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Inhibition of ADAMTS-5 (unknown origin)
Assay data:4 Active, 2 Activity ≤ 1 µM, 4 Tested
SummaryRelated BioAssays by Target
Inhibition of human ADAMTS-5
Assay data:1 Active, 2 Tested
Inhibition of ADAMTS-5 (unknown origin) by FRET assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of recombinant human ADAMTS-5
Assay data:4 Active, 3 Activity ≤ 1 µM, 5 Tested
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:45 Active, 45 Activity ≤ 1 µM, 122 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Assay data:2 Active, 2 Activity ≤ 1 µM, 18 Tested
hADAMTS-5 assay from US Patent US10550100: "5-[3-[piperzin-1-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS 4 and 5 inhibitors for treating E.G. osteoarthritis"
Assay data:38 Active, 108 Activity ≤ 1 µM, 108 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
ADAMTS-5 Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2009.02.024: "Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors."
Assay data:27 Active, 20 Activity ≤ 1 µM, 27 Tested
In Vitro Assay from US Patent US9926281: "5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis"
Assay data:315 Active, 293 Activity ≤ 1 µM, 337 Tested
Assay data:149 Active, 131 Activity ≤ 1 µM, 160 Tested
Kinesin ATPase In Vitro Assay from Article 10.1016/j.bmcl.2007.07.074: "Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP."
Assay data:15 Active, 1 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Kinesin ATPase In Vitro Assay from Article 10.1016/j.bmcl.2006.03.040: "Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP."
Assay data:25 Active, 24 Activity ≤ 1 µM, 25 Tested
Kinesin ATPase In Vitro Assay from Article 10.1016/j.bmcl.2006.01.030: "Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP."
Assay data:16 Active, 14 Activity ≤ 1 µM, 16 Tested
ADAMTS-5 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:25 Active, 6 Activity ≤ 1 µM, 30 Tested
Inhibition of human recombinant ADAMTS5 using synthetic peptide as substrate by FRET assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of full-length human ADAMTS-5 expressed in HEK293-6E cells using AGC incubated for 50 mins by ELISA
Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 in presence of 2% HSA by biochemical assay
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
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