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In Vitro Assay from US Patent US10829478: "5-[3-[piperazin-1-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS 4 and 5 inhibitors for treating e.g. osteoarthritis"
Assay data:28 Active, 28 Activity ≤ 1 µM, 94 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
AlphaScreen Assay from US Patent US9206139: "Aggrecanase inhibitors"
Assay data:5 Active, 2 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Enzyme Assay from Article 10.1074/jbc.M112.380782: "Simple Pseudo-dipeptides with a P2' Glutamate: A NOVEL INHIBITOR FAMILY OF MATRIX METALLOPROTEASES AND OTHER METZINCINS."
Assay data:12 Active, 3 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Immunoblotting from US Patent US10322143: "Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure"
Assay data:61 Active, 13 Activity ≤ 1 nM, 61 Activity ≤ 1 µM, 61 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Aggrecanase-1 Inhibition Assay from Article 10.1016/j.bmcl.2005.10.001: "Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors."
Assay data:15 Active, 4 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Aggrecanase-1 Inhibition Assay from Article 10.1016/j.bmcl.2007.07.048: "5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2)."
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Aggrecanase-1 Inhibition Assay from Article 10.1124/jpet.103.059675: "Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human recombinant ADAMTS4 using synthetic peptide as substrate by FRET assay
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of human recombinant ADAMTS-4 (AA1 to 520) assessed as cleavage of fluorescent substrate using as TBIS-1 substrate incubated for 180 mins by biochemical assay
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
Inhibition of human ADAMTS4 using 43-mer VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate measured after 3 hrs by AlphaScreen assay
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of human ADAMTS4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assay
Assay data:8 Active, 2 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Human ADAMTS4 (M12: Astacin/Adamalysin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of full length recombinant ADAMTS4 (unknown origin) expressed in insect Sf9 cells after 6 hrs by alkaline phosphatase-based assay
Inhibition of recombinant human ADAMTS4 (213 to 575 amino acid residues) using WAAG-3R as substrate preincubated for 15 mins followed by substrate addition measured every 30 secs for 1 hr
Assay data:31 Active, 23 Activity ≤ 1 µM, 33 Tested
Genome-wide siRNA screen of genes regulating the Lipopolysaccharide-induced TNF-alpha response in human macrophages_Primary screen TNF readout
Assay data:2853 Active, 18113 Tested
SummaryRelated BioAssays by Same Project
Inhibition of human ADAMTS-4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assay
Assay data:9 Active, 1 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
A screen to identify synthetic lethal interactions with E-cadherin in an MCF10A isogenic cell line
Assay data:2442 Active, 18052 Tested
SummaryPubMed Citation
A screen to identify genes that regulate lymphatic endothelial cell migration - Primary Screen
Assay data:1034 Active, 18120 Tested
SummaryRelated BioAssays by Depositor
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