Target Validation Information
Target ID T37693
Target Name Cannabinoid receptor 2
Target Type
Successful
Drug Potency against Target PRAVADOLINE Drug Info IC50 = 3155 nM
NABILONE Drug Info Ki = 1.8 nM [531196]
A-796260 Drug Info Ki = 4.6 nM [530525]
Dodeca-2E,4E-dienoic acid isobutylamide Drug Info Ki = 52 nM [528831]
WIN-55212-2 Drug Info IC50 = 2200 nM [528907]
JWH-295 Drug Info Ki = 3759 nM [529084]
5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole Drug Info Ki = 4700 nM [529434]
N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 1000 nM [529838]
JWH-314 Drug Info Ki = 76 nM [527630]
JWH-243 Drug Info Ki = 41 nM [528355]
JWH-297 Drug Info Ki = 1506 nM [529084]
JWH-202 Drug Info Ki = 645 nM [527630]
JWH-296 Drug Info Ki = 2060 nM [529084]
JWH-347 Drug Info Ki = 169 nM [528355]
JWH-246 Drug Info Ki = 16 nM [528355]
JWH-229 Drug Info Ki = 18 nM [529920]
JWH-206 Drug Info Ki = 498 nM [527630]
JWH-315 Drug Info Ki = 182 nM [527630]
JWH-293 Drug Info Ki = 41 nM [528355]
JWH-253 Drug Info Ki = 84 nM [527630]
JWH-294 Drug Info Ki = 3972 nM [529084]
JWH-401 Drug Info Ki = 1120 nM [529084]
JWH-311 Drug Info Ki = 39 nM [527630]
JWH-307 Drug Info Ki = 3.3 nM [528355]
JWH-303 Drug Info Ki = 138 nM [527630]
JWH-348 Drug Info Ki = 53 nM [528355]
JWH-207 Drug Info Ki = 3723 nM [527630]
JWH-209 Drug Info Ki = 1353 nM [527630]
JWH-248 Drug Info Ki = 657 nM [527630]
JWH-325 Drug Info Ki = 700 nM [529084]
JWH-392 Drug Info Ki = 1782 nM [529084]
JWH-249 Drug Info Ki = 20 nM [527630]
JWH-313 Drug Info Ki = 365 nM [527630]
JWH-385 Drug Info Ki = 421 nM [529084]
JWH-440 Drug Info Ki = 553 nM [531027]
JWH-372 Drug Info Ki = 8.2 nM [528355]
AM-4768 Drug Info Ki = 4.8 nM [529170]
JWH-150 Drug Info Ki = 15 nM [528355]
JWH-344 Drug Info Ki = 221 nM [529084]
JWH-306 Drug Info Ki = 82 nM [527630]
JWH-305 Drug Info Ki = 29 nM [527630]
N1-(4-bromophenyl)-N2,N2-dipentylphthalamide Drug Info Ki < 25 nM [529920]
JWH-146 Drug Info Ki = 62 nM [528355]
JWH-203 Drug Info Ki = 7 nM [527630]
JWH-364 Drug Info Ki = 29 nM [528355]
JWH-366 Drug Info Ki = 24 nM [528355]
JWH-302 Drug Info Ki = 89 nM [527630]
JWH-251 Drug Info Ki = 146 nM [527630]
JWH-205 Drug Info Ki = 180 nM [527630]
JWH-345 Drug Info Ki = 173 nM [529084]
JWH-208 Drug Info Ki = 570 nM [527630]
JWH-250 Drug Info Ki = 33 nM [527630]
JWH-308 Drug Info Ki = 33 nM [528355]
JWH-167 Drug Info Ki = 159 nM [527630]
JWH-237 Drug Info Ki = 106 nM [527630]
JWH-407 Drug Info Ki = 546 nM [529084]
JWH-204 Drug Info Ki = 25 nM [527630]
JWH-145 Drug Info Ki = 6.4 nM [528355]
4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide Drug Info Ki = 2407 nM [530617]
(1S,2S)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 290 nM [530070]
Rac-cis-N-arachidonoylcyclopropanolamide Drug Info Ki = 150 nM [530070]
(1R,2S)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 190 nM [530070]
(1R,2S)-N-Oleoylcyclopropanolamide Drug Info Ki = 1630 nM [530070]
Cis-N-oleoylcyclopropanolamide Drug Info Ki = 340 nM [530070]
N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 81 nM [528112]
4'-(1,1-dimethyl-heptyl)-3,5-dimethyl-biphenyl Drug Info Ki = 2138 nM [528844]
4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol Drug Info Ki = 580 nM [528844]
2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 17 nM [528844]
O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 2400 nM [528112]
N-oleoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 5400 nM [528112]
4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 1000 nM [528844]
N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 10130 nM [530929]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 6610 nM [530929]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 7450 nM [530929]
SCH-356036 Drug Info Ki = 0.8 nM [530597]
DELTA 8-TETRAHYDROCANNOBINOL Drug Info Ki = 39.3 nM [529727]
N-benzyl-4-bromo-3-(morpholinosulfonyl)benzamide Drug Info Ki = 800 nM [529872]
N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 95 nM [529106]
KM-233-M Drug Info Ki = 0.9 nM [529515]
1,4-dihydroindeno[1,2-c]-pyrazole Drug Info Ki = 0.34 nM [527858]
NAPHTHYRIDINONE Drug Info IC50 = 4100 nM [527839]
JWH-442 Drug Info Ki = 693 nM [531027]
AM-1715 Drug Info Ki = 5.9 nM [529170]
JWH-244 Drug Info Ki = 18 nM [528355]
JWH-156 Drug Info Ki = 104 nM [528355]
AM-1714 Drug Info Ki = 0.82 nM [529170]
JWH-405 Drug Info Ki = 154 nM [529084]
JWH-365 Drug Info Ki = 3.4 nM [528355]
GNF-PF-5188 Drug Info Ki = 1.78 nM [529920]
JWH-343 Drug Info Ki = 1362 nM [529084]
JWH-268 Drug Info Ki = 40 nM [529920]
JWH-441 Drug Info Ki = 808 nM [531027]
JWH-403 Drug Info Ki = 460 nM [529084]
JWH-406 Drug Info Ki = 215 nM [529084]
AM-1710 Drug Info Ki = 6.7 nM [529170]
JWH-309 Drug Info Ki = 49 nM [528355]
JWH-369 Drug Info Ki = 5.2 nM [528355]
JWH-245 Drug Info Ki = 25 nM [528355]
JWH-346 Drug Info Ki = 39 nM [528355]
JWH-373 Drug Info Ki = 69 nM [528355]
JWH-252 Drug Info Ki = 19 nM [527630]
JWH-337 Drug Info Ki = 238 nM [529084]
JWH-367 Drug Info Ki = 23 nM [528355]
JWH-370 Drug Info Ki = 4 nM [528355]
JWH-363 Drug Info Ki = 71 nM [528355]
JWH-147 Drug Info Ki = 7.1 nM [528355]
JWH-371 Drug Info Ki = 64 nM [528355]
JWH-323 Drug Info Ki = 639 nM [529084]
JWH-404 Drug Info Ki = 672 nM [529084]
JWH-402 Drug Info Ki = 1077 nM [529084]
VER-156085 Drug Info Ki = 10900 nM [530200]
5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one Drug Info Ki = 3490 nM [530009]
AM-281 Drug Info Ki = 4200 nM [530009]
(1S,2S)-N-Oleoylcyclopropanolamide Drug Info Ki = 2420 nM [530070]
(E)-N-(4-methoxyphenyl)undec-2-enamide Drug Info Ki = 2500 nM [527788]
(1R,2R)-N-Oleoylcyclopropanolamide Drug Info Ki = 4410 nM [530070]
(E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide Drug Info Ki = 5200 nM [527788]
AM-1241 Drug Info Ki = 11.5 nM [530525]
(1S,2R)-N-Oleoylcyclopropanolamide Drug Info Ki = 2040 nM [530070]
(1R,2R)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 240 nM [530070]
(E)-N-(4-methoxyphenethyl)undec-2-enamide Drug Info Ki = 5100 nM [527788]
2-(2-Methoxybenzyl)-3H-benzo[f]chromen-3-one Drug Info Ki = 2060 nM [530009]
4-benzhydryl-N-butylpiperazine-1-carboxamide Drug Info Ki = 2833 nM [530617]
N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) Drug Info Ki = 1800 nM [529563]
3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 44 nM [528844]
(4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone Drug Info Ki = 3050 nM [530617]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 3390 nM [530929]
(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 3450 nM [530929]
N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 12000 nM [530929]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 2330 nM [530929]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 5400 nM [530929]
(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 3400 nM [530929]
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 7600 nM [530929]
(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 10000 nM [530929]
N-oleoyl-O-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 3800 nM [528112]
O-oleoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 8600 nM [528112]
N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) Drug Info IC50 = 220 nM [530871]
SCH-225336 Drug Info Ki = 4.5 nM [530693]
3-Benzyl-5-isopropyl-8-methylchromen-2-one Drug Info Ki = 4270 nM [530009]
5-Biphenyl-4-ylmethyl-1-isobutyl-1H-tetrazole Drug Info Ki = 7700 nM [529434]
N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 100 nM [529838]
JWH-151 Drug Info Ki = 30 nM [529920]
JWH-120 Drug Info Ki = 6.1 nM [529920]
3-benzoyl-1-pentyl-1,4-dihydroquinolin-4-one Drug Info Ki = 446 nM [529079]
Rac-trans-N-oleoylcyclopropanolamide Drug Info Ki = 380 nM [530070]
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info IC50 = 2480 nM [530929]
JWH-324 Drug Info Ki = 231 nM [531027]
N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 1900 nM [528112]
CP-55940 Drug Info Ki = 1.11 nM [528562]
N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide Drug Info Ki = 7900 nM [529563]
AM-630 Drug Info Ki = 36 nM [529106]
JWH-133 Drug Info Ki = 65 nM [528452]
JWH-292 Drug Info Ki = 20 nM [528355]
JWH-368 Drug Info Ki = 9.1 nM [528355]
AM-404 Drug Info Ki = 1300 nM [529838]
SR-147778 Drug Info Ki = 442 nM [527671]
JWH-201 Drug Info Ki = 444 nM [527630]
JWH-312 Drug Info Ki = 91 nM [527630]
5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol Drug Info Ki = 20 nM [528844]
4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol Drug Info Ki = 1 nM [528844]
AM-411 Drug Info Ki = 52 nM [531004]
VER-156084 Drug Info Ki = 7190 nM [530200]
Action against Disease Model SR141716A N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride (SR141716A), a cannabinoid CB(2) receptor antagonist, has inverse agonist effects in cannabinoid CB(2) receptor-expressing cell lines, brain and peripheral organs. [552248] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Using the Cannabinoid receptor 2-/- knockout mice investigators have discovered the involvement of Cannabinoid receptor 2 on immune cell function and development, infection, embryonic development, bone loss, liver disorders, pain, autoimmune inflammation, allergic dermatitis, atherosclerosis, apoptosis and chemotaxis; CB2R-/- mice showed accelerated age-related trabecular bone loss and cortical expansion, although cortical thickness remained the same.CB2R-/- osteoclast n uMber and trabecular osteoblast activity were increased.CB2R-/- mice have a lower threshold of pain compared to wild-type mice in the presence of cannabinoids. [552248]
References
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Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 529084Bioorg 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.
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Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 529084Bioorg 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.
Ref 531027Bioorg Med Chem. 2010 Aug 1;18(15):5475-82. Epub 2010 Jun 22.Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.
Ref 528355Bioorg 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.
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Ref 528355Bioorg 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.
Ref 529084Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 529920J Med Chem. 2009 Jan 22;52(2):369-78.Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.
Ref 528355Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 528355Bioorg 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.
Ref 528355Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 529084Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 528355Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 529084Bioorg 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.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 528355Bioorg 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.
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Ref 528355Bioorg 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.
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Ref 529084Bioorg 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.
Ref 529084Bioorg 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.
Ref 529084Bioorg 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.
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Ref 530871J Med Chem. 2010 May 27;53(10):4028-37.Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Ref 530693Bioorg 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.
Ref 530009Bioorg 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.
Ref 529434Bioorg Med Chem Lett. 2008 May 1;18(9):2820-4. Epub 2008 Apr 4.New tetrazole-based selective anandamide uptake inhibitors.
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Ref 529920J Med Chem. 2009 Jan 22;52(2):369-78.Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.
Ref 529079J Med Chem. 2007 Nov 1;50(22):5471-84. Epub 2007 Oct 4.Pharmacomodulations around the 4-oxo-1,4-dihydroquinoline-3-carboxamides, a class of potent CB2-selective cannabinoid receptor ligands: consequences in receptor affinity and functionality.
Ref 530070J Med Chem. 2009 May 14;52(9):3001-9.Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Ref 530929Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. Epub 2010 Apr 21.Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Ref 531027Bioorg Med Chem. 2010 Aug 1;18(15):5475-82. Epub 2010 Jun 22.Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.
Ref 528112J Med Chem. 2006 Apr 6;49(7):2333-8.Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.
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Ref 529563Bioorg Med Chem. 2008 Aug 1;16(15):7510-5. Epub 2008 Jun 7.Novel sterically hindered cannabinoid CB1 receptor ligands.
Ref 529106Bioorg 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.
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Ref 528355Bioorg 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.
Ref 528355Bioorg 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.
Ref 529838J 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.
Ref 527671J Med Chem. 2005 Aug 11;48(16):5059-87.The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 527630Bioorg Med Chem Lett. 2005 Sep 15;15(18):4110-3.1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.
Ref 528844Bioorg Med Chem Lett. 2007 Jul 1;17(13):3652-6. Epub 2007 Apr 25.Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.
Ref 528844Bioorg Med Chem Lett. 2007 Jul 1;17(13):3652-6. Epub 2007 Apr 25.Biaryl cannabinoid mimetics--synthesis and structure-activity relationship.
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Ref 530200Bioorg 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.

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