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TPA Serine protease panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Enzymatic Activity Assay from US Patent US20230391761: "SUBSTITUTED S-ALANINATE DERIVATIVES"
Assay data:17 Active, 14 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human tissue plasminogen activator preincubated for 5 mins followed by substrate addition by fluorometer analysis
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to human tissue type plasminogen assessed as inhibition constant using Methanesulfonyl-D-Cyclohexylalanyl-glycylarginine p-Nitroaniline as substrate measured upto 120 mins by spectrophotometric analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition Assay from US Patent US8598206: "Trypsin-like serine protease inhibitors, and their preparation and use"
Assay data:14 Active, 1 Activity ≤ 1 µM, 22 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Enzymatic Assay from Article 10.1074/jbc.M109.067967: "Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1."
Assay data:12 Active, 9 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Determination of Inhibition Constants from Article 10.1016/s0969-2126(00)00551-7: "Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors."
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Determination of Inhibition Constants from Article 10.1006/jmbi.2000.3966: "Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design."
Assay data:4 Active, 2 Activity ≤ 1 µM, 5 Tested
Determination of Inhibitor Potency and Selectivity from Article 10.1021/jm061066t: "Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines."
Assay data:45 Active, 43 Activity ≤ 1 µM, 45 Tested
Serine Protease Inhibition Assay from Article 10.1074/jbc.M409068200: "A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo."
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Enzyme Assay and Determination of the Inhibition Constants from Article 10.1016/j.jmb.2004.09.032: "Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA)."
Assay data:14 Active, 12 Activity ≤ 1 µM, 15 Tested
Enzyme Assay and Determination of the Inhibition Constants from Article 10.1016/S1074-5521(00)00104-6: "Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator."
Assay data:2 Active, 2 Activity ≤ 1 µM, 4 Tested
Enzyme Assay and Determination of the Inhibition Constants from Article 10.1016/S1074-5521(01)00084-9: "Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets."
Assay data:18 Active, 16 Activity ≤ 1 µM, 18 Tested
Plasma-based Clot Lysis Assay from US Patent US10118930: "Piperidinylpyrazolopyrimidinones and their use"
Assay data:459 Active, 459 Activity ≤ 1 µM, 459 Tested
Fluorometric PAI-1/tPA IC50 Plate Assay at pH 7.8 from US Patent US9718760: "Plasminogen activator inhibitor-1 inhibitors and methods of use thereof"
Assay data:8 Active, 3 Activity ≤ 1 µM, 11 Tested
Inhibition of recombinant human tPA using H-D-Isoleucyl-L-prolyl-L-arginine p-nitroaniline dihydrochloride as substrate measured after 5 mins by plate reader analysis
Inhibition of tPA (unknown origin) assessed as inhibition of release of AMC fluorescent product using Z-GGR-AMC as substrate at 10 uM incubated for 30 mins by microplate reader relative to control
Assay data:7 Tested
Inhibition of human uPA using Tos-Gly-Pro-Arg-AMC as fluorogenic substrate at 5 uM measured at 1 min interval for 1 hr by fluorometric assay relative to control
Inhibition of purified human plasma tPA up to 20 uM using CH3SO2-DPhe-Gly-Arg-AMC substrate incubated for 30 mins by fluorescence based assay
Inhibition of TPA (unknown origin) at 10 uM relative to control
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