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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 125 hits in this display   

TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  0.600nMAssay Description:Inhibition of human 20S proteasome chymotrypsin like activity using Suc-Leu-Leu-Val-Tyr-AMC as substrate measured over 10 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  9.80nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  9.80nMAssay Description:Inhibition of chymotrypsin-like activity of 20S proteasome in human erythrocytes using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
TargetChymotrypsinogen B(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  320nMAssay Description:Inhibitory activity against human ChymotrypsinogenMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin G(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  630nMAssay Description:Inhibitory activity against human cathepsin GMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 2(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  1.16E+3nMAssay Description:Inhibition of human carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 2(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  1.16E+3nMAssay Description:Inhibition of human CA2 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 1(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  1.29E+3nMAssay Description:Inhibition of human CA1 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 1(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  1.29E+3nMAssay Description:Inhibition of human carbonic anhydrase-1 preincubated for 15 mins by stopped-flow CO2 hydration assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeutrophil elastase(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  2.30E+3nMAssay Description:Inhibitory activity against human leukocyte elastaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymotrypsinogen A(Bos taurus (bovine))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  2.40E+3nMAssay Description:Inhibition of bovine pancreatic alpha-chymotrypsin using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 15(Mus musculus)
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  2.68E+3nMAssay Description:Inhibition of mouse CA15 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 14(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  3.28E+3nMAssay Description:Inhibition of human CA14 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 9(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  3.38E+3nMAssay Description:Inhibition of human CA9 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 6(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  4.38E+3nMAssay Description:Inhibition of human CA6 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 3(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  4.57E+3nMAssay Description:Inhibition of human CA3 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 12(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  5.87E+3nMAssay Description:Inhibition of human CA12 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 4(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  6.51E+3nMAssay Description:Inhibition of human CA4 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 5B, mitochondrial(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  6.83E+3nMAssay Description:Inhibition of human CA5B by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 5A, mitochondrial(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  6.92E+3nMAssay Description:Inhibition of human CA5A by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 7(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  6.94E+3nMAssay Description:Inhibition of human CA7 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCarbonic anhydrase 13(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  8.45E+3nMAssay Description:Inhibition of human CA13 by stopped-flow CO2 hydrase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataKi:  1.30E+4nMAssay Description:Inhibitory activity against thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.30nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.90nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of chymotrypsin like activity of human 20S proteasome using ZGlyGlyLeuAMC/SucLeuLeuValTyrAMC as substrate measured every minute for 25 min...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.90nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2nMAssay Description:Inhibition of human 20S immunoproteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presence of P...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.40nMAssay Description:In vitro inhibition of dihydropteroate synthase from Escherichia coli.More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of 20S proteasome beta5 subunit (unknown origin) using Suc-LLVY-AMC as flurogenic substrate measured after 1 hr by fluorescence based anal...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of 20S proteasome beta5 subunit (unknown origin) using Suc-LLVY-AMC as flurogenic substrate measured after 1 hr by fluorescence based anal...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-9(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.90nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProteasome subunit beta type-9(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human peripheral blood derived 20s immunoproteasome beta1 caspase-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-9(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human peripheral blood derived 20s immunoproteasome beta1 caspase-like activity using Suc-PAL-AMC as substrate preincubated for 15 mins...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  3.20nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4nMAssay Description:Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate after 2 hrs by fluorescence ...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4nMAssay Description:Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVYaminoluciferin as substrate pretreated for 2 hrs followe...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human peripheral blood derived 20s immunoproteasome beta5 chymotrypsin-like activity using Suc-PAL-AMC as substrate preincubated for 15...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4nMAssay Description:Inhibition of human peripheral blood derived 20s immunoproteasome beta5 chymotrypsin-like activity using Suc-PAL-AMC as substrate preincubated for 15...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4.40nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome beta 5 subunit using Suc-LLVY-AMC as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-9(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human 20S immunoproteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence of PA2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-9(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  5.5nMAssay Description:Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human 20S constitutive proteasome beta 5 subunit chymotrypsin-like activity using fluorogenic peptide Ac-WLA-AMC as substrate in presen...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  6.20nMAssay Description:Inhibition of human 20S proteasome chymotryptic-like activity using Suc-LLVY-AMC as substrate measured for 30 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  6.70nMAssay 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...More data for this Ligand-Target Pair
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  6.90nMAssay 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
TargetProteasome subunit beta type-7(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-LLVY-AMC as substrateMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7nMAssay Description:Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7.10nMAssay Description:Inhibition of chymotrypsin like activity of human erythrocyte-derived 20S proteasome preincubated for 10 mins using Suc-LLVY-AMC as substrate after 6...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-7(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7.10nMAssay Description:Inhibition of chymotrypsin-like enzyme activity of purified human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate by fluorescence methodMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  7.90nMAssay Description:Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta5 after 30 mins by fluorogenic assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  8nMAssay Description:Inhibition of human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  8.10nMAssay Description:Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  8.30nMAssay Description:Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate after 1 hr by fluorescence analysisMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  8.96nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit alpha type-6(Homo sapiens (Human))
Jiangsu Chia Tai Fenghai Pharmaceutical

US Patent
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  9.92nMAssay Description:The proteasome used in the present invention is human erythrocyte 20S proteasome, and the enzyme, fluorescent substrate and test buffer are all purch...More data for this Ligand-Target Pair
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human 20S proteasome preincubated for 15 mins followed by substrate additionMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  11nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta5 chymotrypsin-like activity using Suc-WLA-AMC as substrate preincubated for...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-8(Mus musculus)
The University Of Adelaide

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  17nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  19nMAssay Description:Inhibition of PGPH activity of human 26S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  24nMAssay Description:Evaluated for norepinephrine as agonist.More data for this Ligand-Target Pair
TargetProteasome subunit beta type-6(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  25nMAssay Description:Inhibition of human 20S immunoproteasome beta1 subunit using Ac-nLPnLD-AMC as substrate preincubated for 2 hrs followed by substrate addition and mea...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  28nMAssay Description:Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  30nMAssay Description:Inhibition of caspase-like activity of 20S proteasome in human HL60 cells using Z-nLPnLDaminoluciferin as substrate after 2 hrs by fluorescence analy...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  30nMAssay 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...More data for this Ligand-Target Pair
TargetNACHT, LRR and PYD domains-containing protein 3(Mus musculus)
Guangzhou Medical University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  41nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  53nMAssay Description:Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta1 after 30 mins by fluorogenic assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  70nMAssay Description:Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
TargetHistone deacetylase 8(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  72nMAssay Description:Inhibition of HDAC8 in human RPMI-8226 cells incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  78nMAssay Description:Inhibition of beta5i subunit of immunoproteasome (unknown origin) by active-site ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  90nMAssay Description:Inhibition of human 20S constitutive proteasome beta 1 subunit caspase-like activity using fluorogenic peptide Ac-nLPnLD-AMC as substrate in presence...More data for this Ligand-Target Pair
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  97nMAssay Description:Inhibition of human erythrocytes 20S proteasome using QXL520-YRGITCSGRQK(5-FAM)-NH2 fluorogenic peptide as substrate preincubated for 10 mins followe...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  97nMAssay Description:Inhibition of caspase-like activity of human 20S proteasomeMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  104nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta1 caspase-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  104nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta1 caspase-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-7(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  120nMAssay Description:Inhibition of caspase-like activity of human 20S proteasome using Ac-nLPnLD-AMC as substrateMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  128nMAssay 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...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  130nMAssay Description:Inhibition of caspase-like activity of human 20S proteasome beta 1 subunit using Ac-nLPnLD-AMC as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  140nMAssay Description:Inhibition of beta5 subunit of immunoproteasome (unknown origin) by active-site ELISAMore data for this Ligand-Target Pair
TargetLon protease homolog, mitochondrial(Homo sapiens)
Genomics Institute Of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  183nMAssay 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 assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  261nMAssay Description:Inhibition of 20S proteasome beta2 subunit (unknown origin) using Boc-LRR-AMC as flurogenic substrate measured after 1 hr by fluorescence based analy...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  297nMAssay Description:Inhibition of 20S proteasome beta1 subunit (unknown origin) using Z-LLE-AMC as flurogenic substrate measured after 1 hr by fluorescence based analysi...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  440nMAssay Description:Dissociation constant against galectin-3 using competitive fluorescence polarizationMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  440nMAssay 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...More data for this Ligand-Target Pair
TargetCathepsin G(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  520nMAssay Description:Inhibition of human cathepsin GMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-10(Homo sapiens (Human))
The University Of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  540nMAssay Description:Inhibition of human 20S immunoproteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of PA28al...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  590nMAssay Description:Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta2 after 30 mins by fluorogenic assayMore data for this Ligand-Target Pair
TargetHistone deacetylase 1(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  620nMAssay Description:Inhibition of HDAC1 in human RPMI-8226 cells incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-1(Homo sapiens (Human))
Nagahama Institute Of Bio-Science And Technology

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  700nMAssay Description:Inhibition of PGPH activity of human 20S proteasome using Z-LLE-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetHistone deacetylase 2(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  800nMAssay Description:Inhibition of HDAC2 in human RPMI-8226 cells incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-10(Homo sapiens (Human))
The University Of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  940nMAssay Description:Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone deacetylase 3(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.18E+3nMAssay Description:Inhibition of HDAC3 in human RPMI-8226 cells incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChymase(Homo sapiens (Human))
Cephalon

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.19E+3nMAssay Description:Inhibition of human chymaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of human 20S constitutive proteasome beta 2 subunit trypsin-like activity using fluorogenic peptide Ac-WLR-AMC as substrate in presence of...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.20E+3nMAssay Description:Inhibition of human platelet Thromboxane synthetaseMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-10(Homo sapiens (Human))
The University Of Melbourne

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.63E+3nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.88E+3nMAssay Description:Inhibition of trypsin-like activity of human 20S proteasome beta 2 subunit using Ac-RLR-AMC as substrate after 60 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.93E+3nMAssay Description:Inhibition of trypsin-like activity of human 20S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-7(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of trypsin-like activity of human 20S proteasome using Ac-RLR-AMC as substrateMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-5(Homo sapiens (Human))
Universit£

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.10E+3nMAssay Description:Inhibition of chymotrypsin-like activity of human 26S proteasome using Suc-LLVY-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.12E+3nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta2 trypsin-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...More data for this Ligand-Target Pair
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  2.12E+3nMAssay Description:Inhibition of human hepatic cell derived 20s constitutive proteasome beta2 trypsin-like activity using Suc-LLE-AMC as substrate preincubated for 15 m...More data for this Ligand-Target Pair
TargetCathepsin G(Homo sapiens (Human))
Proscript

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  3.10E+3nMAssay Description:Inhibition of recombinant cathepsin G (unknown origin) using Suc-Ala-Ala-Pro-Phe-AMC as substrate by spectrofluorometer analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  4.00E+3nMAssay Description:Inhibition of trypsin-like activity of human 20S proteasomeMore data for this Ligand-Target Pair
TargetATP-dependent Clp protease proteolytic subunit(Staphylococcus aureus (strain NCTC 8325))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  5.30E+3nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLysosomal protective protein(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  9.20E+3nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-7(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  1.28E+4nMAssay 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...More data for this Ligand-Target Pair
TargetCathepsin B(Homo sapiens (Human))
Hokkaido University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of recombinant cathepsin B (unknown origin) using Z-Leu-Arg-AMC as substrate by spectrofluorometer analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteasome subunit beta type-2(Homo sapiens (Human))
Hangzhou Institute Of Innovative Medicine

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of trypsin-like activity of human 26S proteasome using Boc-LRR-MCA as substrate measured for 1 hr by fluorescence assayMore data for this Ligand-Target Pair
TargetHistone deacetylase 6(Homo sapiens (Human))
Mansoura University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50:  6.94E+4nMAssay Description:Inhibition of HDAC6 in human RPMI-8226 cells incubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >1.33E+5nMAssay 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 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >1.33E+5nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataIC50: >1.33E+5nMAssay 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...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCystic fibrosis transmembrane conductance regulator(Homo sapiens (Human))
Southern Research Institute

Curated by PubChem BioAssay
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataEC50: >5.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails PCBioAssay
TargetATP-dependent Clp protease proteolytic subunit(Staphylococcus aureus (strain NCTC 8325))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50069989((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxa...)
Affinity DataEC50:  2.35E+4nMAssay Description:Inhibition of ClpP in methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as reduction in bacteria-induced hemolysis of sheep erythrocyte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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