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  100 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 32 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
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 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-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
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:  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
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:  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:  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-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:  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-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:  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
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:  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-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-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:  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:  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 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:  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:  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-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-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