Target family: GPR18, GPR55 and GPR119 (type: gpcr)
Target: <i>GPR55</i>

Ligand: 2-arachidonoylglycerol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.52 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: 2-arachidonoylglycerolphosphoinositol (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): 2-Arachidonoyl-sn-glycero-3-phosphoinositol: a possible natural ligand for GPR55.
Published in: J Biochem

Ligand: 2-arachidonyl glyceryl ether (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: abnormal cannabidiol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: abnormal cannabidiol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pEC50
Reference (Journal): The novel endocannabinoid receptor GPR55 is activated by atypical cannabinoids but does not mediate their vasodilator effects.
Published in: Br J Pharmacol

Ligand: AM251 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: AM251 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands.
Published in: J Biol Chem

Ligand: AM251 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): GPR55 ligands promote receptor coupling to multiple signalling pathways.
Published in: Br J Pharmacol

Ligand: AM281 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): GPR55 ligands promote receptor coupling to multiple signalling pathways.
Published in: Br J Pharmacol

Ligand: AM281 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: anandamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.74 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: cannabidiol (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Median affinity:  pIC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: cannabidiol (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019), UK (2019)
Median affinity:  pIC50
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB₁ and CB₂.
Published in: Pharmacol Rev

Ligand: Chgb (511-532) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.619999885559082 pEC50

Ligand: CID1172084 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands.
Published in: Biochemistry

Ligand: CID16020046 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pA2
Reference (Journal): A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function.
Published in: J Pharmacol Exp Ther

Ligand: CID1792197 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands.
Published in: Biochemistry

Ligand: CID2440433 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands.
Published in: Biochemistry

Ligand: CLUL1 (52-77) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.739999771118164 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: compound 3a [Badolato et al., 2019] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of 1,4-Naphthoquinones as a New Class of Antiproliferative Agents Targeting GPR55.
Published in: ACS Med Chem Lett

Ligand: CP55,244 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist.
Published in: J Pharmacol Exp Ther

Ligand: CP55,667 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist.
Published in: J Pharmacol Exp Ther

Ligand: CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.3 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.3 pEC50
Reference (Journal): In silico patent searching reveals a new cannabinoid receptor.
Published in: Trends Pharmacol Sci

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1985)
Median affinity: 8.1 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: GSK494581A (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.19 pEC50
Reference (Journal): Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist.
Published in: J Pharmacol Exp Ther

Ligand: GSK575594A (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.17 pEC50
Reference (Journal): Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist.
Published in: J Pharmacol Exp Ther

Ligand: HU-210 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.59 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: N-palmitoylethanolamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: O-1602 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: O-1602 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine.
Published in: J Pharmacol Exp Ther

Ligand: O-1602 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB₁ and CB₂.
Published in: Pharmacol Rev

Ligand: O-arachidonoyl ethanolamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.92 pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Median affinity:  pEC50
Reference (Journal): Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist.
Published in: J Pharmacol Exp Ther

Ligand: rimonabant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2007)
Median affinity:  pEC50
Reference (Journal): GPR55 ligands promote receptor coupling to multiple signalling pathways.
Published in: Br J Pharmacol

Ligand: SPAG11B (61-103) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.690000057220459 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: [3H]CP55940 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: [3H]rimonabant (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol

Ligand: T1117 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Fluorescent ligand binding reveals heterogeneous distribution of adrenoceptors and 'cannabinoid-like' receptors in small arteries.
Published in: Br J Pharmacol

Ligand: lysophosphatidylinositol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: lysophosphatidylinositol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of GPR55 as a lysophosphatidylinositol receptor.
Published in: Biochem Biophys Res Commun

Ligand: lysophosphatidylinositol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): GPR55 ligands promote receptor coupling to multiple signalling pathways.
Published in: Br J Pharmacol

Ligand: MANSC (415-431) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.510000228881836 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: ML193 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pIC50
Reference (Journal): Screening for Selective Ligands for GPR55 - Antagonists
Published in: Probe Reports from the NIH Molecular Libraries Program

Ligand: MSMB (91-114) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.650000095367432 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The orphan receptor GPR55 is a novel cannabinoid receptor.
Published in: Br J Pharmacol