortin: sequence and evidence for C-terminal amidation. Biochem Biophys Res Commun. 1981 Sep 30;102(2):710-6.
  15. 6274691 Takahashi H, Teranishi Y, Nakanishi S, Numa S: Isolation and structural organization of the human corticotropin--beta-lipotropin precursor gene. FEBS Lett. 1981 Nov 30;135(1):97-102.
  16. 6299668 Whitfeld PL, Seeburg PH, Shine J: The human pro-opiomelanocortin gene: organization, sequence, and interspersion with repetitive DNA. DNA. 1982;1(2):133-43.
  17. 6314261 Takahashi H, Hakamata Y, Watanabe Y, Kikuno R, Miyata T, Numa S: Complete nucleotide sequence of the human corticotropin-beta-lipotropin precursor gene. Nucleic Acids Res. 1983 Oct 11;11(19):6847-58.
  18. 6945581 Seidah NG, Chretien M: Complete amino acid sequence of a human pituitary glycopeptide: an important maturation product of pro-opiomelanocortin. Proc Natl Acad Sci U S A. 1981 Jul;78(7):4236-40.
  19. 7828531 Morris JC, Savva D, Lowry PJ: Reduced expression of a naturally deleted form of human proopiomelanocortin complementary deoxyribonucleic acid after transfection into Chinese hamster ovary cells. Endocrinology. 1995 Jan;136(1):195-201.
  20. 9768693 Hinney A, Becker I, Heibult O, Nottebom K, Schmidt A, Ziegler A, Mayer H, Siegfried W, Blum WF, Remschmidt H, Hebebrand J: Systematic mutation screening of the pro-opiomelanocortin gene: identification of several genetic variants including three different insertions, one nonsense and two missense point mutations in probands of different weight extremes. J Clin Endocrinol Metab. 1998 Oct;83(10):3737-41.
Target 9 Drug References
  1. Nomura A, Iwasaki Y, Aoki Y, Yamamori E, Mutsuga N, Yoshida M, Asai M, Oiso Y, Saito H: Effects of loperamide and other opioid-related substances on the transcriptional regulation of the rat pro-opiomelanocortin gene in AtT20 cells. Neuroendocrinology. 2001 Aug;74(2):87-94. [PubMed Link Image]
  2. Auernhammer CJ, Stalla GK, Lange M, Pfeiffer A, Muller OA: Effects of loperamide on the human hypothalamo-pituitary-adrenal axis in vivo and in vitro. J Clin Endocrinol Metab. 1992 Aug;75(2):552-7. [PubMed Link Image]
  3. Ambrosi B, Bochicchio D, Ferrario R, Colombo P, Faglia G: Effects of the opiate agonist loperamide on pituitary-adrenal function in patients with suspected hypercortisolism. J Endocrinol Invest. 1989 Jan;12(1):31-5. [PubMed Link Image]
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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.