dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Chemokine receptors (type: gpcr)
Target: ACKR3

Ligand: adrenomedullin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): Identification of an orphan receptor gene as a type 1 calcitonin gene-related peptide receptor.
Published in: Biochem Biophys Res Commun

Ligand: α-CGRP (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pEC50
Reference (Journal): Identification of an orphan receptor gene as a type 1 calcitonin gene-related peptide receptor.
Published in: Biochem Biophys Res Commun

Ligand: CXCL11 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: CXCL12α (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains.
Published in: J Biol Chem

Ligand: CXCL12α (Peptide)
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: LIH383 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pEC50
Reference (Journal): The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides.
Published in: Nat Commun

Ligand: plerixafor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2009)
Median affinity: 6.85 pEC50
Reference (Journal): The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains.
Published in: J Biol Chem

Ligand: plerixafor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2009)
Median affinity: 6.85 pEC50
Reference (Journal): AMD3100 is a CXCR7 ligand with allosteric agonist properties.
Published in: Mol Pharmacol

Ligand: TC14012 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.46 pEC50
Reference (Journal): The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains.
Published in: J Biol Chem
Target family: Chemokine receptors (type: gpcr)
Target: ACKR4

Ligand: CCL19 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem

Ligand: CCL19 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem

Ligand: CCL21 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem

Ligand: CCL21 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem

Ligand: CCL25 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem

Ligand: CCL25 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR.
Published in: J Biol Chem
Target family: Chemokine receptors (type: gpcr)
Target: CCR10

Ligand: BI-6901 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): N-Arylsulfonyl-α-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.
Published in: Bioorg Med Chem Lett

Ligand: BI-6901 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): N-Arylsulfonyl-α-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity.
Published in: Bioorg Med Chem Lett

Ligand: CCL27 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Cutting edge: the orphan chemokine receptor G protein-coupled receptor-2 (GPR-2, CCR10) binds the skin-associated chemokine CCL27 (CTACK/ALP/ILC).
Published in: J Immunol

Ligand: CCL28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Target family: Chemokine receptors (type: gpcr)
Target: CCR6

Ligand: beta-defensin 4A (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Beta-defensins: linking innate and adaptive immunity through dendritic and T cell CCR6.
Published in: Science

Ligand: CCL20 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Identification of CCR6, the specific receptor for a novel lymphocyte-directed CC chemokine LARC.
Published in: J Biol Chem

Ligand: CCL20 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mutating the four extracellular cysteines in the chemokine receptor CCR6 reveals their differing roles in receptor trafficking, ligand binding, and signaling.
Published in: Biochemistry

Ligand: CCL20 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and characterization of a specific receptor for the novel CC chemokine MIP-3alpha from lung dendritic cells.
Published in: J Exp Med

Ligand: CCL20-SEAP(His)6 (Peptide)
Interaction type: Agonist
Action: Full agonist
Median affinity: 9 pKd
Reference (Journal): Identification of CCR6, the specific receptor for a novel lymphocyte-directed CC chemokine LARC.
Published in: J Biol Chem

Ligand: PF-07054894 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): A Novel C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) Antagonist (PF-07054894) Distinguishes between Homologous Chemokine Receptors, Increases Basal Circulating CCR6<sup>+</sup> T Cells, and Ameliorates Interleukin-23-Induced Skin Inflammation.
Published in: J Pharmacol Exp Ther

Ligand: [125I]CCL20 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): CCR6, a CC chemokine receptor that interacts with macrophage inflammatory protein 3alpha and is highly expressed in human dendritic cells.
Published in: J Exp Med
Target family: Chemokine receptors (type: gpcr)
Target: CCR9

Ligand: CCL25 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: compound 24 [PMID: 26987013 ] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pKi
Reference (Journal): A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease.
Published in: J Med Chem

Ligand: [125I]CCL25 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: vercirnon (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease.
Published in: J Pharmacol Exp Ther
Target family: Chemokine receptors (type: gpcr)
Target: CCRL2

Ligand: CCL19 (Peptide)
Interaction type: Agonist
Action: Unknown
Ligand approved: no
Median affinity: 7.36 pIC50
Reference (Journal): CCL19 is a specific ligand of the constitutively recycling atypical human chemokine receptor CRAM-B.
Published in: Immunology
Target family: Chemokine receptors (type: gpcr)
Target: CXCR5

Ligand: CXCL13 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKd
Reference (Journal): EBI2 regulates CXCL13-mediated responses by heterodimerization with CXCR5.
Published in: FASEB J

Ligand: [125I]CXCL13 (mouse) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Quantitative analysis of target coverage and germinal center response by a CXCL13 neutralizing antibody in a T-dependent mouse immunization model.
Published in: Pharm Res
Target family: Chemokine receptors (type: gpcr)
Target: CXCR6

Ligand: CXCL16 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Expression cloning of the STRL33/BONZO/TYMSTRligand reveals elements of CC, CXC, and CX3C chemokines.
Published in: J Immunol

Ligand: [125I]CXCL16 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Target family: Chemokine receptors (type: gpcr)
Target: CX<sub>3</sub>CR1

Ligand: CX3CL1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.9 pIC50
Reference (Journal): Two novel fully functional isoforms of CX3CR1 are potent HIV coreceptors.
Published in: J Immunol

Ligand: JMS-17-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.489999771118164 pIC50
Reference (Journal): Novel Small-Molecule CX3CR1 Antagonist Impairs Metastatic Seeding and Colonization of Breast Cancer Cells.
Published in: Mol Cancer Res

Ligand: [125I]CX3CL1 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Target family: Chemokine receptors (type: gpcr)
Target: XCR1

Ligand: [125I]XCL1 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Identification of single C motif-1/lymphotactin receptor XCR1.
Published in: J Biol Chem

Ligand: XCL1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Structural and agonist properties of XCL2, the other member of the C-chemokine subfamily.
Published in: Cytokine

Ligand: XCL2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Structural and agonist properties of XCL2, the other member of the C-chemokine subfamily.
Published in: Cytokine
Target family: Chitinases (type: enzyme)
Target: chitinase 1

Ligand: GLPG4716 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Discovery of <b>OATD-01</b>, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem

Ligand: GLPG4716 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pIC50
Reference (Journal): Discovery of <b>OATD-01</b>, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem
Target family: Chitinases (type: enzyme)
Target: chitinase acidic

Ligand: compound 7f [PMID: 29283260] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma.
Published in: J Med Chem

Ligand: compound 7f [PMID: 29283260] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma.
Published in: J Med Chem

Ligand: GLPG4716 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery of <b>OATD-01</b>, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem

Ligand: GLPG4716 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.109999656677246 pIC50
Reference (Journal): Discovery of <b>OATD-01</b>, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem
Target family: Choline transporter (type: transporter)
Target: CHT

Ligand: [3H]hemicholinium-3 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  pKd

Ligand: hemicholinium-3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): High-affinity choline transporter.
Published in: Neurochem Res
Target family: Chromatin modifying enzymes (<i>Plasmodium</i> spp.) (type: other_protein)
Target: Plasmodium falciparum histone acetyltransferase GCN5

Ligand: SGC-CBP30 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.5 pIC50
Reference (Journal): Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites.
Published in: Int J Parasitol Drugs Drug Resist

Ligand: L-45 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pKd
Reference (Journal): Discovery of a PCAF Bromodomain Chemical Probe.
Published in: Angew Chem Int Ed Engl
Target family: Circadian clock proteins (type: other_protein)
Target: cryptochrome circadian regulator 1

Ligand: KL044 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 7.199999809265137 pEC50
Reference (Journal): Development of Small-Molecule Cryptochrome Stabilizer Derivatives as Modulators of the Circadian Clock.
Published in: ChemMedChem
Target family: Citrate metabolism (type: enzyme)
Target: ATP citrate lyase

Ligand: bempedoic acid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2020)
Primary target: no
Median affinity: 5.699999809265137 pKi
Reference (Journal): Opportunities and Challenges for Inhibitors Targeting Citrate Transport and Metabolism in Drug Discovery.
Published in: J Med Chem

Ligand: BMS-303141 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: NDI-091143 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pKd
Reference (Journal): An allosteric mechanism for potent inhibition of human ATP-citrate lyase.
Published in: Nature

Ligand: NDI-091143 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.680000305175781 pIC50
Reference (Journal): An allosteric mechanism for potent inhibition of human ATP-citrate lyase.
Published in: Nature
Target family: Citrate metabolism (type: enzyme)
Target: isocitrate dehydrogenase (NADP(+)) 1

Ligand: AGI-5198 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 4.889999866485596 pKi

Ligand: ivosidenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2023)
Primary target: yes
Median affinity:  -
Reference (Patent): Therapeutically active compounds and their methods of use

Ligand: LY3410738 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Patent): 7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors

Ligand: LY3410738 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 pIC50
Reference (Patent): 7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors

Ligand: olutasidenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022)
Primary target: no
Median affinity:  pIC50
Reference (Patent): Pyridin-2(1H)-one quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors

Ligand: safusidenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): A Potent Blood-Brain Barrier-Permeable Mutant IDH1 Inhibitor Suppresses the Growth of Glioblastoma with IDH1 Mutation in a Patient-Derived Orthotopic Xenograft Model.
Published in: Mol Cancer Ther

Ligand: vorasidenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Published in: ACS Med Chem Lett
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR17</i>

Ligand: LTC4 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor.
Published in: EMBO J

Ligand: cangrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2015)
Median affinity: 8.92 pIC50
Reference (Journal): The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair.
Published in: PLoS ONE

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.43 pEC50
Reference (Journal): Innovative functional cAMP assay for studying G protein-coupled receptors: application to the pharmacological characterization of GPR17.
Published in: Purinergic Signal

Ligand: ASN06917370 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.57 pEC50
Reference (Journal): In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases.
Published in: J Comput Aided Mol Des

Ligand: ASN04885796 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.96 pEC50
Reference (Journal): In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases.
Published in: J Comput Aided Mol Des

Ligand: ASN04450772 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.93 pEC50
Reference (Journal): In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases.
Published in: J Comput Aided Mol Des

Ligand: ASN04421891 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.44 pEC50
Reference (Journal): In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases.
Published in: J Comput Aided Mol Des

Ligand: ASN02563583 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.96 pEC50
Reference (Journal): In silico identification of new ligands for GPR17: a promising therapeutic target for neurodegenerative diseases.
Published in: J Comput Aided Mol Des
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR174</i>

Ligand: lysophosphatidylserine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): TGFα shedding assay: an accurate and versatile method for detecting GPCR activation.
Published in: Nat Methods
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR161</i>

Ligand: CART(55-102) (Peptide)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): GPR162 is a beta cell CART receptor.
Published in: iScience
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR15</i>

Ligand: GPR15L (71-81) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: GPR15L (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.849999904632568 pEC50
Reference (Journal): A natural ligand for the orphan receptor GPR15 modulates lymphocyte recruitment to epithelia.
Published in: Sci Signal
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR142</i>

Ligand: compound 33 [Toda et al., 2013] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pEC50
Reference (Journal): Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.
Published in: ACS Med Chem Lett
Target family: Class A Orphans (type: gpcr)
Target: <i>GPR132</i>

Ligand: ONC212 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pEC50
Reference (Journal): Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia.
Published in: Leukemia

Ligand: NOX-6-7 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
Published in: Nat Metab

Ligand: NOX-6-18 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pIC50
Reference (Journal): Functional screening and rational design of compounds targeting GPR132 to treat diabetes.
Published in: Nat Metab

Ligand: 9-hydroxyoctadecadienoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pEC50
Reference (Journal): Identification of 9-hydroxyoctadecadienoic acid and other oxidized free fatty acids as ligands of the G protein-coupled receptor G2A.
Published in: J Biol Chem