The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28088085 |
42 |
New pyridazinone-4-carboxamides as new cannabinoid receptor type-2 inverse agonists: Synthesis, pharmacological data and molecular docking. |
University of Sassari |
27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
27560280 |
138 |
Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
Pontificia Universidad Cat£Lica De Chile |
27448919 |
69 |
Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality. |
German University In Cairo |
27671499 |
46 |
Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists. |
Janssen Research and Development |
27671496 |
46 |
Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists. |
Janssen Research and Development |
27240274 |
37 |
A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives. |
Neuroscienze Pharmaness S.C.A R.L. |
27096053 |
4 |
Discovery of KLS-13019, a Cannabidiol-Derived Neuroprotective Agent, with Improved Potency, Safety, and Permeability. |
Kannalife Sciences |
27078864 |
46 |
Synthesis and pharmacological evaluation of new biphenylic derivatives as CB2 receptor ligands. |
Universit£ |
26888301 |
34 |
Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain. |
University of Siena |
26876931 |
36 |
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket. |
Abbott Healthcare Products |
26789378 |
57 |
Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology. |
Instituto De Qu£Mica M£Dica |
26756097 |
56 |
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solubility. |
Universit£ |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26890113 |
41 |
Tricyclic pyrazoles. Part 8. Synthesis, biological evaluation and modelling of tricyclic pyrazole carboxamides as potential CB2 receptor ligands with antagonist/inverse agonist properties. |
Universit£ |
26922225 |
91 |
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
Universit£ |
26827137 |
26 |
Pyrazole antagonists of the CB1 receptor with reduced brain penetration. |
Rti International |
26209834 |
46 |
Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists. |
Universit£ |
26275680 |
68 |
Synthesis and biological evaluation of (3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist. |
University of Tennessee Health Science Center |
26149623 |
7 |
Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria. |
University of California Berkeley |
26203658 |
39 |
Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors. |
University of Auckland |
26151231 |
154 |
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor. |
Zhejiang University |
26000707 |
20 |
Isolation and Pharmacological Evaluation of Minor Cannabinoids from High-Potency Cannabis sativa. |
The University of Mississippi |
25466197 |
32 |
Novel azoles as potent and selective cannabinoid CB2 receptor agonists. |
Ipsen Innovation |
21511945 |
7 |
Cannabinoid type 1 receptor antagonists modulate transport activity of multidrug resistance-associated proteins MRP1, MRP2, MRP3, and MRP4. |
Radboud University Nijmegen Medical Centre |
25935384 |
26 |
New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity. |
University of Pisa |
25699149 |
52 |
Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis. |
University of Lille |
25671648 |
6 |
Selective, nontoxic CB(2) cannabinoid o-quinone with in vivo activity against triple-negative breast cancer. |
Instituto De Qu£Mica M£Dica |
25644673 |
186 |
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor. |
Zhejiang University |
25599952 |
20 |
Synthesis, radiolabeling and evaluation of novel 4-oxo-quinoline derivatives as PET tracers for imaging cannabinoid type 2 receptor. |
Institute of Pharmaceutical Sciences |
25797163 |
34 |
Structure-activity relationships of substituted 1H-indole-2-carboxamides as CB1 receptor allosteric modulators. |
Research Triangle Institute |
25556098 |
36 |
Selective CB2 receptor agonists. Part 1: the identification of novel ligands through computer-aided drug design (CADD) approaches. |
Boehringer Ingelheim Pharmaceuticals |
25486424 |
30 |
Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands. |
Universit£ |
25096297 |
63 |
Design, synthesis and in vitro evaluation of novel uni- and bivalent ligands for the cannabinoid receptor type 1 with variation of spacer length and structure. |
Julius-Maximilians-Universit£T W£Rzburg |
25072877 |
40 |
One-pot heterogeneous synthesis of¿(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. |
University of Perugia |
25065940 |
77 |
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist. |
Universit£ |
24984935 |
24 |
Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB2R selective benzimidazoles reveal unexpected intrinsic properties. |
Julius-Maximilians-Universit£T W£Rzburg |
24972328 |
26 |
Identification of endocannabinoid system-modulating N-alkylamides from Heliopsis helianthoides var. scabra and Lepidium meyenii. |
University of Szeged |
24863744 |
15 |
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
University of Missouri |
23902803 |
9 |
Peripherally restricted CB1 receptor blockers. |
Jenrin Discovery |
25575658 |
83 |
Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model. |
Boehringer Ingelheim Pharmaceuticals |
25556092 |
85 |
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds. |
Boehringer Ingelheim Pharma |
25499880 |
51 |
Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome. |
Raqualia Pharma |
25488844 |
154 |
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists. |
Arena Pharmaceuticals |
25487422 |
93 |
Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists. |
University of Oxford |
25466177 |
24 |
The SAR development of substituted purine derivatives as selective CB2 agonists for the treatment of chronic pain. |
Eli Lilly |
25272206 |
88 |
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides. |
Universit£ |
25241924 |
47 |
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor. |
Novartis Institutes For Biomedical Research |
25162172 |
51 |
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
Research Triangle Institute |
24922543 |
24 |
Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands. |
Universit£ |
24900877 |
107 |
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors. |
Merck Research Laboratories |
24856183 |
4 |
Ultrapure ajulemic acid has improved CB2 selectivity with reduced CB1 activity. |
Corbus Pharmaceuticals |
24731541 |
1 |
The cannabinoid acids, analogs and endogenous counterparts. |
The University of Massachusetts Medical School |
24182233 |
57 |
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties. |
Bristol-Myers Squibb |
23865723 |
169 |
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. |
Arena Pharmaceuticals |
24461289 |
46 |
Benzimidazole CB2 agonists: design, synthesis and SAR. |
Merck Research Laboratories |
23621789 |
69 |
Novel adamantyl cannabinoids as CB1 receptor probes. |
Northeastern University |
23466226 |
26 |
Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors. |
University of Arkansas For Medical Sciences |
23434135 |
27 |
Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21. |
Instituto De Qu£Mica M£Dica |
23380378 |
127 |
Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening. |
F. Hoffmann-La Roche |
24729834 |
79 |
Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB |
University of Pittsburgh |
24900561 |
25 |
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55. |
University of Bonn |
23406429 |
83 |
Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation. |
University of Pittsburgh |
23350768 |
196 |
Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
Universit£ |
23227781 |
119 |
Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
Astrazeneca |
17027269 |
23 |
Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
Ucb Pharma |
22548457 |
60 |
Design, synthesis, and pharmacological characterization of indol-3-ylacetamides, indol-3-yloxoacetamides, and indol-3-ylcarboxamides: potent and selective CB2 cannabinoid receptor inverse agonists. |
Universit£ |
21334892 |
39 |
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists. |
Msd |
21316962 |
31 |
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. |
Merck Research Laboratories |
20634067 |
23 |
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists. |
Schering-Plough Research Institute |
20005703 |
66 |
Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain. |
Glaxosmithkline |
19864133 |
42 |
2-Amino-5-aryl-pyridines as selective CB2 agonists: synthesis and investigation of structure-activity relationships. |
Glaxosmithkline |
19406638 |
35 |
Predictive models of Cannabinoid-1 receptor antagonists derived from diverse classes. |
Korea Research Institute of Chemical Technology |
23147076 |
163 |
Structure-activity relationships of 2-arylamido-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxamide derivatives as cannabinoid receptor agonists and their analgesic action. |
Nycomed Pharma |
22341572 |
61 |
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
Rti International |
23098108 |
36 |
Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists. |
Research Triangle Institute |
23072339 |
132 |
Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors. |
University of Pittsburgh |
22916707 |
76 |
7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists. |
University of Bonn |
23017078 |
62 |
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. |
University of Lille |
22738271 |
250 |
7-Oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxamides as selective CB(2) cannabinoid receptor ligands: structural investigations around a novel class of full agonists. |
Universit£ |
23164658 |
78 |
2-Arylbenzofuran-based molecules as multipotent Alzheimer's disease modifying agents. |
University of Bologna |
23151320 |
37 |
Scaffold hopping strategy toward original pyrazolines as selective CB2 receptor ligands. |
Avenue De L'Universit£ |
23085772 |
82 |
Investigations on the 4-quinolone-3-carboxylic acid motif. 6. Synthesis and pharmacological evaluation of 7-substituted quinolone-3-carboxamide derivatives as high affinity ligands for cannabinoid receptors. |
Universit£ |
22959249 |
79 |
JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. |
Jenrin Discovery |
22832315 |
85 |
Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers. |
Astrazeneca |
22571451 |
46 |
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB1 receptor. |
Sapienza University of Rome |
24900484 |
64 |
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
TBA |
22765893 |
32 |
Discovery and optimization of novel purines as potent and selective CB2 agonists. |
Eli Lilly |
22607668 |
66 |
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration. |
Astrazeneca |
22372835 |
71 |
Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity. |
Research Triangle Institute |
22421019 |
62 |
Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent. |
Shionogi |
24900275 |
1 |
Identification of a Potent and Selective Cannabinoid CB1 Receptor Antagonist from Auxarthron reticulatum. |
TBA |
24936232 |
16 |
Discovery of Potent Dual PPARa Agonists/CB1 Ligands. |
TBA |
22483967 |
38 |
Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold. |
Universit£ |
22444677 |
45 |
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent. |
Shionogi |
22437111 |
34 |
CB 1/2 dual agonists with 3-carbamoyl 2-pyridone derivatives as antipruritics: reduction of CNS side effects by introducing polar functional groups. |
Shionogi |
22421020 |
9 |
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
Merck Research Laboratories |
22370265 |
63 |
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management. |
Abbott Laboratories |
21428406 |
70 |
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors. |
National Institute of Mental Health |
20875743 |
90 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
Pfizer |
20943404 |
24 |
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-¿(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor. |
Clemson University |
20684563 |
176 |
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. |
H. Lundbeck |
20718492 |
74 |
Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands. |
Universit£ |
20363132 |
34 |
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern. |
Solvay Pharma |
20137935 |
46 |
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
Solvay Pharma |
20031412 |
36 |
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. |
Solvay Pharma |
20018510 |
73 |
Diaryl piperidines as CB1 receptor antagonists. |
Merck Research Laboratories |
19595596 |
114 |
Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile. |
Sapienza University of Rome |
19520572 |
55 |
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. |
Vernalis (R&D) |
19435366 |
34 |
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists. |
Universita Di Pisa |
19278853 |
67 |
Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. |
University of Bonn |
19143566 |
52 |
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow. |
University of Innsbruck |
19115816 |
38 |
6-Methoxy-N-alkyl isatin acylhydrazone derivatives as a novel series of potent selective cannabinoid receptor 2 inverse agonists: design, synthesis, and binding mode prediction. |
The University of Texas M.D. Anderson Cancer Center |
18680277 |
198 |
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists. |
Amgen |
18680276 |
46 |
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo. |
Universit£ |
18666769 |
32 |
Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 agonists for the treatment of neuropathic pain. |
The University of Texas M.D. Anderson Cancer Center |
18579386 |
40 |
Novel sterically hindered cannabinoid CB1 receptor ligands. |
University of Salerno |
16562853 |
22 |
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro. |
Tom'S of Maine |
18448340 |
27 |
Aminopyrazine CB1 receptor inverse agonists. |
Neurogen |
18440813 |
55 |
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives. |
Pfizer |
18430570 |
76 |
Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands. |
Adolor |
18424134 |
114 |
New tetrazole-based selective anandamide uptake inhibitors. |
Sapienza University of Rome |
18006322 |
43 |
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action. |
Taisho Pharmaceutical |
18333607 |
4 |
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist. |
Merck Research Laboratories |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
17942307 |
34 |
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. |
Universit£ |
17884496 |
51 |
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability. |
Taisho Pharmaceutical |
17630726 |
32 |
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration. |
Novartis Institutes For Biomedical Research |
17561406 |
67 |
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors. |
Universit£ |
16279809 |
23 |
1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists. |
Universit£ |
16279794 |
46 |
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. |
Universit£ |
17181138 |
27 |
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. |
Merck Research Laboratories |
16451053 |
37 |
Synthesis and activity of 1,3,5-triphenylimidazolidine-2,4-diones and 1,3,5-triphenyl-2-thioxoimidazolidin-4-ones: characterization of new CB1 cannabinoid receptor inverse agonists/antagonists. |
Universit£ |
16392793 |
42 |
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling. |
Universit£ |
16213718 |
93 |
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies. |
Institute of Biomolecular Chemistry |
16140010 |
32 |
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
Solvay Pharma |
15771428 |
66 |
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists. |
Solvay Pharma |
16078824 |
48 |
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. |
Universit£ |
12747783 |
17 |
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties. |
Bristol-Myers Squibb |
11960486 |
6 |
Exploration of the pharmacophore of 3-alkyl-5-arylimidazolidinediones as new CB(1) cannabinoid receptor ligands and potential antagonists: synthesis, lipophilicity, affinity, and molecular modeling. |
Universit£ |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
9857088 |
16 |
The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes. |
Kennesaw State University |
9784115 |
15 |
Potent cyano and carboxamido side-chain analogues of 1', 1'-dimethyl-delta8-tetrahydrocannabinol. |
Organix |
9057852 |
74 |
Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor. |
Hebrew University |
10465552 |
10 |
3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands. |
Universit£ |
22284817 |
82 |
¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration. |
Astrazeneca R&D Montreal |
22209458 |
114 |
Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity. |
Vernalis (R&D) |
22130134 |
58 |
5-sulfonyl-benzimidazoles as selective CB2 agonists-part 2. |
Janssen Pharmaceutica |
22172309 |
12 |
Novel bioactive metabolites of dipyrone (metamizol). |
Philipps-Universit£T |
21999614 |
11 |
Cannabinomimetic lipid from a marine cyanobacterium. |
University of California |
22044209 |
56 |
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor. |
Universit£ |
21996466 |
40 |
1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: an effective scaffold for the design of either CB1 or CB2 receptor ligands. |
Sapienza University of Rome |
21962575 |
8 |
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies. |
Bristol-Myers Squibb |
21937154 |
9 |
Asymmetric synthesis and biological evaluation of N-cyclohexyl-4-[1-(2,4-dichlorophenyl)-1-(p-tolyl)methyl]piperazine-1-carboxamide as hCB1 receptor antagonists. |
Shanghai Institute of Materia Medica |
21880487 |
21 |
Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands. |
Northeastern University |
21875798 |
30 |
Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity. |
Rti International |
21835510 |
14 |
Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor. |
Universit£ |
21902175 |
24 |
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa). |
Universita` Del Piemonte Orientale |
21872477 |
43 |
Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives. |
The University of Texas |
21702498 |
34 |
Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice. |
Universita Degli Studi Di Siena |
21667972 |
5 |
Benzyl derivatives with in vitro binding affinity for human opioid and cannabinoid receptors from the fungus Eurotium repens. |
The University of Mississippi |
21737287 |
3 |
Synthesis, in vitro and in vivo evaluation of fluorine-18 labelled FE-GW405833 as a PET tracer for type 2 cannabinoid receptor imaging. |
Imir K.U. Leuven |
20615693 |
37 |
Tricyclic imidazole antagonists of the Neuropeptide S Receptor. |
Merck Research Laboratories |
21675776 |
22 |
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors. |
Universidad Complutense De Madrid |
21669533 |
26 |
Optimisation of a novel series of selective CNS penetrant CB(2) agonists. |
Pfizer |
20971001 |
45 |
Indazole derivatives as novel bradykinin B1 receptor antagonists. |
Merck Research Laboratories |
21420857 |
115 |
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia. |
Merck Research Laboratories |
21376588 |
4 |
Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity. |
Chiba University |
21354795 |
95 |
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability. |
Boehringer Ingelheim Pharmaceuticals |
21420860 |
34 |
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy. |
Merck Research Laboratories |
21183257 |
202 |
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2. |
Universit£ |
20979417 |
83 |
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series. |
Universite£? Lille-Nord De France |
21115245 |
69 |
Structure-activity relationships of 2,4-diphenyl-1H-imidazole analogs as CB2 receptor agonists for the treatment of chronic pain. |
Merck Research Laboratory |
20943290 |
54 |
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands. |
Sapienza University of Rome |
21074998 |
80 |
Synthesis, binding studies and molecular modeling of novel cannabinoid receptor ligands. |
German University In Cairo |
20845959 |
94 |
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor. |
Research Triangle Institute |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20719511 |
17 |
Identification and hit-to-lead optimization of a novel class of CB1 antagonists. |
Ligand Pharmaceuticals |
20688519 |
58 |
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists. |
Abbott Healthcare Products |
20667724 |
2 |
Discovery of cannabinoid-1 receptor antagonists by virtual screening. |
Korea Research Institute of Chemical Technology |
20643546 |
10 |
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant. |
Merck Research Laboratories |
20584609 |
13 |
Rational design of a novel peripherally-restricted, orally active CB(1) cannabinoid antagonist containing a 2,3-diarylpyrrole motif. |
Sanofi-Aventis R&D |
20483606 |
71 |
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation. |
Merck Research Laboratories |
20218623 |
68 |
Emerging targets in osteoporosis disease modification. |
Amgen |
20423086 |
93 |
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. |
Merck Research Laboratories |
20096577 |
42 |
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1. |
Merck Research Laboratories |
20137936 |
7 |
Radiosynthesis of novel carbon-11-labeled triaryl ligands for cannabinoid-type 2 receptor. |
National Institute of Radiological Sciences |
20047779 |
86 |
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach. |
Chinese Academy of Sciences |
19767206 |
9 |
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors. |
National Institute of Mental Health |
20045337 |
117 |
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand. |
Green Cross |
20022504 |
9 |
Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase. |
University of Salerno |
20189815 |
20 |
Synthesis and in vitro biological evaluation of carbon-11-labeled quinoline derivatives as new candidate PET radioligands for cannabinoid CB2 receptor imaging. |
Indiana University School of Medicine |
20079638 |
61 |
Synthesis and structure-activity relationship of substitutions at the C-1 position of Delta9-tetrahydrocannabinol. |
Amri |
20015647 |
64 |
Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood-brain-barrier. |
7Tm Pharma |
20005710 |
70 |
Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors. |
Merck Research Laboratories |
20005704 |
7 |
Novel thioamide derivatives as neutral CB1 receptor antagonists. |
Astrazeneca R & D M£Lndal |
19954978 |
55 |
Exploring SAR features in diverse library of 4-cyanomethyl-pyrazole-3-carboxamides suitable for further elaborations as CB1 antagonists. |
7Tm Pharma |
19919895 |
54 |
Novel sulfamoyl benzamides as selective CB(2) agonists with improved in vitro metabolic stability. |
Adolor |
20047331 |
30 |
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
Solvay Pharma |
19921781 |
220 |
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
Abbott Laboratories |
19743867 |
51 |
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain. |
Glaxosmithkline |
19736007 |
31 |
Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists. |
Adolor |
19683918 |
36 |
Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles. |
Pfizer |
19646869 |
54 |
Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists. |
Adolor |
19632830 |
47 |
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists. |
Merck Research Laboratories |
19699640 |
12 |
Synthesis and SAR of 1,4,5,6-tetrahydropyridazines as potent cannabinoid CB1 receptor antagonists. |
Solvay Pharma |
19500981 |
26 |
Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis. |
Pfizer |
19515560 |
24 |
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. |
Vernalis (R&D) |
19161308 |
4 |
Total synthesis of photoactivatable or fluorescent anandamide probes: novel bioactive compounds with angiogenic activity. |
University of Montpellier |
| 33 |
Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors |
TBA |
| 38 |
New class of potent ligands for the human peripheral cannabinoid receptor |
TBA |
19530697 |
59 |
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice. |
National Health Research Institutes |
19331413 |
54 |
New resorcinol-anandamide"hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo. |
Universita Degli Studi Di Siena |
19328684 |
67 |
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. |
Merck Research Laboratories |
19328683 |
22 |
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect. |
Zydus Research Centre |
19320488 |
171 |
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity. |
Merck Research Laboratories |
19250829 |
46 |
Quantitative structure-activity relationship (QSAR) for a series of novel cannabinoid derivatives using descriptors derived from semi-empirical quantum-chemical calculations. |
St. Jude Children'S Research Hospital |
19230659 |
12 |
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands. |
University of Tennessee-Memphis |
19095444 |
48 |
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists. |
National Central University |
19091565 |
101 |
CB2 selective sulfamoyl benzamides: optimization of the amide functionality. |
Adolor |
19062274 |
72 |
Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties. |
Amgen |
19053765 |
15 |
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide. |
Martin-Luther-Universitaet |
18977140 |
43 |
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs. |
Shionogi |
18831576 |
66 |
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism. |
Sapienza University of Rome |
18754613 |
23 |
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors. |
National Institute of Mental Health |
18712856 |
129 |
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists. |
National Health Research Institutes |
18640038 |
74 |
Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. |
Amgen |
18595717 |
2 |
Comparative molecular dynamics simulations of the potent synthetic classical cannabinoid ligand AMG3 in solution and at binding site of the CB1 and CB2 receptors. |
The National Hellenic Research Foundation |
18570365 |
29 |
The many roles for fluorine in medicinal chemistry. |
Merck Research Laboratories |
18524604 |
36 |
Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs. |
University of Tennessee-Memphis |
18522867 |
149 |
Novel benzimidazole derivatives as selective CB2 agonists. |
Astrazeneca R&D MontréAl |
18512901 |
27 |
Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations. |
Research Triangle Institute |
18511157 |
15 |
Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity. |
Johns Hopkins University School of Medicine |
18342403 |
13 |
Rational design, synthesis and biological evaluation of new 1,5-diarylpyrazole derivatives as CB1 receptor antagonists, structurally related to rimonabant. |
Università |
18243711 |
76 |
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands. |
Central Research Institute |
17582659 |
22 |
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. |
Monash University (Parkville Campus) |
11678659 |
1 |
Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum. |
University of Mississippi |
18255291 |
45 |
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity. |
Evotec (Uk) |
17979261 |
8 |
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model. |
Zydus Research Centre |
17884494 |
79 |
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
Astrazeneca R&D Montreal |
17827022 |
16 |
Novel, potent THC/anandamide (hybrid) analogs. |
Organix |
17643986 |
11 |
Sulfonamide derivatives as new potent and selective CB2 cannabinoid receptor agonists. |
Taisho Pharmaceutical |
17608398 |
14 |
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use. |
TBA |
17604171 |
20 |
Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs. |
Università |
17531479 |
65 |
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds. |
Shionogi |
17521907 |
50 |
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds. |
Shionogi |
17521177 |
90 |
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2. |
The National Hellenic Research Foundation |
17513109 |
32 |
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series. |
Pharmaceutical Research Institute |
17507224 |
82 |
Biaryl cannabinoid mimetics--synthesis and structure-activity relationship. |
Adolor |
17466519 |
39 |
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands. |
Schering-Plough Research Institute |
17383180 |
52 |
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity. |
Bayer Healthcare |
17293109 |
69 |
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists. |
Merck Research Laboratories |
17270441 |
72 |
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists. |
Merck Research Laboratories |
17110113 |
2 |
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand. |
Teikyo University |
17107792 |
38 |
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives. |
Bayer Healthcare |
17004712 |
18 |
Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction. |
University of North Carolina At Greensboro |
16682198 |
4 |
Synthesis of a potential photoactivatable anandamide analog. |
University of Montpellier |
16570929 |
29 |
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity. |
University of Piemonte Orientale |
16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College of Physicians and Surgeons |
16263284 |
36 |
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists. |
Merck Research Laboratories |
16263283 |
55 |
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists. |
Pfizer |
15801840 |
19 |
Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation. |
Université |
15713403 |
40 |
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists. |
Merck Research Laboratories |
15664857 |
24 |
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies. |
Schering-Plough Research Institute |
15664830 |
64 |
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists. |
Merck Research Laboratories |
14980654 |
26 |
Potent imidazole and triazole CB1 receptor antagonists related to SR141716. |
Neurocrine Biosciences |
14736243 |
49 |
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
Solvay Pharma |
14613317 |
14 |
An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
Forbes Norris Als/Mda Research Center |
14505654 |
14 |
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids. |
University of Tennessee-Memphis |
12166938 |
8 |
Conformational memories and the endocannabinoid binding site at the cannabinoid CB1 receptor. |
Kennesaw State University |
12161142 |
34 |
C-3 Amido-indole cannabinoid receptor modulators. |
Bristol-Myers Squibb |
11020293 |
42 |
Novel cannabinol probes for CB1 and CB2 cannabinoid receptors. |
Organix |
10633038 |
36 |
QSAR analysis of Delta(8)-THC analogues: relationship of side-chain conformation to cannabinoid receptor affinity and pharmacological potency. |
Research Triangle Institute |
9379452 |
8 |
Importance of the C-1 substituent in classical cannabinoids to CB2 receptor selectivity: synthesis and characterization of a series of O,2-propano-delta 8-tetrahydrocannabinol analogs. |
Kennesaw State University |
8831752 |
9 |
Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor. |
Clemson University |
29400965 |
83 |
Structure-Activity Relationships and Computational Investigations into the Development of Potent and Balanced Dual-Acting Butyrylcholinesterase Inhibitors and Human Cannabinoid Receptor 2 Ligands with Pro-Cognitive in Vivo Profiles. |
Julius Maximilian University of W£Rzburg |
29298069 |
206 |
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. |
Pfizer |
29111736 |
92 |
Structure-Affinity Relationships and Structure-Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists. |
Leiden University |
27305312 |
4 |
Capture-Tag-Release: A Strategy for Small Molecule Labeling of Native Enzymes. |
Fairfield University |
27113261 |
12 |
2-Prenylated m-dimethoxybenzenes as potent inhibitors of 15-lipo-oxygenase: inhibitory mechanism and SAR studies. |
Ferdowsi University of Mashhad |
27376460 |
5 |
Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives. |
Nirma University |
26808391 |
6 |
A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition. |
Jawaharlal Nehru Centre For Advanced Scientific Research |
26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
26575582 |
15 |
Development of 2-(Substituted Benzylamino)-4-Methyl-1, 3-Thiazole-5-Carboxylic Acid Derivatives as Xanthine Oxidase Inhibitors and Free Radical Scavengers. |
Jamia Hamdard |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
12235229 |
26 |
Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. |
University of Arkansas |
20827790 |
21 |
A novel competitive class of α-glucosidase inhibitors: (E)-1-phenyl-3-(4-styrylphenyl)urea derivatives. |
Gyeongsang National University |
8730737 |
23 |
Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety. |
Smithkline Beecham Pharmaceuticals |
8667026 |
14 |
The C-terminal domain of the mGluR1 metabotropic glutamate receptor affects sensitivity to agonists. |
Cns Research |
8022403 |
113 |
A binding site model and structure-activity relationships for the rat A3 adenosine receptor. |
National Institute of Diabetes, Digestive and Kidney Diseases |
19385613 |
60 |
Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties. |
Novo Nordisk |
17467988 |
21 |
Novel glucocorticoids containing a 6,5-bicyclic core fused to a pyrazole ring: synthesis, in vitro profile, molecular modeling studies, and in vivo experiments. |
Merck Research Laboratories |
17125251 |
20 |
A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region. |
University of Prince Edward Island |
17201405 |
9 |
Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. |
Glaxosmithkline |
8894098 |
20 |
Discovery and optimization of nonpeptide HIV-1 protease inhibitors. |
Parke-Davis Pharmaceutical Research |
17393456 |
4 |
Identification of novel fragment compounds targeted against the pY pocket of v-Src SH2 by computational and NMR screening and thermodynamic evaluation. |
University College London |
8164260 |
23 |
The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors. |
Merck Research Laboratories |
2200122 |
1 |
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease. |
Abbott Laboratories |