Target Information
| Target General Information | Top | |||||
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| Target ID |
T15571
(Former ID: TTDR00565)
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| Target Name |
5-HT 5A receptor (HTR5A)
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| Synonyms |
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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| Gene Name |
HTR5A
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
| Function |
The activity of this receptor is mediated by G proteins. This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLL
VLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIAC DVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFG WGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVS PISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIP FFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Metergolin | Drug Info | Approved | Hyperprolactinaemia | [2] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Antagonist | [+] 5 Antagonist drugs | + | ||||
| 1 | Metergolin | Drug Info | [1] | |||
| 2 | bufotenine | Drug Info | [6] | |||
| 3 | MPDT | Drug Info | [7] | |||
| 4 | SB 699551 | Drug Info | [9] | |||
| 5 | SB-699551-A | Drug Info | [10] | |||
| Inhibitor | [+] 16 Inhibitor drugs | + | ||||
| 1 | (+/-)-nantenine | Drug Info | [3] | |||
| 2 | 3,4-dihydroquinazolin-2-amine hydrobromide | Drug Info | [4] | |||
| 3 | 4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 4 | 4-methyl-N-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | [5] | |||
| 5 | 4-propyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 6 | 5,6-dichloro-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 7 | 5-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 8 | 5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 9 | 5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 10 | 8-chloro-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 11 | 8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 12 | METHIOTHEPIN | Drug Info | [8] | |||
| 13 | N,4-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [5] | |||
| 14 | N,N-dimethyl-3,4-dihydroquinazolin-2-amine | Drug Info | [4] | |||
| 15 | N-butyl-4-methyl-3,4-dihydroquinazolin-2-amine | Drug Info | [5] | |||
| 16 | SEROTONIN | Drug Info | [11] | |||
| Agonist | [+] 6 Agonist drugs | + | ||||
| 1 | 5-CT | Drug Info | [6] | |||
| 2 | EDMT | Drug Info | [7] | |||
| 3 | lysergic acid | Drug Info | [6] | |||
| 4 | TFMPP | Drug Info | [12] | |||
| 5 | [125I]LSD | Drug Info | [13] | |||
| 6 | [3H]5-CT | Drug Info | [13] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Serotonergic synapse | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | |||||
| Reactome | [+] 2 Reactome Pathways | + | ||||
| 1 | Serotonin receptors | |||||
| 2 | G alpha (i) signalling events | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | Monoamine GPCRs | |||||
| 2 | GPCRs, Class A Rhodopsin-like | |||||
| 3 | GPCR ligand binding | |||||
| 4 | GPCR downstream signaling | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Cloning and characterisation of the human 5-HT5A serotonin receptor. FEBS Lett. 1994 Dec 5;355(3):242-6. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. | |||||
| REF 4 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. | |||||
| REF 5 | Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. Bioorg Med Chem Lett. 2008 Jan 1;18(1):262-6. | |||||
| REF 6 | Expression of functional mouse 5-HT5A serotonin receptor in the methylotrophic yeast Pichia pastoris: pharmacological characterization and localization. FEBS Lett. 1995 Dec 27;377(3):451-6. | |||||
| REF 7 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8. | |||||
| REF 8 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812. | |||||
| REF 9 | Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8. | |||||
| REF 10 | 5-ht5A receptors as a therapeutic target. Pharmacol Ther. 2006 Sep;111(3):707-14. | |||||
| REF 11 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69. | |||||
| REF 12 | Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. Mol Pharmacol. 1993 Mar;43(3):313-9. | |||||
| REF 13 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. Eur J Pharmacol. 2001 Apr 27;418(3):157-67. | |||||
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