Table 4.

C-4 SAR

Compd	R4	Kd (μM)a	AlogP	LipE	Compd	R4	Kd (μM)b	AlogP	LipE	Compd	R4	Kd (μM)b	AlogP	LipE
29	H	0.46 ± 0.078	5.10	1.23	39		0.30 ± 0.078	7.59	−1.06	49		0.14 ± 0.009	6.02	0.85
30		0.27 ± 0.005	6.62	−0.06	40		0.20 ± 0.003	6.18	0.51	50		0.24 ± 0.056	5.47	1.16
31		0.21 ± 0.010b	7.11	−0.44	41		0.13 ± 0.030	4.95	1.95	51		0.33 ± 0.027a	5.47	1.01
32		0.21 ± 0.029	7.56	−0.88	42		0.14 ± 0.013	5.22	1.65	52		0.45 ± 0.104	5.43	0.92
33		0.39 ± 0.093	7.82	−1.41	43		0.25 ± 0.057a	5.14	1.46	53		0.39 ± 0.064	4.75	1.66
34		0.44 ± 0.139	7.90	−1.54	44		0.24 ± 0.083a	4.41	2.21	54		0.35 ± 0.001	4.84	1.61
35		0.15 ± 0.048	7.56	−0.74	45		0.31 ± 0.083	5.22	1.30	55		0.11 ± 0.018	5.12	1.82
36		0.67 ± 0.007	7.56	−1.39	46		0.38 ± 0.025	5.22	1.20	56		0.10 ± 0.011	6.25	0.74
37		1.05 ± 0.056	7.56	−1.59	47		0.14 ± 0.009	4.93	1.92	57		0.18 ± 0.081	5.06	1.68
38		0.12 ± 0.034	7.29	−0.43	48		0.24 ± 0.036	4.93	1.69	58		<0.10	5.49	--c

Measurements are reported as the mean ± SD of two or more independent experiments, each conducted in duplicate.

^aEvaluated through displacement of probe S1 (Supplementary Figure S2).

^bEvaluated through displacement of probe S2 (Supplementary Figure S2).

^cLipE was not determined.