. Author manuscript; available in PMC: 2015 May 1.

Published in final edited form as: Bioorg Med Chem Lett. 2014 Mar 20;24(9):2193–2197. doi: 10.1016/j.bmcl.2014.03.016

Table 3.

IC₅₀, K_i and k_off for a selection of the best compounds

#	IC₅₀ nM^a	K_i nM^b	k_off (10⁻³ s⁻¹)^b	t_1/2 (min)^b
1c	0.4	3.4	1.16	10
2b	1.2	2.7	1.42	8
3b	0.5	3.1	1.05	11
3d	2.6	2.4	4.61	2.5

As determined via a kinetic fluorescent assay.²⁵

As determined via FRET-based displacement assay.²⁶