. Author manuscript; available in PMC: 2018 Jun 8.

Published in final edited form as: J Med Chem. 2017 May 22;60(11):4584–4593. doi: 10.1021/acs.jmedchem.6b01727

Table 1. Structure Activity of Compound 1 Analogs^a.

Compound	EC₅₀ (nM) n=3	Trans-activation (%)* n=2	Purity (%)
1 (INT131)	170±10	24±4	>95
2	600±61	29±6	>99
3	4±1	21±9	>99
4	134±13	27±8	85
5	957±499	18±7	97
6	94±10	34±10	93
7	ND	2±1	>99
8	2±1	13±7	88
9	169±14	9±5	94
10	131±6	10±6	>98
11	151±20	11±6	96
12	4289±289	23±12	90
13	5810±945	19±11	99
14	3314±2923	14±6	>99
15	ND	14±8	>99

Each data point in the EC₅₀ dose response was repeated in triplicate, and standard deviation was derived from these values. In addition, two biological replicates were performed to ensure reproducibility of the data. ND means not determined.

Table 1. Structure Activity of Compound 1 Analogsa.

Table 1. Structure Activity of Compound 1 Analogs^a.