Compile Data Set for Download or QSAR
Report error Found 1627 Enz. Inhib. hit(s) with Target = 'A disintegrin and metalloproteinase with thrombospondin motifs 5'
LigandPNGBDBM28308((2S)-2-{[4-(4-chlorophenyl)benzene](methyl)sulfona...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28309((2R)-2-{[4-(4-chlorophenyl)benzene](cyclopropylmet...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28310((2R)-2-{[4-(4-chlorophenyl)benzene](cyclohexylmeth...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28311((2R)-2-{benzyl[4-(4-chlorophenyl)benzene]sulfonami...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28315((2R)-2-{[4-(4-chlorophenyl)benzene][2-(2-oxopyrrol...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28320((1R,2S)-1-{[2-(2-oxopyrrolidin-1-yl)ethyl][4-(pyri...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28321((1R,2S)-1-{[4-(3-hydroxyprop-1-yn-1-yl)benzene][2-...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM28322((1R,2S)-1-{[4-(3-methoxyprop-1-yn-1-yl)benzene][2-...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The ADAMTS-5 (Aggrecanase-2) assay was performed using fluorescent peptide substrate WAAG-3R and the recombinant Agg-2 pre-incubated with various con...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2009
Entry Details Article
PubMed
LigandPNGBDBM24103(1-[(4R)-4-[3-(dimethylamino)propyl]-1-(2-fluoro-5-...)
Affinity DataIC50: 0.200nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM194638(US9206139, 1)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:The compounds of the present invention can be evaluated by using an aggrecanase ADAMTS-4 and ADAMTS-5 AlphaScreen assay (Miller J. A., et al. Anal. B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2016
Entry Details
Go to US Patent

LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMed
LigandPNGBDBM194638(US9206139, 1)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM24096(1-[1-(2,5-difluorophenyl)-4-{3-[(1S,4S)-2-oxa-5-az...)
Affinity DataIC50: 1.20nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM50167609((2R,5R)-1-[4-(2,4-Dichloro-benzyloxy)-benzenesulfo...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human recombinant aggrecanase 2 after 150 mins by fluorescence plate readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
LigandPNGBDBM24104(1-[(5R,6R)-5-[3-(4-acetylpiperazin-1-yl)propyl]-12...)
Affinity DataIC50: 1.60nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24089((5S)-5-(3-aminopropyl)-3-(2,5-difluorophenyl)-N,N-...)
Affinity DataIC50: 1.90nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24060((2S)-2-amino-2-cyclopropyl-1-[(2S)-4-(2,5-difluoro...)
Affinity DataIC50: 2nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2008
Entry Details Article
PubMed
LigandPNGBDBM24102(1-{4-[3-(4-acetylpiperazin-1-yl)propyl]-1-(2-fluor...)
Affinity DataIC50: 2nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM194639(US9206139, 2)
Affinity DataIC50: 2nMpH: 7.5 T: 2°CAssay Description:The compounds of the present invention can be evaluated by using an aggrecanase ADAMTS-4 and ADAMTS-5 AlphaScreen assay (Miller J. A., et al. Anal. B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2016
Entry Details
Go to US Patent

LigandPNGBDBM194644(US9206139, 3)
Affinity DataIC50: 2nMpH: 7.5 T: 2°CAssay Description:The compounds of the present invention can be evaluated by using an aggrecanase ADAMTS-4 and ADAMTS-5 AlphaScreen assay (Miller J. A., et al. Anal. B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2016
Entry Details
Go to US Patent

LigandPNGBDBM194639(US9206139, 2)
Affinity DataIC50: 2nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM194644(US9206139, 3)
Affinity DataIC50: 2nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM194644(US9206139, 3)
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant ADAMTS5 using synthetic peptide as substrate by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
LigandPNGBDBM24097(1-[1-(2,5-difluorophenyl)-4-[3-(dimethylamino)prop...)
Affinity DataIC50: 2.10nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24054((2S)-4-(2,5-difluorophenyl)-N-methyl-2-phenyl-N-(p...)
Affinity DataIC50: 2.60nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2008
Entry Details Article
PubMed
LigandPNGBDBM24061((2S)-2-amino-1-[(2S)-4-(2,5-difluorophenyl)-2-phen...)
Affinity DataIC50: 2.70nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2008
Entry Details Article
PubMed
LigandPNGBDBM50341819((1S,2R,3R)-1-(6-Chloro-4H-thieno[3,2-b]indole-2-su...)
Affinity DataIC50: 2.90nMAssay Description:Inhibition of human recombinant aggrecanase 2 after 150 mins by fluorescence plate readerMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/3/2011
Entry Details Article
PubMed
LigandPNGBDBM50033806(CHEMBL3358156)
Affinity DataIC50: 3nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50532313(CHEMBL4436740)
Affinity DataIC50: 3nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50532313(CHEMBL4436740)
Affinity DataIC50: 3nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50033806(CHEMBL3358156)
Affinity DataIC50: 3nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM24058((2S)-2-amino-1-[(2S)-4-(2,5-difluorophenyl)-2-phen...)
Affinity DataIC50: 3.60nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/4/2008
Entry Details Article
PubMed
LigandPNGBDBM24090(1-[1-(2,5-difluorophenyl)-4-[3-(4-acetylpiperazin-...)
Affinity DataIC50: 3.80nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24095(1-[1-(2,5-difluorophenyl)-4-phenyl-4-[3-(pyrrolidi...)
Affinity DataIC50: 3.80nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24098(Racemate | 1-[1-(5-chloro-2-fluorophenyl)-4-[3-(4-...)
Affinity DataIC50: 3.90nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24091(1-[1-(2,5-difluorophenyl)-4-(3-{methyl[(3-methyl-1...)
Affinity DataIC50: 4nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM194646(US9206139, 5)
Affinity DataIC50: 4nMpH: 7.5 T: 2°CAssay Description:The compounds of the present invention can be evaluated by using an aggrecanase ADAMTS-4 and ADAMTS-5 AlphaScreen assay (Miller J. A., et al. Anal. B...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/3/2016
Entry Details
Go to US Patent

LigandPNGBDBM50033808(CHEMBL3358158)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMed
LigandPNGBDBM194646(US9206139, 5)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM50033808(CHEMBL3358158)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50532312(CHEMBL4450729)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50033808(CHEMBL3358158)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50532312(CHEMBL4450729)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM24093(1-[1-(2,5-difluorophenyl)-4-[3-(morpholin-4-yl)pro...)
Affinity DataIC50: 4.20nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM24099(Racemate | 1-[1-(5-bromo-2-fluorophenyl)-4-[3-(4-a...)
Affinity DataIC50: 4.70nMpH: 7.0 T: 2°CAssay Description:The kinesin motor domain is incubated with microtubules, 1 mM ATP (1: 1 MgCl2 : Na-ATP), and compound at 23°C in buffer. After reaction was term...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/1/2008
Entry Details Article
PubMed
LigandPNGBDBM50238241(CHEMBL4102193)
Affinity DataIC50: 5nMAssay Description:Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/30/2019
Entry Details Article
PubMed
LigandPNGBDBM50238243(CHEMBL4097165)
Affinity DataIC50: 5nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM50238243(CHEMBL4097165)
Affinity DataIC50: 5nMAssay Description:Inhibition of human ADAMTS5 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/27/2021
Entry Details Article
PubMed
LigandPNGBDBM695895(US20240299360, Example 68-2)
Affinity DataIC50: 5nMAssay Description:Table 2: In this assay, the enzymatic activity of recombinant ADAMTS-5 protein (catalog #2198-AD, R&D Systems) was assayed with a protein substrate, ...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
1/8/2025
Entry Details
Go to US Patent

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