Target family: Hydroxycarboxylic acid receptors (type: gpcr)
Target: HCA<sub>2</sub> receptor

Ligand: [3H]nicotinic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular identification of nicotinic acid receptor.
Published in: Biochem Biophys Res Commun

Ligand: [3H]nicotinic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect.
Published in: Nat Med

Ligand: [3H]nicotinic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular identification of high and low affinity receptors for nicotinic acid.
Published in: J Biol Chem

Ligand: SCH 900271 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
Published in: ACS Med Chem Lett

Ligand: para-coumaric acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.51 pEC50
Reference (Journal): Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).
Published in: J Lipid Res

Ligand: nicotinic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect.
Published in: Nat Med

Ligand: nicotinic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Molecular identification of nicotinic acid receptor.
Published in: Biochem Biophys Res Commun

Ligand: nicotinic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Molecular identification of high and low affinity receptors for nicotinic acid.
Published in: J Biol Chem

Ligand: monomethyl fumarate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.74 pKi
Reference (Journal): Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).
Published in: Bioorg Med Chem Lett

Ligand: monomethyl fumarate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.03000020980835 pEC50
Reference (Journal): The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist.
Published in: Biochem Biophys Res Commun

Ligand: MK 6892 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pEC50
Reference (Journal): Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Published in: J Med Chem

Ligand: MK 6892 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Published in: J Med Chem

Ligand: MK 1903 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.559999942779541 pEC50
Reference (Journal): (1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.
Published in: J Med Chem

Ligand: MK 0354 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.78 pEC50
Reference (Journal): 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Published in: J Med Chem

Ligand: GSK256073 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist.
Published in: Eur J Pharmacol

Ligand: compound 9n [PMID: 18752940] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.77 pEC50
Reference (Journal): Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
Published in: Bioorg Med Chem Lett

Ligand: compound 8f [PMID: 20615702] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.41 pIC50
Reference (Journal): GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.
Published in: Bioorg Med Chem Lett

Ligand: compound 42 [PMID: 22420767] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.59 pEC50
Reference (Journal): Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).
Published in: J Med Chem

Ligand: compound 2g [PMID: 19309152] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.89 pIC50
Reference (Journal): Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Published in: J Med Chem

Ligand: compound 21 [PMID: 21185185] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.92 pIC50
Reference (Journal): The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.
Published in: Bioorg Med Chem Lett

Ligand: compound 1q [PMID: 18029181] (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.85 pIC50
Reference (Journal): Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Published in: Bioorg Med Chem Lett

Ligand: compound (+)17a [PMID: 20363624] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.35 pEC50
Reference (Journal): Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Published in: Bioorg Med Chem Lett

Ligand: cinnamic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.62 pEC50
Reference (Journal): Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).
Published in: J Lipid Res

Ligand: butyric acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 2.799999952316284 pEC50

Ligand: β-D-hydroxybutyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.5 pEC50
Reference (Journal): (D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G.
Published in: J Biol Chem

Ligand: β-D-hydroxybutyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 3.0999999046325684 pEC50
Reference (Journal): (D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G.
Published in: J Biol Chem

Ligand: acipimox (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2003)
Primary target: no
Median affinity:  pEC50
Reference (Journal): Molecular identification of nicotinic acid receptor.
Published in: Biochem Biophys Res Commun