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Compile Data Set for Download or QSAR
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
(change energy unit to
kcal/mol
)
Found
125
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 0.600nM
Assay Description:
Inhibition of human 20S proteasome chymotrypsin like activity using Suc-Leu-Leu-Val-Tyr-AMC as substrate measured over 10 mins by fluorescence assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 9.80nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit assessed as Suc-Leu-Leu-Val-Tyr-AMC substrate hydrolysis after 10 min...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 9.80nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay
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Target
Chymotrypsinogen B
(Homo sapiens (Human))
Proscript
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 320nM
Assay Description:
Inhibitory activity against human Chymotrypsinogen
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Target
Cathepsin G
(Homo sapiens (Human))
Proscript
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 630nM
Assay Description:
Inhibitory activity against human cathepsin G
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Target
Carbonic anhydrase 2
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 1.16E+3nM
Assay Description:
Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assay
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Target
Carbonic anhydrase 2
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 1.16E+3nM
Assay Description:
Inhibition of human CA2 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 1
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 1.29E+3nM
Assay Description:
Inhibition of human CA1 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 1
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 1.29E+3nM
Assay Description:
Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assay
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Target
Neutrophil elastase
(Homo sapiens (Human))
Proscript
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 2.30E+3nM
Assay Description:
Inhibitory activity against human leukocyte elastase
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Target
Chymotrypsinogen A
(Bos taurus (bovine))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 2.40E+3nM
Assay Description:
Inhibition of bovine pancreatic alpha-chymotrypsin using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay
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Target
Carbonic anhydrase 15
(Mus musculus)
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 2.68E+3nM
Assay Description:
Inhibition of mouse CA15 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 14
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 3.28E+3nM
Assay Description:
Inhibition of human CA14 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 9
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 3.38E+3nM
Assay Description:
Inhibition of human CA9 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 6
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 4.38E+3nM
Assay Description:
Inhibition of human CA6 by stopped-flow CO2 hydrase assay
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Carbonic anhydrase 3
(Homo sapiens (Human))
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Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 4.57E+3nM
Assay Description:
Inhibition of human CA3 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 12
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 5.87E+3nM
Assay Description:
Inhibition of human CA12 by stopped-flow CO2 hydrase assay
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Carbonic anhydrase 4
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 6.51E+3nM
Assay Description:
Inhibition of human CA4 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 5B, mitochondrial
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 6.83E+3nM
Assay Description:
Inhibition of human CA5B by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 5A, mitochondrial
(Homo sapiens (Human))
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 6.92E+3nM
Assay Description:
Inhibition of human CA5A by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 7
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 6.94E+3nM
Assay Description:
Inhibition of human CA7 by stopped-flow CO2 hydrase assay
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Target
Carbonic anhydrase 13
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 8.45E+3nM
Assay Description:
Inhibition of human CA13 by stopped-flow CO2 hydrase assay
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Target
Prothrombin
(Homo sapiens (Human))
Proscript
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
Ki: 1.30E+4nM
Assay Description:
Inhibitory activity against thrombin
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 0.5nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assay
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.30nM
Assay Description:
Inhibition of human 20S immunoproteasome beta-5i subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and me...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.90nM
Assay Description:
Inhibition of chymotrypsin like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 10 mins followed by subs...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.90nM
Assay Description:
Inhibition of chymotrypsin like activity of human 20S proteasome using ZGlyGlyLeuAMC/SucLeuLeuValTyrAMC as substrate measured every minute for 25 min...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Copy SMILES
Copy InChI
Affinity Data
IC50: 1.90nM
Assay Description:
Inhibition of chymotrypsin like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 10 mins followed by subs...
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2nM
Assay Description:
Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of P...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.40nM
Assay Description:
In vitro inhibition of dihydropteroate synthase from Escherichia coli.
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.80nM
Assay Description:
Inhibition of 20S proteasome beta5 subunit (unknown origin) using Suc-LLVY-AMC as flurogenic substrate measured after 1 hr by fluorescence based anal...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.80nM
Assay Description:
Inhibition of 20S proteasome beta5 subunit (unknown origin) using Suc-LLVY-AMC as flurogenic substrate measured after 1 hr by fluorescence based anal...
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Target
Proteasome subunit beta type-9
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.90nM
Assay Description:
Inhibition of human 20S immunoproteasome beta-1i subunit using (Ac-PAL)2R110 as substrate preincubated for 2 hrs followed by substrate addition and m...
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Target
Proteasome subunit beta type-9
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 3nM
Assay Description:
Inhibition of human peripheral blood derived 20s immunoproteasome beta1 caspase-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins...
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Target
Proteasome subunit beta type-9
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 3nM
Assay Description:
Inhibition of human peripheral blood derived 20s immunoproteasome beta1 caspase-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 3.20nM
Assay Description:
Inhibition of human 20S proteasome beta5 subunit using Suc-LLVY-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured a...
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 3.30nM
Assay Description:
Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate after 2 hrs by fluorescence ...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate pretreated for 2 hrs followe...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4nM
Assay Description:
Inhibition of chymotrypsin-like activity of 26S proteasome beta 5 subunit in human U266 cells using Suc-LLVY-aminoluciferin as substrate after 1 hr b...
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4nM
Assay Description:
Inhibition of human peripheral blood derived 20s immunoproteasome beta5 chymotrypsin-like activity using Suc-PAL-AMC as substrate preincubated for 15...
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Copy SMILES
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Affinity Data
IC50: 4nM
Assay Description:
Inhibition of human peripheral blood derived 20s immunoproteasome beta5 chymotrypsin-like activity using Suc-PAL-AMC as substrate preincubated for 15...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4.40nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Gl...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4.5nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4.70nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assay
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Target
Proteasome subunit beta type-9
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 5nM
Assay Description:
Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA2...
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Target
Proteasome subunit beta type-9
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 5.5nM
Assay Description:
Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 6nM
Assay Description:
Inhibition of human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presen...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 6.20nM
Assay Description:
Inhibition of human 20S proteasome chymotryptic-like activity using Suc-LLVY-AMC as substrate measured for 30 mins by fluorescence assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 6.70nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-G...
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Target
A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436
(Homo sapiens (Human))
Zhejiang University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 6.90nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu Leu-Val-Tyr-AMC as substrate preincubated for 15 mins followed by subs...
More data for this Ligand-Target Pair
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Target
Proteasome subunit beta type-7
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-AMC as substrate
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 10 mins followed by substra...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7nM
Assay Description:
Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assay
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7.10nM
Assay Description:
Inhibition of chymotrypsin like activity of human erythrocyte-derived 20S proteasome preincubated for 10 mins using Suc-LLVY-AMC as substrate after 6...
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Target
Proteasome subunit beta type-7
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7.10nM
Assay Description:
Inhibition of chymotrypsin-like enzyme activity of purified human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence method
More data for this Ligand-Target Pair
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 7.90nM
Assay Description:
Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta5 after 30 mins by fluorogenic assay
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 8nM
Assay Description:
Inhibition of human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate addition
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 8.10nM
Assay Description:
Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISA
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 8.30nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 1 hr by fluorescence analysis
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 8.96nM
Assay Description:
The assay was carried out in 50 uL volume, where 1 uL compound was added to 10 uL purified human proteasome (25 ug/mL) and incubated for 15 min and t...
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Target
Proteasome subunit alpha type-6
(Homo sapiens (Human))
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 9.92nM
Assay Description:
The proteasome used in the present invention is human erythrocyte 20S proteasome, and the enzyme, fluorescent substrate and test buffer are all purch...
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Target
A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436
(Homo sapiens (Human))
Zhejiang University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 11nM
Assay Description:
Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate addition
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 11nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 11nM
Assay Description:
Inhibition of human 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 11nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...
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Target
Proteasome subunit beta type-8
(Mus musculus)
The University Of Adelaide
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 17nM
Assay Description:
Inhibition of chymotrypsin like activity of mouse spleen 20S proteasome beta5i subunit using Suc-Leu-Leu-Val-Tyr-AMC as substrate preincubated for 15...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 19nM
Assay Description:
Inhibition of PGPH activity of human 26S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assay
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 24nM
Assay Description:
Evaluated for norepinephrine as agonist.
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Target
Proteasome subunit beta type-6
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 25nM
Assay Description:
Inhibition of human 20S immunoproteasome beta1 subunit using Ac-nLPnLD-AMC as substrate preincubated for 2 hrs followed by substrate addition and mea...
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Target
Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 28nM
Assay Description:
Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 30nM
Assay Description:
Inhibition of caspase-like activity of 20S proteasome in human HL60 cells using Z-nLPnLDaminoluciferin as substrate after 2 hrs by fluorescence analy...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 30nM
Assay Description:
Inhibition of PGPH-like activity of 20S proteasome in human HL60 cells using Z-nLPnLDaminoluciferin as substrate pretreated for 2 hrs followed by sub...
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NACHT, LRR and PYD domains-containing protein 3
(Mus musculus)
Guangzhou Medical University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 41nM
Assay Description:
Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion preincubated for 1 hr follo...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 53nM
Assay Description:
Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta1 after 30 mins by fluorogenic assay
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 70nM
Assay Description:
Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assay
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Target
Histone deacetylase 8
(Homo sapiens (Human))
Mansoura University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 72nM
Assay Description:
Inhibition of HDAC8 in human RPMI-8226 cells incubated for 2 hrs by ELISA
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Target
Proteasome subunit beta type-8
(Homo sapiens (Human))
Merck
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 78nM
Assay Description:
Inhibition of beta5i subunit of immunoproteasome (unknown origin) by active-site ELISA
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 90nM
Assay Description:
Inhibition of human 20S constitutive proteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence...
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A5LHX3/O14818/P20618/P25786/P25787/P25788/P25789/P28062/P28065/P28066/P28070/P28072/P28074/P40306/P49720/P49721/P60900/Q8TAA3/Q99436
(Homo sapiens (Human))
Zhejiang University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 97nM
Assay Description:
Inhibition of human erythrocytes 20S proteasome using QXL520-YRGITCSGRQK(5-FAM)-NH2 fluorogenic peptide as substrate preincubated for 10 mins followe...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 97nM
Assay Description:
Inhibition of caspase-like activity of human 20S proteasome
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 104nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta1 caspase-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...
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Target
Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 104nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta1 caspase-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...
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Proteasome subunit beta type-7
(Homo sapiens (Human))
Hokkaido University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 120nM
Assay Description:
Inhibition of caspase-like activity of human 20S proteasome using Ac-nLPnLD-AMC as substrate
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 128nM
Assay Description:
Inhibition of human 20s proteasome subunit beta2 caspase-like activity using Z-LLE-AMC as substrate preincubated for 15 mins followed by substrate ad...
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Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 130nM
Assay Description:
Inhibition of caspase-like activity of human 20S proteasome beta 1 subunit using Ac-nLPnLD-AMC as substrate after 60 mins by fluorescence assay
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Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 140nM
Assay Description:
Inhibition of beta5 subunit of immunoproteasome (unknown origin) by active-site ELISA
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Lon protease homolog, mitochondrial
(Homo sapiens)
Genomics Institute Of The Novartis Research Foundation
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 183nM
Assay Description:
Inhibition of LONP1 (unknown origin) using QXL520-YRGITCSGRQK(5-FAM)-NH2 peptide as substrate incubated for 50 mins in presence of ATP by HTRF assay
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 261nM
Assay Description:
Inhibition of 20S proteasome beta2 subunit (unknown origin) using Boc-LRR-AMC as flurogenic substrate measured after 1 hr by fluorescence based analy...
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Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 297nM
Assay Description:
Inhibition of 20S proteasome beta1 subunit (unknown origin) using Z-LLE-AMC as flurogenic substrate measured after 1 hr by fluorescence based analysi...
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 440nM
Assay Description:
Dissociation constant against galectin-3 using competitive fluorescence polarization
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 440nM
Assay Description:
Inhibition of trypsin-like activity of 20S proteasome in human HL60 cells using Z-LRRaminoluciferin as substrate pretreated for 2 hrs followed by sub...
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Cathepsin G
(Homo sapiens (Human))
Proscript
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ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 520nM
Assay Description:
Inhibition of human cathepsin G
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Proteasome subunit beta type-10
(Homo sapiens (Human))
The University Of Melbourne
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 540nM
Assay Description:
Inhibition of human 20S immunoproteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of PA28al...
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 590nM
Assay Description:
Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta2 after 30 mins by fluorogenic assay
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Histone deacetylase 1
(Homo sapiens (Human))
Mansoura University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 620nM
Assay Description:
Inhibition of HDAC1 in human RPMI-8226 cells incubated for 2 hrs by ELISA
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Proteasome subunit beta type-1
(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 700nM
Assay Description:
Inhibition of PGPH activity of human 20S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assay
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Histone deacetylase 2
(Homo sapiens (Human))
Mansoura University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 800nM
Assay Description:
Inhibition of HDAC2 in human RPMI-8226 cells incubated for 2 hrs by ELISA
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Proteasome subunit beta type-10
(Homo sapiens (Human))
The University Of Melbourne
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 940nM
Assay Description:
Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assay
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Histone deacetylase 3
(Homo sapiens (Human))
Mansoura University
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 1.18E+3nM
Assay Description:
Inhibition of HDAC3 in human RPMI-8226 cells incubated for 2 hrs by ELISA
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Chymase
(Homo sapiens (Human))
Cephalon
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 1.19E+3nM
Assay Description:
Inhibition of human chymase
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.20E+3nM
Assay Description:
Inhibition of human 20S constitutive proteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of...
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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IC50: 1.20E+3nM
Assay Description:
Inhibition of human platelet Thromboxane synthetase
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.50E+3nM
Assay Description:
Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assay
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Proteasome subunit beta type-10
(Homo sapiens (Human))
The University Of Melbourne
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.63E+3nM
Assay Description:
Inhibition of human 20S immunoproteasome beta-2i subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and meas...
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.88E+3nM
Assay Description:
Inhibition of trypsin-like activity of human 20S proteasome beta 2 subunit using Ac-RLR-AMC as substrate after 60 mins by fluorescence assay
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.93E+3nM
Assay Description:
Inhibition of trypsin-like activity of human 20S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assay
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Proteasome subunit beta type-7
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.00E+3nM
Assay Description:
Inhibition of trypsin-like activity of human 20S proteasome using Ac-RLR-AMC as substrate
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Proteasome subunit beta type-5
(Homo sapiens (Human))
Universit£
Curated by
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Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.10E+3nM
Assay Description:
Inhibition of chymotrypsin-like activity of human 26S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assay
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.12E+3nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta2 trypsin-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 2.12E+3nM
Assay Description:
Inhibition of human hepatic cell derived 20s constitutive proteasome beta2 trypsin-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...
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Target
Cathepsin G
(Homo sapiens (Human))
Proscript
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 3.10E+3nM
Assay Description:
Inhibition of recombinant cathepsin G (unknown origin) using Suc-Ala-Ala-Pro-Phe-AMC as substrate by spectrofluorometer analysis
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Target
Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 4.00E+3nM
Assay Description:
Inhibition of trypsin-like activity of human 20S proteasome
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ATP-dependent Clp protease proteolytic subunit
(Staphylococcus aureus (strain NCTC 8325))
Sichuan University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 5.30E+3nM
Assay Description:
Inhibition of N-terminal His6-sumo-tagged full length Staphylococcus aureus ClpP expressed in Escherichia coli BL2 (DE3) pre-incubated for 10 mins be...
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Lysosomal protective protein
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 9.20E+3nM
Assay Description:
Inhibition of recombinant cathepsin A (unknown origin) using Mca-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(Dnp)-OH as substrate incubated with enzyme for 5...
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Proteasome subunit beta type-7
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 1.28E+4nM
Assay Description:
Inhibition of human 20S proteasome beta2 subunit using Ac-RLR-AMC as substrate preincubated for 2 hrs followed by substrate addition and measured aft...
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Cathepsin B
(Homo sapiens (Human))
Hokkaido University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >3.00E+4nM
Assay Description:
Inhibition of recombinant cathepsin B (unknown origin) using Z-Leu-Arg-AMC as substrate by spectrofluorometer analysis
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Proteasome subunit beta type-2
(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >4.00E+4nM
Assay Description:
Inhibition of trypsin-like activity of human 26S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assay
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Target
Histone deacetylase 6
(Homo sapiens (Human))
Mansoura University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: 6.94E+4nM
Assay Description:
Inhibition of HDAC6 in human RPMI-8226 cells incubated for 2 hrs by ELISA
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Target
Bile salt export pump
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >1.33E+5nM
Assay Description:
Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...
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Target
ATP-binding cassette sub-family C member 3
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...
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ATP-binding cassette sub-family C member 4
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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ATP-binding cassette sub-family C member 2
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
IC50: >1.33E+5nM
Assay Description:
Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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Cystic fibrosis transmembrane conductance regulator
(Homo sapiens (Human))
Southern Research Institute
Curated by
PubChem BioAssay
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
EC50: >5.00E+4nM
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Target
ATP-dependent Clp protease proteolytic subunit
(Staphylococcus aureus (strain NCTC 8325))
Sichuan University
Curated by
ChEMBL
Ligand
BDBM50069989
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
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Affinity Data
EC50: 2.35E+4nM
Assay Description:
Inhibition of ClpP in methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as reduction in bacteria-induced hemolysis of sheep erythrocyte...
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