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
Cytotoxicity against human MV4-11 cells assessed as defect in cell proliferation at 3 to 10 uM incubated for 15 days with replacement of fresh medium containing compound on every third day
Cytotoxicity against human MV4-11 cells expressing VHL assessed as defect in cell proliferation at 3 to 10 uM incubated for 15 days with replacement of fresh medium containing compound on every third day