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. Author manuscript; available in PMC: 2022 Jun 12.
Published in final edited form as: Angew Chem Int Ed Engl. 2021 Jun 14;60(29):15905ā€“15911. doi: 10.1002/anie.202101328

Table 3.

Biochemical IC50s of FGFR2 for BGJ398-VHL based degraders.

graphic file with name nihms-1705093-t0018.jpg

Compound Linker E3 binder FGFR2 IC50 (nM)[a]
DGY-09-192 graphic file with name nihms-1705093-t0019.jpg C 34
NJH-05ā€“166 graphic file with name nihms-1705093-t0020.jpg C 30
NJH-05ā€“132 graphic file with name nihms-1705093-t0021.jpg C 10
NJH-05-123 graphic file with name nihms-1705093-t0022.jpg C 16
NJH-05-043 graphic file with name nihms-1705093-t0023.jpg C 30
NJH-05-044 graphic file with name nihms-1705093-t0024.jpg C 33
DGY-11-123 graphic file with name nihms-1705093-t0025.jpg D 59
DGY-11-122 graphic file with name nihms-1705093-t0026.jpg E 43
DGY-09-192-Neg graphic file with name nihms-1705093-t0027.jpg F 28
[a]

All the IC50s are measured by Zā€™-LYTE kinase assay by Invitrogen.