Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T07806 | Target Info | |||
| Target Name | 5-HT 1B receptor (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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| Target Type | Successful Target | ||||
| Gene Name | HTR1B | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| 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) | Metergolin | Drug Info | Ki = 0.5 nM | [1] | ||
| 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) | Zolmitriptan | Drug Info | Ki = 0.76 nM | Click to Show More | [2] | |
| 2 | Naratriptan | Drug Info | EC50 = 1.6 nM | [4] | ||
| 3 | Frovatriptan | Drug Info | Ki = 4.4 nM | [4] | ||
| 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) | Fluphenazine | Drug Info | Ki = 1.44 nM | [3] | ||
| 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 | [5] | |
| 2 | Naratriptan | Drug Info | Ki = 45 nM | [4] | ||
| 3 | Frovatriptan | Drug Info | Ki = 62 nM | [4] | ||
| 4 | Zolmitriptan | Drug Info | Ki = 78.6 nM | [6] | ||
| Co-Target Name | Dopamine D3 receptor (D3R) | Successful Target | ||||
| UniProt ID | DRD3_HUMAN | |||||
| Gene Name | DRD3 | |||||
| Synonyms |
D(3) dopamine receptor
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| Representative Drug(s) | Fluphenazine | Drug Info | Ki = 3.21 nM | [3] | ||
| Co-Target Name | Dopamine D5 receptor (D5R) | Successful Target | ||||
| UniProt ID | DRD5_HUMAN | |||||
| Gene Name | DRD5 | |||||
| Synonyms |
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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| Representative Drug(s) | Fluphenazine | Drug Info | Ki = 21 nM | [3] | ||
| Co-Target Name | Histamine H1 receptor (H1R) | Successful Target | ||||
| UniProt ID | HRH1_HUMAN | |||||
| Gene Name | HRH1 | |||||
| Synonyms |
HH1R; H1R
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| Representative Drug(s) | Fluphenazine | Drug Info | Ki = 40 nM | [3] | ||
| Co-Target Name | Dopamine D1 receptor (D1R) | Successful Target | ||||
| UniProt ID | DRD1_HUMAN | |||||
| Gene Name | DRD1 | |||||
| Synonyms |
D(1A) dopamine receptor
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| Representative Drug(s) | Fluphenazine | Drug Info | Ki = 179 nM | [3] | ||
| 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 | [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) | Fluphenazine | Drug Info | Ki < 50 nM | [8] | ||
| Co-Target Name | Histamine H3 receptor (H3R) | Clinical trial Target | ||||
| UniProt ID | HRH3_HUMAN | |||||
| Gene Name | HRH3 | |||||
| Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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| Representative Drug(s) | Fluphenazine | Drug Info | Ki ~ 1000 nM | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1-12. | ||||
| REF 2 | 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 3 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42. | ||||
| REF 4 | N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. J Med Chem. 1999 Feb 11;42(3):526-31. | ||||
| REF 5 | 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 6 | 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 7 | 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 8 | Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. J Med Chem. 2005 Mar 24;48(6):1781-95. | ||||
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