| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4324028 | Binding | Competitive inhibition of human topoisomerase 2alpha ATPase activity assessed as Vmax for ATP hydrolysis with DNA relaxation at 20 uM using supercoiled plasmid DNA as susbtrate after 1 hr by malachite green assay/Michelis-Menten kinetics analysis (Rvb = 0.652 to 0.6529 pmol/s) | Homo sapiens | 2 | ALA4321838 | single protein format | Scientific Literature | |
| 2. | ALA4324029 | Binding | Competitive inhibition of human topoisomerase 2alpha ATPase activity assessed as Km for ATP hydrolysis with DNA relaxation at 20 uM using supercoiled plasmid DNA as susbtrate after 1 hr by malachite green assay/Michelis-Menten kinetics analysis (Rvb = 317.8 to 350.1 microM) | Homo sapiens | 2 | ALA4321838 | single protein format | Scientific Literature | |
| 3. | ALA4324032 | Binding | Competitive inhibition of human topoisomerase 2alpha ATPase activity assessed as Vmax for ATP hydrolysis with DNA relaxation at 30 uM using supercoiled plasmid DNA as susbtrate after 1 hr by malachite green assay/Michelis-Menten kinetics analysis (Rvb = 0.652 to 0.6529 pmol/s) | Homo sapiens | 1 | ALA4321838 | single protein format | Scientific Literature | |
| 4. | ALA4324033 | Binding | Competitive inhibition of human topoisomerase 2alpha ATPase activity assessed as Km for ATP hydrolysis with DNA relaxation at 30 uM using supercoiled plasmid DNA as susbtrate after 1 hr by malachite green assay/Michelis-Menten kinetics analysis (Rvb = 317.8 to 350.1 microM) | Homo sapiens | 1 | ALA4321838 | single protein format | Scientific Literature | |
| 5. | ALA4324034 | ADME | Poison activity at topoisomerase 2alpha in human SW620 cells assessed as induction of DNA double stranded break by measuring gamma H2AX phosphorylation up to 40 uM after 6 hrs by Hoechst-33342 staining based immunofluorescence assay | Homo sapiens | 2 | ALA4321838 | cell-based format | Scientific Literature | |
| 6. | ALA4324036 | Binding | Inhibition of topoisomerase 2alpha dependent TCF transcription in human SW620 organoids transduced with TOPflash luminescent reporter at 10 uM after 72 hrs by luciferase based TOPFlash reporter gene assay | Homo sapiens | 2 | ALA4321838 | single protein format | Scientific Literature | |
| 7. | ALA4324037 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with VimPro-GFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring reduction in vimentin expression at 10 uM after 72 hrs by Hoechst 33342 staining based GFP reporter gene assay | Homo sapiens | 2 | ALA4321838 | assay format | Scientific Literature | |
| 8. | ALA4324038 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with EcadPro-RFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring increase in E-cadherin expression at 10 uM after 72 hrs by Hoechst 33342 staining based mCherryRFP reporter gene assay | Homo sapiens | 2 | ALA4321838 | assay format | Scientific Literature | |
| 9. | ALA4324039 | Functional | Anticlonogenic activity against human SW620 cells assessed as loss of cancer stem cell stemness by measuring inhibition of colony formation at 10 uM incubated for 24 hrs followed by replating and measured after 7 days by clonogenic assay | Homo sapiens | 8 | ALA4321838 | cell-based format | Scientific Literature | |
| 10. | ALA4324040 | Functional | Antiinvasive activity in human SW620 organoids transduced with NucLight-Red virus assessed as inhibition of cell invasion at 10 uM incubated for 72 hrs and measured after 72 hrs by matrigel based fluorescence analysis | Homo sapiens | 8 | ALA4321838 | cell-based format | Scientific Literature | |
| 11. | ALA4324041 | Binding | Inhibition of human topoisomerase 2alpha mediated decatenation at 30 uM using kDNA as susbtrate preincubated for 20 mins followed by substrate and ATP addition and measured after 1 hr by ethidium bromide staining based gel electrophoresis method relative to control | Homo sapiens | 30 | ALA4321838 | single protein format | Scientific Literature | |
| 12. | ALA4324042 | Binding | Inhibition of human topoisomerase 2alpha mediated decatenation using kDNA as susbtrate preincubated for 20 mins followed by substrate and ATP addition and measured after 1 hr by ethidium bromide staining based gel electrophoresis method | Homo sapiens | 30 | ALA4321838 | single protein format | Scientific Literature | |
| 13. | ALA4324043 | Binding | Inhibition of topoisomerase 2alpha dependent TCF transcription in human SW620 organoids transduced with TOPflash luminescent reporter after 72 hrs by luciferase based TOPFlash reporter gene assay | Homo sapiens | 10 | ALA4321838 | single protein format | Scientific Literature | |
| 14. | ALA4324044 | Functional | Cytotoxicity against human SW620 organoids assessed as cell death with loss of membrane integrity after 72 hrs by CellTox Green assay | Homo sapiens | 10 | ALA4321838 | cell-based format | Scientific Literature | |
| 15. | ALA4324045 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with VimPro-GFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring reduction in vimentin expression after 72 hrs by Hoechst 33342 staining based GFP reporter gene assay | Homo sapiens | 10 | ALA4321838 | assay format | Scientific Literature | |
| 16. | ALA4324046 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with EcadPro-RFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring increase in E-cadherin expression after 72 hrs by Hoechst 33342 staining based mCherryRFP reporter gene assay | Homo sapiens | 10 | ALA4321838 | assay format | Scientific Literature | |
| 17. | ALA4324047 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with VimPro-GFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring reduction in vimentin expression up to 40 uM after 72 hrs by Hoechst 33342 staining based GFP reporter gene assay | Homo sapiens | 3 | ALA4321838 | assay format | Scientific Literature | |
| 18. | ALA4324048 | Binding | Inhibition of topoisomerase 2alpha in human SW620 organoids transfected with EcadPro-RFP reporter assessed as reversion of epithelial-mesenchymal transition by measuring increase in E-cadherin expression up to 40 uM after 72 hrs by Hoechst 33342 staining based mCherryRFP reporter gene assay | Homo sapiens | 3 | ALA4321838 | assay format | Scientific Literature | |
| 19. | ALA4324049 | Functional | Cytotoxicity against human SW620 organoids assessed as growth inhibition at 10 uM after 72 hrs by CellTox Green assay | Homo sapiens | 3 | ALA4321838 | cell-based format | Scientific Literature | |
| 20. | ALA4324050 | Functional | Induction of apoptosis in human SW620 organoids assessed as increase in cleaved caspase 3/7 level at 40 uM after 72 hrs by caspase-glo 3/7 luminescence assay relative to control | Homo sapiens | 3 | ALA4321838 | cell-based format | Scientific Literature |
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