Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T64765 | Target Info | |||
| Target Name | Histamine H3 receptor (H3R) | ||||
| Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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|
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| Target Type | Successful Target | ||||
| Gene Name | HRH3 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 12 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-Cyclohexyl-3-[4-(2-piperidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024391; BDBM50382864
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|
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| Activity |
IC50 = 53800 nM
|
[1] | |||
| Compound Name |
N-(3-Bromo-4-(2-morpholinoethoxy)phenethyl)-1H-pyrrole-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL563666; BDBM50293614
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| Activity |
IC50 = 59200 nM
|
[2] | |||
| Compound Name |
N-(3-Bromo-4-(2-morpholinoethoxy)phenethyl)-5-bromofuran-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL559448; BDBM50293629
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| Activity |
IC50 = 73200 nM
|
[2] | |||
| Compound Name |
Ethyl 1-[2-[4-(phenylcarbamoylsulfamoyl)phenoxy]ethyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024394; BDBM50382867
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|
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| Activity |
IC50 = 77900 nM
|
[1] | |||
| Compound Name |
1-[4-(2-Piperidin-1-ylethoxy)phenyl]sulfonyl-3-[4-(trifluoromethyl)phenyl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024393; BDBM50382866
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|
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| Activity |
IC50 = 82000 nM
|
[1] | |||
| Compound Name |
6-(4-Fluorophenyl)-4-piperazin-1-yl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2314497; BDBM50424331
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|
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| Activity |
Ki = 84660 nM
|
[3] | |||
| Compound Name |
1-Phenyl-3-[4-(2-pyrrolidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024385; BDBM50382858
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|
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| Activity |
IC50 = 88600 nM
|
[1] | |||
| Compound Name |
Ethyl 1-[3-[4-(phenylcarbamoylsulfamoyl)phenoxy]propyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2021969; BDBM50382876
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|
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| Activity |
IC50 = 91100 nM
|
[1] | |||
| Compound Name |
1-(2,5-Dichlorophenyl)-3-[4-(2-piperidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024392; BDBM50382865
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|
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| Activity |
IC50 = 93600 nM
|
[1] | |||
| Compound Name |
1-Cyano-3-[[(2S,5S)-5-(1H-imidazol-5-yl)oxolan-2-yl]methyl]-2-methylguanidine
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL106570; BDBM50474243
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
1-[4-(2-Pyrrolidin-1-ylethoxy)phenyl]sulfonyl-3-[4-(trifluoromethyl)phenyl]urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024388; BDBM50382861
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|
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| Activity |
IC50 = 107000 nM
|
[1] | |||
| Compound Name |
1-[7-(3-Chlorophenoxy)heptyl]azepane;oxalic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3747465; BDBM50134532
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|
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| Activity |
Ki ~ 150000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 9 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(4-Cyclobutylpiperazin-1-yl)-(6-cyclohexylspiro[2.5]octan-2-yl)methanone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3127673; BDBM50496274
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|
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| Activity |
Ki > 10000000 nM
|
[6] | |||
| Compound Name |
Ethyl 1-[3-(4-sulfamoylphenoxy)propyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024379; BDBM50382855
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|
||||
| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
1-(2,5-Dichlorophenyl)-3-[4-(2-pyrrolidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024387; BDBM50382860
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|
||||
| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
Ethyl 1-[2-(4-sulfamoylphenoxy)ethyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024310; BDBM50382853
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|
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| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
1-Cyclohexyl-3-[4-(4-piperidin-1-ylbutoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2021977; BDBM50382883
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|
||||
| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
1-Cyclohexyl-3-[4-(2-pyrrolidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024386; BDBM50382859
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|
||||
| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
Ethyl 1-[4-(4-sulfamoylphenoxy)butyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024383; BDBM50382857
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|
||||
| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Compound Name |
Ethyl 1-[4-[4-(phenylcarbamoylsulfamoyl)phenoxy]butyl]piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2021980; BDBM50382838
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|
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| Activity |
IC50 > 100000000 nM
|
[1] | |||
| Compound Name |
1-Propan-2-yl-3-[4-(2-pyrrolidin-1-ylethoxy)phenyl]sulfonylurea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2024384; BDBM50382832
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|
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| Activity |
IC50 > 100000000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies. Eur J Med Chem. 2012 Jun;52:1-13. | ||||
| REF 2 | A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3204-8. | ||||
| REF 3 | Synthesis and evaluation of novel ligands for the histamine H1 receptor based on a pyrrolo[2,3-d]pyrimidine scaffold. Bioorg Med Chem Lett. 2013 Jan 1;23(1):132-7. | ||||
| REF 4 | Histamine H4 receptor agonists. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7191-9. | ||||
| REF 5 | Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents. Bioorg Med Chem. 2016 Jan 15;24(2):53-72. | ||||
| REF 6 | Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition. J Med Chem. 2014 Feb 13;57(3):733-58. | ||||
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