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Inhibition of recombinant full length GST-MALT1 (unknown origin) expressed in Escherichia coli using Ac-LRSR-AMC as substrate by fluorescence analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant Malt1 (unknown origin) at 10 to 1000 uM preincubated for 1 hr followed by (S)-1-((6-(4-(4-(5,5-Difluoro-3,7-bis(4-methoxyphenyl)-5H-4l4,5l4-dipyrrolo[1,2-c:20,10-f][1,3,2]diazaborinin-10-yl)butyl)-1H-1,2,3-triazol-1-yl)hexanoyl)-L-valyl-L-arginyl)-N-((S)-1-fluoro-6-guanidino-2-oxohexan-3-yl)pyrrolidine-2-carboxamide addition and incubated for 1 hr by SDS-PAGE based competitive activity-based protein profiling assay
Assay data:4 Active, 19 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to Malt1 in phorbol 12-myristate 13-acetate/ionomycin stimulated human Jurkat T cells assessed as protein labeling at 1 to 3 uM after 50 mins by SDS-PAGE based activity-based protein profiling assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to Malt1 C/A mutant (unknown origin) overexpressed in human Jurkat T cells assessed as protein labeling at 1 uM after 50 mins by Western blot analysis
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed Citation
Inhibition of MALT1 in human Jurkat cell lysate preincubated for 2 hrs followed by addition of 25 uM Ac-LRSR-AMC substrate for 3 hrs by fluorescence based assay
Assay data:9 Active, 18 Tested
Inhibition of MALT1 paracaspase activity in human OCI-LY3 cells assessed as decrease in cleaved CYLD level after 24 hrs by western blot analysis
Assay data:2 Tested
Antiproliferative activity against human SupT1 cells
Assay data:1 Active, 1 Tested
Antiproliferative activity against human HUT78 cells
SummaryPubMed Citation
Antiproliferative activity against human NK92 cells
Antiproliferative activity against human MJ cells
Antiproliferative activity against human OCI-LY3 cells after 48 hrs by MTT assay
Assay data:9 Active, 13 Tested
In Vitro Protease Cleavage Assay from US Patent US9504692: "Selective inhibition of MALT1 protease by phenothiazine derivatives"
Assay data:30 Active, 4 Activity ≤ 1 µM, 45 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of MALT1 (329-824 residues) (unknown origin) using PT14 as substrate incubated for 60 mins by fluorescence based assay
Inhibition of GST-tagged human MALT1 (325-760 residues) expressed in Escherichia coli using Ac-LVSR-AMC as substrate by microplate reader based assay
Inhibition of N-terminal his-tagged GCN4 leucine zipper fused human MALT1 (340-281 residues) expressed in Escherichia coli using Ac-LVSR-AMC as substrate by HTS assay
Assay data:42 Active, 71 Tested
Inhibition of Protease Activity Assay from US Patent US10662156: "Guanidine derivative and medical use thereof"
Assay data:90 Active, 68 Activity ≤ 1 µM, 90 Tested
Cmax in CD-1 mouse at 10 mg/kg, po by LC-MS/MS analysis
Toxicity in NCG mouse xenografted with human TMD8 cells assessed as body weight loss at 30 mg/kg/day, po measured for 13 days
Tmax in CD-1 mouse at 1 mg/kg, ip by LC-MS/MS analysis
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
Assay data:17 Active, 2 Activity ≤ 1 µM, 44 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
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