Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T92653 | Target Info | |||
| Target Name | Neuropeptide Y receptor (NPYR) | ||||
| Synonyms |
NPY receptor
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| Target Type | Discontinued Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 15 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 | Neuropeptide Y receptor type 1 |
IC50 = 51000 nM
|
[1] | ||
| Compound Name |
2-[[2-(4-Chlorophenyl)-2-phenylacetyl]amino]-5-(diaminomethylideneamino)-N-[(1S)-2,3-dihydro-1H-inden-1-yl]pentanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL41686; BDBM50090271; 2-[2-(4-Chloro-phenyl)-2-phenyl-acetylamino]-5-guanidino-pentanoic acid (S)-indan-1-ylamide
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| Activity | Neuropeptide Y receptor type 2 |
IC50 = 59000 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 | Neuropeptide Y receptor type 1 |
IC50 = 60000 nM
|
[2] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL41981; BDBM50090276
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| Activity | Neuropeptide Y receptor type 5 |
IC50 = 68000 nM
|
[1] | ||
| 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 | Neuropeptide Y receptor type 1 |
IC50 = 70000 nM
|
[3] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid [1-(4-hydroxy-phenyl)-ethyl]-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL288355; BDBM50090281
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|
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| Activity | Neuropeptide Y receptor type 5 |
IC50 = 75000 nM
|
[1] | ||
| 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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|
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| Activity | Neuropeptide Y receptor type 1 |
IC50 = 76000 nM
|
[1] | ||
| Compound Name |
N-[1-(7-Hydroxy-1,3,4,5-tetrahydro-2-benzazepin-2-yl)-1-oxo-5-[[N'-(3-phenylpropyl)carbamimidoyl]amino]pentan-2-yl]-2-(4-phenylphenyl)acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL290175; BDBM50090282
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|
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| Activity | Neuropeptide Y receptor type 2 |
IC50 = 78000 nM
|
[1] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid 4-hydroxy-benzylamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL44246; BDBM84996; BDBM50065469; NSC_5311023; L000127; 2-(2,2-Diphenylacetamido)-5-guanidino-N-(4-hydroxybenzyl)pentanamide; 5-carbamimidamido-2-(2,2-diphenylacetamido)-N-[(4-hydroxyphenyl)methyl]pentanamide
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| Activity | Neuropeptide Y receptor type 5 |
IC50 = 80000 nM
|
[1] | ||
| Neuropeptide Y receptor type 2 |
IC50 ~ 100000 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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|
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| Activity | Neuropeptide Y receptor type 1 |
Ki = 88000 nM
|
[4] | ||
| Compound Name |
2-[2-(4-Chloro-phenyl)-2-phenyl-acetylamino]-5-guanidino-pentanoic acid benzylamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL41457; BDBM50090274
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|
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| Activity | Neuropeptide Y receptor type 2 |
IC50 = 97000 nM
|
[1] | ||
| Compound Name |
N-[4beta-[(2-Naphthylsulfonylamino)methyl]cyclohexane-1alpha-ylmethyl]-2-tetralincarboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL297509; SCHEMBL6039221; BDBM50114990
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|
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| Activity | Neuropeptide Y receptor type 5 |
Ki ~ 100000 nM
|
[5] | ||
| 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 | Neuropeptide Y receptor type 1 |
Ki ~ 100000 nM
|
[6] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid ((R)-carbamoyl-phenyl-methyl)-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL42686; BDBM50090272
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|
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| Activity | Neuropeptide Y receptor type 5 |
IC50 = 163000 nM
|
[1] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid ((R)-1-phenyl-ethyl)-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL41673; BDBM50090288
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|
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| Activity | Neuropeptide Y receptor type 2 |
IC50 = 177000 nM
|
[1] | ||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 6 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[4-Guanidino-1-(7-hydroxy-1,3,4,5-tetrahydro-benzo[c]azepine-2-carbonyl)-butyl]-2,2-diphenyl-acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL42747; BDBM50090277
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|
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| Activity | Neuropeptide Y receptor type 2 |
IC50 = 247000 nM
|
[1] | ||
| 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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|
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| Activity | Neuropeptide Y receptor type 1 |
IC50 = 320000 nM
|
[3] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid ((R)-carbamoyl-phenyl-methyl)-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL42686; BDBM50090272
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|
||||
| Activity | Neuropeptide Y receptor type 2 |
IC50 > 400000 nM
|
[1] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid ((S)-2-hydroxy-1-phenyl-ethyl)-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL41981; BDBM50090276
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|
||||
| Activity | Neuropeptide Y receptor type 2 |
IC50 = 540000 nM
|
[1] | ||
| Compound Name |
2-Diphenylacetylamino-5-guanidino-pentanoic acid [1-(4-hydroxy-phenyl)-ethyl]-amide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL288355; BDBM50090281
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|
||||
| Activity | Neuropeptide Y receptor type 2 |
IC50 = 575000 nM
|
[1] | ||
| 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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|
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| Activity | Neuropeptide Y receptor type 1 |
IC50 > 1000000 nM
|
[3] | ||
| Click to Show/Hide the Information of All Non Binders | |||||
| 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 | High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1771-4. | ||||
| REF 6 | 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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