Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T83875 Target Info
Target Name Monoamine oxidase type A (MAO-A)
Synonyms
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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Target Type Successful Target
Gene Name MAOA
Biochemical Class CH-NH(2) donor oxidoreductase
UniProt ID
AOFA_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 B (MAO-B) Successful Target
UniProt ID AOFB_HUMAN
Gene Name MAOB
Synonyms
MAO-B; Amine oxidase [flavin-containing] B
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Representative Drug(s) Tranylcypromine Drug Info IC50 = 9.4 nM Click to Show More [2]
2 PIPERINE Drug Info IC50 = 483 nM [6]
3 Clorgyline Drug Info IC50 ~ 1000 nM [8]
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 [3]
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 [3]
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 [4]
Co-Target Name Opioid receptor sigma 1 (OPRS1) Successful Target
UniProt ID SGMR1_HUMAN
Gene Name SIGMAR1
Synonyms
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) Moclobemide Drug Info Ki ~ 100 nM [5]
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 [7]
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 [9]
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 [10]
Co-Target Name Sigma intracellular receptor 2 (TMEM97) Clinical trial Target
UniProt ID SGMR2_HUMAN
Gene Name TMEM97
Synonyms
Transmembrane protein 97; Sigma2 receptor; Sigma-2 receptor; Meningioma-associated protein 30; MAC30
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Representative Drug(s) Moclobemide Drug Info Ki ~ 200 nM [5]
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 [11]
References  Top
REF 1 Alpha-ethyltryptamines as dual dopamine-serotonin releasers. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4754-8.
REF 2 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 3 Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors. J Med Chem. 1996 Jan 5;39(1):314-22.
REF 4 Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1-12.
REF 5 Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 protein ligands. Eur J Med Chem. 2017 Sep 29;138:964-78.
REF 6 Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7183-8.
REF 7 Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr Drug Metab. 2005 Oct;6(5):413-54.
REF 8 Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors. Bioorg Med Chem. 2015 Oct 1;23(19):6486-96.
REF 9 5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS. Med Chem Res. 2005;4:1-18.
REF 10 Structure-activity relationships of serotonin 5-HT 7 receptors ligands: A review. Eur J Med Chem. 2019 Dec 1;183:111705.
REF 11 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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