Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T09572 | Target Info | |||
| Target Name | Melanin-concentrating hormone receptor 1 (MCHR1) | ||||
| Synonyms |
Somatostatinreceptor-like protein; Somatostatin receptor-like protein; SLC1; SLC-1; Melanin-concentrating hormone receptor subtype 1; MCHR-1; MCHR; MCH1R; MCH-R1; MCH-1R; MCH(1) receptor; MCH receptor1; MCH receptor 1; GPR24; G-protein coupled receptor 24; G protein coupled receptor 24
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| Target Type | Clinical trial Target | ||||
| Gene Name | MCHR1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 16 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(S)-1-(6-((1H-Imidazol-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-(4-fluorophenethyl)piperazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL214983; BDBM50198571
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| Activity |
Ki = 52000 nM
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[1] | |||
| Compound Name |
1-((S)-6-(((2R,6S)-2,6-Dimethylpiperidin-1-yl)methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-(4-fluorophenethyl)piperazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL215266; BDBM50198583
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| Activity |
Ki = 62000 nM
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[1] | |||
| Compound Name |
1-[(2S)-6-[(1,1-Dioxo-1,4-thiazinan-4-yl)methyl]-1,2,3,4-tetrahydronaphthalen-2-yl]-4-[2-(4-fluorophenyl)ethyl]piperazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216959; BDBM50198580
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| Activity |
Ki = 94000 nM
|
[1] | |||
| Compound Name |
N-[2-(Diethylamino)ethyl]-2-methoxy-4-[2-oxo-3-(4-phenoxyphenyl)imidazolidin-1-yl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL184854; SCHEMBL6107917; BDBM50153245
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
N-(2-Diethylamino-ethyl)-2-methoxy-4-(3-phenyl-ureido)-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL183358; SCHEMBL6107859; BDBM50153234; ZINC28388839; N-[2-(diethylamino)ethyl]-2-methoxy-4-(phenylcarbamoylamino)benzamide
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
N-(2-Diethylamino-ethyl)-2-methoxy-N-methyl-4-[3-(4-phenoxy-phenyl)-ureido]-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL364178; BDBM50153214
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
3,5-Dimethoxy-N-(2,2,6,6-tetramethyl-1-(naphthalen-2-ylmethyl)piperidin-4-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL385875; BDBM50192180
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
(1R,5S,6r)-N-(3,4-Difluorobenzyl)-3-(naphthalen-2-ylmethyl)-3-azabicyclo[3.1.0]hexane-6-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216472; CHEMBL216765; BDBM50192173; BDBM50192185; (1R,5S,6s)-N-(3,4-difluorobenzyl)-3-(naphthalen-2-ylmethyl)-3-azabicyclo[3.1.0]hexane-6-carboxamide
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
N-[4-[2-(Dimethylamino)ethylcarbamoyl]phenyl]-4-phenylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL186601; SCHEMBL5582704; BDBM50153243; Biphenyl-4-carboxylic acid [4-(2-dimethylamino-ethylcarbamoyl)-phenyl]-amide; n-[4-({[2-(dimethylamino)ethyl]amino}carbonyl)phenyl](4-biphenylyl)carboxamide; n-[4-[[[2-(dimethylamino)ethyl]amino]carbonyl]phenyl] 4-biphenylylcarboxamide; N-[4-[[[2-(Dimethylamino)ethyl]amino]carbonyl]phenyl]4-biphenylylcarboxamide
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
3,5-Dimethoxy-N-(1-(3-phenylpropyl)piperidin-4-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL214382; BDBM50192156
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| Activity |
Ki ~ 100000 nM
|
[3] | |||
| Compound Name |
4-(4-(3-Bromophenylamino)phthalazin-1-yl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL370193; BDBM50173041; 4-[4-(3-Bromo-phenylamino)-phthalazin-1-yl]-benzamide; 3,5-dimethoxy-N-(1-(naphthalen-2-ylmethyl)piperidin-3-yl)benzamide
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
3,5-Dimethoxy-N-(3-(naphthalen-2-ylmethylamino)propyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216751; BDBM50192176
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| Activity |
Ki ~ 100000 nM
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[3] | |||
| Compound Name |
N-[2-(Diethylamino)ethyl]-2-methoxy-4-[methyl-[methyl-(4-phenoxyphenyl)carbamoyl]amino]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL184475; SCHEMBL6110083; BDBM50153233
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
(S)-4-(4-Fluorophenethyl)-1-(6-((2,2,2-trifluoroethylamino)methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)piperazin-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL216103; BDBM50198578
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| Activity |
Ki = 100000 nM
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[1] | |||
| Compound Name |
5-Chloro-N-(2-diethylamino-ethyl)-2-methoxy-4-[3-(4-phenoxy-phenyl)-ureido]-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL365689; BDBM50153246
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-(4-Benzyloxy-benzylamino)-N-[3-(2-pyrrolidin-1-yl-ethyl)-3H-benzoimidazol-5-yl]-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL360896; BDBM50162119; 2-(4-Benzyloxy-phenyl)-N-[3-(2-pyrrolidin-1-yl-ethyl)-3H-benzoimidazol-5-yl]-acetamide
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| Activity |
IC50 = 161000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-((((S)-6-(4-(4-Fluorophenethyl)-2-oxopiperazin-1-yl)-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)(methyl)amino)-3-hydroxy-N,N-dimethylpropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL385710; BDBM50198579
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| Activity |
Ki = 270000 nM
|
[1] | |||
| Compound Name |
2-(3,4-Dichlorophenyl)-N-[2-(4-ethylpiperazin-1-yl)-4-methylquinolin-6-yl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL193768; SCHEMBL5910347; BDBM50172417; ZINC20108641; MCULE-3244622852; SR-01000549029; SR-01000549029-1; 2-(3,4-Dichloro-phenyl)-N-[2-(4-ethyl-piperazin-1-yl)-4-methyl-quinolin-6-yl]-acetamide
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| Activity |
IC50 = 727000 nM
|
[5] | |||
| Compound Name |
2-(4-Benzyloxy-phenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H-benzoimidazol-5-yl]-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL178989; BDBM50162118
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| Activity |
IC50 = 772000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG. Bioorg Med Chem Lett. 2007 Feb 1;17(3):819-22. | ||||
| REF 2 | 4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5075-80. | ||||
| REF 3 | Identification of substituted 4-aminopiperidines and 3-aminopyrrolidines as potent MCH-R1 antagonists for the treatment of obesity. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5445-50. | ||||
| REF 4 | Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. J Med Chem. 2005 Mar 10;48(5):1318-21. | ||||
| REF 5 | 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and ... J Med Chem. 2005 Sep 8;48(18):5684-97. | ||||
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