Target family: Glycine receptors (type: lgic)
Target: Glycine Receptor (All subtypes)

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Mutations affecting the glycine receptor agonist transduction mechanism convert the competitive antagonist, picrotoxin, into an allosteric potentiator.
Published in: J Biol Chem

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The atypical M2 segment of the beta subunit confers picrotoxinin resistance to inhibitory glycine receptor channels.
Published in: EMBO J

Ligand: picrotoxinin (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): The atypical M2 segment of the beta subunit confers picrotoxinin resistance to inhibitory glycine receptor channels.
Published in: EMBO J

Ligand: onternabez (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Subunit-specific modulation of glycine receptors by cannabinoids and N-arachidonyl-glycine.
Published in: Biochem Pharmacol

Ligand: NV-31 (Synthetic organic)
Interaction type: Subunit-specific
Action: Potentiation
Ligand approved: no
Median affinity:  -
Reference (Journal): Subunit-specific potentiation of recombinant glycine receptors by NV-31, a bilobalide-derived compound.
Published in: Neurosci Lett

Ligand: NBBCC (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Developmental regulation of beta-carboline-induced inhibition of glycine-evoked responses depends on glycine receptor beta subunit expression.
Published in: Mol Pharmacol

Ligand: ivermectin (Synthetic organic)
Interaction type: Agonist
Action: Irreversible agonist
Ligand approved: yes
Approval source: FDA (1996), UK (2015)
Median affinity: 6.4 pEC50
Reference (Journal): Ivermectin, an unconventional agonist of the glycine receptor chloride channel.
Published in: J Biol Chem

Ligand: HU-210 (Synthetic organic)
Interaction type: Subunit-specific
Action: Potentiation
Ligand approved: no
Median affinity: 6.57 pEC50
Reference (Journal): Subunit-specific modulation of glycine receptors by cannabinoids and N-arachidonyl-glycine.
Published in: Biochem Pharmacol

Ligand: HU-210 (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Subunit-specific modulation of glycine receptors by cannabinoids and N-arachidonyl-glycine.
Published in: Biochem Pharmacol

Ligand: glycine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of intracellular and extracellular domains mediating signal transduction in the inhibitory glycine receptor chloride channel.
Published in: EMBO J

Ligand: glycine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Residues within transmembrane segment M2 determine chloride conductance of glycine receptor homo- and hetero-oligomers.
Published in: EMBO J

Ligand: ginkgolide J (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Structure-activity analysis of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: ginkgolide C (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular determinants of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: ginkgolide B (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Structure-activity analysis of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: ginkgolide B (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular determinants of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: ginkgolide A (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular determinants of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: GABA (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Mutation of glycine receptor subunit creates beta-alanine receptor responsive to GABA.
Published in: Science

Ligand: GABA (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Activation of human alpha1 and alpha2 homomeric glycine receptors by taurine and GABA.
Published in: J Physiol (Lond.)

Ligand: ethanol (Metabolite)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: no
Median affinity:  -
Reference (Journal): A single amino acid determines differences in ethanol actions on strychnine-sensitive glycine receptors.
Published in: Mol Pharmacol

Ligand: dehydroepiandrosterone (Metabolite)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2016), EMA (2018)
Median affinity:  -
Reference (Journal): Subunit-specific modulation of glycine receptors by neurosteroids.
Published in: Neuropharmacology

Ligand: cyanotriphenylborate (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pIC50
Reference (Journal): Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels.
Published in: Proc Natl Acad Sci USA

Ligand: cyanotriphenylborate (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels.
Published in: Proc Natl Acad Sci USA

Ligand: colchicine (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009)
Median affinity:  -
Reference (Journal): Colchicine competitively antagonizes glycine receptors expressed in Xenopus oocytes.
Published in: Neuropharmacology

Ligand: bilobalide (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular determinants of ginkgolide binding in the glycine receptor pore.
Published in: J Neurochem

Ligand: β-alanine (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Median affinity: 4.3 pEC50
Reference (Journal): Identification of intracellular and extracellular domains mediating signal transduction in the inhibitory glycine receptor chloride channel.
Published in: EMBO J

Ligand: atropine (Natural product)
Interaction type: Subunit-specific
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1973)
Median affinity:  -
Reference (Journal): Selective blocking effects of tropisetron and atropine on recombinant glycine receptors.
Published in: J Neurochem

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity: 3.6 pIC50
Reference (Journal): Selective blocking effects of tropisetron and atropine on recombinant glycine receptors.
Published in: J Neurochem

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity: 3.6 pIC50
Reference (Journal): Tropisetron modulation of the glycine receptor: femtomolar potentiation and a molecular determinant of inhibition.
Published in: J Neurochem

Ligand: anandamide (Metabolite)
Interaction type: Subunit-specific
Action: Potentiation
Ligand approved: no
Median affinity: 7.2 pEC50
Reference (Journal): Subunit-specific modulation of glycine receptors by cannabinoids and N-arachidonyl-glycine.
Published in: Biochem Pharmacol

Ligand: α-Emtbl (Synthetic organic)
Interaction type: Subunit-specific
Action: Mixed
Ligand approved: no
Median affinity:  -
Reference (Journal): Subunit-specific action of an anticonvulsant thiobutyrolactone on recombinant glycine receptors involves a residue in the M2 membrane-spanning region.
Published in: Mol Pharmacol

Ligand: alkylbenzene sulfonate (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Median affinity:  -
Reference (Journal): Selective actions of a detergent on ligand-gated ion channels expressed in Xenopus oocytes.
Published in: J Pharmacol Exp Ther

Ligand: 5,7-dichlorokynurenic acid (Synthetic organic)
Interaction type: Subunit-specific
Action: Inhibition
Median affinity:  -
Reference (Journal): Selective antagonism of rat inhibitory glycine receptor subunits.
Published in: J Physiol (Lond.)