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

Ligand: atomoxetine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2002)
Primary target: no
Median affinity: 5.96999979019165 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: benzatropine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1954)
Primary target: no
Median affinity: 6.929999828338623 pKi
Reference (Journal): Novel 4'-substituted and 4',4&quot;-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
Published in: J Med Chem

Ligand: bupropion (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity: 6.349999904632568 pIC50
Reference (Journal): Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
Published in: J Med Chem

Ligand: clomipramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 5.659999847412109 pKd
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: cocaine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Published in: J Med Chem

Ligand: compound 58 [PMID: 25037917] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.210000038146973 pIC50
Reference (Journal): Novel inhibitors of the high-affinity L-proline transporter as potential therapeutic agents for the treatment of cognitive disorders.
Published in: Bioorg Med Chem Lett

Ligand: desvenlafaxine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2008)
Primary target: no
Median affinity: 6.070000171661377 pKi
Reference (Journal): Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Published in: ACS Med Chem Lett

Ligand: dexamfetamine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1955, in complex; 1975 as Dextroamphetamine sulphate)
Primary target: yes
Median affinity: 6.960000038146973 pKi
Reference (Journal): An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Published in: Bioorg Med Chem Lett

Ligand: dexmethylphenidate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2001)
Primary target: yes
Median affinity: 7.599999904632568 pKi
Reference (Journal): Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.
Published in: Bioorg Med Chem

Ligand: GBR12935 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi

Ligand: levomilnacipran (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013)
Primary target: no
Median affinity: 5.489999771118164 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: mazindol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity: 8 pKi

Ligand: methylphenidate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1955)
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
Published in: J Med Chem

Ligand: modafinil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1998)
Primary target: no
Median affinity: 5.420000076293945 pKi
Reference (Journal): Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.
Published in: J Med Chem

Ligand: nomifensine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (approval date not specified, withdrawn 1992)
Primary target: yes
Median affinity:  -

Ligand: phenelzine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Primary target: no
Median affinity: 5.079999923706055 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: sibutramine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 6.300000190734863 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: solriamfetol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: no
Median affinity: 4.849999904632568 pKi
Reference (Journal): Characterization of the Neurochemical and Behavioral Effects of Solriamfetol (JZP-110), a Selective Dopamine and Norepinephrine Reuptake Inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: solriamfetol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: no
Median affinity: 5.539999961853027 pIC50
Reference (Journal): Characterization of the Neurochemical and Behavioral Effects of Solriamfetol (JZP-110), a Selective Dopamine and Norepinephrine Reuptake Inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]GBR12935 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): Pharmacological heterogeneity of the cloned and native human dopamine transporter: disassociation of [3H]WIN 35,428 and [3H]GBR 12,935 binding.
Published in: Mol Pharmacol

Ligand: [3H]WIN35428 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pKd
Reference (Journal): Pharmacological heterogeneity of the cloned and native human dopamine transporter: disassociation of [3H]WIN 35,428 and [3H]GBR 12,935 binding.
Published in: Mol Pharmacol

Ligand: toludesvenlafaxine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2022)
Primary target: no
Median affinity: 6.309999942779541 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: 5.420000076293945 pKi
Reference (Journal): Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Published in: Eur J Pharmacol

Ligand: vanoxerine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action.
Published in: Eur J Pharmacol

Ligand: vanoxerine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Behavioral properties of GBR 12909, GBR 13069 and GBR 13098: specific inhibitors of dopamine uptake.
Published in: Eur J Pharmacol

Ligand: vanoxerine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Pharmacological characterization of the discriminative-stimulus effects of GBR 12909.
Published in: J Pharmacol Exp Ther

Ligand: WIN35428 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Translocation of dopamine and binding of WIN 35,428 measured under identical conditions in cells expressing the cloned human dopamine transporter.
Published in: Naunyn Schmiedebergs Arch Pharmacol