Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58937 | Target Info | |||
| Target Name | Glycine transporter-2 (SLC6A5) | ||||
| Synonyms |
Solute carrier family 6 member 5; Sodium-and chloride-dependent glycine transporter 2; SLC6A5; GlyT2; GlyT-2
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| Target Type | Literature-reported Target | ||||
| Gene Name | SLC6A5 | ||||
| Biochemical Class | Neurotransmitter:sodium symporter | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 28 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
8-[(1R,2R)-2-(4-Fluorophenyl)-2-hydroxycyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL425753; BDBM50175956; 8-[(cis, rac)-2-(4-fluoro-phenyl)-2-hydroxy-cyclohexyl]-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 = 57000 nM
|
[1] | |||
| Compound Name |
8-[(1R,2R)-2-Hydroxy-2-(4-methoxyphenyl)cyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL371966; BDBM50175952; 8-[(cis, rac)-2-hydroxy-2-(4-methoxy-phenyl)-cyclohexyl]-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 = 67000 nM
|
[1] | |||
| Compound Name |
8-[(1R,2R)-2-Hydroxy-2-(2-methylphenyl)cyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL381419; BDBM50175940; 8-((cis, rac)-2-hydroxy-2-o-tolyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 = 70000 nM
|
[1] | |||
| Compound Name |
8-(2-Hydroxy-2-phenyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL211373; SCHEMBL5556683; BDBM50188376
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| Activity |
EC50 = 72000 nM
|
[2] | |||
| Compound Name |
8-[(1R,2R)-2-Hydroxy-2-phenylcyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL200204; SCHEMBL5556686; BDBM50175955; 8-((cis, rac)-2-hydroxy-2-phenyl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 = 72000 nM
|
[1] | |||
| Compound Name |
3,4-Dichloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324476; SCHEMBL14836635; BDBM50427187
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
N-[[1-(4-Propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-3-(trifluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324164; BDBM50427192
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2,6-Difluoro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324477; SCHEMBL14836637; BDBM50427186
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2-Fluoro-4-methoxy-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324166; BDBM50427190
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
4-Fluoro-2-methoxy-6-methylsulfanyl-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324480; SCHEMBL14836648; BDBM50427183
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|
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
N-[[1-(4-Propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-2-(trifluoromethoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324161; SCHEMBL14836304; BDBM50427195
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2-Chloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-3-(trifluoromethyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324165; SCHEMBL14836483; BDBM50427191
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2-Amino-6-chloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324158; SCHEMBL16497093; BDBM50427198
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
4-Fluoro-2-methyl-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324168; SCHEMBL14836266; BDBM50427188
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
4-Chloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324162; SCHEMBL14836515; BDBM50427194
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2,4-Dichloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324167; SCHEMBL14836341; BDBM50427189
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|
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2,6-Dichloro-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324478; SCHEMBL14836080; BDBM50427185
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
N-[[1-(4-Propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324159; SCHEMBL14836666; BDBM50427197
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|
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
N-[[1-(4-Propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-2-(trifluoromethyl)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324160; SCHEMBL14836660; BDBM50427196
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
2-Methoxy-N-[[1-(4-propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-4,6-bis(trifluoromethyl)benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324479; SCHEMBL14837957; BDBM50427184
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
N-[[1-(4-Propylsulfonylpiperazin-1-yl)cyclohexyl]methyl]-4-(trifluoromethoxy)benzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2324163; SCHEMBL14836539; BDBM50427193
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| Activity |
IC50 ~ 75000 nM
|
[3] | |||
| Compound Name |
8-((1S,2S)-2-Phenyl-cyclohexyl)-1-propyl-1,3,8-triaza-spiro[4.5]decan-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL372402; BDBM50175901; 8-((cis, rac)-2-phenyl-cyclohexyl)-1-propyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
8-[(1R,2S)-2-Hydroxy-2-pyridin-2-ylcyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL371550; BDBM50175949; 8-((cis, rac)-2-hydroxy-2-pyridin-2-yl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
1-Cyclopentyl-8-((1S,2S)-2-phenyl-cyclohexyl)-1,3,8-triaza-spiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL199571; BDBM50175896
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
1-Benzyl-8-((1S,2S)-2-phenyl-cyclohexyl)-1,3,8-triaza-spiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL383827; SCHEMBL14573343; BDBM50175917
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
8-[(1R,2R)-2-Hydroxy-2-pyridin-4-ylcyclohexyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL372995; BDBM50175947; 8-((cis, rac)-2-hydroxy-2-pyridin-4-yl-cyclohexyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
1-Cyclobutyl-8-((1S,2S)-2-phenyl-cyclohexyl)-1,3,8-triaza-spiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL200877; BDBM50175921
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
8-[(3R,4R)-3-Hydroxy-3-phenyloxan-4-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL200053; BDBM50175943; 8-((cis, rac)-3-hydroxy-3-phenyl-tetrahydro-pyran-4-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one
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| Activity |
EC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile. Bioorg Med Chem Lett. 2006 Jan 15;16(2):354-7. | ||||
| REF 2 | Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4311-5. | ||||
| REF 3 | Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1257-61. | ||||
| REF 4 | Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors. Bioorg Med Chem Lett. 2006 Jan 15;16(2):349-53. | ||||
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