Target family: Histamine receptors (type: gpcr)
Target: H<sub>4</sub> receptor

Ligand: 2-(3-bromophenyl)histamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: 2-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: 2-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: 4-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: 4-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: adriforant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.3100004196167 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:  pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: burimamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: CCL16 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Liver-expressed chemokine/CC chemokine ligand 16 attracts eosinophils by interacting with histamine H4 receptor.
Published in: J Immunol

Ligand: ciproxifan (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.730000019073486 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: 5.730000019073486 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
Primary target: no
Median affinity: 5.730000019073486 pKi
Reference (Journal): Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
Published in: Biochem Pharmacol

Ligand: clobenpropit (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
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: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
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: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: clobenpropit (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
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: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 5.5 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 5.7 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
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: dimaprit (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: dimaprit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: dimaprit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: dimaprit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: H4 antagonist 48 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.570000171661377 pIC50
Reference (Journal): Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.
Published in: J Med Chem

Ligand: H4 antagonist 48 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.539999961853027 pIC50
Reference (Journal): Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis.
Published in: J Med Chem

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

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: 7.4 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: histamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: HTMT (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: imetit (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
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: 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: 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): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: improgan (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: impromidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: impromidine (Synthetic organic)
Interaction type: Agonist
Action: Partial 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: INCB-38579 (Synthetic organic)
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: N-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: N-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: N-ethylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: N-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
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): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: N-[3H]methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKd
Reference (Journal): Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
Published in: Mol Pharmacol

Ligand: N,N-dimethylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.
Published in: Br J Pharmacol

Ligand: iodophenpropit (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
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): Cloning, expression, and pharmacological characterization of a novel human histamine receptor.
Published in: Mol Pharmacol

Ligand: (R)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
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): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
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): 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: 6.4 pKi
Reference (Journal): Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation.
Published in: J Pharmacol Exp Ther

Ligand: (S)-α-methylhistamine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Cloning and characterization of a novel human histamine receptor.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-10191584 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKi
Reference (Journal): Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: JNJ-39758979 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev

Ligand: JNJ-39758979 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.
Published in: J Med Chem

Ligand: JNJ 7777120 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
Published in: J Med Chem

Ligand: JNJ 7777120 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.
Published in: J Pharmacol Exp Ther

Ligand: JNJ 7777120 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Published in: J Pharmacol Exp Ther

Ligand: methimepip (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 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: 5 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: no
Median affinity: 4 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev