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Potency data for probe VZ185 and control cisVZ185


In vitro potency


Target name Target information Species Assay description Probe result (SD) Control result (SD) 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 = 5.100 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 Probe result (SD) Control result (SD) Publication of assay conditions
BRD7 RI-1 cells Homo sapiens Degradation of BRD7 in RI-1 cells (8 h): Western Blot degradation assay DC50 = 4.500 nM PMID: 30540463
BRD9 RI-1 cells Homo sapiens Degradation of BRD9 in RI-1 cells (8 h): Western Blot degradation assay DC50 = 1.760 nM PMID: 30540463
BRD7 HEK293 cells; HiBiT-Brd7 Homo sapiens Live-cell degradation (HEK293 cells, HiBiT-Brd7) DC50 = 34.500 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 = 2.300 nM PMID: 30540463
BRD9 A204 cells Homo sapiens WES degradation assay (18 h, A204 cells)  DC50 = 8.300 nM PMID: 30540463
EOL-1 cells Homo sapiens Cell viability (EOL-1 cells) : CellTiterGlo EC50 = 3.400 nM PMID: 30540463
A204 cells Homo sapiens Cell viability (A204 cells) : CellTiterGlo EC50 = 39.800 nM PMID: 30540463