Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T89213 | Target Info | |||
| Target Name | Neuropeptide Y receptor type 1 (NPY1R) | ||||
| Synonyms |
Neuropeptide Y-Y1 receptor; Neuropeptide Y receptor Y1; Neuropeptide Y Y(1) receptor; NPY1R; NPY1-R
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| Target Type | Clinical trial Target | ||||
| Gene Name | NPY1R | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 6 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[4-Guanidino-1-(1,3,4,5-tetrahydro-benzo[c]azepine-2-carbonyl)-butyl]-2,2,2-triphenyl-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL42861; BDBM50090290
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| Activity |
IC50 = 51000 nM
|
[1] | |||
| Compound Name |
2-[1-(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-piperidin-4-yl]-2,3-dihydro-isoindol-1-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL18016; SCHEMBL11481492; BDBM50089035; 2-[1-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperidin-4-yl]-3H-isoindol-1-one
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| Activity |
IC50 = 60000 nM
|
[2] | |||
| Compound Name |
2-(6-((4,5-Dimethyloxazol-2-ylthio)methyl)-4-morpholinopyridin-2-ylamino)acetonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL563011; SCHEMBL961141; BDBM50295998
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| Activity |
IC50 = 70000 nM
|
[3] | |||
| Compound Name |
2-Biphenyl-4-yl-N-[4-guanidino-1-(1,3,4,5-tetrahydro-benzo[c]azepine-2-carbonyl)-butyl]-acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL42625; BDBM50090291
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| Activity |
IC50 = 76000 nM
|
[1] | |||
| Compound Name |
{3-[2-(4-Dimethylamino-piperidin-1-yl)-ethyl]-benzo[b]thiophen-2-yl}-methanol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL142292; BDBM50075270
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| Activity |
Ki = 88000 nM
|
[4] | |||
| Compound Name |
2-(4-Chlorophenoxymethyl)-1-(2-piperidinoethyl)-1H-benzimidazole
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL93324; BDBM50065480; 2-(4-Chloro-phenoxymethyl)-1-(2-piperidin-1-yl-ethyl)-1H-benzoimidazole
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(6-(2-(5-Ethyl-4-methyloxazol-2-yl)ethyl)-4-morpholinopyridin-2-yl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL559987; BDBM50295995
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| Activity |
IC50 = 320000 nM
|
[3] | |||
| Compound Name |
2-(6-((4,5-Dimethyloxazol-2-yloxy)methyl)-4-morpholinopyridin-2-ylamino)acetonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL560263; BDBM50295999
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| Activity |
IC50 > 1000000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1597-600. | ||||
| REF 2 | Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists. Bioorg Med Chem Lett. 2000 Jun 5;10(11):1175-9. | ||||
| REF 3 | Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4325-9. | ||||
| REF 4 | Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2 side chain. Bioorg Med Chem Lett. 1999 Feb 8;9(3):475-80. | ||||
| REF 5 | Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists. J Med Chem. 1998 Jul 16;41(15):2709-19. | ||||
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