Compile Data Set for Download or QSAR
Report error Found 619 Enz. Inhib. hit(s) with Target = 'A disintegrin and metalloproteinase with thrombospondin motifs 4'
LigandPNGBDBM8465(CGS 27023 | CHEMBL514138 | hydroxamate analogue 1 ...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The recombinant Agg-1 proteins pretreated with the various concentrations of the compound for 10 to 15 min. The reaction was initiated by addition of...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM13139((2S)-N-hydroxy-2-[(4-methoxybenzene)(pyridin-3-ylm...)
Affinity DatapH: 7.5 T: 2°CAssay Description:The recombinant Agg-1 proteins pretreated with the various concentrations of the compound for 10 to 15 min. The reaction was initiated by addition of...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM50337721(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 DepthDetails Article
PubMed
LigandPNGBDBM50337721(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 DepthDetails
US Patent

LigandPNGBDBM50337722(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 DepthDetails Article
PubMed
LigandPNGBDBM50337735(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 DepthDetails
US Patent

LigandPNGBDBM50337723(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 DepthDetails Article
PubMed
LigandPNGBDBM50337723(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 DepthDetails
US Patent

LigandPNGBDBM50337724(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 DepthDetails Article
PubMed
LigandPNGBDBM50337724(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 DepthDetails
US Patent

LigandPNGBDBM50337727(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 DepthDetails Article
PubMed
LigandPNGBDBM50337725(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 DepthDetails Article
PubMed
LigandPNGBDBM50337726(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 DepthDetails Article
PubMed
LigandPNGBDBM50337725(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 DepthDetails
US Patent

LigandPNGBDBM50337726(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 DepthDetails
US Patent

LigandPNGBDBM50337727(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 DepthDetails
US Patent

LigandPNGBDBM50337736(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 DepthDetails Article
PubMed
LigandPNGBDBM50337736(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 DepthDetails
US Patent

LigandPNGBDBM50337731(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 DepthDetails Article
PubMed
LigandPNGBDBM50337731(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 DepthDetails
US Patent

LigandPNGBDBM50337734(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 DepthDetails Article
PubMed
LigandPNGBDBM50337734(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 DepthDetails
US Patent

LigandPNGBDBM50337739(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 DepthDetails Article
PubMed
LigandPNGBDBM50337739(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 DepthDetails
US Patent

LigandPNGBDBM50337735(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 DepthDetails Article
PubMed
LigandPNGBDBM50337735(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 DepthDetails
US Patent

LigandPNGBDBM50337743(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 DepthDetails Article
PubMed
LigandPNGBDBM50337743(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 DepthDetails
US Patent

LigandPNGBDBM50337733(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 DepthDetails Article
PubMed
LigandPNGBDBM50168737((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 DepthDetails Article
PubMed
LigandPNGBDBM194638(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 DepthDetails Article
PubMed
LigandPNGBDBM50168737((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 DepthDetails Article
PubMed
LigandPNGBDBM50337733(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 DepthDetails
US Patent

LigandPNGBDBM50167609((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 DepthDetails Article
PubMed
LigandPNGBDBM50337744(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 DepthDetails Article
PubMed
LigandPNGBDBM50337744(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 DepthDetails
US Patent

LigandPNGBDBM50345535(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 DepthDetails Article
PubMed
LigandPNGBDBM50345537(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 DepthDetails Article
PubMed
LigandPNGBDBM50345537(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 DepthDetails
US Patent

LigandPNGBDBM50345535(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 DepthDetails
US Patent

LigandPNGBDBM50345534(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 DepthDetails Article
PubMed
LigandPNGBDBM50337730(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 DepthDetails Article
PubMed
LigandPNGBDBM398042(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 DepthDetails
US Patent

LigandPNGBDBM50345534(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 DepthDetails
US Patent

LigandPNGBDBM50345539(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 DepthDetails Article
PubMed
LigandPNGBDBM50337737(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 DepthDetails Article
PubMed
LigandPNGBDBM50337737(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 DepthDetails
US Patent

LigandPNGBDBM50345539(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 DepthDetails
US Patent

LigandPNGBDBM194638(US9206139, 1)
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 DepthDetails
US Patent

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 DepthDetails
US Patent

Displayed 1 to 50 (of 619 total ) | Next | Last >>
Jump to: