Table 3.

SAR of 4-substitution on the thiophene ring

Cmpd	Ar	R	aRORβ IC50 (μM)	bRORγ IC50 (μM)
16		2-C1	0.23 ± 0.04	14 ± 3
5		2-C1	0.57 ± 0.13	5%
26		2-C1	0.36	50%
27		2-C1	0.087±0.02	14 ± 3
28		2-C1	0.98 ± 0.16	20%
29		2-C1	0.09±0.02	0.33±0.076
30		2-C1	0.38±0.06	30%
31		2-C1	0.47±0.09	30%
32		2-C1	0.015±0.006	0.46±0.24
33		2-OMe	0.18±0.02	0.78±0.17
34		2-OMe	0.22±0.02	0.79±0.32
35		2-OMe	0.23±0.04	10.7

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

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