Target family: Monoamine transporter subfamily (type: transporter)
Target: SERT

Ligand: duloxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2004)
Primary target: yes
Median affinity: 8.300000190734863 pKi
Reference (Journal): Design and synthesis of morpholine derivatives. SAR for dual serotonin &amp; noradrenaline reuptake inhibition.
Published in: Bioorg Med Chem Lett

Ligand: imipramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 7.690000057220459 pKi
Reference (Journal): The role of receptor binding in drug discovery.
Published in: J Nat Prod

Ligand: levomilnacipran (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013)
Primary target: yes
Median affinity: 6.489999771118164 pIC50
Reference (Journal): Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: lofepramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity: 7.21999979019165 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: lumateperone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.210000038146973 pKi
Reference (Journal): Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission.
Published in: Psychopharmacology (Berl.)

Ligand: lumateperone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.210000038146973 pKi
Reference (Journal): Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Published in: J Med Chem

Ligand: milnacipran (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009)
Primary target: yes
Median affinity: 7.300000190734863 pIC50
Reference (Journal): A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.
Published in: Bioorg Med Chem Lett

Ligand: nefazodone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1994)
Primary target: yes
Median affinity: 6.699999809265137 pKd
Reference (Journal): Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
Published in: Bioorg Med Chem Lett

Ligand: nortriptyline (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1964)
Primary target: yes
Median affinity: 8.15999984741211 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: norzotepine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.210000038146973 pIC50
Reference (Journal): Norzotepine, a major metabolite of zotepine, exerts atypical antipsychotic-like and antidepressant-like actions through its potent inhibition of norepinephrine reuptake.
Published in: J Pharmacol Exp Ther

Ligand: paroxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity: 10.100000381469727 pKd
Reference (Journal): X-ray structures and mechanism of the human serotonin transporter.
Published in: Nature

Ligand: paroxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1992)
Primary target: yes
Median affinity: 9.600000381469727 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: phenelzine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: protriptyline (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity: 7.710000038146973 pKd
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: sertraline (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 9.100000381469727 pKi

Ligand: sibutramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: no
Median affinity: 5.960000038146973 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: [3H]citalopram (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd

Ligand: [3H]paroxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKd

Ligand: toludesvenlafaxine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2022)
Primary target: no
Median affinity: 6.139999866485596 pIC50
Reference (Journal): Correction to "Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges".
Published in: J Med Chem

Ligand: trimipramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 6.829999923706055 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: venlafaxine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity: 7.570000171661377 pIC50
Reference (Journal): Heterocyclic cycloalkanol ethylamines as norepinephrine reuptake inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: vilazodone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Published in: J Med Chem

Ligand: vilazodone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders.
Published in: CNS Neurosci Ther

Ligand: vortioxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: yes
Median affinity: 8.800000190734863 pKi
Reference (Journal): Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Published in: J Med Chem

Ligand: ziprasidone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2001)
Primary target: no
Median affinity: 7.28000020980835 pKi

Ligand: zotepine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 5.139999866485596 pIC50
Reference (Journal): Norzotepine, a major metabolite of zotepine, exerts atypical antipsychotic-like and antidepressant-like actions through its potent inhibition of norepinephrine reuptake.
Published in: J Pharmacol Exp Ther