Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T48873 | Target Info | |||
| Target Name | Synaptic vesicle amine transporter (SLC18A2) | ||||
| Synonyms |
Vesicular amine transporter; Vesicular Monoamine Transporter; VMAT; VAT; Solute carrier family 18 member 2; SLC18A2; Monoamine transporter
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| Target Type | Successful Target | ||||
| Gene Name | SLC18A2 | ||||
| Biochemical Class | Major facilitator superfamily | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Serotonin transporter (SERT) | Successful Target | ||||
| UniProt ID | SC6A4_HUMAN | |||||
| Gene Name | SLC6A4 | |||||
| Synonyms |
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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| Representative Drug(s) | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | Ki = 0.73 nM | [1] | ||
| Co-Target Name | Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2) | Successful Target | ||||
| UniProt ID | ACHA4_HUMAN-ACHB2_HUMAN | |||||
| Gene Name | CHRNA4-CHRNB2 | |||||
| Synonyms |
CHRN; nAChR
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| Representative Drug(s) | Lobeline | Drug Info | Ki = 5.012 nM | [2] | ||
| Co-Target Name | 5-HT 2A receptor (HTR2A) | Successful Target | ||||
| UniProt ID | 5HT2A_HUMAN | |||||
| Gene Name | HTR2A | |||||
| Synonyms |
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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| Representative Drug(s) | NBI-98854 | Drug Info | Ki = 6.7 nM | Click to Show More | [3] | |
| 2 | Reserpine | Drug Info | Ki ~ 1000 nM | [3] | ||
| Co-Target Name | Multidrug resistance protein 1 (ABCB1) | Clinical trial Target | ||||
| UniProt ID | MDR1_HUMAN | |||||
| Gene Name | ABCB1 | |||||
| Synonyms |
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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| Representative Drug(s) | Reserpine | Drug Info | Ki = 100 nM | [4] | ||
| Co-Target Name | Norepinephrine transporter (NET) | Successful Target | ||||
| UniProt ID | SC6A2_HUMAN | |||||
| Gene Name | SLC6A2 | |||||
| Synonyms |
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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| Representative Drug(s) | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | Ki = 398 nM | [5] | ||
| Co-Target Name | Dopamine transporter (DAT) | Successful Target | ||||
| UniProt ID | SC6A3_HUMAN | |||||
| Gene Name | SLC6A3 | |||||
| Synonyms |
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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| Representative Drug(s) | METHYLENEDIOXYMETHAMPHETAMINE | Drug Info | Ki = 897 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter. Bioorg Med Chem. 2008 Jun 15;16(12):6364-70. | ||||
| REF 2 | Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1448-54. | ||||
| REF 3 | Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter. J Med Chem. 2018 Oct 25;61(20):9121-31. | ||||
| REF 4 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). J Med Chem. 2002 Dec 19;45(26):5671-86. | ||||
| REF 5 | An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3411-5. | ||||
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