Table 1.

Kinase inhibitors with anti-NAK activity used in this study. Dissociation constant (K_d), enzymatic activity (IC₅₀), percent binding of control (% of control) values measured in vitro on the four NAKs and NanoBRET GAK IC₅₀ values measured in cells of the indicated kinase inhibitors. The source of KINOMEscan data (if available) and other targets of these compounds are also shown. K_d, IC₅₀, and % of control are shown as *, ** and *** respectively. ^ represents data obtained in this study.

Compound	Status	${\text{K}}_{\text{d}}^{\text{*}}{\text{,IC}}_{50}{(\text{nM})}^{\text{**}}\text{or}\%\text{of}{\text{control}}^{\ast \ast \ast }$				NanoBRET GAK IC50 (nM)	Reference	Kinome	Other targets
		AAK1	BIKE	GAK	STK16
(5Z)-7- Oxozeaenol	Investigational	13%***	3.8%***	10%***	100%***	NA	Pu et al.,2020	ID: 20211	TAK1 (8 nM), VEGFR2 (52 nM), ERK2 (80 nM)
Sunitinib	Approved (cancer)	11 nM*	5.5 nM*	20 nM*	250 nM*	NA	Davis et al.,2011	Davis et al.,2011	VEGFR2 (80 nM), PDGFRβ (2 nM), FLT3, KIT, PDGFRα
Erlotinib	Approved (cancer)	1200 nM*	1200 nM*	3 nM*	>9000 nM*	910 nM	Asquith et al., 2019a, Asquith et al., 2019b	Davis et al.,2011	ErbB1 (0.7 nM), STK10 (19 nM), YSK4 (25 nM), SLK (26 nM)
Gefitinib	Approved (cancer)	>10,000 nM**a	>10,000 nM**a	13 nM*	NA	420 nM	Asquith et al., 2019a, Asquith et al., 2019b	Davis et al.,2011	EGFR
Baricitinib	Approved (RA)	17 nM*	40 nM*	134 nM∗	69 nM*	NA	Stebbing et al.,2021	Klaeger et al.,2017	JAK1 (5.9 nM), JAK2 (5.7 nM), ROCK1/2, TYK2 (53 nM), CAMK2A, MAP3K2, PRPF4B
RMC-76	Experimental	4 nM**	3.8 nM*a	280 nM*a	NA	NA	Figure S1	NA	CDC42BPB, PRKD3, CLK1, CLK4, ULK3, MINK1
RMC-242	Experimental	4100 nM*a	>15000 n M*a	12 nM**	NA	78 nMa	Martinez-Gualda et al.,2021	NA	NA
SGC-GAK-1	Experimental	NA 86%***	NA 92%***	2 nM* 9.7%***	NA 84%***	48 nM	Asquith et al., 2019a, Asquith et al., 2019b	Asquith et al., 2019a, Asquith et al., 2019b	RIPK2 (110 nM), ADCK3 (190 nM), NLK (520 nM)
STK-16-1N-1	Experimental	NA 13%***	NA 9.5%***	NA 46%***	295 nM** 0.65%***	NA	Liu et al., 2016	Liu et al.,2016	PI3Kδ (856 nM), PI3Kγ (867 nM)

^aData obtained in this study, RA= Rheumatoid Arthritis