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. 2022 Apr 9;41:135. doi: 10.1186/s13046-022-02352-y

Table 3.

Summary of current TBK1 inhibitors

Compounds Targets Reference Clinical Trial
Amlexanox (AMX) TBK1/IKKε [40, 246252] NCT01842282; NCT01975935
AZ13102909 (AZ909) TBK1 [223]
BAY-985 TBK1/IKKε [253]
BX795

TBK1/IKKε

Aurora B

NUAK1

PDK1

[254256]
Compound I TBK1/IKKε [244]
Compound II TBK1/IKKε [229, 257]
DMX-14 TBK1/IKKε [258]
GSK8612 TBK1 [259]
MDK10496 TBK1/IKKε [260]
MMB/CYT387/GS-0387

TBK1/IKKε

ACVR1

ALK2

JAK1/2

[231, 261267] NCT02101021; NCT02206763; NCT02258607; NCT04173494/MOMENTUM; NCT01969838/SIMPLIFY1; NCT02101268
MPI-0485520 TBK1/IKKε [268]
MRT67307

TBK1/IKKε

ULK1/2

[99]
MRT68601 TBK1 [255]
UNC6587/Cereblon-TBK1 PROTAC TBK1 [81]
15a

TBK1/IKKε

Aurora A

GSK3β

Aurora A

PDK1

[269]
200A TBK1/IKKε [270]
3i/pVHL-TBK1 PROTAC TBK1 [271]