Target family: Histamine receptors (type: gpcr)
Target: H<sub>3</sub> receptor

Ligand: A-304121 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: A-304121 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: A-304121 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-304121 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: A-317920 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: A331440 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: A-349821 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: A-349821 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: ABT-239 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Published in: J Pharmacol Exp Ther

Ligand: ABT-239 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Published in: J Pharmacol Exp Ther

Ligand: adriforant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.730000019073486 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: cipralisant (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: cipralisant (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 5.8 pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: compound 3a [PMID: 18606542] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.
Published in: Bioorg Med Chem Lett

Ligand: conessine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: dimaprit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: enerisant (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): A Novel Potent and Selective Histamine H<sub>3</sub> Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents.
Published in: J Pharmacol Exp Ther

Ligand: enerisant (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.779999732971191 pKi
Reference (Journal): A Novel Potent and Selective Histamine H<sub>3</sub> Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents.
Published in: J Pharmacol Exp Ther

Ligand: FUB 349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: FUB 349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: FUB 349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: FUB 465 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: GR 175737 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: GR 175737 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: GSK-189254 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.
Published in: J Pharmacol Exp Ther

Ligand: GSK334429 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.
Published in: Eur J Med Chem

Ligand: GSK334429 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pKi
Reference (Journal): Histamine H3 receptor as a drug discovery target.
Published in: J Med Chem

Ligand: GT2394 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: GT2394 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Published in: J Med Chem

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: imbutamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Published in: J Med Chem

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.8 pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: immepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Published in: J Med Chem

Ligand: immethridine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKi
Reference (Journal): Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.
Published in: J Med Chem

Ligand: impentamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: impentamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: impentamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists.
Published in: J Med Chem

Ligand: impromidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: INCB-38579 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: N-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: N-[3H]α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: N-[3H]methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: N-[3H]methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: iodoproxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.6 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: iodoproxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Molecular and pharmacological characterization of the mouse histamine H3 receptor.
Published in: Eur J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: (S)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: (S)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: JB 98064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: JB 98064 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: JNJ-39758979 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: JNJ-5207852 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
Published in: J Med Chem

Ligand: methimepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
Published in: J Med Chem

Ligand: MK-0249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: MK-0249 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pKi
Reference (Journal): Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Published in: J Med Chem

Ligand: PF-03654746 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.640000343322754 pKi
Reference (Journal): Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Published in: J Med Chem

Ligand: PF-03654746 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.429999828338623 pKi
Reference (Journal): Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).
Published in: J Med Chem

Ligand: pitolisant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2016), FDA (2019)
Primary target: yes
Median affinity:  pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: pitolisant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2016), FDA (2019)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
Published in: Bioorg Med Chem

Ligand: proxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: proxyfan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: proxyfan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: proxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: proxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: proxyfan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: ST-1478 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pKi
Reference (Journal): Novel compounds with dual S1P receptor agonist and histamine H<sub>3</sub> receptor antagonist activities act protective in a mouse model of multiple sclerosis.
Published in: Neuropharmacology

Ligand: ST-1505 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.25 pKi
Reference (Journal): Novel compounds with dual S1P receptor agonist and histamine H<sub>3</sub> receptor antagonist activities act protective in a mouse model of multiple sclerosis.
Published in: Neuropharmacology

Ligand: [123I]iodoproxyfan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.3 pKd
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: [123I]iodoproxyfan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: [125I]iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Characterization of the binding of the first selective radiolabelled histamine H3-receptor antagonist, [125I]-iodophenpropit, to rat brain.
Published in: Br J Pharmacol

Ligand: [3H]histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Discovery of a novel member of the histamine receptor family.
Published in: Mol Pharmacol

Ligand: [3H]histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: [3H](R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: SUVN-G3031 (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.0600004196167 pKi
Reference (Journal): Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H<sub>3</sub> Receptor Inverse Agonist with Robust Wake-Promoting Activity.
Published in: J Med Chem

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Published in: Biochem J

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The rat H3 receptor: gene organization and multiple isoforms.
Published in: Biochem Biophys Res Commun

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characteristics of recombinantly expressed rat and human histamine H3 receptors.
Published in: Eur J Pharmacol

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
Published in: J Pharmacol Exp Ther

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
Published in: Br J Pharmacol

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
Published in: J Neurochem

Ligand: thioperamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: UCL-2138 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: VUF14738 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pKi
Reference (Journal): Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology.
Published in: J Am Chem Soc

Ligand: VUF14862 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 pKi
Reference (Journal): Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology.
Published in: J Am Chem Soc

Ligand: VUF 4904 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: VUF 5207 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther

Ligand: VUF 8328 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
Published in: J Pharmacol Exp Ther