Target family: Sigma receptors (type: other_protein)
Target: sigma non-opioid intracellular receptor 1

Ligand: 1,3-ditolylguanidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.449999809265137 pKi
Reference (Journal): Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503.
Published in: Synapse

Ligand: BD-1047 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism.
Published in: Eur J Pharmacol

Ligand: BD-1063 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Published in: J Med Chem

Ligand: blarcamesine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.070000171661377 pIC50
Reference (Journal): Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative.
Published in: J Psychopharmacol

Ligand: dextromethorphan (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1982)
Primary target: no
Median affinity: 6.28000020980835 pKi
Reference (Journal): Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line.
Published in: J Pharmacol Exp Ther

Ligand: E-52862 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.769999980926514 pKi
Reference (Journal): Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Published in: J Med Chem

Ligand: EST64454 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pKi
Reference (Journal): EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management
Published in: J Med Chem

Ligand: EST73502 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.929999828338623 pKi
Reference (Journal): Discovery of EST73502, a Dual &#x3bc;-Opioid Receptor Agonist and &#x3c3;<sub>1</sub> Receptor Antagonist Clinical Candidate for the Treatment of Pain.
Published in: J Med Chem

Ligand: fluvoxamine (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA (1994)
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
Published in: ACS Med Chem Lett

Ligand: fluvoxamine (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA (1994)
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): The sigma enigma: can sigma receptors provide a novel target for disorders of mood and cognition?
Published in: J Clin Psychiatry

Ligand: NE-100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): NE-100, a novel sigma receptor ligand: in vivo tests.
Published in: Life Sci

Ligand: opipramol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 9.699999809265137 pKi
Reference (Journal): Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
Published in: J Med Chem

Ligand: PD-144418 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKi
Reference (Journal): The pharmacology of the novel and selective sigma ligand, PD 144418.
Published in: Neuropharmacology

Ligand: (-)-pentazocine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  -

Ligand: PRE-084 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand.
Published in: J Pharmacol Exp Ther

Ligand: (RS)-PPCC (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Novel sigma receptor ligands: synthesis and biological profile.
Published in: J Med Chem

Ligand: (+)-SKF 10.047 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]pentazocine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: vanoxerine (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain.
Published in: Life Sci