Table 1 – Small Molecules and PROTACs Targeting TBK1.

Select references indicating cancer-related and non-cancer related studies, data on cross reactivity against other kinases, and IC50 (inhibitors) or DC50 (for proteolysis targeting chimeras).

TBK1i	Non-cancer related	Cancer-related	Cross reactivity	IC50 / DC50
Amlexanox	Inflammatory diseases, obesity, asthma, allergies [188,189]	breast cancer [158], colorectal cancer [157], prostate cancer [129,190], glioblastoma [156], leukemia	TBK1/IKKε Binds also to some S100 proteins and alters cell signaling and cytoskelston organization [191,192]	0.85uM 4.7uM 1-300 μg/ml for cell culture assays [193]
BX795	Herpes Simplex infections [194]	Lung cancer [116], bladder cancer [155], melanoma [131,167], squamous cell carcinoma [154]	TBK1/IKKε PDK1 Aurora B, ERK 8 And more [22]	1nM 1nM 1.3 nM 2 nM Working concentrations 100 nM - 10 μM
MRT67307	rheumatoid arthritis	T cell Leukemia [195]	TBK1/IKKε ULK1/2 [196] SIK [197]	19 nM 160 nM 40nM 1-20 μM for cell culture assays
CYT387 (Momelotinib) [198]	Myelofibrosis [199]	Lymphoma [200]; AML [162]; PDAC [171]; NSCLC [123,170],	JAK1 JAK2 TBK1/IKKε	11nM 18nM 58 nM / 42 nM
Cmpd1	N/A	Colon cancer (mouse model) [147]; Renal cell carcinoma [134]	TBK1/IKKε (less potent against JAK1/2/3) [147]	1nM (TBK1) / 5.6 nM (IKKε)
GSK8612	N/A	N/A	TBK1 [201]	N/A
Compound II	Autoimmune diseases [202,203]	melanoma [131]	TBK1/IKKε [203]	N/A
Compound 3i	N/A	KRAS mutant lung cancer [166]	Selective for TBK1	DC50 = 12 nM
UNC6587	N/A	VHL-mutant renal cell carcinoma [134]	Selective for TBK1	N/A