Skip to main content
. 2015 Sep 8;2015:816856. doi: 10.1155/2015/816856

Table 2.

Crystal structures of PPARγ partial agonists.

Ligand Ligand type PDB Reference Transactivation
PA-082 Isoquinoline 2FVJ [62] EC50 = 260 nM
40% efficacy
Compound 2: 3-fluoro-N-[1-(4-fluorophenyl)-3-(2-thienyl)-1H-pyrazol-5-yl]benzenesulfonamide Sulfonamide 2G0G [58] IC50 = 512 nM
31% efficacy
Compound 1: N-[1-(4-fluorophenyl)-3-(2-thienyl)-1H-pyrazol-5-yl]-3,5-bis(trifluoro- methyl)benzenesulfonamide Sulfonamide 2G0H [58] IC50 = 22.7 nM
50% efficacy
(S)-1 (LT127): 2-(4-2-[1,3-benzoxazol-2-yl(heptyl)amino]ethyl-phenoxy)-2-methyl-butanoic acid Misc. acid (ureidofibrate derivative) 2I4Z
2I4P		 [63] EC50 = 593 nM
50.4% efficacy
SPPARγM2 Indole 2P4Y [50] EC50 = 3 nM
18% efficacy
2t Acetamide 2POB [64] EC50 = 6.0 μM
IC50 = 5.6 μM
54% efficacy
MRL-24 Indole 2Q5P [47] 45% efficacy
nTZDpa Indole 2Q5S [47] ~20% efficacy
SR145 Indole 2Q61 [47] ~20% efficacy
SR147 Indole 2Q6R [47] ~20% efficacy
BVT.13 Misc. acid 2Q6S [47] ~20% efficacy
Amorfrutin 1 Misc. acid 2YFE [65] EC50 = 458 nM
39% efficacy
Cerco-A (−)-Cercosporamide derivative 3B1M [54] EC50 = 3.5 nM
27% efficacy
(R)-1: (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid Misc. acid 3D6D [66] EC50 = 5.93 μM
24% efficacy
INT131 Sulfonamide 3FUR [60] EC50 = 4 nM
30% efficacy
T2384 Sulfonamide 3K8S [67] EC50 = 560 nM
25% efficacy
Compound 23 (−)-Cercosporamide derivative 3LMP [55] EC50 = 180 nM
47% efficacy
TCBPA Bisphenol 3OSI [68] IC50 = 6.0 μM
37% efficacy
TBBPA Bisphenol 3OSW [68] IC50 = 70 nM
37% efficacy
2l: (S)-3-(5-(2-(1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-2-ethyl-5-isobutyl-7-methyl-3H-imidazo[4,5-b]pyridine Misc. pyridine 3R8A [69] EC50 = 212 nM
31% efficacy
Compound 13 Benzimidazole 3S9S [52] pEC50 = 7.4
75% activation
GQ-16 Thiazolidine 3T03 [61] k i = 160 nM
30% efficacy
Compound 17 (−)-Cercosporamide derivative 3V9T [57] EC50 = 240 nM
22% efficacy
Compound 21 (−)-Cercosporamide derivative 3V9V [57] EC50 = 130 nM
79% efficacy
Telmisartan Benzimidazole 3VN2 [53] EC50 = 4.5 μM
25–30% efficacy
(R)-7j: (R)-2-benzyl-3-(4-propoxy-3-((4-(pyrimidin-2-yl)benzamido)methyl)phenyl)propanoic acid Misc. acid 3VSO [70] EC50 = 34.6 nM
65% efficacy
Amorfrutin 2 Misc. acid 4A4V [71] EC50 = 1.2 μM
30% efficacy
Amorfrutin B Misc. acid 4A4W [71] EC50 = 50 nM
20% efficacy
Compound 15 (−)-Cercosporamide derivative 4F9M [56] EC50 = 12 nM
64% efficacy
12b: imidazo[4,5-c]pyridin-4-one derivative Misc. pyridine 4HEE [72] EC50 = 292 nM
25% efficacy
GW0072 Thiazolidine 4PRG [41] IC50 = 110 nM
15–20% efficacy