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Metabolic stability of the compound assessed as recombinant carboxylesterase-1 (unknown origin)-mediated hydrolysis after 60 mins
Assay data:4 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Drug metabolism in intact human U937 cells assessed as human CE1-mediated 5-(4-{6-Amino-5-[(2,4-difluorophenyl)carbonyl]-2-oxopyridiny1(2H)-yl}-3,5-difluorophenoxy)-L-norvaline formation per million cells at 2.5 uM after 6 hrs by LC/MS/MS analysis
Assay data:1 Tested
SummaryRelated BioAssays by Target
Drug metabolism in intact human U937 cells assessed as human CE1-mediated N-[2-(4-{6-Amino-5-[(2,4-difluorophenyl)carbonyl]-2-oxopyridin-1(2H)-yl}-3,5 difluorophenyl)ethyl]-L-leucine formation per million cells at 2.5 uM after 6 hrs by LC/MS/MS analysis
Drug metabolism in human U937 cell lysate assessed as human CE1-mediated 5-(4-{6-Amino-5-[(2,4-difluorophenyl)carbonyl]-2-oxopyridiny1(2H)-yl}-3,5-difluorophenoxy)-L-norvaline formation at 2.5 uM after 10 to 80 mins by LC/MS/MS analysis
Drug metabolism in human U937 cell lysate assessed as human CE1-mediated N-[2-(4-{6-Amino-5-[(2,4-difluorophenyl)carbonyl]-2-oxopyridin-1(2H)-yl}-3,5 difluorophenyl)ethyl]-L-leucine formation at 2.5 uM after 10 to 80 mins by LC/MS/MS analysis
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
SummaryPubMed Citation
Metabolic stability of the compound in human liver microsomes assessed as carboxylesterase-1-mediated hydrolysis by measuring half life in absence of NADPH
Assay data:9 Tested
SummaryPubMed CitationRelated BioAssays by Target
Metabolic stability of the compound in human liver microsomes assessed as carboxylesterase-1-mediated hydrolysis by measuring intrinsic clearance at 1 uM in absence of NADPH
Metabolic stability of the compound in human liver microsomes assessed as carboxylesterase-1-mediated hydrolysis after 3 hrs in presence of 1% bovine serum albumin
Assay data:9 Active, 9 Tested
Identification of proteins required for the processing of the EWS-FLI1 nascent transcript
Assay data:59220 Tested
Summary
Metabolic stability of the compound in human liver microsomes assessed as carboxylesterase-1-mediated hydrolysis by chromatographic analysis
Assay data:2 Active, 2 Tested
Metabolic stability of the compound assessed as recombinant carboxylesterase-1 (unknown origin)-mediated hydrolysis by chromatographic analysis
RNAi screen for vorinostat resistance genes - Primary Screen
Assay data:450 Active, 18118 Tested
Druggable Genome siRNA Screen for Enhancers of Camptothecin in MDA-MB-231 Breast Cancer Cells
Assay data:167 Active, 26449 Tested
Inhibition of human CE1 using o-NPA as substrate by spectrophotometric assay
Assay data:14 Active, 12 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Genome-wide high-content siRNA screens for regulators of Parkin translocation in selective mitophagy (Ambion Library)
Assay data:9227 Active, 64752 Tested
Genome-wide high-content siRNA screens for regulators of Parkin translocation in selective mitophagy (Dharmacon Library)
Assay data:826 Active, 18119 Tested
An siRNA screen for human genes that are involved in human papilloma virus (HPV) E2 transcriptional repression of the E6 and E7 oncogenes
Assay data:497 Active, 21019 Tested
A screen to identify genes that regulate lymphatic endothelial cell migration - Primary Screen
Assay data:1034 Active, 18120 Tested
SummaryRelated BioAssays by Depositor
A screen to identify synthetic lethal interactions with E-cadherin in an MCF10A isogenic cell line
Assay data:2442 Active, 18052 Tested
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