Table 1. Initial SAR Exploration.

				RORγ-LUC EC50a (μM)
compd	R1	X	R2	human	mouse	LEb	Fsp3c
1	2-indanyl	SCH2	1-naphthyl	1.7	0.70	0.25	0.24
2		OCH2		>20	>20	<0.21	0.24
3a		(CH2)2		1.0	0.40	0.26	0.27
3bd		CH(Me)CH2		1.7	1.1	0.25	0.30
3cd		CH2CH(Me)		1.3	0.67	0.25	0.30
3dd		CH(OH)CH2		>20	>20	<0.20	0.27
3e	c-Hex	(CH2)2		>20	4.5	<0.23	0.43
3f	c-HexCH2			14	2.6	0.23	0.46
3g	c-Hex(CH2)2			0.82	0.30	0.28	0.48
3h	i-Pr(CH2)2			13.0	1.4	0.25	0.41
3i	t-Bu(CH2)2			6.7	0.83	0.25	0.43
3j	Ph(CH2)2			2.5	0.63	0.25	0.24
3k	c-Hex(CH2)2		3-Cl-2-Me-Ph	0.96	0.64	0.29	0.59
3l			2,4-di-Me-Ph	0.90	0.60	0.30	0.61
3m			3,5-di-Me-Ph	2.9	3.1	0.27	0.61

^aThe EC₅₀s are mean values of at least two replicates.

^bLE = −1.37 log EC₅₀(LUC hRORγ)/number of heavy atoms.

^cFsp³ = number of sp³ hybridized carbons/total carbon count.

^dRacemic.