# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA5054769 | B | Bump and hole PROTAC activity at BromoTag-Brd2/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation at 0.001 to 10 uM measured after 6 hrs by Western blot analysis | Homo sapiens | 11 | ALA5053531 | cell-based format | Scientific Literature | |
2. | ALA5054770 | B | Bump and hole PROTAC activity at BromoTag-Brd2 BD2 L387A mutant/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation measured after 6 hrs by Western blot analysis | Homo sapiens | 11 | ALA5053531 | cell-based format | Scientific Literature | |
3. | ALA5054771 | B | Bump and hole PROTAC activity at BromoTag-Brd2 BD2 L387A mutant/VHL-bound E3 ligase in HEK293 cells assessed as maximal Brd2 degradation measured after 6 hrs by Western blot analysis relative to control | Homo sapiens | 11 | ALA5053531 | cell-based format | Scientific Literature | |
4. | ALA5054772 | B | Bump and hole PROTAC activity at BromoTag-Brd2/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation by measuring protein half life measured after 6 hrs by Western blot analysis | Homo sapiens | 3 | ALA5053531 | cell-based format | Scientific Literature | |
5. | ALA5054773 | B | Binding affinity to VHL (unknown origin) assessed as displacement of HIF-1alpha by binary binding competitive fluorescence polarization assay | Homo sapiens | 3 | ALA5053531 | single protein format | Scientific Literature | |
6. | ALA5054774 | B | Binding affinity to VHL/BRD4 BD2 domain L387A mutant (unknown origin) assessed as displacement of HIF-1alpha by ternary binding competitive fluorescence polarization assay | Homo sapiens | 3 | ALA5053531 | assay format | Scientific Literature | |
7. | ALA5054775 | F | Antiproliferative activity against human BET-sensitive MV4-11 cells assessed as reduction in cell viability measured after 24 hrs by Celltiter-Glo assay | Homo sapiens | 2 | ALA5053531 | cell-based format | Scientific Literature | |
8. | ALA5054778 | B | Bump and hole PROTAC activity at BromoTag-Brd2 BD2 L387A mutant/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation measured in presence of MLN4924 after 6 hrs by Western blot analysis | Homo sapiens | 1 | ALA5053531 | cell-based format | Scientific Literature | |
9. | ALA5054779 | B | Bump and hole PROTAC activity at BromoTag-Brd2 BD2 L387A mutant/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation measured in presence of VH298 after 6 hrs by Western blot analysis | Homo sapiens | 1 | ALA5053531 | cell-based format | Scientific Literature | |
10. | ALA5054780 | B | Reversibility of Bump and hole PROTAC activity at BromoTag-Brd2 BD2 L387A mutant/VHL-bound E3 ligase in HEK293 cells assessed as Brd2 degradation at 200 nM treated for 3 hrs measured after 24 hrs of compound washout by Western blot analysis | Homo sapiens | 1 | ALA5053531 | cell-based format | Scientific Literature | |
11. | ALA5054781 | A | Stability in mouse plasma measured up to 60 mins | Mus musculus | 1 | ALA5053531 | cell-free format | Scientific Literature | |
12. | ALA5054782 | A | Clearance in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
13. | ALA5054783 | A | Volume of distribution at steady state in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
14. | ALA5054784 | A | Half life in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
15. | ALA5054785 | A | Half life in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
16. | ALA5054786 | A | AUC (0 to last) in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | Mus musculus | 1 | ALA5053531 | organism-based format | Scientific Literature | |
17. | ALA5054787 | A | AUC (0 to last) in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | Mus musculus | 1 | ALA5053531 | organism-based format | Scientific Literature | |
18. | ALA5054788 | A | AUC (0 to infinity) in C57BL/6 mouse at 5 mg/kg, iv measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
19. | ALA5054789 | A | AUC (0 to infinity) in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature | |
20. | ALA5054790 | A | MRT (0 to infinity) in C57BL/6 mouse at 5 mg/kg, sc measured up to 8 hrs by LC-MS analysis | Mus musculus | 2 | ALA5053531 | organism-based format | Scientific Literature |