Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
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
AOFB_HUMAN
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 PF9601N 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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