. Author manuscript; available in PMC: 2022 Apr 8.

Published in final edited form as: J Med Chem. 2019 Oct 25;62(21):9521–9540. doi: 10.1021/acs.jmedchem.9b00870

Table 4.

Bioactivity data for fluorescent, biotin and photoreactive analogs of compound 1.

Compound	NF-κB^a		ISRE^a		MTT^a
Compound	% Activation	SEM	% Activation	SEM	% Viability	SEM
56	100	1.3	96	4.2	98.1	1.7
57	111	2.1	123	5.4	76.9	1.3
58	195	4.7	175	8.6	69.6	1.2
59	215	13.8	201	3.8	76.6	2.6
60	158	5.9	166	2.4	77.3	2.5
61	104	5.1	104	3.1	87.2	1.8
62	217	13.9	182	2.5	73.4	1.5
63	138	4.2	117	1.2	68.9	0.8
64	162	5.1	140	1.4	73.8	0.6

The % activation values in NF-ĸB and ISRE induction assays were two point normalized between compound 1 as 200% and LPS (10 ng/mL) for NF-κB or IFN-α (100 U/mL) for ISRE as 100%. The mean SEAP response in NF-ĸB assay for compound 1 + LPS and LPS alone was 3.44 ± 0.08 and 0.56 ± 0.06 μg/mL, respectively. The mean emission ratio in ISRE assay for compound 1 + IFN-α and IFN-α alone was 1.88 ± 0.04 and 0.69 ± 0.05 μg/mL, respectively. The % viability values for compounds in MTT assay were normalized to DMSO as 100%. The mean OD value at 405 nm for DMSO was 1.24 ± 0.03. All raw values used for normalization are represented as mean ± SEM.