Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00314

Target Information
NameCannabinoid receptor 2    
Type of targetClinical trial target    
SynonymsCB-2    
CB2    
CX5    
Cannabinoid CB2 receptor    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1]
Pain, unspecified
[ICD9: 338,780   ICD10: R52, G89]
[1]
Drug(s)S-777469Phase IIAtopic dermatitis (AD)[2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP34972
PDB Structure2KI9.    
FunctionInvolved in cannabinoid-induced cns effects through G-protein mediated inhibition of adenylate cyclase. Could be a receptor for anandamide.    
SequenceMEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILS SHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTAS VGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCS ELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLD VRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYA LRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorA-796260[3]
AM-1241[3]
AM-1710[4]
AM-1714[4]
AM-1715[4]
AM-281[5]
AM-404[6]
AM-411[7]
AM-4768[4]
AM-630[8]
CP-55940[9]
GNF-PF-5188[10]
HU-210[11]
HU-210,   HU-211[12]
JWH-120[10]
JWH-133[13]
JWH-145[14]
JWH-146[14]
JWH-147[14]
JWH-150[14]
JWH-151[10]
JWH-156[14]
JWH-167[15]
JWH-201[15]
JWH-202[15]
JWH-203[15]
JWH-204[15]
JWH-205[15]
JWH-206[15]
JWH-207[15]
JWH-208[15]
JWH-209[15]
JWH-229[10]
JWH-237[15]
JWH-243[14]
JWH-244[14]
JWH-245[14]
JWH-246[14]
JWH-248[15]
JWH-249[15]
JWH-250[15]
JWH-251[15]
JWH-252[15]
JWH-253[15]
JWH-268[10]
JWH-292[14]
JWH-293[14]
JWH-294[16]
JWH-295[16]
JWH-296[16]
JWH-297[16]
JWH-302[15]
JWH-303[15]
JWH-305[15]
JWH-306[15]
JWH-307[14]
JWH-308[14]
JWH-309[14]
JWH-311[15]
JWH-312[15]
JWH-313[15]
JWH-314[15]
JWH-315[15]
JWH-323[16]
JWH-324[17]
JWH-325[16]
JWH-337[16]
JWH-342[16]
JWH-342[17]
JWH-343[16]
JWH-344[16]
JWH-345[16]
JWH-346[14]
JWH-347[14]
JWH-348[14]
JWH-363[14]
JWH-364[14]
JWH-365[14]
JWH-366[14]
JWH-367[14]
JWH-368[14]
JWH-369[14]
JWH-370[14]
JWH-371[14]
JWH-372[14]
JWH-373[14]
JWH-385[16]
JWH-392[16]
JWH-401[16]
JWH-402[16]
JWH-403[16]
JWH-404[16]
JWH-405[16]
JWH-406[16]
JWH-407[16]
JWH-440[17]
JWH-441[17]
JWH-442[17]
KM-233[18]
KM-233[18]
KM-233[18]
KM-233-M[18]
NABILONE[19]
NAPHTHYRIDINONE[20]
PRAVADOLINE[21]
RIMONABANT HYDROCHLORIDE[22]
SCH-225336[23]
SCH-356036[24]
SR-144,528[9]
SR-147778[25]
VER-156084[26]
VER-156085[26]
WIN-55212-2[27]
AgonistJWH-015[28]
Palmitoylethanolamide[28]
S-777469[2]
AntagonistSR144528[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Antinociceptive activity of the endogenous fatty acid amide, palmitylethanolamide. Eur J Pharmacol. 2001 May 11;419(2-3):191-8. To Reference
Ref 2Emerging drugs for atopic dermatitis. Expert Opin Emerg Drugs. 2009 Mar;14(1):165-79. To Reference
Ref 3J Med Chem. 2010 Jan 14;53(1):295-315.Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. To Reference
Ref 4J Med Chem. 2007 Dec 27;50(26):6493-500. Epub 2007 Nov 27.Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. To Reference
Ref 5Bioorg Med Chem. 2009 Apr 1;17(7):2842-51. Epub 2009 Feb 21.Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. To Reference
Ref 6J Med Chem. 2008 Dec 25;51(24):7800-5.New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide. To Reference
Ref 7J Med Chem. 2010 Aug 12;53(15):5656-66.Heteroadamantyl cannabinoids. To Reference
Ref 8Bioorg Med Chem Lett. 2007 Dec 1;17(23):6505-10. Epub 2007 Oct 1.New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. To Reference
Ref 9J Med Chem. 2006 Dec 14;49(25):7502-12.Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. To Reference
Ref 10J Med Chem. 2009 Jan 22;52(2):369-78.Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow. To Reference
Ref 11J Med Chem. 2009 Apr 23;52(8):2506-14.New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo. To Reference
Ref 12Bioorg Med Chem. 2007 Aug 15;15(16):5406-16. Epub 2007 May 31.Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors. To Reference
Ref 13J Med Chem. 2006 Oct 5;49(20):5947-57.Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists. To Reference
Ref 14Bioorg Med Chem Lett. 2006 Oct 15;16(20):5432-5. Epub 2006 Aug 4.1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors. To Reference
Ref 15Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles. To Reference
Ref 16Bioorg Med Chem. 2008 Jan 1;16(1):322-35. Epub 2007 Sep 22.Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940. To Reference
Ref 17Bioorg Med Chem. 2010 Aug 1;18(15):5475-82. Epub 2010 Jun 22.Synthesis and pharmacology of 1-methoxy analogs of CP-47,497. To Reference
Ref 18Bioorg Med Chem. 2008 Jul 1;16(13):6489-500. Epub 2008 May 20.Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs. To Reference
Ref 19J Med Chem. 2010 Oct 14;53(19):6996-7010.Novel 1',1'-chain substituted hexahydrocannabinols: 9-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist. To Reference
Ref 20Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. Epub 2005 Nov 2.Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists. To Reference
Ref 21Bioorg. Med. Chem. Lett. 5(4):381-386 (1995) To Reference
Ref 22J Med Chem. 2010 Feb 11;53(3):1338-46.Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. To Reference
Ref 23Bioorg Med Chem Lett. 2010 Mar 1;20(5):1565-8. Epub 2010 Jan 21.Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor. To Reference
Ref 24Bioorg Med Chem Lett. 2010 Feb 1;20(3):1084-9. Epub 2009 Dec 11.Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. To Reference
Ref 25J Med Chem. 2005 Aug 11;48(16):5059-87.The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. To Reference
Ref 26Bioorg Med Chem Lett. 2009 Aug 1;19(15):4241-4. Epub 2009 May 29.Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. To Reference
Ref 27Eur J Med Chem. 2008 Mar;43(3):513-39. Epub 2007 May 6.Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. To Reference
Ref 28Posttraining activation of CB1 cannabinoid receptors in the CA1 region of the dorsal hippocampus impairs object recognition long-term memory. Neurobiol Learn Mem. 2008 Sep;90(2):374-81. Epub 2008 Jun 3. To Reference



 

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