Potency data for probe VZ185 and control cisVZ185
In vitro potency
| Target name | Target information | Species | Assay description | VZ185 | cisVZ185 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| VHL | Homo sapiens | ITC (VHL:VZ185): ITC binray compley (VHL:VZ185) | Kd = 26 nM ± 9.000 nM (n=2) | PMID: 30540463 | ||
| BRD9, VHL | BRD9 BD domain | Homo sapiens | ITC (VHL:VZ185:BRD9-BD): ITC: ternary complex (VHL:VZ185:BRD9-BD) | Kd = 27 nM ± 3.000 nM (n=2) | PMID: 30540463 | |
| BRD9 | BD domain | Homo sapiens | ITC (VZ185:BRD9-BD) | Kd = 5.1 nM ± 0.600 nM (n=2) | PMID: 30540463 | |
| VHL | Homo sapiens | FP (VHL:VZ185): Fluorescence polarization: binray compley (VHL:VZ185) | Kd = 35 nM ± 5.000 nM (n=2) | PMID: 30540463 | ||
| BRD9, VHL | BRD9 BD domain | Homo sapiens | FP (VHL:VZ185:BRD9-BD): Fluorescence polarization: ternary complex (VHL:VZ185:BRD9-BD) | Kd = 35 nM ± 6.000 nM (n=2) | PMID: 30540463 |
In cell potency
| Target name | Target information | Species | Assay description | VZ185 | cisVZ185 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BRD7 | RI-1 cells | Homo sapiens | Degradation of BRD7 in RI-1 cells (8 h): Western Blot degradation assay | DC50 = 4.5 nM | PMID: 30540463 | |
| BRD9 | RI-1 cells | Homo sapiens | Degradation of BRD9 in RI-1 cells (8 h): Western Blot degradation assay | DC50 = 1.76 nM | PMID: 30540463 | |
| BRD7 | HEK293 cells; HiBiT-Brd7 | Homo sapiens | Live-cell degradation (HEK293 cells, HiBiT-Brd7) | DC50 = 34.5 nM | PMID: 30540463 | |
| BRD9 | HEK293 cells; HiBiT-Brd9 | Homo sapiens | Live-cell degradation (HEK293 cells, HiBiT-Brd9) | DC50 = 4 nM | PMID: 30540463 | |
| BRD9 | EOL-1 cells | Homo sapiens | WES degradation assay (18 h, EOL-1 cells) | DC50 = 2.3 nM | PMID: 30540463 | |
| BRD9 | A204 cells | Homo sapiens | WES degradation assay (18 h, A204 cells) | DC50 = 8.3 nM | PMID: 30540463 | |
| EOL-1 cells | Homo sapiens | Cell viability (EOL-1 cells) : CellTiterGlo | EC50 = 3.4 nM | PMID: 30540463 | ||
| A204 cells | Homo sapiens | Cell viability (A204 cells) : CellTiterGlo | EC50 = 39.8 nM | PMID: 30540463 |