Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T11072 Target Info
Target Name 5-HT 1D receptor (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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Target Type Successful Target
Gene Name HTR1D
Biochemical Class GPCR rhodopsin
UniProt ID
5HT1D_HUMAN
Co-Targets of This Target  Top
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) Drug Info Ki = 0.5 nM Click to Show More [1]
2 Drug Info IC50 = 7.3 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) Drug Info IC50 = 0.5012 nM Click to Show More [2]
2 Zolmitriptan Drug Info Ki = 4.2 nM [4]
3 Rizatriptan Drug Info Ki = 10.1 nM [6]
4 Frovatriptan Drug Info Ki = 10.3 nM [6]
Co-Target Name 5-HT 1A receptor (HTR1A) Successful Target
UniProt ID 5HT1A_HUMAN
Gene Name HTR1A
Synonyms
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) Drug Info Ki = 2.3 nM Click to Show More [3]
2 Frovatriptan Drug Info Ki = 62 nM [6]
3 Zolmitriptan Drug Info Ki = 78.6 nM [8]
4 Rizatriptan Drug Info Ki = 140 nM [6]
5 Drug Info Ki = 230 nM [6]
Co-Target Name 5-HT 3A receptor (HTR3A) Successful Target
UniProt ID 5HT3A_HUMAN
Gene Name HTR3A
Synonyms
Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
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Representative Drug(s) Drug Info IC50 = 9.3 nM [5]
Co-Target Name 5-HT 1F receptor (HTR1F) Successful Target
UniProt ID 5HT1F_HUMAN
Gene Name HTR1F
Synonyms
Serotonin receptor 1F; HTR1EL; 5-hydroxytryptamine receptor 1F; 5-HT1F receptor; 5-HT1F; 5-HT-1F
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Representative Drug(s) Drug Info Ki = 25.7 nM [7]
Co-Target Name Dopamine D2 receptor (D2R) Successful Target
UniProt ID DRD2_HUMAN
Gene Name DRD2
Synonyms
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) Drug Info Ki ~ 218 nM [9]
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) Drug Info Ki = 376 nM [9]
Co-Target Name 5-HT 5A receptor (HTR5A) Successful Target
UniProt ID 5HT5A_HUMAN
Gene Name HTR5A
Synonyms
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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Representative Drug(s) Drug Info IC50 = 501.19 nM [10]
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) Drug Info Ki = 6.31 nM Click to Show More [11]
2 Drug Info Ki = 1000 nM [12]
References  Top
REF 1 Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1-12.
REF 2 Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation. J Med Chem. 2001 Mar 1;44(5):681-93.
REF 3 Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1834-8.
REF 4 Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist. Bioorg Med Chem Lett. 1998 Mar 17;8(6):675-80.
REF 5 Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents. J Med Chem. 1997 Oct 24;40(22):3501-3.
REF 6 N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. J Med Chem. 1999 Feb 11;42(3):526-31.
REF 7 N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy. J Med Chem. 2001 Nov 22;44(24):4031-4.
REF 8 Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors. J Med Chem. 1995 Sep 1;38(18):3602-7.
REF 9 Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects. J Med Chem. 1998 Jun 18;41(13):2180-3.
REF 10 Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor. J Med Chem. 1994 Sep 16;37(19):3023-32.
REF 11 Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives. J Med Chem. 2003 Dec 18;46(26):5638-50.
REF 12 Structure-activity relationships of serotonin 5-HT 7 receptors ligands: A review. Eur J Med Chem. 2019 Dec 1;183:111705.

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