Target family: Cannabinoid receptors (type: gpcr)
Target: CB<sub>2</sub> receptor

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity:  pKi
Reference (Journal): (-)-Delta9-tetrahydrocannabinol antagonizes the peripheral cannabinoid receptor-mediated inhibition of adenylyl cyclase.
Published in: J Biol Chem

Ligand: olorinab (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.119999885559082 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: onternabez (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor.
Published in: Proc Natl Acad Sci USA

Ligand: pepcan-12 (Peptide)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage.
Published in: Sci Rep

Ligand: phenylacetylrinvanil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pKi
Reference (Journal): Development of the first ultra-potent &quot;capsaicinoid&quot; agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential.
Published in: J Pharmacol Exp Ther

Ligand: Sch.336 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 9.399999618530273 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: Sch.336 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pKi
Reference (Journal): A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo.
Published in: J Pharmacol Exp Ther

Ligand: SR144528 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Published in: J Pharmacol Exp Ther

Ligand: SR144528 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular characterization of a peripheral receptor for cannabinoids.
Published in: Nature

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): Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor.
Published in: Biochim Biophys Acta

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors.
Published in: Mol Pharmacol

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Signaling pathway associated with stimulation of CB2 peripheral cannabinoid receptor. Involvement of both mitogen-activated protein kinase and induction of Krox-24 expression.
Published in: Eur J Biochem

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]HU-243 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling.
Published in: FEBS Lett

Ligand: [3H]WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase.
Published in: Mol Pharmacol

Ligand: [3H]WIN55212-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular characterization of a peripheral receptor for cannabinoids.
Published in: Nature

Ligand: surinabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.349999904632568 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: Agonist
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.539999961853027 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: no
Median affinity: 6.21999979019165 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: VCE-004.3 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.690000057220459 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: vicasinabin (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pEC50
Reference (Patent): [1, 2, 3] triazolo [4, 5 -d] pyrimidine derivatives as agonists of the cannabinoid receptor 2

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): 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): Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor.
Published in: Biochim Biophys Acta