Target family: Nicotinic acetylcholine receptors  (nACh) (type: lgic)
Target: nicotinic acetylcholine receptor &alpha;4 subunit

Ligand: A-867744 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Published in: J Pharmacol Exp Ther

Ligand: atracurium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1983), UK (1999)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Distinct pharmacologic properties of neuromuscular blocking agents on human neuronal nicotinic acetylcholine receptors: a possible explanation for the train-of-four fade.
Published in: Anesthesiology

Ligand: hexamethonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.039999961853027 pIC50

Ligand: hexamethonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: LY2087101 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators.
Published in: J Pharmacol Exp Ther

Ligand: mecamylamine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2013)
Primary target: no
Median affinity:  pIC50

Ligand: mecamylamine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2013)
Primary target: no
Median affinity:  pIC50

Ligand: nicotine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 8.65999984741211 pKi
Reference (Journal): Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Published in: J Med Chem

Ligand: NS1738 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo.
Published in: J Pharmacol Exp Ther

Ligand: NS9283 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): α4β2 neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of α4β2 nAChR agonists in pain.
Published in: Biochem Pharmacol

Ligand: rivanicline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): 3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.
Published in: Bioorg Med Chem Lett

Ligand: rivanicline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pKi
Reference (Journal): RJR-2403: a nicotinic agonist with CNS selectivity I. In vitro characterization.
Published in: J Pharmacol Exp Ther

Ligand: [125I]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [125I]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [125I]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [125I]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.729999542236328 pKd

Ligand: [3H]cytisine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [3H]cytisine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKd

Ligand: [3H]cytisine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKd

Ligand: [3H]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [3H]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.729999542236328 pKd

Ligand: [3H]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [3H]epibatidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [3H]nicotine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKd

Ligand: SUVN-911 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 pKi
Reference (Journal): Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Published in: J Med Chem

Ligand: TC-2559 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices.
Published in: Neuropharmacology

Ligand: tebanicline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 10.430000305175781 pKi
Reference (Journal): ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization.
Published in: J Pharmacol Exp Ther

Ligand: varenicline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: no
Median affinity: 10.399999618530273 pKi
Reference (Journal): Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Published in: J Med Chem

Ligand: varenicline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: yes
Median affinity: 9.960000038146973 pKi
Reference (Journal): 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation.
Published in: Bioorg Med Chem Lett