Target family: Cannabinoid receptors (type: gpcr)
Target: CB<sub>1</sub> receptor

Ligand: 2-arachidonoylglycerol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.
Published in: Biochem Pharmacol

Ligand: 2-arachidonoylglycerol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity.
Published in: Eur J Pharmacol

Ligand: AM11542 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.960000038146973 pKi
Reference (Journal): Crystal structures of agonist-bound human cannabinoid receptor CB<sub>1</sub>.
Published in: Nature

Ligand: AM1710 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pKi
Reference (Journal): Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.
Published in: J Med Chem

Ligand: AM2201 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.420000076293945 pEC50
Reference (Journal): Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135.
Published in: ACS Chem Neurosci

Ligand: AM2201 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Patent): Cannabimimetic indole derivatives

Ligand: AM251 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.
Published in: J Med Chem

Ligand: AM281 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Design and synthesis of the CB1 selective cannabinoid antagonist AM281: a potential human SPECT ligand.
Published in: AAPS PharmSci

Ligand: AM6538 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.34000015258789 pKi
Reference (Journal): Crystal Structure of the Human Cannabinoid Receptor CB1.
Published in: Cell

Ligand: AM6545 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pKi
Reference (Journal): A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome.
Published in: Proc Natl Acad Sci USA

Ligand: AM7499 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pKi
Reference (Journal): Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
Published in: J Med Chem

Ligand: AM841 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.9399995803833 pKi
Reference (Journal): Crystal structures of agonist-bound human cannabinoid receptor CB<sub>1</sub>.
Published in: Nature

Ligand: anandamide (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: anandamide (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: arachidonyl-2-chloroethylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKi
Reference (Journal): Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1).
Published in: J Pharmacol Exp Ther

Ligand: arachidonylcyclopropylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1).
Published in: J Pharmacol Exp Ther

Ligand: AZD1940 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.929999828338623 pKi
Reference (Journal): Benzo[d]thiazol-2(3H)-ones as new potent selective CB<sub>2</sub> agonists with anti-inflammatory properties.
Published in: Eur J Med Chem

Ligand: BAY-593074 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pKi
Reference (Journal): 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
Published in: J Pharmacol Exp Ther

Ligand: BAY-593074 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pKi
Reference (Journal): 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
Published in: J Pharmacol Exp Ther

Ligand: BMS-202 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.989999771118164 pIC50
Reference (Journal): Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135.
Published in: ACS Chem Neurosci

Ligand: cannabidiol (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Primary target: no
Median affinity:  -
Reference (Journal): Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor.
Published in: Br J Pharmacol

Ligand: cannabinol (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: cannabinol (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: compound 70 [PMID: 26161824] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pKi
Reference (Journal): A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents.
Published in: Expert Opin Ther Pat

Ligand: CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Agonist-inverse agonist characterization at CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors of L759633, L759656 and AM630.
Published in: Br J Pharmacol

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: GAT100 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pEC50
Reference (Journal): Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
Published in: J Med Chem

Ligand: GAT100 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pEC50
Reference (Journal): Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe.
Published in: ACS Chem Neurosci

Ligand: GAT211 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.
Published in: ACS Chem Neurosci

Ligand: HU-210 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: HU-210 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: ibipinabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.109999656677246 pKi
Reference (Journal): Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.
Published in: J Med Chem

Ligand: R-(+)-methanandamide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand.
Published in: J Med Chem

Ligand: JD5037 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.460000038146973 pKi
Reference (Journal): Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance.
Published in: Cell Metab

Ligand: JWH-018 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): The third transmembrane helix of the cannabinoid receptor plays a role in the selectivity of aminoalkylindoles for CB2, peripheral cannabinoid receptor.
Published in: J Pharmacol Exp Ther

Ligand: lenabasum (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pKi
Reference (Journal): Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.
Published in: J Med Chem

Ligand: lenabasum (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pKi
Reference (Journal): Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
Published in: J Med Chem

Ligand: levonantradol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pKi
Reference (Journal): Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
Published in: J Med Chem

Ligand: LY320135 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pKi
Reference (Journal): LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation.
Published in: J Pharmacol Exp Ther

Ligand: MDMB-Fubinaca (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.010000228881836 pKi
Reference (Journal): Pharmacological evaluation of new constituents of &quot;Spice&quot;: synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds.
Published in: Forensic Toxicol

Ligand: MRI-1867 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.640000343322754 pKi
Reference (Journal): Hybrid inhibitor of peripheral cannabinoid-1 receptors and inducible nitric oxide synthase mitigates liver fibrosis.
Published in: JCI Insight

Ligand: nabilone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.
Published in: Eur J Med Chem

Ligand: O-1812 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Highly selective CB<sub>1</sub> cannabinoid receptor ligands and novel CB<sub>1</sub>/VR1 vanilloid receptor "hybrid" ligands.
Published in: Biochem Biophys Res Commun

Ligand: olorinab (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Discovery of APD371: Identification of a Highly Potent and Selective CB<sub>2</sub> Agonist for the Treatment of Chronic Pain.
Published in: ACS Med Chem Lett

Ligand: olorinab (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Discovery of APD371: Identification of a Highly Potent and Selective CB<sub>2</sub> Agonist for the Treatment of Chronic Pain.
Published in: ACS Med Chem Lett

Ligand: Org27569 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 6.849999904632568 pEC50
Reference (Journal): Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor.
Published in: J Med Chem

Ligand: otenabant (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.550000190734863 pKi
Reference (Journal): Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Published in: J Med Chem

Ligand: otenabant (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 pKi
Reference (Journal): Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Published in: J Med Chem

Ligand: pepcan-12 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Identification and quantification of a new family of peptide endocannabinoids (Pepcans) showing negative allosteric modulation at CB1 receptors.
Published in: J Biol Chem

Ligand: PF-514273 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.09000015258789 pKi
Reference (Journal): Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Published in: J Med Chem

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor.
Published in: J Pharmacol Exp Ther

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): SR141716A, a potent and selective antagonist of the brain cannabinoid receptor.
Published in: FEBS Lett

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation.
Published in: J Pharmacol Exp Ther

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: Sch.336 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo.
Published in: J Pharmacol Exp Ther

Ligand: Sch.336 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 6.039999961853027 pKi
Reference (Journal): Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Published in: Bioorg Med Chem Lett

Ligand: [123I]AM251 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKd
Reference (Journal): Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors.
Published in: Life Sci

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Cannabinoid agonists stimulate both receptor- and non-receptor-mediated signal transduction pathways in cells transfected with and expressing cannabinoid receptor clones.
Published in: Mol Pharmacol

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular cloning of a human cannabinoid receptor which is also expressed in testis.
Published in: Biochem J

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1.
Published in: Biochem J

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A.
Published in: J Biol Chem

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Stimulation of cannabinoid receptor CB1 induces krox-24 expression in human astrocytoma cells.
Published in: J Biol Chem

Ligand: [3H]HU-243 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.4 pKd
Reference (Journal): A novel probe for the cannabinoid receptor.
Published in: J Med Chem

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Effects of chronic treatment with delta9-tetrahydrocannabinol on cannabinoid-stimulated [35S]GTPgammaS autoradiography in rat brain.
Published in: J Neurosci

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization and distribution of binding sites for [<sup>3</sup>H]-SR 141716A, a selective brain (CB<sub>1</sub>) cannabinoid receptor antagonist, in rodent brain.
Published in: Life Sci

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Comparative receptor binding analyses of cannabinoid agonists and antagonists.
Published in: J Pharmacol Exp Ther

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Regional differences in cannabinoid receptor/G-protein coupling in rat brain.
Published in: J Pharmacol Exp Ther

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of CB<sub>1</sub> receptors on rat neuronal cell cultures: binding and functional studies using the selective receptor antagonist SR 141716A.
Published in: J Neurochem

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Biochemical and pharmacological characterization of cannabinoid binding sites using [<sup>3</sup>H]SR141716A.
Published in: Neuroreport

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist.
Published in: Neurosci Lett

Ligand: [3H]WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2.
Published in: Mol Pharmacol

Ligand: [3H]WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1.
Published in: J Neurochem

Ligand: surinabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.460000038146973 pKi
Reference (Journal): SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Published in: J Pharmacol Exp Ther

Ligand: taranabant (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.520000457763672 pKi
Reference (Journal): Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.
Published in: Bioorg Med Chem Lett

Ligand: TM38837 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.069999694824219 pIC50
Reference (Journal): Optimizing and characterizing 4-methyl substituted pyrazol-3-carboxamides leading to the peripheral cannabinoid 1 receptor inverse agonist TM38837.
Published in: Bioorg Med Chem Lett

Ligand: TM38837 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Optimizing and characterizing 4-methyl substituted pyrazol-3-carboxamides leading to the peripheral cannabinoid 1 receptor inverse agonist TM38837.
Published in: Bioorg Med Chem Lett

Ligand: TM38837 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.069999694824219 pIC50
Reference (Journal): Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist.
Published in: ChemMedChem

Ligand: TM39875 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 7.289999961853027 pIC50
Reference (Journal): Optimizing and characterizing 4-methyl substituted pyrazol-3-carboxamides leading to the peripheral cannabinoid 1 receptor inverse agonist TM38837.
Published in: Bioorg Med Chem Lett

Ligand: TM39875 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 pIC50
Reference (Journal): Optimizing and characterizing 4-methyl substituted pyrazol-3-carboxamides leading to the peripheral cannabinoid 1 receptor inverse agonist TM38837.
Published in: Bioorg Med Chem Lett

Ligand: VCE-004.3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.610000133514404 pKi
Reference (Journal): VCE-004.3, a cannabidiol aminoquinone derivative, prevents bleomycin-induced skin fibrosis and inflammation through PPARγ- and CB<sub>2</sub> receptor-dependent pathways.
Published in: Br J Pharmacol

Ligand: WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands.
Published in: J Pharmacol Exp Ther

Ligand: WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor.
Published in: Biochim Biophys Acta

Ligand: ZCZ011 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pEC50
Reference (Journal): A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects.
Published in: Neuropsychopharmacology

Ligand: ZCZ011 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.309999942779541 pEC50
Reference (Journal): A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects.
Published in: Neuropsychopharmacology