Compile Data Set for Download or QSAR
Report error Found 933 of affinity data for UniProtKB/TrEMBL: O75173
LigandChemical structure of BindingDB Monomer ID 50337721BDBM50337721(N-((2S,4S)-1-(4-(4-fluoro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.180nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337721BDBM50337721(N-((2S,4S)-1-(4-(4-fluoro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.180nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337735BDBM50337735(N-[(2S,4S)-1-({4-[2-(3,5-dimethyl-1,2-oxazol-4-yl)...)
Affinity DataIC50: 0.260nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337722BDBM50337722(N-((2S,4S)-1-(4-(2-(3,5-dimethylisothiazol-4-yl)et...)
Affinity DataIC50: 0.260nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337723BDBM50337723(N-((2S,4S)-1-(4-(4-chloro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.360nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337723BDBM50337723(N-((2S,4S)-1-(4-(4-chloro-2-methylphenethyl)piperi...)
Affinity DataIC50: 0.360nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337724BDBM50337724(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-4-yl)ethyl...)
Affinity DataIC50: 0.430nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337724BDBM50337724(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-4-yl)ethyl...)
Affinity DataIC50: 0.430nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337725BDBM50337725(N-((2S,4S)-1-(4-(2-chloro-4-(trifluoromethyl)phene...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337726BDBM50337726(N-((2S,4S)-1-(4-(2-bromo-4-fluorophenethyl)piperid...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337727BDBM50337727(N-((2S,4S)-1-(4-(2,5-dimethylphenethyl)piperidin-1...)
Affinity DataIC50: 0.480nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337726BDBM50337726(N-((2S,4S)-1-(4-(2-bromo-4-fluorophenethyl)piperid...)
Affinity DataIC50: 0.480nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337727BDBM50337727(N-((2S,4S)-1-(4-(2,5-dimethylphenethyl)piperidin-1...)
Affinity DataIC50: 0.480nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337725BDBM50337725(N-((2S,4S)-1-(4-(2-chloro-4-(trifluoromethyl)phene...)
Affinity DataIC50: 0.480nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337736BDBM50337736(N-((2S,4S)-4-(5-fluoropyrimidin-2-yl)-2-methyl-1-(...)
Affinity DataIC50: 0.490nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337736BDBM50337736(N-((2S,4S)-4-(5-fluoropyrimidin-2-yl)-2-methyl-1-(...)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337731BDBM50337731(N-((2S,4S)-1-(4-(4-fluoro-2-(trifluoromethyl)phene...)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337731BDBM50337731(N-((2S,4S)-1-(4-(4-fluoro-2-(trifluoromethyl)phene...)
Affinity DataIC50: 0.520nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337734BDBM50337734(N-((2S,4S)-1-(4-(2-chloro-4-(methylsulfonyl)phenet...)
Affinity DataIC50: 0.570nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337734BDBM50337734(N-((2S,4S)-1-(4-(2-chloro-4-(methylsulfonyl)phenet...)
Affinity DataIC50: 0.570nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337739BDBM50337739(N-((2S,4S)-1-(4-(2-(4,6-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 0.680nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337739BDBM50337739(N-((2S,4S)-1-(4-(2-(4,6-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 0.680nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337735BDBM50337735(N-[(2S,4S)-1-({4-[2-(3,5-dimethyl-1,2-oxazol-4-yl)...)
Affinity DataIC50: 0.690nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337735BDBM50337735(N-[(2S,4S)-1-({4-[2-(3,5-dimethyl-1,2-oxazol-4-yl)...)
Affinity DataIC50: 0.690nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337743BDBM50337743(N-((2S,4S)-1-(4-(2-cyclopropyl-4-(trifluoromethyl)...)
Affinity DataIC50: 0.940nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337743BDBM50337743(N-((2S,4S)-1-(4-(2-cyclopropyl-4-(trifluoromethyl)...)
Affinity DataIC50: 0.940nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337733BDBM50337733(N-((2S,4S)-1-(4-(2,4-dichlorobenzyloxy)piperidin-1...)
Affinity DataIC50: 1nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337733BDBM50337733(N-((2S,4S)-1-(4-(2,4-dichlorobenzyloxy)piperidin-1...)
Affinity DataIC50: 1nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 194638BDBM194638(US9206139, 1)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS4 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
LigandChemical structure of BindingDB Monomer ID 50168737BDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS-4 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
LigandChemical structure of BindingDB Monomer ID 50168737BDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ADAMTS4 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
LigandChemical structure of BindingDB Monomer ID 50167609BDBM50167609((2R,5R)-1-[4-(2,4-Dichloro-benzyloxy)-benzenesulfo...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human recombinant aggrecanase 1 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
LigandChemical structure of BindingDB Monomer ID 50337744BDBM50337744(N-((2S,4S)-1-(4-(2,4-dichlorophenethyl)piperidin-1...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337744BDBM50337744(N-((2S,4S)-1-(4-(2,4-dichlorophenethyl)piperidin-1...)
Affinity DataIC50: 1.10nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50345537BDBM50345537(N-(4-((4-(4-chloro-2-methylphenethyl)piperidin-1-y...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage after 16 hrs by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50345535BDBM50345535(N-(1-(cyclobutanecarbonyl)-4-((4-(2-methyl-4-(trif...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage after 16 hrs by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50345537BDBM50345537(N-(4-((4-(4-chloro-2-methylphenethyl)piperidin-1-y...)
Affinity DataIC50: 1.20nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50345535BDBM50345535(N-(1-(cyclobutanecarbonyl)-4-((4-(2-methyl-4-(trif...)
Affinity DataIC50: 1.20nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 398042BDBM398042(US10322143, Compound 1 | US10323000, Compound 1 | ...)
Affinity DataIC50: 1.40nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50345534BDBM50345534(N-(4-((4-(2-cyclopropyl-4-(methylsulfonyl)phenethy...)
Affinity DataIC50: 1.40nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337730BDBM50337730(N-((2S,4S)-1-(4-(4-fluorophenyl)piperazin-1-ylsulf...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50345534BDBM50345534(N-(4-((4-(2-cyclopropyl-4-(methylsulfonyl)phenethy...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage after 16 hrs by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50337737BDBM50337737(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 1.90nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50345539BDBM50345539(N-(1-(cyclobutanecarbonyl)-4-((4-(4-fluoro-2-methy...)
Affinity DataIC50: 1.90nMAssay Description:Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/10/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50337737BDBM50337737(N-((2S,4S)-1-(4-(2-(2,5-dimethylpyridin-3-yl)ethyl...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50345539BDBM50345539(N-(1-(cyclobutanecarbonyl)-4-((4-(4-fluoro-2-methy...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of ADAMTS-4 assessed as substrate cleavage after 16 hrs by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 194644BDBM194644(US9206139, 3)
Affinity DataIC50: 2nMAssay Description:Inhibition of human ADAMTS4 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
LigandChemical structure of BindingDB Monomer ID 194644BDBM194644(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
US Patent

LigandChemical structure of BindingDB Monomer ID 194644BDBM194644(US9206139, 3)
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant ADAMTS4 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
LigandChemical structure of BindingDB Monomer ID 194639BDBM194639(US9206139, 2)
Affinity DataIC50: 2nMAssay Description:Inhibition of human ADAMTS4 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
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