Target family: Histamine receptors (type: gpcr)
Target: H<sub>2</sub> receptor

Ligand: ABT-239 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 5.2 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: amthamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): N(G)-acylated aminothiazolylpropylguanidines as potent and selective histamine H(2) receptor agonists.
Published in: ChemMedChem

Ligand: arpromidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors.
Published in: Proc Natl Acad Sci USA

Ligand: burimamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Constitutive activity and structural instability of the wild-type human H2 receptor.
Published in: J Neurochem

Ligand: cimetidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: cimetidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 6.849999904632568 pKi
Reference (Journal): Synthesis and structure-activity relationship studies in serotonin 5-HT1A receptor agonists based on fused pyrrolidone scaffolds.
Published in: Eur J Med Chem

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: clobenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 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: conessine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: famotidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: yes
Median affinity:  -

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.8 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: impromidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: INCB-38579 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: iodoaminopotentidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br 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: metiamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: MK-0249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: oxo-arpromidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther

Ligand: pitolisant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2016), FDA (2019)
Primary target: no
Median affinity: 4.960000038146973 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: ranitidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity: 6.199999809265137 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: ranitidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity: 7.099999904632568 pKi
Reference (Journal): Pharmacological characterization of the human histamine H2 receptor stably expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: ST-1006 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
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: [125I]iodoaminopotentidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): G proteins of the Gq family couple the H2 histamine receptor to phospholipase C.
Published in: Mol Endocrinol

Ligand: [3H]tiotidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model.
Published in: Mol Pharmacol

Ligand: tiotidine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: UR-PG146 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Probing ligand-specific histamine H1- and H2-receptor conformations with NG-acylated Imidazolylpropylguanidines.
Published in: J Pharmacol Exp Ther