| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4219513 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 short isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 2. | ALA4219514 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 long isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 3. | ALA4219515 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD3 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 4. | ALA4219517 | B | Proteolysis targeting chimera activity in human MV4-11 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular protein depletion at 50 nM incubated for 4 hrs by Western blotting method | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 5. | ALA4219518 | F | Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 6. | ALA4219519 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 short isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method relative to control | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 7. | ALA4219520 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD4 long isoform for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method relative to control | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 8. | ALA4219521 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD3 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method relative to control | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 9. | ALA4219522 | B | Proteolysis targeting chimera activity in human HeLa cells assessed as induction of VCB-mediated delivery of BRD2 for protein degradation by proteasome by measuring drug level causing 50% cellular protein depletion incubated for 24 hrs by Western blotting method relative to control | Homo sapiens | 7 | ALA4219029 | cell-based format | Scientific Literature | |
| 10. | ALA4219523 | F | Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent cell viability assay | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 11. | ALA4219524 | B | Proteolysis targeting chimera activity in human MV4-11 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular cMyc protein depletion at 50 nM incubated for 4 hrs by Western blotting method | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 12. | ALA4219525 | B | Proteolysis targeting chimera activity in human HL60 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular protein depletion at 50 nM incubated for 4 hrs by Western blotting method | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 13. | ALA4219526 | B | Proteolysis targeting chimera activity in human HL60 cells assessed as induction of VCB-mediated delivery of BRD4 for protein degradation by proteasome by measuring cellular cMyc protein depletion at 50 nM incubated for 4 hrs by Western blotting method | Homo sapiens | 9 | ALA4219029 | cell-based format | Scientific Literature | |
| 14. | ALA4219527 | B | Binding affinity to N-terminal His6-tagged recombinant human Brd4 BD2 expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titration calorimetry-based assay | Homo sapiens | 6 | ALA4219029 | assay format | Scientific Literature | |
| 15. | ALA4219528 | B | Binding affinity to N-terminal His6-tagged recombinant human VHL (54 to 213 residues)/elongin C (17 to 112 residues)/elongin B (1 to 104 residues) expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titration calorimetry-based assay | Homo sapiens | 6 | ALA4219029 | assay format | Scientific Literature | |
| 16. | ALA4219529 | B | Induction of interaction of N-terminal His6-tagged recombinant human VHL (54 to 213 residues)/elongin C (17 to 112 residues)/elongin B (1 to 104 residues) co-expressed in Escherichia coli BL21 (DE3) with recombinant human Brd4 BD2 assessed as VCB/BRD4/compound ternary complex formation by isothermal titration calorimetry-based assay | Homo sapiens | 6 | ALA4219029 | assay format | Scientific Literature | |
| 17. | ALA4730315 | P | Partition coefficient, logD of the compound in 1,9-decadiene and phosphate buffer at pH 7.4 measured after 30 mins under shaking condition by LC-MS analysis | 16 | ALA4725409 | small-molecule physicochemical format | Scientific Literature | ||
| 18. | ALA4730316 | A | Permeability of the compound in phosphate buffer containing 5% DMSO at pH 7.4 incubated for 15 hrs by PAMPA based LC/MS analysis | 11 | ALA4725409 | assay format | Scientific Literature | ||
| 19. | ALA5108373 | B | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay | Homo sapiens | 5 | ALA5107947 | protein format | Scientific Literature | |
| 20. | ALA5108379 | B | Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from BRD4 bromodomain 2/VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay | Homo sapiens | 5 | ALA5107947 | protein format | Scientific Literature |
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