BDBM50069989 (R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid::(R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-6-carboxamido)propanamido)butylboronic acid::BORTEZOMIB::CHEMBL325041::Dipeptidyl boronic acid derivative::LDP-341::N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE::PS-341::Peptidyl boronic acid derivative::US11542283, Compound Velcade::Velcade::cid_387447

SMILES CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1cnccn1)B(O)O

InChI Key InChIKey=GXJABQQUPOEUTA-RDJZCZTQSA-N

Data  23 KI  97 IC50  2 EC50

PDB links: 30 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 122 hits for monomerid = 50069989   

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 CA2 by stopped-flow CO2 hydrase 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 carbonic anhydrase-2 preincubated for 15 mins by stopped-flow CO2 hydration 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
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
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:  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
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
TargetProteasome subunit beta type-8(Homo sapiens (Human))
Hokkaido University

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-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-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
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
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
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-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
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:  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-8(Homo sapiens (Human))
Hokkaido University

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:  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 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:  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:  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-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
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
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-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-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-2(Homo sapiens (Human))
Hokkaido University

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-1(Homo sapiens (Human))
Hokkaido University

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-1(Homo sapiens (Human))
Hokkaido University

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-2(Homo sapiens (Human))
Hokkaido University

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
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-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
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