Target family: GABA<sub>B</sub> receptors (type: gpcr)
Target: GABA<sub>B</sub> receptor

Ligand: [3H]CGP 54626 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2.
Published in: Nature

Ligand: [125I]CGP 71872 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
Published in: Nature

Ligand: [125I]CGP 64213 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Ca(2+) requirement for high-affinity gamma-aminobutyric acid (GABA) binding at GABA(B) receptors: involvement of serine 269 of the GABA(B)R1 subunit.
Published in: Mol Pharmacol

Ligand: SCH 50911 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: SCH 50911 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: SCH 50911 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): The pharmacology of SCH 50911: a novel, orally-active GABA-beta receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: saclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: saclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: saclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pIC50
Reference (Journal): International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
Published in: Pharmacol Rev

Ligand: phaclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 3.9 pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: phaclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.1 pIC50
Reference (Journal): International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
Published in: Pharmacol Rev

Ligand: rac-BHFF (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 pEC50
Reference (Journal): Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors.
Published in: Br J Pharmacol

Ligand: GS39783 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.679999828338623 pKB
Reference (Journal): N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.
Published in: J Pharmacol Exp Ther

Ligand: GS39783 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.679999828338623 pKB
Reference (Journal): &quot;Selective&quot; Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu<sub>5</sub> Allosteric Ligands.
Published in: Mol Pharmacol

Ligand: GABA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Book): Chemistry of GABA<sub>B</sub> modulators.
Published in: The GABA Receptors

Ligand: GABA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: GABA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: compound 14 [PMID: 25050158] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 4.420000076293945 pIC50
Reference (Journal): Discovery of a Negative Allosteric Modulator of GABAB Receptors.
Published in: ACS Med Chem Lett

Ligand: CGP7930 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501.
Published in: Mol Pharmacol

Ligand: CGP 62349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: CGP 62349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: CGP 55845 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pIC50
Reference (Journal): International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
Published in: Pharmacol Rev

Ligand: CGP 55845 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: CGP 54626A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: CGP 54626A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: CGP 46381 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: CGP 44532 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Book): Chemistry of GABA<sub>B</sub> modulators.
Published in: The GABA Receptors

Ligand: CGP 36742 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
Published in: Pharmacol Rev

Ligand: CGP 35348 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pIC50
Reference (Journal): International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function.
Published in: Pharmacol Rev

Ligand: CGP 35348 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: baclofen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: baclofen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: (-)-baclofen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Book): Chemistry of GABA<sub>B</sub> modulators.
Published in: The GABA Receptors

Ligand: 3-APPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterisation of a cell line expressing GABA B1b and GABA B2 receptor subunits.
Published in: Biochem Pharmacol

Ligand: 3-APPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Book): Chemistry of GABA<sub>B</sub> modulators.
Published in: The GABA Receptors

Ligand: 3-APMPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): The human GABA(B1b) and GABA(B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen.
Published in: Br J Pharmacol

Ligand: 3-APMPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Book): Chemistry of GABA<sub>B</sub> modulators.
Published in: The GABA Receptors

Ligand: 2-hydroxy-saclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.1 pIC50
Reference (Journal): Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
Published in: Nature