Table 1. Results of the Ramos Blue NFκB Reporter Assay and PAMPA Permeability Screening^a.

compd	R1	R2	EC50 (nM)	Cmax (nM)	Papp (10–6 cm/s)	log Papp
R848	(see Figure 1)		616 ± 24	1870	5.30	–5.29
1	–NH2	–H	69 ± 10	620	8.51	–5.08
14	–H	–NH2	199 ± 26	620	5.26	–5.28
13b	–H	–NHBoc	1310 ± 230	5600	1.24	–5.91
13c	–OMe	–H	232 ± 0.9	620	4.01	–5.58
13d	–H	–OMe	540 ± 14	1870	2.50	–5.62
15a	–OH	–H	275 ± 29	1870	3.06	–5.52
15b	–H	–OH	231 ± 7	620	0.98	–6.02
16a	–NHAc	–H	107 ± 10	620	3.45	–5.46
16b	–NHC(O)nBu	–H	59 ± 4	210	1.59	–5.80
16c	–NHC(O)OEt	–H	84 ± 4	210	8.78	–5.07
16d	–NHC(O)OiPr	–H	168 ± 7	620	5.12	–5.29
16e	–NHC(O)OnBu	–H	344 ± 9	1870	14.2	–4.85
17a	–NHC(O)CH2NHBoc	–H	44 ± 2	210	4.48	–5.35
17b	–NHC(O)(CH2)2NHBoc	–H	18 ± 1	69	0.434	–6.36
17c	–NHC(O)(CH2)3NHBoc	–H	39 ± 3	210	1.33	–5.88
17d	–NHC(O)(CH2)4NHBoc	–H	62 ± 5	210	1.95	–5.73
17e	–NHC(O)(CH2)5NHBoc	–H	176 ± 9	620	1.91	–5.73
18a	–NHC(O)CH2NH2	–H	209 ± 12	620	0.834	–6.08
18b	–NHC(O)(CH2)2NH2	–H	2060 ± 92	5600	0.131b	–6.89b
18c	–NHC(O)(CH2)3NH2	–H	840 ± 60	1870	0.159	–6.80
18d	–NHC(O)(CH2)4NH2	–H	1340 ± 51	5600	0.838	–6.11
18e	–NHC(O)(CH2)5NH2	–H	485 ± 14	5600	0.436	–6.36

^aAll experiments were performed in triplicate, and the numbers shown represent averages of three experiments.

^bPermeability was assessed using the absorbance at 320 nm instead of 280 nm.