Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T83011 | Target Info | |||
| Target Name | Monoamine oxidase type B (MAO-B) | ||||
| Synonyms |
MAO-B; Amine oxidase [flavin-containing] B
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| Target Type | Successful Target | ||||
| Gene Name | MAOB | ||||
| Biochemical Class | CH-NH(2) donor oxidoreductase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | TRYPTAMINE | Drug Info | EC50 = 7.36 nM | [1] | ||
| Co-Target Name | Monoamine oxidase type A (MAO-A) | Successful Target | ||||
| UniProt ID | AOFA_HUMAN | |||||
| Gene Name | MAOA | |||||
| Synonyms |
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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| Representative Drug(s) | Pargyline | Drug Info | IC50 = 11.52 nM | Click to Show More | [2] | |
| 2 | Selegiline | Drug Info | IC50 = 67.25 nM | [7] | ||
| 3 | Tranylcypromine | Drug Info | IC50 = 85 nM | [8] | ||
| 4 | Phenelzine | Drug Info | Ki = 163 nM | [9] | ||
| 5 | Drug Info | IC50 = 287.3 nM | [10] | |||
| 6 | Rasagiline | Drug Info | IC50 = 410 nM | [11] | ||
| Co-Target Name | Acetylcholinesterase (AChE) | Successful Target | ||||
| UniProt ID | ACES_HUMAN | |||||
| Gene Name | ACHE | |||||
| Synonyms |
YT; N-ACHE; ARACHE
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| Representative Drug(s) | Rasagiline | Drug Info | IC50 = 19 nM | [3] | ||
| Co-Target Name | Membrane copper amine oxidase (AOC3) | Successful Target | ||||
| UniProt ID | AOC3_HUMAN | |||||
| Gene Name | AOC3 | |||||
| Synonyms |
Vascular adhesion protein-1; Vascular adhesion protein 1; VAP1; VAP-1; Semicarbazide-sensitive amine oxidase; SSAO; Membrane primary amine oxidase; HPAO; Copper amine oxidase
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| Representative Drug(s) | Phenelzine | Drug Info | IC50 = 19.95 nM | [4] | ||
| Co-Target Name | 5-HT 1D receptor (HTR1D) | Successful Target | ||||
| UniProt ID | 5HT1D_HUMAN | |||||
| Gene Name | HTR1D | |||||
| Synonyms |
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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| Representative Drug(s) | TRYPTAMINE | Drug Info | Ki = 23 nM | [5] | ||
| Co-Target Name | 5-HT 1B receptor (HTR1B) | Successful Target | ||||
| UniProt ID | 5HT1B_HUMAN | |||||
| Gene Name | HTR1B | |||||
| Synonyms |
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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| Representative Drug(s) | TRYPTAMINE | Drug Info | Ki = 36 nM | [5] | ||
| Co-Target Name | 5-HT 2C receptor (HTR2C) | Successful Target | ||||
| UniProt ID | 5HT2C_HUMAN | |||||
| Gene Name | HTR2C | |||||
| Synonyms |
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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| Representative Drug(s) | TRYPTAMINE | Drug Info | Ki = 50 nM | [6] | ||
| Co-Target Name | Cytochrome P450 2A6 (CYP2A6) | Successful Target | ||||
| UniProt ID | CP2A6_HUMAN | |||||
| Gene Name | CYP2A6 | |||||
| Synonyms |
Cytochrome P450(I); Cytochrome P450 IIA3; Coumarin 7-hydroxylase; CYPIIA6; CYP2A6; CYP2A3
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| Representative Drug(s) | Psoralen | Drug Info | Ki = 600 nM | [12] | ||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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| Representative Drug(s) | Budipine | Drug Info | IC50 = 851.14 nM | [13] | ||
| Co-Target Name | 5-HT 6 receptor (HTR6) | Clinical trial Target | ||||
| UniProt ID | 5HT6R_HUMAN | |||||
| Gene Name | HTR6 | |||||
| Synonyms |
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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| Representative Drug(s) | TRYPTAMINE | Drug Info | Ki = 70 nM | [14] | ||
| Co-Target Name | 5-HT 7 receptor (HTR7) | Clinical trial Target | ||||
| UniProt ID | 5HT7R_HUMAN | |||||
| Gene Name | HTR7 | |||||
| Synonyms |
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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| Representative Drug(s) | TRYPTAMINE | Drug Info | Ki = 158.49 nM | [15] | ||
| Co-Target Name | Myeloperoxidase (MPO) | Clinical trial Target | ||||
| UniProt ID | PERM_HUMAN | |||||
| Gene Name | MPO | |||||
| Synonyms |
MPO
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| Representative Drug(s) | TRYPTAMINE | Drug Info | IC50 = 770 nM | [16] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Alpha-ethyltryptamines as dual dopamine-serotonin releasers. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4754-8. | ||||
| REF 2 | Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid- aggregation for the treatment of Alzheimer's disease. Eur J Med Chem. 2017 Sep 29;138:715-728. | ||||
| REF 3 | Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease. Bioorg Med Chem Lett. 2017 Nov 15;27(22):5053-9. | ||||
| REF 4 | Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1. J Med Chem. 2010 Sep 9;53(17):6301-15. | ||||
| REF 5 | Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors. J Med Chem. 1996 Jan 5;39(1):314-22. | ||||
| REF 6 | Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1-12. | ||||
| REF 7 | Synthesis and selective human monoamine oxidase inhibition of 3-carbonyl, 3-acyl, and 3-carboxyhydrazido coumarin derivatives. Eur J Med Chem. 2011 Oct;46(10):4846-52. | ||||
| REF 8 | Identification of selective and reversible LSD1 inhibitors with anti-metastasis activity by high-throughput docking. Bioorg Med Chem Lett. 2019 Feb 15;29(4):544-548. | ||||
| REF 9 | Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B. J Nat Prod. 2016 Oct 28;79(10):2538-2544. | ||||
| REF 10 | N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor. J Med Chem. 2014 Dec 26;57(24):10455-63. | ||||
| REF 11 | Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72. | ||||
| REF 12 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr Drug Metab. 2005 Oct;6(5):413-54. | ||||
| REF 13 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
| REF 14 | 5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS. Med Chem Res. 2005;4:1-18. | ||||
| REF 15 | Structure-activity relationships of serotonin 5-HT 7 receptors ligands: A review. Eur J Med Chem. 2019 Dec 1;183:111705. | ||||
| REF 16 | Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors. J Med Chem. 2013 May 23;56(10):3943-58. | ||||
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