| Assay ID | Title | Year | Journal | Article |
|---|
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 1995 | Molecular pharmacology, Aug, Volume: 48, Issue:2
| Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase. |
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 1993 | Nature, Sep-02, Volume: 365, Issue:6441
| Molecular characterization of a peripheral receptor for cannabinoids. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 1998 | Journal of neurochemistry, Jan, Volume: 70, Issue:1
| Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 1996 | Molecular pharmacology, May, Volume: 49, Issue:5
| A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2. |
| AID493017 | Wombat Data for BeliefDocking | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. |
| AID1798067 | Radioligand Binding Assay from Article 10.1021/jm7011613: \\Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.\\ | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID1800327 | CB1 & 2 Binding Assays from Article 10.1021/cb500177c: \\Functionalization of u00DF-Caryophyllene Generates Novel Polypharmacology in the Endocannabinoid System.\\ | 2014 | ACS chemical biology, Jul-18, Volume: 9, Issue:7
| Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID751688 | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| AID227372 | Effect on cannabinoid tetrad (nociception, temperature, spontaneous motility and catalepsy) of behavioral test; inhibit spontaneous motility | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. |
| AID1360055 | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cell membranes after 90 mins | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system. |
| AID1601890 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 8.1 x 10'-6 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID457719 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase. |
| AID309951 | Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated contraction | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID1601889 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 2.7 x 10'-6 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID550006 | Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO cells after 1 hr | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series. |
| AID620186 | Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as maximum solubility | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID324970 | Selectivity for human recombinant CB2 receptor over human recombinant CB1 receptor | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID304980 | Agonist activity at human recombinant CB1 receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID308131 | Displacement of [3H]CP-55940 from human CB2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID444914 | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID537911 | Antinociceptive effect in iv dosed mouse assessed as increase in tail-flick latency period by tail flick test | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists. |
| AID457720 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase. |
| AID289136 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors. |
| AID1573472 | Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
| AID1202982 | Agonist activity at human CB2 receptor after 1 hr by [35S]-GTPgammaS binding assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis. |
| AID1601887 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 3 x 10'-7 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID308133 | Displacement of [3H]CP-55940 from mouse CB2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID304998 | Induction of hypotonia NMRI mouse at 0.3 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID304357 | Displacement of [3H]CP-55940 from CB2 receptor in mouse spleen membranes | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. |
| AID633466 | Displacement of [3H]CP55940 from human CB1 receptor expressed in human HEK293 cells | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor. |
| AID304359 | Agonist activity at CB2 receptor in mouse spleen membranes at 1 uM after 2 hrs by [35S]GTP-gamma-S binding assay | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. |
| AID1638015 | Displacement of [3H]-CP-55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID302384 | Activity at human CB2 receptor expressed in CHO cells assessed as stimulated [35S]GTP-gamma-S binding relative to control | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| 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. |
| AID620185 | Kinetic solubility of the compound in 0.01 M phosphate buffered saline at pH 7.4 assessed as minimum solubility | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID656261 | Intrinsic clearance in human liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID550009 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series. |
| AID1054642 | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthetic cannabinoid quinones: preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity. |
| AID1188346 | Inhibition of CB2 receptor in HL60 cells assessed as inhibition of ERK1/2 phosphorylation after 15 mins by Western blotting analysis | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Tricyclic pyrazoles part 7. Discovery of potent and selective dihydrothienocyclopentapyrazole derived CB2 ligands. |
| AID1657314 | Inhibition of carrageenan-induced paw edema in Swiss mouse at 1.5 mg/kg, ip pretreated for 30 mins followed by carrageenan-stimulation and measured after 6 hrs | | | |
| AID474948 | Antagonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID259201 | Effect on [35S]GTP-gamma-S binding to human CB2 receptor | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling. |
| AID444920 | Agonist activity at rat CB2 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID738106 | Binding affinity to CB1 receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| 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. |
| AID238759 | Binding affinity to displace [3H]CP-55940 from cloned human CB2 receptor | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| 1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles. |
| AID282919 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in COS cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. |
| AID49689 | Compound was evaluated for its binding affinity against Cannabinoid receptor 2 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
| The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes. |
| AID254405 | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [131I]-(R)-8 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor. |
| AID1185844 | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cell membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
| Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist. |
| AID243030 | Ratio of the binding affinity towards CB1 receptor to that of CB2 receptor | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| 1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles. |
| AID362458 | Binding affinity to CB2 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists. |
| AID1333348 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID406791 | Displacement of [3H]CP-55940 from human CB1 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
| Novel benzimidazole derivatives as selective CB2 agonists. |
| AID662937 | Thermodynamic solubility of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID80452 | Compound was evaluated for maximum inhibition of electrically evoked contractions of the myenteric plexus-longitudinal muscle of the Guinea pig small intestine | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
| The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes. |
| AID579498 | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in insect Sf9 cells | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. |
| AID1847541 | Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by radioligand binding assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis. |
| AID781178 | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cells after 1.5 hrs by microbeta liquid scintillation counting analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Mastering tricyclic ring systems for desirable functional cannabinoid activity. |
| AID296816 | Agonist activity at human CB2 receptor expressed in CHOK1 cells assessed as reversal of forskolin-evoked cAMP accumulation | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID383281 | Displacement of [3H]WIN-55212-2 from CB2 receptor in Sprague-Dawley rat spleen membrane | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. |
| AID617995 | Displacement of [3H]-CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cells membrane incubated for 90 mins | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9
| Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa). |
| AID49160 | Compound was evaluated for its binding affinity against Cannabinoid receptor 1 in Guinea pig ileum (GPI) using [3H]CP-55940 ligand | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
| The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes. |
| AID417014 | Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. |
| AID259200 | Effect on human CB2 receptor stimulation by [35S]GTP-gamma-S binding at 10 uM (basal value set at 100%) | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling. |
| AID415514 | Selectivity index, ratio of Ki for human CB2 receptor to Ki for human CB1 receptor expressed in african green monkey COS cells | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo. |
| AID1657324 | Psychoactive effect in Swiss mouse assessed as antinociceptive effect by measuring paw withdrawal latencies at 1.5 mg/kg, ip and measured for 6 hrs | | | |
| AID636835 | Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10
| Cannabinomimetic lipid from a marine cyanobacterium. |
| AID282923 | Activity at CB1 receptor in mouse N18TG2 cells assessed as inhibition of forskolin-induced cyclic AMP formation | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. |
| AID1333349 | Cytotoxicity against human H1975-1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID309956 | Induction of catalepsy in ICR mouse at 1.5 mg/kg, ip by ring test | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID296812 | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID1590130 | Inhibition of IL1aplha-induced PGE2 production in bovine articular chondrocytes at 5 uM incubated for 48 hrs by ELISA relative to control | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Eicosanoid mediation of cannabinoid actions. |
| AID195418 | Concentration required for stimulation of [35S]GTP-gamma-S, binding in rat microsomal membranes expressed as Emax | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
| Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability. |
| AID502210 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists. |
| AID1601888 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 9 x 10'-7 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID714717 | Hypothermic activity in iv dosed Harlan ICR mouse assessed as change in rectal temperature at 30 mins | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID1352391 | Displacement of [3H]-CP-55940 from human CB2 expressed in CHO cells after 90 mins by TopCount scintillation counting method | | | |
| AID656296 | Analgesic activity in sc dosed rat Chung von Frey model of neuropathic pain assessed as anti-allodynic effect against mechanical stimulus | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID699049 | Displacement of [3H]CP-55940 from CB2 receptor in Sprague-Dawley rat spleen by scintillation counting | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID1237885 | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis | 2015 | Journal of natural products, Jul-24, Volume: 78, Issue:7
| Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria. |
| AID362459 | Binding affinity to CB1 receptor | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists. |
| AID49300 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.36 (201)A mutant Cannabinoid receptor 1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID620182 | Lipophilicity, log D of the compound at pH 7.4 | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID1185845 | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in HEK293 cell membranes | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
| Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist. |
| AID49298 | Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes | 1999 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 9, Issue:15
| 3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands. |
| AID1068376 | Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. |
| AID1626208 | Agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis. |
| AID656260 | Intrinsic clearance in rat liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID309953 | Antinociceptive activity in ICR mouse at 1.5 mg/kg, ip by hot plate test | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID444921 | Agonist activity at rat CB2 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay relative to CP-55940 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID227370 | Effect on cannabinoid tetrad (nociception, temperature, spontaneous motility and catalepsy) of behavioral test; induce catalepsy | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. |
| AID49304 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with wild type Cannabinoid receptor 1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID324971 | Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID714689 | Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID49299 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with F3.25 (190)A mutant Cannabinoid receptor 1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID724449 | Inhibition of transient lower esophageal sphincter relaxations in dog at 0.06 umol/kg, iv measured after 30 mins | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID620179 | Selectivity ratio of Ki for human CB2 receptor to Ki for human CB1 receptor | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID1068378 | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK-293EBNA cells after 90 mins by luminescence counting analysis | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. |
| AID49835 | Binding affinity against human Cannabinoid receptor 2 expressed in CHO cells by using WIN-55212-2 Mesylate [573H] as Radioactive tracer | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| C-3 Amido-indole cannabinoid receptor modulators. |
| AID114593 | Inhibition of LPS-induced nuclear factor-kappa B (NFkB) activation and TNF production in mouse | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| C-3 Amido-indole cannabinoid receptor modulators. |
| AID1054643 | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, , Volume: 70 | Synthetic cannabinoid quinones: preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity. |
| AID49676 | Displacement of [3H]CP-55940 from Cannabinoid receptor 1 of rat forebrain membranes | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Three-dimensional quantitative structure-activity relationship study of the cannabimimetic (aminoalkyl)indoles using comparative molecular field analysis. |
| AID283042 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells at 10 uM | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| 1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists. |
| AID383283 | Agonist activity at CB1 receptor | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. |
| AID724452 | Agonist activity at dog CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID383278 | Agonist activity at CB1 receptor in electrically-stimulated Swiss mouse vas deferens | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. |
| AID502213 | Selectivity ratio of Ki for human recombinant CB1 receptor to Ki for human recombinant CB2 receptor | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists. |
| AID1186021 | Partial agonist activity at human cannabinoid CB2 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. |
| AID444909 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID1285174 | Inverse agonist activity at human CB2 receptor transfected in CHO cells assessed as increase in forksolin stimulated cAMP production by scintillation counting analysis | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID550007 | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells after 1 hr | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series. |
| AID724451 | Inhibition of transient lower esophageal sphincter relaxations in dog at 0.006 umol/kg, iv measured after 30 mins | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID1601884 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 8.1 x 10'-6 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID1404281 | Effect on forskolin-stimulated cAMP level in HEK293 cells at 1 uM by BRET assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment. |
| AID1601875 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 3 x 10'-7 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID289135 | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors. |
| AID769550 | Binding affinity to CB1 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Contributions of academic laboratories to the discovery and development of chemical biology tools. |
| AID1638019 | Agonist activity at human CB2 receptor expressed in CHO cell membranes assessed as [35S]GTPgammaS binding after 1 hr by beta-counting analysis | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID227371 | Effect on cannabinoid tetrad (nociception, temperature, spontaneous motility and catalepsy) of behavioral test; induce hypothermia | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. |
| AID444911 | Selectivity ratio of Ki for human recombinant CB1 receptor to Ki for human recombinant CB2 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID415512 | Binding affinity to human recombinant CB1 receptor expressed in african green monkey COS cells by radioligand binding assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo. |
| AID769549 | Selectivity ratio of Ki for CB1 receptor (unknown origin) to Ki for CB2 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Contributions of academic laboratories to the discovery and development of chemical biology tools. |
| AID1706232 | Displacement of [3H]CP55940 from recombinant human CB2R expressed in CHO cell membranes incubated for 90 mins | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. |
| AID764558 | Displacement of [3H]-CP55,940 from human CB2 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis. |
| AID699048 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID296815 | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation relative to CP-55940 | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID620189 | Ratio of permeability from apical to basolateral over basolateral to apical side in human Caco2 cells by LC-MS/MS analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID1601883 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 2.7 x 10'-6 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID656264 | Solubility of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID472421 | Antagonist activity at human recombinant alpha 2 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID259614 | Displacement of [3H]SR141716A from human CB1 receptor | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| 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. |
| AID1237887 | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by scintillation counting analysis | 2015 | Journal of natural products, Jul-24, Volume: 78, Issue:7
| Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria. |
| AID296814 | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID656265 | Oral bioavailability in rat | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID662958 | Ratio of drug level in brain to plasma in rat by microdialysis assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID714707 | Antinociceptive activity in iv dosed Harlan ICR mouse assessed as latency to heat-induced tail flicking at 20 mins | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID310006 | Binding affinity to human CB1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
| AID1601881 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 3 x 10'-7 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID636834 | Displacement of [3H]CP55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10
| Cannabinomimetic lipid from a marine cyanobacterium. |
| AID1416642 | Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB1 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB |
| AID537910 | Displacement of [3H]-CP55940 from human CB2 expressed in insect Sf9 membranes | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists. |
| AID273076 | Agonist activity against rat CB1 receptor expressed in superior cervical ganglion neurons assessed as increase in calcium ion current at 1 uM relative to control | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction. |
| AID282918 | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors. |
| AID324968 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID1244365 | Displacement of [3H]-CP55940 from human CB2 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists. |
| AID1657326 | Psychoactive effect in Swiss mouse assessed as hypothermic effects at 1.5 mg/kg, ip and measured for 6 hrs by thermometric method | | | |
| AID49138 | Inhibition of 0.5 nM [3H](Aminoalkyl)indole binding to cannabinoid receptor in rat cerebellum membranes at 1 uM | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID620187 | Dissociation constant, pKa of the compound by fast UV-metric method | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID736461 | Agonist activity at CB1 receptor in mouse N1E-115 cells assessed as increase in ERK1/2 phosphorylation at 25 nM after 10 mins by Western blot analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Novel pyrazole derivatives as neutral CB₁ antagonists with significant activity towards food intake. |
| AID1202981 | Displacement of [3H]-CP55940 from human CB1 receptor after 1 hr by scintillation counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis. |
| AID324969 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID1127517 | Binding affinity to CB2 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. |
| AID1601882 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 9 x 10'-7 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID444917 | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production relative to CP-55940 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID693537 | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO cell membranes after 1 hr by scintillation counting | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands. |
| AID1286535 | Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology. |
| AID472422 | Antagonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx up to 30 uM by whole cell patch clamp assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. |
| AID693539 | Agonist activity at human CB2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands. |
| AID1057093 | Displacement of [3H]CP-55,940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Development of fluorinated CB(2) receptor agonists for PET studies. |
| AID406792 | Agonist activity at cloned human CB2 receptor in Sf9 cells assessed as stimulation of [35S]GTPgammaS binding assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
| Novel benzimidazole derivatives as selective CB2 agonists. |
| AID1657325 | Psychoactive effect in Swiss mouse assessed as catalepsy effect at 1.5 mg/kg, ip and measured for 6 hrs | | | |
| AID310545 | Selectivity for human CB2 over human CB1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. |
| AID310010 | Agonist activity at human CB2 receptor by GTPgamma[35S] assay relative to WIN-55212-2 | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
| AID1285169 | Displacement of [3H]CP-55,940 from human CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID620180 | Agonist activity at human CB1 receptor expressed in CHO cells assessed as stimulation of [3H]-arachidonic acid release | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID693536 | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by scintillation counting | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands. |
| AID1573471 | Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
| AID132804 | in vivo antinociceptive effect was tested in the mouse acetylcholine writhing assay after iv administration | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID49301 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W5 43(280)A mutant Cannabinoid receptor 1 at 5 uM | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID656266 | Ratio of drug level in brain to plasma in mouse | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID283040 | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells at 10 uM | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| 1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists. |
| AID304983 | Agonist activity at CB1 receptor assessed as inhibition of electrically-induced twitch contraction amplitude in mouse vas deferens | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID1706231 | Displacement of [3H]CP55940 from recombinant human CB1R expressed in CHO cell membranes incubated for 90 mins | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. |
| AID620177 | Displacement of [3H]-CP55940 from human CB2 receptor expressed in CHO cells by liquid scintillation counting | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID1155627 | Intrinsic activity at CB1 receptor in mouse N1E115 cells assessed as upregulation of phosphorylated ERK1/2 expression at 25 nM after 10 mins by Western blotting analysis | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands. |
| AID633468 | Selectivity index, ratio of Ki for human CB2 receptor to Ki for human CB1 receptor | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor. |
| AID1333346 | Cytotoxicity against resistant human HCT116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID309959 | Prevention of spontaneous activity reduction in ICR mouse at 1 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID1601879 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 1.82 x 10'-5 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID724453 | Ratio of drug level in brain to plasma in Sprague-Dawley rat | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID304987 | Reduction of nociception in ip dosed NMRI mouse during late phase (10 to 30 mins) | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID1546673 | Displacement of [3H]WIN 55212-2 from human CB2 receptor incubated for 120 mins by scintillation counting method | 2020 | Journal of natural products, 01-24, Volume: 83, Issue:1
| Isolation of a High-Affinity Cannabinoid for the Human CB1 Receptor from a Medicinal |
| AID1186020 | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. |
| AID444910 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID304997 | Induction of hypokinesia NMRI mouse at 0.3 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID49326 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W4 64(256)A mutant Cannabinoid receptor 1; Not determined | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID1626197 | Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis. |
| AID227369 | Effect on cannabinoid tetrad (nociception, temperature, spontaneous motility and catalepsy) of behavioral test; induce antinociception | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
| Discovery of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. |
| AID231507 | Ratio of binding affinity of the CB1 receptor to that of CB2 receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| C-3 Amido-indole cannabinoid receptor modulators. |
| AID704204 | Agonist activity at human recombinant CB2 receptor expressed in CHO cells membrane by [35S]-GTPgammaS assay relative to control | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| 4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. |
| AID781179 | Displacement of [3H]-CP55940 from CB1 receptor in rat brain homogenate after 1.5 hrs by microbeta liquid scintillation counting analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Mastering tricyclic ring systems for desirable functional cannabinoid activity. |
| AID272972 | Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain relative to control | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| 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. |
| AID304981 | Reversal of agonist activity at CB1 receptor expressed in CHO cells by a [35S]GTP-gamma-S binding assay assessed in presence of 0.1 uM AM251 CB1 antagonist | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID662936 | Inhibition of human ERG | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID49302 | Ability to displace [3H]CP-55940 from the membranes prepared from HEK cell line with W6 48(357)A mutant Cannabinoid receptor 1 | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
| An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region. |
| AID1601880 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 10'-7 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID258588 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1
| New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies. |
| AID444916 | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID1573470 | Agonist activity at CB1 receptor (unknown origin) assessed as increase in cAMP accumulation after 1 hr by FLIPR assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
| AID1601877 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 2.7 x 10'-6 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID49851 | Binding affinity towards cloned human cannabinoid receptor 2 | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
| A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors. |
| AID195417 | Effective concentration required for stimulation of [35S]GTP-gamma-S, binding in rat microsomal membranes | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
| Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability. |
| AID662935 | Intrinsic clearance in human liver microsomes at 1 uM in presence of NADPH | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID296813 | Displacement of [3H]CP-55940 human CB2 receptor expressed in CHOK1 cells | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID340066 | Antagonist activity at human CB1 receptor assessed as forskolin-stimulated cAMP accumulation per ug of protein at 100 uM | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist. |
| AID740008 | Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins relative to WIN55,212-2 | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Novel adamantyl cannabinoids as CB1 receptor probes. |
| AID620184 | Thermodynamic solubility of the compound in phosphate buffer at pH 4 after 24 hrs by HPLC analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID656301 | Ratio of MED for toxicity in sc dosed rat assessed as catalepsy to ED50 for anti-allodynic activity in sc dosed rat Chung von Frey model of neuropathic pain | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID1416639 | Displacement of [3H]CP55940 from beta-galactosidase reporter fused human CB2 receptor expressed in CHOK1 cell membranes after 1 hr by scintillation spectrometric analysis | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB |
| AID1155628 | Intrinsic activity at CB1 receptor in mouse N1E115 cells assessed as upregulation of phosphorylated ERK1/2 expression at 5 to 250 nM after 10 mins by Western blotting analysis | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands. |
| AID1186023 | Partial agonist activity at human cannabinoid CB1 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. |
| AID722932 | Displacement of [3H]CP-55,940 from Sprague-Dawley rat brain CB1 receptor by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID1638016 | Displacement of [3H]-CP-55940 from human CB1 receptor expressed in CHO cell membranes after 1 hr by beta-counting analysis | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID321305 | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation per ug of protein at 1 uM | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole. |
| AID1286534 | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells after 90 mins by liquid scintillation spectrophotometer | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology. |
| AID1638017 | Selectivity index, ratio of Ki for human CB1 receptor expressed in CHO cell membranes to Ki for human CB2 receptor expressed in CHO cell membranes | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID417013 | Binding affinity to human cannabinoid CB1 receptor | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. |
| AID1285172 | Inverse agonist activity at human CB2 receptor transfected in CHO cells assessed as increase in forksolin stimulated cAMP production at 10 uM by scintillation counting analysis relative to control | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID1360054 | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cell membranes after 90 mins | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system. |
| AID358257 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10
| Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum. |
| AID617994 | Displacement of [3H]-CP-55,940 from human recombinant CB1 receptor expressed in HEK293 cells membrane incubated for 90 mins | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9
| Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa). |
| AID304986 | Reversal of the agonistic activity at CB1 receptor in mouse vas deferens model of electrically induced twitch contraction assessed in presence of 10 uM JTE907 CB2 antagonist | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID722653 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as forskolin-stimulated [3H]cyclic-AMP accumulation by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID620181 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as increase of forskolin-stimulated cAMP accumulation after 20 mins | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID714692 | Binding affinity to human CB2 receptor by filtration assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID1286536 | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cells at 40 uM after 90 mins by liquid scintillation spectrophotometer | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology. |
| AID764553 | Agonist activity at human CB2 receptor expressed in CHO membranes assessed as [35S]-GTPgammaS binding after 1 hr | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis. |
| AID273078 | Binding affinity to human CB1 receptor | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction. |
| AID304999 | Reversal of the agonistic activity at CB1 receptor in mouse vas deferens model of electrically induced twitch contraction assessed in presence of AM251 CB1 antagonist | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID406793 | Agonist activity at cloned human CB2 receptor in Sf9 cells assessed by [35S]GTPgammaS binding assay relative to delta9-THC | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
| Novel benzimidazole derivatives as selective CB2 agonists. |
| AID1626194 | Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis. |
| AID738107 | Binding affinity to CB2 receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| 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. |
| AID1068367 | Agonist activity at CB1 receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractile response at 10'-7 to 2 X 10'-5 M after 10 mins | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease. |
| AID308135 | Agonist activity at human CB2 in CHO cells assessed as inhibition of cAMP production | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID310008 | Selectivity for human CB2 receptor over human CB1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
| AID1285173 | Inverse agonist activity at human CB2 receptor transfected in CHO cells assessed as increase in forksolin stimulated cAMP production at 1 uM by scintillation counting analysis relative to control | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID769551 | Binding affinity to CB2 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
| Contributions of academic laboratories to the discovery and development of chemical biology tools. |
| AID321304 | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation per ug of protein at 100 uM | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole. |
| AID764552 | Agonist activity at human CB2 receptor expressed in CHO membranes assessed as [35S]-GTPgammaS binding after 1 hr relative to basal constitutive activity | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis. |
| AID722929 | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID656299 | Toxicity in sc dosed rat assessed as catalepsy by ring immobility test | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain. |
| AID415513 | Binding affinity to human recombinant CB2 receptor expressed in african green monkey COS cells by radioligand binding assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo. |
| AID238321 | Binding affinity for cannabinoid receptor 2 | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. |
| AID537909 | Displacement of [3H]-CP55940 from human CB1 expressed in insect Sf9 membranes | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists. |
| AID1156303 | Analgesic activity in Sprague-Dawley rat complete Freund's adjuvant-induced inflammatory pain model assessed as reversal of mechanical allodynia at 2 mg/kg/day, ip measured up to 5 days | 2014 | ACS medicinal chemistry letters, Jun-12, Volume: 5, Issue:6
| Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain. |
| AID309955 | Inhibition of spontaneous motility in ICR mouse at 1.5 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID1657323 | Psychoactive effect in Swiss mouse assessed as reduction in locomotor activity by measuring change in distance travelled at 1.5 mg/kg, ip and measured for 6 hrs | | | |
| AID1352389 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition for 30 mins measured after 1 hr by HTRF assay (Rvb = 100%) | | | |
| AID49503 | Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26
| Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors. |
| AID699045 | Agonist activity at human recombinant CB2 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-induced cAMP accumulation | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID633467 | Displacement of [3H]CP55940 from human CB2 receptor expressed in human HEK293 cells | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor. |
| AID1601878 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 8.1 x 10'-6 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID308139 | AUC in rat at 30 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID444919 | Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay relative to CP-55940 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID662931 | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID620183 | Thermodynamic solubility of the compound in phosphate buffer at pH 7.4 after 24 hrs by HPLC analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID704199 | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in CHO cells membrane by scintillation counting | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| 4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. |
| AID380500 | Displacement of [3H]WIN-55212-2 from human CB1 receptor in HEK293 cells | 2006 | Journal of natural products, Mar, Volume: 69, Issue:3
| 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. |
| AID296820 | Antihyperalgesic activity in rat assessed as reversal of hyperalgesia | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID1333345 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID704200 | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in CHO cells membrane by scintillation counting | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| 4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. |
| AID714948 | Induction of catalepsy in iv dosed Harlan ICR mouse at 90 mins measured for 5 mins by ring immobility test | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID620188 | Apparent permeability from apical to basolateral side in human Caco2 cells by LC-MS/MS analysis | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID502212 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists. |
| AID304985 | Reversal of the agonistic activity at CB1 receptor in mouse vas deferens model of electrically induced twitch contraction assessed in presence of SR-141716A CB1 antagonist | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID49001 | Concentration required to displace 50% of 0.5 nM [3H](aminoalkyl)indole binding to cannabinoid receptor in rat cerebellum membranes | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID1601885 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 1.82 x 10'-5 M after 10 mins in presence of CB1 antagonist AM251 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID444913 | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay relative to CP-55940 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID49306 | Binding affinity against human Cannabinoid receptor 1 expressed in CHO cells by using CP-55940 as Radioactive tracer | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| C-3 Amido-indole cannabinoid receptor modulators. |
| AID722930 | Displacement of [3H]CP-55,940 from Sprague-Dawley rat spleen CB2 receptor by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID310009 | Agonist activity at human CB2 receptor by GTPgamma[35S] assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
| AID1372614 | Displacement of [3H]CP,55-940 from recombinant human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method | | | |
| AID1724600 | Displacement of [3H]CP55940 from human CB2R transfected in HEK293EBNA cell membrane incubated for 90 mins by Microbeta TriLux based luminescence analysis | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
| New cannabinoid receptor antagonists as pharmacological tool. |
| AID740007 | Agonist activity at human CB1 receptor transfected in human U2OS cells assessed as beta-arrestin2-GFP aggregation after 40 mins | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Novel adamantyl cannabinoids as CB1 receptor probes. |
| AID1601886 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 10'-7 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID566247 | Inhibition of human cannabinoid CB1 receptor | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
| 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: de |
| AID1573473 | Agonist activity at CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment after 20 mins by BRET-based luciferase reporter gene assay relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
| AID1601891 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 1.82 x 10'-5 M after 10 mins in presence of CB2 antagonist AM630 relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID1601876 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 9 x 10'-7 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID1071862 | Agonist activity at human CB2 receptor by [35S]-GTPgammaS binding assay relative to control | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Switching cannabinoid response from CB(2) agonists to FAAH inhibitors. |
| AID569314 | Selectivity ratio of Ki for human CB1 to Ki for human CB2 | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
| Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2. |
| AID254415 | Binding affinity towards mouse hippocampal membranes cannabinoid receptor 1 using [3H]SR-141,716A | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor. |
| AID309954 | Induction of hypothermic effect in ICR mouse at 1.5 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity. |
| AID662938 | Apparent permeability from apical to basal side of human Caco2 cells at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID739283 | Displacement of [3H]-CP55940 from human CB2 receptor after 90 mins by liquid scintillation spectrophotometer analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21. |
| AID444912 | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID1285170 | Displacement of [3H]CP-55,940 from human CB2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting analysis | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID722931 | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID662932 | Binding affinity to human CB2 receptor | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID130354 | In vivo antinociceptive effect was tested in the mouse acetylcholine writhing assay after po administration | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID1244364 | Displacement of [3H]-CP55940 from human CB1 receptor transfected in HEK293EBNA cell membranes after 90 mins by liquid scintillation counting analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists. |
| AID238849 | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
| Substituted 5,5'-diphenyl-2-thioxoimidazolidin-4-one as CB1 cannabinoid receptor ligands: synthesis and pharmacological evaluation. |
| AID444915 | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production relative to CP-55940 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID1155620 | Intrinsic activity at CB2 receptor in human HL60 cells assessed as upregulation of phosphorylated ERK1/2 expression at 75 nM after 15 mins by Western blotting analysis relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands. |
| AID1286537 | Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cells at 40 uM after 90 mins by liquid scintillation spectrophotometer | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology. |
| AID310007 | Binding affinity to human CB2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
| New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists. |
| AID1626195 | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
| Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis. |
| AID308134 | Displacement of [3H]CP-55940 from mouse CB1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID238320 | Binding affinity for cannabinoid receptor 1 | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications. |
| AID49839 | Binding affinity of compound was determined against to human cannabinoid receptor 2 in chinese hamster ovary cells | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties. |
| AID195419 | Effective concentration required for stimulation of [35S]GTP-gamma-S, binding in rat microsomal membranes expressed as log EC50 | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
| Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability. |
| AID1431662 | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method | | | |
| AID308132 | Displacement of [3H]CP-55940 from human CB1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID699047 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cell membranes incubated for 90 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID417016 | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists. |
| AID722928 | Selectivity index, ratio of Ki for human recombinant CB1 receptor to Ki for human recombinant CB2 receptor | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists. |
| AID406790 | Displacement of [3H]CP-55940 from human CB2 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13
| Novel benzimidazole derivatives as selective CB2 agonists. |
| AID383280 | Displacement of [3H]SR141716A from CB1 receptor in Sprague-Dawley rat cerebellum membrane | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
| Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor. |
| AID1202980 | Displacement of [3H]-CP55940 from human CB2 receptor after 1 hr by scintillation counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis. |
| AID579497 | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in insect Sf9 cells | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. |
| AID724457 | Lipophilicity, log D of the compound | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID259197 | Displacement of [3H]CP-55940 from human CB2 receptor | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling. |
| AID283041 | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| 1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists. |
| AID1127518 | Binding affinity to CB1 receptor (unknown origin) | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. |
| AID80451 | Compound was evaluated for inhibition of electrically evoked contractions of the myenteric plexus-longitudinal muscle of the Guinea pig small intestine | 1998 | Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
| The bioactive conformation of aminoalkylindoles at the cannabinoid CB1 and CB2 receptors: insights gained from (E)- and (Z)-naphthylidene indenes. |
| AID1601874 | Agonist activity at cannabinoid receptor in ICR mouse vas deferens assessed as inhibition of electrically induced contractions at 10'-7 M after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Indazolylketones as new multitarget cannabinoid drugs. |
| AID569312 | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
| Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2. |
| AID304978 | Binding affinity to human recombinant CB1 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
| Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. |
| AID764557 | Displacement of [3H]-SR141716A from human CB1 receptor expressed in CHO membranes after 1 hr by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| 3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis. |
| AID238758 | Binding affinity to displace [3H]CP-55940 from CB1 receptor of rat brain | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
| 1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles. |
| AID1724599 | Displacement of [3H]CP55940 from human CB1R transfected in HEK293EBNA cell membranes incubated for 90 mins by Microbeta TriLux based luminescence analysis | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
| New cannabinoid receptor antagonists as pharmacological tool. |
| AID579493 | Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
| Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. |
| AID392487 | Agonist activity at human cloned CB2 receptor assessed as stimulation of [35S]GTPgammaS binding at 10 uM relative to basal [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
| CB2 selective sulfamoyl benzamides: optimization of the amide functionality. |
| AID310543 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. |
| AID132669 | In vitro inhibition of electrically stimulated contractions of isolated mouse vas deferens. | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID724450 | Inhibition of transient lower esophageal sphincter relaxations in dog at 0.019 umol/kg, iv measured after 30 mins | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID1404280 | Effect on forskolin-stimulated cAMP level in HEK293 cells at 10 uM by BRET assay relative to control | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment. |
| AID1186019 | Displacement of [3H]CP55940 from human cannabinoid CB1 receptor expressed in CHO-K1 cells by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors. |
| AID49308 | Binding affinity of compound was determined against to human cannabinoid receptor 1 in chinese hamster ovary cells | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties. |
| AID1071863 | Binding affinity to human CB1 receptor | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Switching cannabinoid response from CB(2) agonists to FAAH inhibitors. |
| AID1431663 | Displacement of [3H]CP55940 from human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation and luminescence counting method | | | |
| AID258587 | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1
| New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies. |
| AID699046 | Selectivity ratio of Ki for human recombinant CB1 receptor to KI for human recombinant CB2 receptor | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID272971 | Activity at CB1 receptor assessed as stimulation of [35S]GTP-gamma-S binding in DBA/J2 mouse brain | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| 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. |
| AID296817 | Agonist activity at human CB2 receptor expressed in CHOK1 cells assessed as reversal of forskolin-evoked cAMP accumulation relative to CP-55940 | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16
| 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. |
| AID704203 | Agonist activity at human recombinant CB2 receptor expressed in CHO cells membrane by [35S]-GTPgammaS assay | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| 4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. |
| AID739282 | Displacement of [3H]-CP55940 from human CB1 receptor after 90 mins by liquid scintillation spectrophotometer analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21. |
| AID660303 | Displacement of [3H]-CP55940 from CB1 receptor after 90 mins by liquid scintillation counting | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Discovery of Potent Dual PPARα Agonists/CB1 Ligands. |
| AID1573535 | Ratio of EC50 for CB1 receptor (unknown origin) assessed as increase in cAMP accumulation to EC50 for CB1 receptor (unknown origin) assessed as increase in beta-arrestin2 recruitment | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
| AID714691 | Binding affinity to human CB1 receptor by filtration assay | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID444918 | Agonist activity at rat CB1 receptor assessed as inhibition of forskolin-induced cAMP production by cell based assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity. |
| AID1638020 | Agonist activity at human CB2 receptor expressed in CHO cell membranes assessed as [35S]GTPgammaS binding after 1 hr by beta-counting analysis relative to control | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Benzo[d]thiazol-2(3H)-ones as new potent selective CB |
| AID714694 | Locomotor activity in iv dosed Harlan ICR mouse from 5 to 15 mins by spontaneous locomotor activity test | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents. |
| AID1333350 | Agonist activity at CB1 receptor (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID1071861 | Agonist activity at human CB2 receptor by [35S]-GTPgammaS binding assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Switching cannabinoid response from CB(2) agonists to FAAH inhibitors. |
| AID1071864 | Binding affinity to human CB2 receptor | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| Switching cannabinoid response from CB(2) agonists to FAAH inhibitors. |
| AID724461 | Agonist activity at human CB1 receptor expressed in HEK293S cell membranes after 1 hr by GTPgamma[35S] binding assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID1431664 | Selectivity ratio of Ki for human CB1 receptor to Ki for human CB2 receptor | | | |
| AID569313 | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
| Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2. |
| AID132689 | Inhibitory activity against PG synthesis was measured in mouse brain microsomes. | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
| Conformationally restrained analogues of pravadoline: nanomolar potent, enantioselective, (aminoalkyl)indole agonists of the cannabinoid receptor. |
| AID550010 | Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding relative to basal activity | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series. |
| AID620178 | Displacement of [3H]-CP55940 from human CB1 receptor expressed in CHO cells by liquid scintillation counting | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. |
| AID1372615 | Displacement of [3H]CP,55-940 from recombinant human CB2 receptor expressed in HEK293 EBNA cell membranes after 90 mins by microbeta scintillation counting method | | | |
| AID308136 | Agonist activity at human CB1 in CHO cells assessed as inhibition of cAMP production | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
| 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. |
| AID693541 | Agonist activity at human CB2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay relative to baseline | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands. |
| AID1662649 | Displacement of [3H]-CP55940 from human recombinant CB2 receptor expressed in HEK cell membrane | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. |
| AID324972 | Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR relative to CP-55940 | 2008 | Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
| Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity. |
| AID724230 | Inhibition of transient lower esophageal sphincter relaxations in iv dosed dog | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID310544 | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists. |
| AID699050 | Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat brain by scintillation counting | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| 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. |
| AID49325 | Binding affinity towards cloned human Cannabinoid receptor 1 | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
| A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors. |
| AID781180 | Selectivity ratio of Ki for rat CB1 receptor to Ki for human CB2 receptor | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Mastering tricyclic ring systems for desirable functional cannabinoid activity. |
| AID1333347 | Cytotoxicity against human Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID342490 | Agonist activity at human recombinant CB1 receptor in N18TG2 cells assessed as inhibition of forskolin-stimulated cAMP formation at 0.1 uM | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Novel sterically hindered cannabinoid CB1 receptor ligands. |
| AID1285171 | Selectivity ratio of Ki for human CB1 receptor expressed in CHO cell membranes to Ki for human CB2 receptor expressed in CHO cell membranes | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists. |
| AID537902 | Agonist activity at human CB1 receptor transfected in CHO cells after 5 hrs by luciferase reporter gene assay | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
| Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists. |
| AID302382 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| 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. |
| AID1662648 | Displacement of [3H]-CP55940 from human recombinant CB1 receptor expressed in HEK cell membrane | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. |
| AID724459 | Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293S cell membranes by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID302381 | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
| 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. |
| AID751753 | Displacement of [3H]SR141716A from human recombinant CB1 receptor expressed in CHEM1 cells at 10 uM after 90 mins relative to control | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| AID1333351 | Agonist activity at CB2 receptor (unknown origin) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor. |
| AID304356 | Displacement of [3H]CP-55940 from CB1 receptor in rat brain synaptosomes | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. |
| AID502211 | Agonist activity at human recombinant CB1 receptor expressed in CHO cells assessed as effect on CP-55940 induced PLA2 activation by [3H]arachidonic acid release assay | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists. |
| AID724458 | Displacement of [3H]-CP55,940 from human CB2 receptor expressed in Sf9 cell membranes by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease. |
| AID662933 | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| 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. |
| AID49842 | Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26
| Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors. |
| AID438797 | Agonist activity at CB1 receptor in CD1 mouse vas deferens assessed as inhibition of electrically-evoked contraction at 0.1 to 50 nM after 15 mins | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
| Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | | | |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | | | |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 1996 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 278, Issue:3
| Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 1995 | Molecular pharmacology, Sep, Volume: 48, Issue:3
| Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 1996 | Biochimica et biophysica acta, Jun-07, Volume: 1307, Issue:2
| Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 1996 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 278, Issue:3
| Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands. |
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 1996 | Biochimica et biophysica acta, Jun-07, Volume: 1307, Issue:2
| Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor. |
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 1995 | Molecular pharmacology, Sep, Volume: 48, Issue:3
| Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |