Binding affinity to recombinant WDR5 (unknown origin) expressed in Escherichia coli BL21 assessed as dissociation constant by isothermal titration calorimetry
Displacement of N-(4'-((17-(5,5-difluoro-7-(1H-pyrrol-2-yl)-5H-5l4,6l4-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-3-yl)-15-oxo-4,7,10-trioxa-14-azaheptadecyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-hydroxy-4-(trifluoromethyl)nicotinamide tracer from N-/C-terminal NanoLuc-fused full-length WDR5 (unknown origin) transfected in HEK293T cells incubated for 2 hrs by NanoBRET assay
Displacement of N-(4'-((17-(5,5-difluoro-7-(1H-pyrrol-2-yl)-5H-5l4,6l4-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-3-yl)-15-oxo-4,7,10-trioxa-14-azaheptadecyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-hydroxy-4-(trifluoromethyl)nicotinamide tracer from N-/C-terminal NanoLuc-fused full-length WDR5 (unknown origin) transfected in HEK293T cell lysate incubated for 2 hrs by NanoBRET assay
Binding affinity to recombinant WDR5 (unknown origin) expressed in Escherichia coli BL21 assessed as change in enthalpy by isothermal titration calorimetry
Binding affinity to recombinant WDR5 (unknown origin) expressed in Escherichia coli BL21 assessed as change in entropy by isothermal titration calorimetry
PROTAC activity at VHL/HiBit-tagged WDR5 in human MV4-11 cells assessed as maximum degradation of WDR5 incubated for 6 to 24 hrs by HiBiT assay relative to control
PROTAC activity at VHL/WDR5 in human MV4-11 cells assessed as reduction in protein stability at 3 uM incubated upto 12 hrs in presence of cycloheximide by immunoblot analysis
PROTAC activity at VHL/WDR5 in human MV4-11 cells assessed as induction of WDR5 degradation at 3 uM incubated for 6 hrs in presence of MG132 by immunoblot analysis
PROTAC activity at VHL/WDR5 in human MV4-11 cells assessed as induction of WDR5 degradation at 3 uM incubated for 6 hrs in presence of MLN4924 by immunoblot analysis
Cytotoxicity against human MV4-11 cells assessed as defect in cell proliferation at 10 uM incubated for 15 days with replacement of fresh medium containing compound on every third day
Cytotoxicity against human MV4-11 cells assessed as defect in cell proliferation at 3 to 5 uM incubated for 15 days with replacement of fresh medium containing compound on every third day