Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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) | Metergolin | Drug Info | Ki = 0.5 nM | Click to Show More | [1] | |
2 | Sumatriptan | 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) | Sumatriptan | 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) | Metergolin | 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 | Sumatriptan | 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) | Sumatriptan | 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) | Sumatriptan | 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) | Sumatriptan | 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) | Sumatriptan | 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) | Sumatriptan | 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) | Metergolin | Drug Info | Ki = 6.31 nM | Click to Show More | [11] | |
2 | Sumatriptan | Drug Info | Ki = 1000 nM | [12] |
References | Top | ||||
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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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