Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T09022 | Target Info | |||
| Target Name | Proteasome beta-10 (PS beta-10) | ||||
| Synonyms |
Proteasome subunit beta-2i; Proteasome subunit beta type-10; Proteasome MECl-1; Multicatalytic endopeptidase complex subunit MECl-1; Macropain subunit MECl-1; MECL1; Low molecular mass protein 10; LMP10
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| Target Type | Patented-recorded Target | ||||
| Gene Name | PSMB10 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4278272
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50464983
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| Activity |
IC50 = 79000 nM
|
[1] | |||
| Compound Name |
(2S)-1-[(2S)-2-[(2-Azidoacetyl)amino]propanoyl]-N-[(2S)-1-[[(2S)-3-cyclohexyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-4,4-difluoropyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319604; BDBM50099953
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(2S)-1-[(2S)-2-[(2-Azidoacetyl)amino]propanoyl]-4,4-difluoro-N-[(2S)-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]pyrrolidine-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319603; BDBM50099952
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
N-[(2R)-1-[[(2S)-3-(1H-Indol-3-yl)-1-[[(E,2S)-4-methylsulfonyl-1-phenylbut-3-en-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-methyl-1H-indene-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319591; LU-055i; BDBM50099836
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(2S)-1-[(2S)-2-[(2-Azidoacetyl)amino]propanoyl]-N-[(2S)-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]pyrrolidine-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319601; BDBM50099950
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
N-[(2R)-1-[[(2S)-1-[[(2S)-3-Cyclohexyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-methyl-1H-indene-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319483; LU-015i; BDBM50099664
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
PR-924
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Investigative | Compound Info | ||
| Synonyms |
UNII-ZI5ZER54A9; ZI5ZER54A9; CHEMBL3319482; SCHEMBL16123959; BDBM50099663; HY-123587; CS-0083586; Q27295555
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
N-[(2R)-1-[[(2S)-1-[[(2S)-3-Cyclohexyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]amino]-3-(4-methoxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-methyl-1H-indene-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3319579; LU-035i; BDBM50099686
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Chembl4281070
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Investigative | Compound Info | ||
| Synonyms |
BDBM50464964
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| Activity |
IC50 = 106000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[(2S)-1-[[(2S)-1-[(2R)-2-Methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]-6-oxo-1H-pyridine-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4101256; SCHEMBL16124070; BDBM50232676
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| Activity |
IC50 > 250000 nM
|
[3] | |||
| Compound Name |
N-((S)-3-Hydroxy-1-(((S)-1-((R)-2-methyloxiran-2-YL)-1-oxo-3-phenylpropan-2-YL)amino)-1-oxopropan-2-YL)-6-oxo-1,6-dihydropyridine-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
KZR-504; CHEMBL4100295; SCHEMBL16123905; BDBM50232675; HY-101786; CS-0021896
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| Activity |
IC50 > 250000 nM
|
[3] | |||
| Compound Name |
N-[(2S)-3-(4-Methoxyphenyl)-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]-6-oxo-1H-pyridine-2-carboxamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4074528; SCHEMBL16124001; BDBM50232677
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| Activity |
IC50 > 250000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-based design of human immuno- and constitutive proteasomes inhibitors. Eur J Med Chem. 2018 Feb 10;145:570-587. | ||||
| REF 2 | Structure-based design of 1i or 5i specific inhibitors of human immunoproteasomes. J Med Chem. 2014 Jul 24;57(14):6197-209. | ||||
| REF 3 | Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417. | ||||
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