PUBCHEM_BIOASSAY: SAR analysis of small molecule inhibitors of APOBEC3A DNA Deaminase via a fluorescence-based single-stranded DNA deaminase assay - Set 2. (Class of assay: confirmatory)
PUBCHEM_BIOASSAY: SAR analysis of small molecule inhibitors of APOBEC3G DNA Deaminase via a fluorescence-based single-stranded DNA deaminase assay - Set 2. (Class of assay: confirmatory)
Drug metabolism in mouse liver microsomes assessed as UGT-mediated glucuronidation of the demethylated metabolite at 20 uM preincubated for 3 mins followed by NADPH and UDPGA addition and measured after 60 mins by LC-MS/MS analysis
Prodrug conversion in mouse liver microsomes assessed as CYP450-mediated 4-Propyl-1-thioxo-2,4-dihydro-[1,2,4]triazolo[4,3-a]quinazolin-5(1H)-one formation at 20 uM preincubated for 3 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Drug metabolism in mouse liver microsomes assessed as CYP450-mediated S-demethylation at 20 uM preincubated for 3 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Drug metabolism in mouse liver microsomes assessed as CYP450-mediated hydroxylation at 20 uM preincubated for 3 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis
Induction of mitotic arrest in human HeLa cells assessed as abnormal spindle morphology at 100 uM measured after 12 hrs by DAPI staining based immunoassay
Inhibition of Plk1 PBD in human HeLa cells assessed as reduction in plk1 localization to kinetochores at 100 uM measured after 12 hrs by immunostaining based assay
Inhibition of Plk1 PBD in human HeLa cells assessed as reduction in plk1 localization to centrosomes at 100 uM measured after 12 hrs by immunostaining based assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell population at 100 uM measured after 3 days by DAPI staining based phase contrast microscopic analysis relative to control
Induction of mitotic arrest in human HeLa cells assessed as apperance of aberrant chromosomal morphology at 100 uM measured after 12 hrs by DAPI staining based phase contrast microscopic analysis
Induction of mitotic arrest in human HeLa cells assessed as rounded cells with apoptosis at 100 uM measured after 12 hrs by DAPI staining based phase contrast microscopic analysis
Inhibition of biotin-Ahx-CETFDPPLHSpTAI-NH2 binding to recombinant human full-length HA-EGFP-tagged Plk1 PBD expressed in HEK293A cells preincubated for 30 mins followed by biotin-Ahx-CETFDPPLHSpTAI-NH2 addition and measured after 1 hr by 3,3',5,5'-tetramethylbenzidine substrate based ELISA