Skip to main content
. Author manuscript; available in PMC: 2019 Oct 15.
Published in final edited form as: Bioorg Med Chem Lett. 2018 Aug 16;28(19):3210–3215. doi: 10.1016/j.bmcl.2018.08.017

Table 4.

SAR of 4 and 5 substitutions of the amino thiophene ring.

graphic file with name nihms-1510755-t0049.jpg
Cmpd Ar R aRORβ IC50 (μM) bRORγ IC50 (μM)
3 graphic file with name nihms-1510755-t0050.jpg 2-C1 0.040±0.011 > 40
36 graphic file with name nihms-1510755-t0051.jpg 2-C1 0.24±0.07 25%
37 graphic file with name nihms-1510755-t0052.jpg 2-C1 <0.010±0.03 > 3.0
38 graphic file with name nihms-1510755-t0053.jpg 2-C1 45% n.t.
39 graphic file with name nihms-1510755-t0054.jpg 2,3-C1 55% n.t.
40 2,4-C1 45% n.t.
41 2,5-C1 15% n.t.
42 2,6-C1 40% n.t.
43 3,4-C1 45% n.t.
44 2-OMe 0.076±0.024 > 5.0
45 graphic file with name nihms-1510755-t0055.jpg 2-OMe 0.13±0.02 2.9±0.73
46 graphic file with name nihms-1510755-t0056.jpg 2-OMe 0.20±0.02 1.0±0.16
47 graphic file with name nihms-1510755-t0057.jpg 2-OMe 0.33±0.04 > 5.0
a

Displacement of [3H]-T09 from human RORp LBD. Values are the mean ± SEM of at least three replicates. IC50 or displacement of [3H]-T09 at 1 μM);

b

Displacement of [3H]-T09 from human RORy LBD. Values are the mean ± SEM of at least three replicates. IC50 or displacement of [3H]-T09 at 1 μM); n.t. = not tested.