Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62276 | Target Info | |||
| Target Name | Glutamate receptor ionotropic NMDA 1 (NMDAR1) | ||||
| Synonyms |
NmethylDaspartate receptor subunit NR1; NMDR1; NMD-R1; N-methyl-D-aspartate receptor subunit NR1; Glutamate receptor ionotropic, NMDA 1; Glutamate [NMDA] receptor subunit zeta1; Glutamate [NMDA] receptor subunit zeta-1; GluN1
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| Target Type | Successful Target | ||||
| Gene Name | GRIN1 | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 21 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1,3-dihydro-indol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL114823; BDBM50091644
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| Activity |
IC50 = 52000 nM
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[1] | |||
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1H-indole-2,3-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL113936; SCHEMBL6967458; BDBM50091630; 5-[4-(4-benzylpiperidin-1-yl)but-1-ynyl]-1H-indole-2,3-dione
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| Activity |
IC50 = 57000 nM
|
[1] | |||
| Compound Name |
5-(3-(4-Benzylpiperidin-1-yl)prop-1-ynyl)-1-methyl-1H-benzo[d]imidazol-2(3H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL114155; BDBM50091631; 5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1-methyl-1,3-dihydro-benzoimidazol-2-one
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| Activity |
IC50 = 62000 nM
|
[1] | |||
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1,3-dihydro-benzoimidazole-2-thione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL115883; BDBM50091633
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| Activity |
IC50 = 75000 nM
|
[1] | |||
| Compound Name |
3-(Benzylamino-methyl)-4,6-dichloro-1H-indole-2-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL163465; BDBM50122607
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| Activity |
Ki = 92000 nM
|
[2] | |||
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1H-indazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL324584; SCHEMBL6973776; BDBM50091648; 5-[4-(4-benzylpiperidin-1-yl)but-1-ynyl]-1H-indazole
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| Activity |
IC50 = 95000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1,3-dihydro-indol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL116224; BDBM50091634
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
6-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1-methyl-1,3-dihydro-benzoimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL114667; BDBM50091649
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1H-indole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL113750; BDBM50091638
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-{3-[4-(4-Methoxy-benzyl)-piperidin-1-yl]-prop-1-ynyl}-1,3-dihydro-benzoimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL326568; BDBM50091628
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1,3-dihydro-benzoimidazole-2-thione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL116223; BDBM50091647
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1H-indazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL114644; BDBM50091641
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzylpiperidino)-1-propynyl]-1H-benzimidazole-2(3H)-one
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Investigative | Compound Info | ||
| Synonyms |
TCS 46B; CHEMBL117260; 1,3-Dihydro-5-[3-[4-(phenylmethyl)-1-2H-benzimidazol-2-one; 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzimidazol-2-one; SCHEMBL12619204; CTK8F0263; ZINC23994; DTXSID30432052; BDBM50091637; AKOS024457292; NCGC00378727-01; B7186; J-017852; 5-(3-(4-benzylpiperidin-1-yl)prop-1-ynyl)-1H-benzo[d]imidazol-2(3H)-one; 5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1,3-dihydro-benzoimidazol-2-one
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
6-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-3H-benzooxazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL113697; BDBM50091642
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1,3-dihydro-benzoimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL117940; SCHEMBL6962120; BDBM50091627; 5-[4-(4-benzylpiperidin-1-yl)but-1-ynyl]-1,3-dihydrobenzimidazol-2-one
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-{3-[4-(3-Fluoro-benzyl)-piperidin-1-yl]-prop-1-ynyl}-1,3-dihydro-benzoimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL19636; BDBM50091635
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-4-hydroxy-piperidin-1-yl)-prop-1-ynyl]-1,3-dihydro-benzoimidazol-2-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL326742; BDBM50091626
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
7-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-4H-benzo[1,4]oxazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL324940; BDBM50091624
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[3-(4-Benzyl-piperidin-1-yl)-prop-1-ynyl]-1H-benzotriazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL115761; BDBM50091639
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-{3-[4-(4-Fluoro-benzyl)-piperidin-1-yl]-prop-1-ynyl}-1,3-dihydro-benzoimidazol-2-one
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL19506; BDBM50091636
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
5-[4-(4-Benzyl-piperidin-1-yl)-but-1-ynyl]-1H-benzotriazole
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL114536; BDBM50091640
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines. J Med Chem. 2000 Sep 7;43(18):3408-19. | ||||
| REF 2 | Hydantoin-substituted 4,6-dichloroindole-2-carboxylic acids as ligands with high affinity for the glycine binding site of the NMDA receptor. J Med Chem. 2003 Jan 2;46(1):64-73. | ||||
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