. Author manuscript; available in PMC: 2021 Oct 1.

Published in final edited form as: Biochim Biophys Acta Mol Cell Res. 2020 Jun 26;1867(10):118786. doi: 10.1016/j.bbamcr.2020.118786

Table 3. Potency and efficacy against the FGF14:FGF14 dimer and FGF14:Nav1.6 complex by JAK2 and Src inhibitors.

Estimated potency (IC₅₀ or EC₅₀, μM) and efficacy (minimal (I_Min) or maximal (E_Max) percent luminescence at the bottom plateau for inhibition and top plateau for stimulation, respectively) and for JAK2 and Src inhibitors based on the LCA data in Figures 4 and 6. Luminescence for each well was normalized to per plate 0.3% DMSO controls (n = 32 per plate).

Inhibitor	Target	FGF14^WT:Nav1.6		FGF14:FGF14^WT		FGF14^Y158A:Nav1.6		FGF14:FGF14^Y158A
Inhibitor	Target	I_Min/E_Max	IC/EC₅₀	I_Min/E_Max	IC/EC₅₀	I_Min/E_Max	IC/EC₅₀	I_Min/E_Max	IC/EC₅₀
Momelotinib	JAK2	53.5	10.9	138.6	10.8	101.8	N/A	90.9	N/A
TG101209	JAK2	43.0	10.3	150.6	7.6	78.0	98.0	73.4	69.4
Fedratinib	JAK2	35.7	9.7	156.7	8.2	76.8	27.1	72.8	28.5
Pacritinib	JAK2	45.0	13.5	136.0	11.6	110.6	N/A	79.3	5.5
Danusertib	Src	38.6	8.4	86.0	34.1
Saracatinib	Src	27.0	12.1	65.7	48.3
Ibrutinib	Src	1.6	15.3	12.8	22.6
Bosutinib	Src	3.2	9.7	26.8	28.1