BDBM50084637 2,2-Dimethyl-propionic acid 4-[2-(carboxymethyl-carbamoyl)-phenylsulfamoyl]-phenyl ester::2,2-Dimethyl-propionic acid 4-[2-(carboxymethyl-carbamoyl)-phenylsulfamoyl]-phenyl ester(ONO-5046)::CHEMBL76688::ONO-5046::Sivelestat

SMILES CC(C)(C)C(=O)Oc1ccc(cc1)S(=O)(=O)Nc1ccccc1C(=O)NCC(O)=O

InChI Key InChIKey=BTGNGJJLZOIYID-UHFFFAOYSA-N

Data  4 KI  20 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 24 hits for monomerid = 50084637   

TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human neutrophil elastase using MeO-Suc-Ala-Ala-Pro-Val-AMC as substrate incubated for 30 mins prior to substrate addition measured for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 128nMAssay Description:Inhibition of elastase in human neutrophil using N-(OMe-succinyl)-Ala-Ala-Pro-Val-p-nitroanilide as substrate preincubated with enzyme for 15 mins fo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of elastase in human neutrophil using MeOSuc-AAPV-AMC as substrate by fluorescence based analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 44nMAssay Description:Inhibition of human neutrophil elastase using N-methylsuccinyl-Ala-Ala-Pro-Val-7-amino-4-methylcoumarin as substrate measured every 30 secs for 10 mi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 704nMAssay Description:Inhibition of human neutrophil elastase incubated for 40 mins in presence of Boc-Gln-Ala-Arg-AMC by fluorescence microtiter plate methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 44nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 50nMAssay Description:Inhibition of human neutrophil elastase using N-methylsuccinyl-Ala-Ala-Pro-Val-7-amino-4-methylcoumarin as substrate measured for every 30 sec for 10...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 1.42E+5nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 136nMAssay Description:Inhibition of human neutrophil elastase assessed as proteolysis using N-(methoxysuccinyl)-Ala-Ala-Pro-Val-p-nitroanilide substrate incubated for 15 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 44nMAssay Description:Inhibitory concentration in vitro against Human neutrophil elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetMyeloblastin(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of human proteinase 3 using N-MeOSuc-Ala-Ala-Pro-Val-p-nitroanilide as substrate measured for 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetCathepsin G(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of human cathepsin G using Suc-Ala-Ala-Pro-Phe-p-nitroanilide as substrate incubated for 30 mins prior to substrate addition measured for ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetKallikrein-1(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of human kallikrein using H-Pro-Phe-Arg-AMC acetate salt as substrate measured for 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 44nMAssay Description:Inhibitory concentration against elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 44nMAssay Description:Inhibition of human neutrophil elastase using N-methylsuccinyl-Ala-Ala-Pro-Val-7-amino-4-methyl-coumarin as substrate measured every 30 secs for 10 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2012
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 70nMAssay Description:Inhibition of human neutrophil elastase measured for 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMed
TargetProthrombin(Bovine)
Chang Gung University

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of bovine plasma thrombin using Benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin hydrochloride by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMed
TargetMyeloblastin(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 340nMAssay Description:Inhibition of Pr3 (unknown origin) using t-butyloxycarbonyl-Ala-Ala-Nva-thiobenzyl ester as substrate measured for 180 mins by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMed
TargetCathepsin G(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human cathepsin G using N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide as substrate measured for 180 mins by spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMed
TargetNeutrophil elastase(Mouse)
Chang Gung University

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataIC50: 145nMAssay Description:Inhibition of recombinant mouse neutrophil elastase using methoxysuccinyl-Ala-Ala-Pro-Val-pnitroanilide as substrate preincubated for 15 mins before ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataKi:  24nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataKi:  37nMAssay Description:Inhibition of human leukocyte elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataKi:  200nMAssay Description:Binding affinity against Elastase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2012
Entry Details Article
PubMed
TargetNeutrophil elastase(Human)
Universidade De Lisboa

Curated by ChEMBL
LigandPNGBDBM50084637(Sivelestat | 2,2-Dimethyl-propionic acid 4-[2-(car...)
Affinity DataKi:  200nMAssay Description:Inhibition of human neutrophil elastaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed