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Inhibition of TMPRSS2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using H-D cyclohexylalanine-Pro-Arg-AM as substrate by Dixon method
Assay data:6 Active, 2 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human TMPRSS2 assessed as remaining activity at 50 uM using Boc-QAR-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorometric assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to TMPRSS2 (unknown origin) at 1.875 to 50 uM by SPR assay
Assay data:2 Tested
Antiviral Activity Assay from Article 10.1021/acs.jmedchem.2c00120: "Potent Inhibition of SARS-CoV-2 nsp14 "
SummaryPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
TMPRSS2 pericellular activity screening assay from Article 10.1038/s41586-022-04661-w: "A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic."
Assay data:5 Active, 4 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Cellular Antiviral Activity from Article : "Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19"
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
No assay is provided from Article 10.1002/med.21724: "The recent outbreaks of human coronaviruses: A medicinal chemistry perspective."
Assay data:146 Active, 2 Activity ≤ 1 nM, 69 Activity ≤ 1 µM, 205 Tested
titration assay from Article 10.1158/2159-8290.CD-13-1010: "The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis."
Assay data:4 Active, 1 Activity ≤ 1 µM, 4 Tested
Inhibition of human TMPRSS2-mediated SARS-CoV-2 entry into human Caco-2 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Induction of downregulation of TMPRSS2 (unknown orgin) human LNCaP cells at 10 uM after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Induction of downregulation of TMPRSS2 (unknown orgin) human LNCaP cells at 2 uM after 24 hrs by Western blot analysis
Induction of downregulation of TMPRSS2 (unknown orgin) human LNCaP cells at 1 uM after 24 hrs by Western blot analysis
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
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
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
Identification of proteins required for the processing of the EWS-FLI1 nascent transcript
Assay data:59220 Tested
InfectX: Pathogen infection siRNA screens
Assay data:115372 Tested
A whole genome RNAi screen highlights components of the ER/Golgi as a prominent source of resistance to immunotoxin-mediated cytotoxicity
Assay data:555 Active, 64752 Tested
RNAi screen for vorinostat resistance genes - Primary Screen
Assay data:450 Active, 18118 Tested
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