TABLE 2

Properties of PPARγ ligands

Ligand	PPARγ WT K_i	PPARγ Y473A K_i	PPARγ WT EC₅₀	PPARγ Y473A EC₅₀	PPARγ WT
		μM				%^a
SPPARγM1	0.003	0.003	0.005	0.003	18
SPPARγM2	0.001	0.001	0.003	0.003	18
SPPARγM3	0.005	0.007	0.002	0.001	13
SPPARγM4	0.053	0.051	0.037	0.047	13
SPPARγM5	0.040	0.047	0.053	0.067	20
SPPARγM6	0.027	0.030	0.023	0.016	24
SPPARγM7	0.049	0.076	0.028	0.036	32
SPPARγM8	0.024	0.022	0.002	0.002	38
nTZDpa	0.145	0.270	0.140	0.142	33
Full1	0.016	0.077	0.015	0.115	70
Full2	0.675	6.667	0.028	>3.000	70
Full3	1.252	4.803	0.056	0.584	74
		μM				%^a
Full4	0.446	4.912	0.015	>3.000	99
Full5	0.066	5.578	0.003	1.630	105
TZDfa	0.272	>15	0.003	0.666	130
COOH	1.054	>15	0.343	>3.000	70
Rosiglitazone	0.992	>15	0.019	>3.000	100

↵ a Percentage of maximal activity in cell-based transcriptional activity assay vs. rosiglitazone.