| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA5251795 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells assessed as induction of SOS1 protein degradation at 0.1 uM incubated for 24 hrs by Immunoblot analysis relative to control | Homo sapiens | 17 | ALA5247656 | cell-based format | Scientific Literature | |
| 2. | ALA5251796 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells assessed as induction of SOS1 protein degradation at 1.0 uM incubated for 24 hrs by Immunoblot analysis relative to control | Homo sapiens | 17 | ALA5247656 | cell-based format | Scientific Literature | |
| 3. | ALA5251797 | F | Antiproliferative activity against human CAL-62 cells harboring KRAS G12R mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 4. | ALA5251799 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells assessed as induction of SOS1 protein degradation incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 2 | ALA5247656 | cell-based format | Scientific Literature | |
| 5. | ALA5251800 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells assessed as induction of SOS1 protein degradation by measuring maximal efficacy at 2 to 2000 nM incubated for 24 hrs by Immunoblot analysis relative to control | Homo sapiens | 7 | ALA5247656 | cell-based format | Scientific Literature | |
| 6. | ALA5251801 | B | Binding affinity to GST tagged human SOS1(564 to 1049 residues)-6his tagged human VHL (54 to 213 residues)-human ElonginC (17 to 112 residues)-human ElonginB (1 to 104 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as ternary complex formation by measuring maximal HTRF signals incubated for 15 mins by HTRF analysis | Homo sapiens | 7 | ALA5247656 | cell-based format | Scientific Literature | |
| 7. | ALA5251802 | B | Binding affinity to GST-tagged human SOS1 (564 to 1049 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as binary complex formation by measuring dissociation constant incubated for 15 mins by fluorescence polarization-based displacement assay | Homo sapiens | 8 | ALA5247656 | cell-based format | Scientific Literature | |
| 8. | ALA5251803 | B | Binding affinity to GST-tagged human SOS1 (564 to 1049 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as ternary complex formation by measuring dissociation constant incubated for 15 mins in the presence of 6His tagged human VCB by fluorescence polarization-based displacement assay | Homo sapiens | 8 | ALA5247656 | cell-based format | Scientific Literature | |
| 9. | ALA5251804 | B | Co-operativity factor, ratio of Kd for binding affinity to GST-tagged human SOS1 (564 to 1049 reisudes) expressed in Escherichia coli BL21 (DE3) cells assessed as binary complex formation to Kd for binding affinity to GST-tagged human SOS1 (564 to 1049 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as ternary complex formation in the presence of 6His tagged human VCB | Homo sapiens | 7 | ALA5247656 | cell-based format | Scientific Literature | |
| 10. | ALA5251807 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells harboring KRAS G12C mutant with shRNA lentivirus mediated VHL knockdown assessed as induction of SOS1 degradation at 1 uM incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 11. | ALA5251808 | B | PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant with shRNA lentivirus mediated VHL knockdown assessed as induction of SOS1 degradation at 1 uM incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 12. | ALA5251809 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation at 1 uM preincubated with VHL ligand for 4 hrs followed by compound treatment and measured after 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 13. | ALA5251810 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation at 1 uM preincubated with (R)-1-(4-(4-((1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)piperidin-1-yl)ethanone for 4 hrs followed by compound treatment and measured after 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 14. | ALA5251811 | B | PROTAC activity at VHL/SOS1 in human NCI-H358 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation at 1 uM preincubated with MG132 for 4 hrs followed by compound treatment and measured after 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 15. | ALA5251812 | B | PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant assessed as induction of SOS1 degradation at 1 uM preincubated with VHL ligand for 4 hrs followed by compound treatment and measured after 24 hrs by immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 16. | ALA5251813 | B | PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant assessed as induction of SOS1 degradation at 1 uM preincubated with (R)-1-(4-(4-((1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)piperidin-1-yl)ethanone for 4 hrs followed by compound treatment and measured after 24 hrs by immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 17. | ALA5251814 | B | PROTAC activity at VHL/SOS1 in human ASPC1 cells harboring KRAS G12D mutant assessed as induction of SOS1 degradation at 1 uM preincubated with MG132 for 4 hrs followed by compound treatment and measured after 24 hrs by immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 18. | ALA5251815 | B | PROTAC activity at VHL/SOS1 in human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 19. | ALA5251816 | B | PROTAC activity at VHL/SOS1 in human Calu-1 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature | |
| 20. | ALA5251817 | B | PROTAC activity at VHL/SOS1 in human UMUC3 cells harboring KRAS G12C mutant assessed as induction of SOS1 degradation incubated for 24 hrs by Immunoblot analysis | Homo sapiens | 1 | ALA5247656 | cell-based format | Scientific Literature |
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