Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T16691 | Target Info | |||
| Target Name | 5-HT 6 receptor (HTR6) | ||||
| Synonyms |
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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| Target Type | Clinical trial Target | ||||
| Gene Name | HTR6 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 1 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-Methyl-8-[(4-methylpiperazin-1-yl)sulfonyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1099283; SCHEMBL801288; BDBM50316298
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| Activity |
IC50 = 62000 nM
|
[1] | |||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
AF353
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Investigative | Compound Info | ||
| Synonyms |
AF-353; AF 353
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| Activity |
Ki = 100000000 nM
|
[2] | |||
| Compound Name |
6-Chloro-3-(1-propylpiperidin-4-yl)-1H-benzimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2207493; BDBM50401403
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| Activity |
IC50 > 580000 nM
|
[3] | |||
| Compound Name |
1-[2-Hydroxy-3-methyl-4-[[4-[4-(2H-tetrazol-5-yl)pyridin-2-yl]oxyphenyl]methoxy]phenyl]ethanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3899832; SCHEMBL3163790; BDBM50207400
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| Activity |
Ki > 1790000 nM
|
[4] | |||
| Compound Name |
N-[4-(3,4-Dihydro-1H-isoquinolin-2-yl)butyl]quinoline-8-sulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1917348; SCHEMBL8979999; BDBM50357982
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| Activity |
Ki = 41858718 nM
|
[5] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 8-Sulfonyl-substituted tetrahydro-1H-pyrido[4,3-b]indoles as 5-HT6 receptor antagonists. Eur J Med Chem. 2010 Feb;45(2):782-9. | ||||
| REF 2 | Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1628-31. | ||||
| REF 3 | Systematic in vivo screening of a series of 1-propyl-4-arylpiperidines against dopaminergic and serotonergic properties in rat brain: a scaffold-jumping approach. J Med Chem. 2012 Nov 26;55(22):9735-50. | ||||
| REF 4 | Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache. Bioorg Med Chem Lett. 2017 Jan 15;27(2):323-328. | ||||
| REF 5 | Arene- and quinoline-sulfonamides as novel 5-HT7 receptor ligands. Bioorg Med Chem. 2011 Nov 15;19(22):6750-9. | ||||
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