dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Glucagon receptor family (type: gpcr)
Target: GLP-2 receptor

Ligand: glucagon-like peptide 2-(2-33) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA

Ligand: glucagon-like peptide 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA

Ligand: glucagon-like peptide 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.2 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA

Ligand: glucagon-like peptide 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): The truncated metabolite GLP-2 (3-33) interacts with the GLP-2 receptor as a partial agonist.
Published in: Regul Pept

Ligand: GLP-2 analogue 10 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.550000190734863 pEC50
Reference (Journal): Stapled, Long-Acting Glucagon-like Peptide 2 Analog with Efficacy in Dextran Sodium Sulfate Induced Mouse Colitis Models.
Published in: J Med Chem

Ligand: GLP-2-(1-29) (rat) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA

Ligand: apraglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pEC50
Reference (Journal): Novel Long-Acting GLP-2 Analogue, FE 203799 (Apraglutide), Enhances Adaptation and Linear Intestinal Growth in a Neonatal Piglet Model of Short Bowel Syndrome with Total Resection of the Ileum.
Published in: JPEN J Parenter Enteral Nutr

Ligand: apraglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pEC50
Reference (Journal): Pharmacological Characterization of Apraglutide, a Novel Long-Acting Peptidic Glucagon-Like Peptide-2 Agonist, for the Treatment of Short Bowel Syndrome.
Published in: J Pharmacol Exp Ther
Target family: Glucagon receptor family (type: gpcr)
Target: GLP-1 receptor

Ligand: albiglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA  and EMA (2014)
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): A recombinant human glucagon-like peptide (GLP)-1-albumin protein (albugon) mimics peptidergic activation of GLP-1 receptor-dependent pathways coupled with satiety, gastrointestinal motility, and glucose homeostasis.
Published in: Diabetes

Ligand: BETP (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 9.899999618530273 pEC50
Reference (Journal): A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification.
Published in: Nat Chem Biol

Ligand: danuglipron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pKi
Reference (Journal): A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Published in: J Med Chem

Ligand: exendin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Exendin-3, a novel peptide from Heloderma horridum venom, interacts with vasoactive intestinal peptide receptors and a newly described receptor on dispersed acini from guinea pig pancreas. Description of exendin-3(9-39) amide, a specific exendin receptor antagonist.
Published in: J Biol Chem

Ligand: exendin-4 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: yes
Median affinity: 9.180000305175781 pIC50
Reference (Journal): Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.
Published in: J Med Chem

Ligand: exendin-4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol

Ligand: exendin-(9-39) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol

Ligand: GLP-1-(9-36) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.909999847412109 pIC50
Reference (Journal): High potency antagonists of the pancreatic glucagon-like peptide-1 receptor.
Published in: J Biol Chem
Target family: Glucagon receptor family (type: gpcr)
Target: GHRH receptor

Ligand: sermorelin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1990)
Primary target: yes
Median affinity:  -

Ligand: tesamorelin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2010)
Primary target: yes
Median affinity:  -
Target family: Glucagon receptor family (type: gpcr)
Target: GIP receptor

Ligand: gastric inhibitory polypeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): GIP(6-30amide) contains the high affinity binding region of GIP and is a potent inhibitor of GIP1-42 action in vitro.
Published in: Regul Pept
Target family: Glucagon receptor family (type: gpcr)
Target: GLP-1 receptor

Ligand: glucagon (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1960)
Median affinity:  pKi
Reference (Journal): Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype.
Published in: Mol Endocrinol
Target family: Glucagon receptor family (type: gpcr)
Target: GIP receptor

Ligand: gastric inhibitory polypeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): Molecular cloning, functional expression, and signal transduction of the GIP-receptor cloned from a human insulinoma.
Published in: FEBS Lett

Ligand: gastric inhibitory polypeptide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pKi
Reference (Journal): N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor.
Published in: Br J Pharmacol
Target family: Glucagon receptor family (type: gpcr)
Target: GLP-2 receptor

Ligand: [Tyr34]GLP-2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Median affinity: 9.2 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA

Ligand: teduglutide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity:  -
Reference (Journal): Teduglutide: a guide to its use in short bowel syndrome.
Published in: Clin Drug Investig

Ligand: glucagon-like peptide 2-(3-33) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): The truncated metabolite GLP-2 (3-33) interacts with the GLP-2 receptor as a partial agonist.
Published in: Regul Pept

Ligand: glucagon-like peptide 2-(3-33) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2.
Published in: Proc Natl Acad Sci USA
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 2

Ligand: (R)-AS-1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pEC50
Reference (Journal): Discovery of (<i>R</i>)-<i>N</i>-Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [<b>(<i>R</i>)-AS-1</b>], a Novel Orally Bioavailable EAAT2 Modulator with Drug-like Properties and Potent Antiseizure Activity <i>In Vivo</i>.
Published in: J Med Chem

Ligand: DL-TBOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 6.9 pKB
Reference (Journal): DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.
Published in: Mol Pharmacol

Ligand: dihydrokainate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5 pKB
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 1

Ligand: UCPH-101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.
Published in: J Med Chem
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 5

Ligand: [3H]L-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: [3H]ETB-TBOA (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKd
Reference (Journal): Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters.
Published in: Mol Pharmacol

Ligand: [3H]D-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: DL-TBOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Effects of threo-beta-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5).
Published in: J Neurochem
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 4

Ligand: threo-3-methylglutamate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 4.3 pKi
Reference (Journal): Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systems.
Published in: J Neurochem

Ligand: [3H]L-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 1

Ligand: [3H]SYM2081 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 4

Ligand: [3H]ETB-TBOA (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters.
Published in: Mol Pharmacol
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 1

Ligand: [3H]L-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 4

Ligand: [3H]D-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 1

Ligand: [3H]ETB-TBOA (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKd
Reference (Journal): Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters.
Published in: Mol Pharmacol

Ligand: [3H]D-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: DL-TBOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5 pKB
Reference (Journal): DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.
Published in: Mol Pharmacol
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 4

Ligand: DL-TBOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): Effects of threo-beta-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5).
Published in: J Neurochem
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 3

Ligand: [3H]L-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: [3H]ETB-TBOA (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.5 pKd
Reference (Journal): Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters.
Published in: Mol Pharmacol

Ligand: [3H]D-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: NBI-59159 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Ligands targeting the excitatory amino acid transporters (EAATs).
Published in: Curr Top Med Chem

Ligand: L-β-BA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pKi
Reference (Journal): The substituted aspartate analogue L-beta-threo-benzyl-aspartate preferentially inhibits the neuronal excitatory amino acid transporter EAAT3.
Published in: Neuropharmacology

Ligand: DL-TBOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pIC50
Reference (Journal): Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers.
Published in: Bioorg Med Chem Lett
Target family: Glutamate transporter subfamily (type: transporter)
Target: Excitatory amino acid transporter 2

Ligand: WAY-213613 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2.
Published in: Mol Pharmacol

Ligand: threo-3-methylglutamate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 4.7 pKB
Reference (Journal): Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2.
Published in: Mol Pharmacol

Ligand: SYM2081 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.5 pKB
Reference (Journal): Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2.
Published in: Mol Pharmacol

Ligand: [3H]SYM2081 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: [3H]L-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: [3H]ETB-TBOA (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKd
Reference (Journal): Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters.
Published in: Mol Pharmacol

Ligand: [3H]D-aspartic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Glycine receptors (type: lgic)
Target: glycine receptor &alpha;2 subunit

Ligand: colchicine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2009)
Primary target: no
Median affinity: 4.199999809265137 pIC50
Target family: Glycine receptors (type: lgic)
Target: glycine receptor &beta; subunit

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 3.700000047683716 pIC50

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.599999904632568 pIC50

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pIC50

Ligand: pregnenolone sulphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi

Ligand: pregnenolone sulphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pKi

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 5.300000190734863 pKi

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.700000047683716 pIC50

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pIC50
Target family: Glycine receptors (type: lgic)
Target: glycine receptor &alpha;2 subunit

Ligand: Cu2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pIC50

Ligand: cyanotriphenylborate (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Cyanotriphenylborate: subtype-specific blocker of glycine receptor chloride channels.
Published in: Proc Natl Acad Sci USA

Ligand: Δ9-tetrahydrocannabinol (Natural product)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 6 pEC50

Ligand: ginkgolide B (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: ginkgolide X (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pIC50

Ligand: HU-210 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50

Ligand: onternabez (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50

Ligand: picrotin (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pIC50
Target family: Glycine receptors (type: lgic)
Target: glycine receptor &alpha;2 subunit

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pIC50

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50

Ligand: PMBA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: pregnenolone sulphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi

Ligand: strychnine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]strychnine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 4.900000095367432 pKi

Ligand: WIN55212-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.4000000953674316 pIC50

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50