Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T59679 | Target Info | |||
| Target Name | 5-HT 4 receptor (HTR4) | ||||
| Synonyms |
Serotonin receptor 4; 5-hydroxytryptamine receptor 4; 5-HT4 receptor; 5-HT4; 5-HT-4
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| Target Type | Successful Target | ||||
| Gene Name | HTR4 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | 5-HT 2B receptor (HTR2B) | Successful Target | ||||
| UniProt ID | 5HT2B_HUMAN | |||||
| Gene Name | HTR2B | |||||
| Synonyms |
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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| Representative Drug(s) | Tegaserod | Drug Info | Ki < 1.995 nM | Click to Show More | [1] | |
| 2 | TD-5108 | Drug Info | Ki < 1.995 nM | [2] | ||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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| Representative Drug(s) | Cisapride | Drug Info | IC50 = 12 nM | [3] | ||
| 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) | Tegaserod | Drug Info | Ki < 100 nM | Click to Show More | [1] | |
| 2 | TD-5108 | Drug Info | Ki < 100 nM | [2] | ||
| 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) | Tegaserod | Drug Info | Ki < 100 nM | Click to Show More | [1] | |
| 2 | TD-5108 | Drug Info | Ki < 100 nM | [2] | ||
| 3 | Drug Info | Ki < 1000 nM | [4] | |||
| 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) | Tegaserod | Drug Info | Ki < 100 nM | Click to Show More | [1] | |
| 2 | TD-5108 | Drug Info | Ki < 100 nM | [2] | ||
| 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 < 1000 nM | [4] | |||
| 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) | Drug Info | Ki < 1000 nM | [4] | |||
| 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 | Ki ~ 1000 nM | [5] | |||
| 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) | Tegaserod | Drug Info | Ki < 100 nM | Click to Show More | [1] | |
| 2 | TD-5108 | Drug Info | Ki < 100 nM | [2] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4210-5. | ||||
| REF 2 | Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6048-52. | ||||
| REF 3 | Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety. Bioorg Med Chem Lett. 2018 Aug 1;28(14):2477-80. | ||||
| REF 4 | N-[(1-butyl-4-piperidinyl)methyl]-3,4dihydro-2H-[1,3]oxazino[3,2- a]indole10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity. J Med Chem. 1995 Nov 24;38(24):4760-3. | ||||
| REF 5 | Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines. Bioorg Med Chem. 2009 Mar 15;17(6):2607-22. | ||||
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