rosiglitazone profile

7,8-diacetoxy-4-methylcoumarin: possess strong antioxidant and radical scavenging activities; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

7,8-diacetoxy-4-methylcoumarin : A coumarin substituted by a methyl group at position 4 and by acetyloxy groups at positions 7 and 8. It exhibits strong antioxidant and radical scavenging properties. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

rosiglitazone is involved in 1 pathway(s), involving a total of 3 unique proteins and 20 unique compounds

ID Source	ID
PubMed CID	390798
CHEMBL ID	86633
CHEBI ID	193139
SCHEMBL ID	3052874
MeSH ID	M0237199
PubMed CID	77999
CHEBI ID	50122
SCHEMBL ID	5169
SCHEMBL ID	14383595
MeSH ID	M0237199

Synonym
(8-acetoxy-4-methyl-2-oxo-chromen-7-yl) acetate
7-(acetyloxy)-4-methyl-2-oxo-2h-chromen-8-yl acetate
CHEMBL86633
nsc-688794
nsc688794
NCI60_031992
OPREA1_472625
CHEBI:193139
damtc
4-methyl-2-oxo-2h-1-benzopyran-7,8-diyl diacetate
7,8-diacetoxy-4-methylcoumarin
4-methyl-2-oxo-2h-chromene-7,8-diyl diacetate
(8-acetyloxy-4-methyl-2-oxochromen-7-yl) acetate
7,8-dihydroxy-4-methylcoumarin diacetate
68454-15-9
SCHEMBL3052874
DTXSID70327812
SR-01000244966-1
sr-01000244966
AC-3459
STL350047
AB00698473-18
AB00698473-17
BRD-A97437073-001-03-1
BRD-A97437073-001-02-3
gtpl1056
5-[[4-[2-(methyl-pyridin-2-ylamino)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
avandaryl
rosiglitazona
CHEBI:50122 ,
5-((4-(2-(methyl-2-pyridinylamino)ethoxy)phenyl)methyl)-2,4-thiazolidinedione
rosiglitazonum
5-(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}benzyl)-1,3-thiazolidine-2,4-dione
SPECTRUM_001703
S00306
SPECTRUM5_001464
BSPBIO_002693
2,4-thiazolidinedione, 5-((4-(2-(methyl-2-pyridinylamino)ethoxy)phenyl)methyl)-
brl 49653
2,4-thiazolidinedione, 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]- (9ci)
122320-73-4
5-[4-[2-(n-methyl-n-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione
rosiglizole
2,4-thiazolidinedione, 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-
ROSIGLITAZONE ,
5-[[4-[2-(methyl-(2-pyridyl)amino)ethoxy]phenyl]methyl] thiazolidine-2,4-dione
brl-49653
5-((4-(2-methyl-2-(pyridinylamino)ethoxy)phenyl)methyl)-2,4-thiazolidinedione-2-butenedioate
5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione
(+/-)-5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione
DB00412
(rs)-5-{4-[2-(methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedion
brl49653
NCGC00095124-01
NCGC00095124-02
tdz 01
rosiglitazone (avandia) ,
rosiglitazone [inn:ban]
c18h19n3o3s
KBIO2_004751
KBIO2_002183
KBIO2_007319
KBIO3_001913
KBIOSS_002183
KBIOGR_001609
SPECTRUM2_001241
SPBIO_001142
SPECTRUM4_001125
SPECTRUM3_000997
SPECTRUM1504263
NCGC00095124-03
rgz ,
rosigilitazone
idmb (1um brl49653, 1um dexamethasone, 0.5um ibmx, 10ug/ml insulin)
rosi
HMS2094O13
gaudil (tn)
rosiglitazone (inn)
D08491
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione
HMS1922J11
5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
NCGC00095124-05
NCGC00095124-04
nsc 758698
unii-05v02f2kdg
hsdb 7555
05v02f2kdg ,
rosvel
gaudil
tdz-01
rezult
nsc-758698
BCP9000017
pharmakon1600-01504263
nsc758698
dtxcid5017131
tox21_111434
cas-122320-73-4
dtxsid7037131 ,
CCG-39102
HY-17386
CS-1088
BCP0726000232
FT-0602578
NCGC00095124-06
AKOS015894872
S2556
rosiglitazone [mi]
5-(4-(2-(n-methyl-n-(2-pyridinyl)amino)ethoxy)benzyl)-2,4-thiazolidinedione
rosiglitazone [inn]
rosiglitazone [vandf]
rosiglitazone [ema epar]
rosiglitazone [iarc]
rosiglitazone [mart.]
rosiglitazone [hsdb]
rosiglitazone [who-dd]
AB00698473-15
SCHEMBL5169
tox21_111434_1
NCGC00095124-08
6P-065
AB00698473-19
5-[4-[2-[n-methyl-n-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione
5-[[4-[2-(methyl-2-pyridinylamino) ethoxy]phenyl]methyl]-2,4-thiazolidinedione
5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione
5-[4-[2-(n-methyl-n-(2-pyridyl)amino)ethoxy]benzyl] thiazolidine-2,4-dione
5-[4-[2-(n-methyl-n-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4dione
5-[4-[2-[n-methyl-n-(2-pyridyl)amino]ethoxy]phenyl methyl]thiazolidine-2,4-dione
SCHEMBL14383595
Q-201681
5-[[4-[2-(methyl-2-pyridinylamino)e thoxy]phenyl]methyl]-2,4-thiazolidinedione
HB2556
HMS3649G08
R0106
AB00698473_20
AB00698473_23
AB00698473_21
AB00698473_22
mfcd00871760
bdbm50030474
sr-01000763023
SR-01000763023-6
SR-01000763023-5
HMS3656K16
rosiglitazone, >=98% (hplc)
dioxopromethazinehydrochloride
rosigltazone
5-[4-[2-[methyl(2-pyridyl)amino]ethoxy]benzyl]thiazolidine-2,4-dione
SW197573-6
rosiglitazone base
Q424771
SY031184
1217260-35-9
SR-01000763023-12
BCP03047
BRD-A97437073-001-04-9
SB17326
HMS3871L03
HMS3884N08
HMS3744M11
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)-benzyl)thiazolidine-2,4-dione
rosiglitazone- bio-x
BR164372
a10bg02
(+-)-5-(p-(2-(methyl-2-pyridylamino)ethoxy)benzyl)-2,4-thiazolidinedione
rosiglitazone (iarc)
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)-1,3-thiazolidine-2,4-dione
rosiglitazon
rosiglitazone (mart.)

Excerpt	Reference
"Rosiglitazone (RSG) is a synthetic agonist of peroxisome proliferator-activated receptor-γ (PPARγ), which plays a central role in the regulation of metabolism. "	( Fang, L; Liu, Y; Liu, YH; Wang, NP; Zhang, X; Zhao, BL, 2022)
"Rosiglitazone is a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, known to stimulate hyperplasia and to efficiently improve insulin sensitivity."	( Fryklund, C; Morén, B; Neuhaus, M; Periwal, V; Stenkula, KG, 2022)
"Rosiglitazone is a synthetic agonist of PPARγ, whose endogenous agonist is 15-deoxy-Δ"	( Chen, Y; Duan, Y; Guo, F; Hajjar, DP; Han, J; Hu, H; Hu, W; Kong, D; Li, Q; Li, X; Ma, C; Miao, QR; Wang, H; Wei, Z; Yang, X; Yu, M; Zhang, S; Zhang, Y; Zhu, Y, 2020)
"Rosiglitazone (RSG) is a member of the thiazolidinedione family and is reported to protect cells from cytotoxicity and endoplasmic reticulum (ER) stress in other cell types, but whether RSG protects granulosa cells remain unknown."	( Liu, S; Wan, J, 2020)
"Rosiglitazone is a ligand of peroxisome proliferation-activated receptor gamma (PPARγ). "	( Chen, J; Huang, F; Li, Y; Zhang, XK; Zhou, H, 2020)
"Rosiglitazone is an effective insulin-sensitizer, however associated with bone loss mainly due to increased bone resorption and bone marrow adiposity. "	( Calzone, R; Cugno, C; Halade, GV; Kizhakayil, D; Rahman, MM; Rahman, SM, 2021)
"Rosiglitazone (ROSG) is a potent PPAR-γ agonist and has been shown to induce neuroprotection in animal models of spinal cord injury (SCI)."	( Li, H; Wang, L; Yang, X; Zhang, Q, 2017)
"Rosiglitazone is an anti-diabetic agent that raised a major controversy over its cardiovascular adverse effects. "	( Al Yacoub, N; Awad, SM; El-Orabi, NF; Kunhi, M; Pharaon, LF; Poizat, C, 2017)
"Rosiglitazone is a PPARγ agonist and can promote the expression of PPARγ to increase the expression of lipogenesis-related genes."	( Guo, J; Li, L; Li, X; Wang, L; Wang, Y; Zhang, H; Zhong, T, 2018)
"Rosiglitazone (RSG) is a member of the thiazolidinedione family and is a peroxisome proliferator-activated receptor-γ (PPARγ) agonist."	( Chen, L; Ge, X; Hu, X; Huang, X; Jing, J; Jueraitetibaike, K; Ma, R; Pan, P; Qiu, X; Yao, B, 2018)
"Rosiglitazone (RG) is a well-known activator of peroxisome proliferator-activated receptor-gamma (PPAR"	( Kang, JH; Liu, MX; Pang, YL; Peng, SG; Wang, Z; Zhu, Q, 2018)
"Rosiglitazone (RGZ) is a highly potent agonist of PPARγ."	( Chen, SZ; Li, JJ; Li, YY; Yu, FX; Zheng, YH; Zhi, SC, 2019)
"Rosiglitazone, which is a peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist, has been shown to exert antifibrotic and anti-inflammatory effects on some renal diseases."	( Deng, J; Shao, M; Shao, X; Wang, X; Xia, Y; Xiong, C; Zhou, Q; Zou, H, 2019)
"Rosiglitazone is an antidiabetic drug in the thiazolidinedione class that regulates metabolic flexibility and glucose uptake in various cell types, but its effects on boar sperm metabolism are unknown."	( Guo, HT; Sun, HH; Sun, LZ; Sun, M; Wang, JR; Wang, N; Wang, SW; Yang, K; Yue, SL; Zhou, JB, 2019)
"Rosiglitazone (RSG) is an antidiabetic drug that has been associated with increased peripheral fractures, primarily in postmenopausal women. "	( Fitzpatrick, LA; Guldberg, RE; Hoffman, SJ; Jolette, J; Kumar, S; Mansell, P; Samadfam, R; Smith, SY, 2013)
"Rosiglitazone is a peroxisome proliferator-activated receptor gamma (PPARγ) synthetic activator from the group of thiazolidinediones often used in the treatment of chronic diseases such as type 2 diabetes and other forms of insulin resistance. "	( Karpeta, A; Rak-Mardyła, A, 2014)
"Rosiglitazone (rosi) is a powerful insulin sensitizer, but serious toxicities have curtailed its widespread clinical use. "	( Lazar, MA; Lim, HW; Marinis, JM; Prokesch, A; Steger, DJ; Step, SE; Won, KJ; You, SH, 2014)
"Rosiglitazone (RSG) is an effective thiazolidinedione hypoglycemic agent, and CHS synergistically enhanced the effect of RSG."	( Chang, YG; Hu, SW; Li, ZJ; Tian, YY; Wang, YM; Xue, CH, 2014)
"Rosiglitazone (RGZ) is a thiazolidinedione ligand of peroxisome proliferator-activated receptor-γ. "	( Fu, J; Huang, H; Huang, Z; Liu, R; Liu, Y; Rui, M; Wang, Z, 2014)
"Rosiglitazone (RGZ) is an insulin sensitizer used for glycaemic control in type 2 diabetes."	( Chiou, TY; Chou, CA; Kuo, WH; Lee, CT; Lee, YT; Li, LC; Ng, HY; Pei, SN, 2015)
"Rosiglitazone (RSG) is a synthetic full agonist of transcription factor peroxisome proliferator activated receptor gamma. "	( Acevedo, AC; Amato, AA; Borges, GA; Coelho, MS; de Lima, CL; Guerra, E; Neves, Fde A; Resende, AP; Rodrigues da Silva, J; Royer, C, 2015)
"Rosiglitazone is a well-known anti-diabetic drug that increases insulin sensitivity via peroxisome proliferator-activated receptor γ (PPARγ) activation, but unfortunately it causes bone loss in animals and humans. "	( Cheon, HG; Choi, HE; Hong, S; Kang, JH; Kim, J; Kim, OH; Kwak, HJ; Oh, BC, 2015)
"Rosiglitazone is a selective ligand for peroxisome proliferator-activated receptor-gamma (PPAR-γ), which serves diverse biological functions. "	( Byun, SH; Choi, HJ; Choi, J; Choi, YS; Chung, JH; Jung, NC; Jung, SY; Kang, S; Lee, JH; Lim, DS; Seo, HG; Song, JY, 2016)
"Rosiglitazone is an antidiabetic compound that enhances metabolic flexibility and glucose utilization in various cell types, but its effects on sperm metabolism are unknown."	( Aitken, RJ; Gibb, Z; Lambourne, SR; Swegen, A, 2016)
"Rosiglitazone (RSG) is a potent drug used in the treatment of insulin resistance; however, it is associated with marked skeletal toxicity. "	( Chen, QZ; Deng, ZL; He, BC; Li, Y; Liu, RX; Ren, WY; Shao, Y; Sun, WJ; Wu, K; Yang, JQ; Yu, Y; Zeng, YH; Zhou, LY, 2016)
"Rosiglitazone (Rosi) is a potent insulin sensitizer and may also slow the development of DN by a mechanism independent of its effect on hyperglycemia."	( Brosius, FC; Feldman, EL; Kretzler, M; Pennathur, S; Sullivan, KA; Wiggin, TD, 2008)
"Rosiglitazone is an insulin sensitizer that, because of minimal associated gastrointestinal disturbance, was used as an alternative to metformin in PCOS patients."	( Aubuchon, M; Haddad, GF; Jodicke, C; Thomas, MA; Williams, DB, 2008)
"Rosiglitazone is a partial GR agonist, affecting GR activation and trafficking to influence engagement of target genes and affect cell function."	( Berry, A; D'Acquisto, F; Ianaro, A; Matthews, L; Ray, D; Tersigni, M, 2009)
"Rosiglitazone is an effective therapy for type 2 diabetes although concerns have grown about the incidence of oedema and cardiovascular adverse events in patients treated with the drug. "	( Waksman, JC, 2008)
"Rosiglitazone is an agonist of the peroxisome proliferator-activated receptor (PPAR) gamma that may modify HDL metabolism in humans, but this effect has not been completely elucidated. "	( Carreón-Torres, E; Cruz, D; Fievet, C; Gamboa, R; López-Marure, R; Luc, G; Menjivar, M; Monter-Garrido, M; Pérez-Méndez, O; Rendón-Sauer, K; Toledo-Ibelles, P; Vargas-Alarcón, G, 2009)
"Rosiglitazone is an insulin-sensitizing oral thiazolidinedione used for treating patients with type 2 diabetes mellitus. "	( Fang, S; Jin, G; Li, G; Ma, K; Qi, J; Wang, Y; Yu, J, 2008)
"Rosiglitazone is a member of the thiazolidinedione family of synthetic peroxisome proliferator-activated receptor (PPAR) agonists. "	( Cotter, TG; Doonan, F; O'Driscoll, C; Wallace, DM, 2009)
"Rosiglitazone is a commonly prescribed insulin-sensitizing drug with a selective agonistic activity on the peroxisome proliferator-activated receptor-gamma (PPAR-gamma). "	( Caboni, P; Carboni, E; Carta, AR; Frau, L; Garau, A; Ibba, M; Schintu, N, 2009)
"Rosiglitazone is an insulin sensitiser used in combination with metformin, a sulfonylurea, or both, for lowering blood glucose in people with type 2 diabetes. "	( Beck-Nielsen, H; Curtis, PS; Gomis, R; Hanefeld, M; Home, PD; Jones, NP; Komajda, M; McMurray, JJ; Pocock, SJ, 2009)
"Rosiglitazone is a peroxisome proliferator-activated receptor (PPAR) gamma agonist that has shown promise as both an antiproliferative and redifferentiating agent for the treatment of thyroid cancer in preclinical studies. "	( Clark, OH; Greenspan, FS; Hawkins, R; Kebebew, E; Lindsay, S; Woeber, KA, 2009)
"Rosiglitazone is a thiazolidinedione used to treat insulin resistance in diabetes. "	( Arrigoni, G; Iori, E; Millioni, R; Puricelli, L; Tessari, P, 2010)
"Rosiglitazone is a peroxisome proliferator-activated receptor (PPAR)-γ agonist. "	( Hsu, BG; Lee, CC; Lee, CJ; Lee, RP; Subeq, YM; Wu, WT, 2011)
"Rosiglitazone is a drug used in human medicine for treating type II diabetes mellitus. "	( Cosola, C; Minoia, G; Punzi, S; Rizzo, A; Roscino, MT; Sciorsci, RL; Spedicato, M, 2009)
"Rosiglitazone maleate is an antihyperglycemic agent in the thiazolidinedione class. "	( Chompootaweep, S; Intanil, N; Khemsri, W; Thaworn, N; Wittayalertpanya, S, 2010)
"Rosiglitazone is a peroxisome proliferators-activated receptor gamma (PPARgamma) ligand, which inhibits tumor growth by activating PPARgamma signaling pathways. "	( Cao, LQ; Peng, HP; Shao, ZL; Xia, T; Xiao, JB, 2010)
"Rosiglitazone is a potent synthetic peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist which improves glucose control in the plasma and reduces ischemic brain injury. "	( Cheng, FC; Cheng, SM; Chou, CC; Chuang, HC; Lee, MR; Sheu, WH, 2011)
"Rosiglitazone is a widely used oral hypoglycaemic agent, which improves insulin resistance in type 2 diabetes. "	( Choi, BH; Hahn, SJ; Jeong, I, 2011)
"Rosiglitazone (RSG) is a member of thiazolidinediones (TDZs) family, which is the ligand of the of nuclear transcription factor peroxisome proliferator-activated receptor-γ (PPARγ), being used clinically for the treatment of type 2 diabetic patients through their insulin-sensitizing effect."	( Chen, HL; Hai, CX; Hu, JX; Li, WL; Liu, JZ; Wang, X; Wang, Z, 2011)
"Rosiglitazone is an oral hypoglycaemic agent of the thiazolidinedione group. "	( Abdullah, WZ; Ibrahim, S; Mustaffa, N; Yusof, Z, 2011)
"Rosiglitazone is an anti-diabetic drug improving insulin sensitivity and glucose uptake in skeletal muscle and adipose tissues. "	( Cui, N; Jiang, C; Jin, X; Yang, Y; Yu, L, 2011)
"Rosiglitazone is a PPARγ agonist commonly used to treat diabetes. "	( Hoo, RL; Huang, Y; Lam, KS; Lau, CW; Lee, VW; Tian, XY; Vanhoutte, PM; Wang, Y; Wong, WT; Xu, A; Yu, J, 2011)
"Rosiglitazone (RSG) is an insulin-sensitizing drug used to treat type 2 diabetes mellitus. "	( Fantus, IG; Grynpas, MD; Renlund, R; Sardone, LD; Willett, TL, 2011)
"Rosiglitazone is a TZD that has been found to increase the risk of cardiovascular events, especially of myocardial ischemic events."	( Chang, YW; Chen, WL; Chou, CC; Kao, TW; Loh, CH; Wang, CC, 2011)
"Rosiglitazone is an FDA-approved peroxisome proliferator-activated receptor gamma (PPARγ) agonist and antidiabetic agent in humans that has been investigated for its ability to reduce tumor cell growth. "	( Allstadt Frazier, S; Guerrero, TA; Kass, PH; LaChapelle, H; McKemie, DS; Rodriguez, CO; Skorupski, KA, 2014)
"Rosiglitazone is a thiazolidinedione, a synthetic PPARγ receptor agonist with insulin-sensitizing properties that is used as an antidiabetic drug. "	( Addabbo, F; Montagnani, M; Potenza, MA; Sgarra, L, 2012)
"Rosiglitazone is an anti-diabetic drug acting as an insulin sensitizer. "	( Cui, N; Jiang, C; Jin, X; Shi, Z; Wu, Y; Yu, L; Zhu, D, 2012)
"Rosiglitazone is a commonly prescribed insulin-sensitizing drug with selective agonistic activity at the peroxisome proliferator-activated receptor-γ (PPARγ). "	( Koh, HC; Lee, EY; Lee, JE; Park, JH; Shin, IC, 2012)
"Rosiglitazone (Rosi) is a drug in the thiazolidinedione class for treatment of type 2 diabetes mellitus (T2DM), which binds and activates PPARγ nuclear receptor in fat cells, sensitizing them to insulin. "	( Aronson, J; Lecka-Czernik, B; Liu, L, 2013)
"Rosiglitazone is an insulin-sensitizing oral agent in the thiazolidinedione class used to treat patients with type 2 diabetes mellitus. "	( DiCicco, RA; Freed, MI; Miller, AK, 2002)
"Rosiglitazone is an FDA-approved oral antidiabetic agent for the treatment of type 2 diabetes. "	( Gaddy, D; Lecka-Czernik, B; Montague, DC; Rzonca, SO; Suva, LJ, 2004)
"Rosiglitazone (Avandia) is a PPAR-gamma agonist (the most potent PPAR-gamma agonist of the thiazolidinedione antidiabetics)."	( Caputi, AP; Chatterjee, PK; Cuzzocrea, E; Cuzzocrea, S; Di Paola, R; Di Rosa, M; Dugo, L; Fulia, F; Genovese, T; Ianaro, A; Patel, NS; Pisano, B; Thiemermann, C, 2004)
"Rosiglitazone is a novel thiazolidinedione antidiabetic drug, but little is known about the drug interaction between rifampin and rosiglitazone."	( Kang, MH; Kim, KA; Kim, SL; Park, JY; Shin, JG, 2004)
"Rosiglitazone is a thiazolidinedione antihyperglycemic drug used in the treatment of type 2 diabetes mellitus. "	( Frye, RF; Hruska, MW, 2004)
"Rosiglitazone is a safe and effective oral agent for the treatment of diabetes mellitus after solid organ transplantation. "	( Baldwin, D; Duffin, KE, 2004)
"Rosiglitazone is an agonist of peroxisome proliferator activated receptor-gamma (PPARgamma) and ameliorates insulin resistance in type II diabetes. "	( McBain, SC; Morgan, NG; Scarpello, JH; Smith, SA; Tadayyon, M; Welters, HJ, 2004)
"Rosiglitazone is a novel thiazolidinedione antidiabetic drug, mainly metabolized by CYP2C8 and to a lesser extent CYP2C9."	( Kim, KA; Lee, KY; Park, JY; Shin, JG, 2004)
"Rosiglitazone (RSG) is an insulin-sensitizing thiazolidinedione (TZD) that exerts peroxisome proliferator-activated receptor-gamma (PPARgamma)-dependent and -independent effects. "	( Chen, ZP; Febbraio, MA; Hashem, M; Hawley, JA; Kemp, BE; Lessard, SJ; Reid, JJ; Watt, MJ, 2006)
"Rosiglitazone is a peroxisome proliferator-activated receptor-gamma (PPARG) agonist that is widely used in the treatment of type 2 diabetes."	( Chen, Y; Han, R; Sun, X; Wang, Z, 2006)
"Rosiglitazone is a new antidiabetic agent of the thiazolidinediones."	( Gu, YY; Li, G; Luo, M; Luo, TH; Tian, JY; Wang, X; Zhang, HL; Zhou, WZ; Zhu, HD, 2006)
"Rosiglitazone is a thiazolidinedione that reduces insulin resistance and might preserve insulin secretion. "	( Bosch, J; Dinccag, N; Gerstein, HC; Hanefeld, M; Holman, RR; Hoogwerf, B; Laakso, M; Mohan, V; Pogue, J; Shaw, J; Sheridan, P; Yusuf, S; Zinman, B, 2006)
"Rosiglitazone is a peroxisome proliferator-activated receptor gamma (PPARgamma) agonist that has been shown to induce differentiation, cell cycle arrest, and apoptosis in a variety of human cancers including thyroid cancer."	( Clark, OH; Duh, QY; Greenspan, FS; Kebebew, E; Lindsay, S; Morita, E; Peng, M; Reiff, E; Treseler, P; Woeber, KA, 2006)
"Rosiglitazone is an insulin-sensitizing agent that has recently been shown to exert beneficial effects on atherosclerosis. "	( Askari, B; Beavo, JA; Bender, AT; Bornfeldt, KE; Coleman, RA; Golej, DL; Hsueh, WA; Kanter, JE; Liu, J; Sherrid, AM, 2007)
"Rosiglitazone is an insulin-sensitizing agent. "	( Avsar, E; Celikel, C; Emekli, E; Eren, F; Haklar, G; Imeryuz, N; Tahan, V; Tozun, N; Uzun, H; Yavuz, D; Yuksel, M, 2007)
"Rosiglitazone (Avandia) is an antihyperglycaemic agent of the thiazolidinedione class that improves glycaemic control (as indicated by glycosylated haemoglobin [HbA1c] and fasting plasma glucose [FPG] levels) primarily by increasing hepatic and peripheral insulin sensitivity, and in addition may help to preserve pancreatic beta-cell function. "	( Deeks, ED; Keam, SJ, 2007)
"Rosiglitazone maleate is a thiazolidinedione approved for treatment of type 2 diabetes mellitus. "	( Al-Kadhi, Y; Al-Omary, M; El-Naggar, MH; Habib, B; Helmy, A; Moawad, M, 2008)
"Rosiglitazone (BRL 49653) is a novel thiazolidinedione which has been reported not to cause vasoleraxation."	( Aaronson, PI; Knock, GA; Mishra, SK, 1999)
"Rosiglitazone is a potent peroxisome proliferator-activated receptor gamma agonist that decreases hyperglycemia by reducing insulin resistance in patients with type 2 diabetes mellitus. "	( Cowley, H; Cox, PJ; Harris, AM; Hollis, FJ; Miller, AK; Ryan, DA; Vousden, M, 2000)
"Rosiglitazone is a potent oral antidiabetic agent of the thiazolidinedione class that works through activation of the peroxisome proliferator-activated nuclear receptor. "	( Allen, A; Carr, A; Di Cicco, RA; Fowles, S; Freed, MI; Jorkasky, DK, 2000)
"Rosiglitazone is a potent insulin-sensitizing oral hypoglycemic agent of the thiazolidinedione class that works through activation of the peroxisome proliferator-activated receptor-gamma (PPAR-gamma) nuclear receptor and improves glycemic control in patients with non-insulin-dependent diabetes mellitus. "	( Di Cicco, RA; Freed, MI; Miller, AK; Patterson, S, 2000)
"Rosiglitazone is a promising insulin sensitizer for treatment of PCOS. "	( Abbasi, F; Cataldo, NA; Lamendola, C; McLaughlin, TL; Reaven, GM, 2001)
"Rosiglitazone(RSG) is an oral antidiabetic agent of the thiazolidinedion(TDZ) class that exerts its antihyperglycemic effect by reducing insulin resistance. "	( Oka, Y; Yonezawa, N, 2001)

Excerpt	Reference
"Rosiglitazone has a null effect on the risk of prostate cancer."	( Tseng, CH, 2023)
"Rosiglitazone has a protective effect in peritonitis, simultaneously decreasing NF-κB phosphorylation, suggesting that NF-κB signaling pathway mediated peritoneal inflammation induced by LPS."	( Wu, J; Yang, X; Yu, XQ; Zhang, YF; Zou, XL, 2015)
"Rosiglitazone has a protective effects in rats with severe acute pancreatitis."	( Chen, C; Feng, JR; Hao, SX; Wang, WX; Yan, H, 2009)
"Rosiglitazone has a substantial antisteatogenic effect in the first year of treatment without additional benefit with longer therapy despite a maintained effect on insulin sensitivity and transaminase levels. "	( Bernhardt, C; Bruckert, E; Charlotte, F; Giral, P; Halbron, M; Hartmann-Heurtier, A; Lenaour, G; Poynard, T; Ratziu, V, 2010)
"Rosiglitazone (RSG) has a variety of actions on both insulin sensitization and anti-atherogenic effects. "	( Chen, CY; Chen, YL; Chuang, LM; Tsai, JS, 2010)
"Rosiglitazone has an ameliorative effect on the DRG and enhances the functional recovery after SNC in rats."	( Karbalay-Doust, S; Noorafshan, A; Omidi, A; Shariat, K, 2012)
"Rosiglitazone has an anti-inflammatory effect in renal tubular epithelial cells through the inhibition of NF-kappaB activation."	( Kang, KP; Kim, DH; Kim, HJ; Kim, W; Lee, S; Moon, SO; Park, SK; Sung, MJ, 2005)
"Rosiglitazone (RGTZ) has a protective effect against various types of injury. "	( Ahn, KO; Bang, BK; Choi, BS; Kim, J; Kim, JY; Kim, SH; Kim, YS; Li, C; Lim, SW; Yang, CW; Yang, HJ, 2007)
"Rosiglitazone, a drug that has an excellent safety profile, may offer a well tolerated systemic treatment option for AD. "	( Behshad, R; Cooper, KD; Korman, NJ, 2008)
"Rosiglitazone has a low risk of gastrointestinal side effects and hypoglycemia, reduced insulin demand, potential sparing effects on beta-cells, and favorable drug interaction profile."	( Travaglini, MT; Werner, AL, 2001)
"Rosiglitazone has shown promising anti-inflammation effect. "	( Chen, WM; Huang, MY; Lin, J; Sun, JR; Sun, PH; Wang, F; Wang, HY, 2014)
"Rosiglitazone has a null effect on the risk of prostate cancer."	( Tseng, CH, 2023)
"Rosiglitazone has recently been considered as a potential neuroprotective factor in epilepsy because of its antioxidative function."	( Chen, L; Peng, Y; Qu, Y; Wang, D; Zhu, Y, 2021)
"Rosiglitazone has been reported to exert dual effects on liver steatosis, and it could exacerbate liver steatosis in obese animal models, which was suggested to be closely related to the elevated hepatic expression of FABP4. "	( Chen, MT; Gao, DD; Huang, JS; Li, YX; Wang, HY, 2021)
"rosiglitazone) have been shown to act on several pathways implicated in the pathogenesis of severe malaria and may improve clinical outcome as an adjunctive intervention."	( Bassat, Q; Bila, R; Crowley, VM; Kain, KC; Madrid, L; Mayor, A; Mucavele, H; Serghides, L; Sitoe, A; Varo, R, 2017)
"Rosiglitazone has been proposed as a treatment strategy for type 2 diabetes mellitus (T2DM), and it could provide robust glucose-lowering capability with risk of cardiovascular events. "	( Cheng, D; Gao, H; Li, W, 2018)
"Rosiglitazone has been proven to enhance the glycolytic capability of stallion spermatozoa maintained at ambient temperature."	( Balao da Silva, C; Gazquez, A; Gil, C; Masot, J; Ortega-Ferrusola, C; Ortiz-Rodriguez, JM; Peña, FJ; Redondo, E; Tapia, JA, 2019)
"Rosiglitazone (ROG) has been shown to exert beneficial effects on glycemic control and renal protection. "	( Hu, M; Huang, Y; Lei, Y; Liu, R; Wang, X; Yu, X; Zheng, Z, 2013)
"Rosiglitazone has been known to attenuate neurodegeneration in Alzheimer's disease (AD), but the underlying mechanisms remain to be fully elucidated. "	( Anwyl, R; Bao, X; Li, S; Liu, G; Wang, Q; Wu, J; Xu, S; Zheng, B, 2014)
"Rosiglitazone (RGL) has been used to ameliorate lipids homeostasis and also to treat inflammatory diseases. "	( Dias, C; Helou, CM; Volpini, RA, 2013)
"Rosiglitazone has been known to attenuate neurodegeneration in Alzheimer's disease (AD), but the underlying mechanisms remain unclear. "	( An, P; Chang, L; Chen, X; Guan, Q; Mody, I; Wang, C; Wang, Q; Wei, X; Xu, S; Zhang, J; Zheng, B; Zhou, W, 2014)
"As rosiglitazone has recently been linked to a higher risk of heart failure, stroke, and all-cause mortality in old patients, it has been interrupted from the European market."	( Antonelli, A; Di Domenicantonio, A; Fallahi, P; Ferrari, SM; Ferri, C; Manfredi, A, 2014)
"Rosiglitazone has been shown to be beneficial for cardiovascular disease because of its pleiotropic effects."	( Chiou, TY; Chou, CA; Kuo, WH; Lee, CT; Lee, YT; Li, LC; Ng, HY; Pei, SN, 2015)
"Rosiglitazone has previously been widely used to treat patients with type 2 diabetes mellitus, but its safety in terms of cardiovascular morbidity and mortality had been called into question. "	( Barendregt, JJ; Doi, SA; Furuya-Kanamori, L; Stone, JC, 2015)
"Rosiglitazone has been found to have anti-atherogenic effects and to increase serum high-density lipoprotein (HDL) cholesterol (HDL-C) levels. "	( Fan, YZ; Guo, ZG; Lai, WY; Li, C; Liu, TR; Tu, Y; Xie, D; Zhong, JK, 2015)
"Rosiglitazone has a protective effect in peritonitis, simultaneously decreasing NF-κB phosphorylation, suggesting that NF-κB signaling pathway mediated peritoneal inflammation induced by LPS."	( Wu, J; Yang, X; Yu, XQ; Zhang, YF; Zou, XL, 2015)
"Rosiglitazone (ROSI) has been reported to have antiproliferative effects against various types of cancer cells and also to induce antioxidant enzymes that can scavenge reactive oxygen species (ROS) and thereby modify radiosensitivity."	( An, Z; Park, WY; Yu, JR, 2017)
"Thus rosiglitazone has direct effects on the renal glomerulus to reduce reactive oxygen species accumulation to prevent type 1 diabetic mice from development of DN."	( Brosius, FC; Byun, J; Feldman, EL; Kennedy, RT; Kretzler, M; Lorenz, M; Pennathur, S; Saha, J; Schin, M; Zhang, H, 2008)
"Rosiglitazone has a protective effects in rats with severe acute pancreatitis."	( Chen, C; Feng, JR; Hao, SX; Wang, WX; Yan, H, 2009)
"Rosiglitazone treatment has been shown to increase adipogenesis in bone marrow and to induce bone loss."	( Arnol, V; Cortizo, AM; Gangoiti, MV; McCarthy, AD; Molinuevo, MS; Schurman, L; Sedlinsky, C; Tolosa, MJ, 2010)
"Rosiglitazone has a substantial antisteatogenic effect in the first year of treatment without additional benefit with longer therapy despite a maintained effect on insulin sensitivity and transaminase levels. "	( Bernhardt, C; Bruckert, E; Charlotte, F; Giral, P; Halbron, M; Hartmann-Heurtier, A; Lenaour, G; Poynard, T; Ratziu, V, 2010)
"Rosiglitazone has been reported to exert the protective effect against acute renal failure in animal models. "	( Choi, IJ; Kim, SY; Kim, YK; Kwon, CH, 2010)
"Rosiglitazone has no effect on chloride secretion in the colon, but it increases expression of the genes encoding carbonic anhydrases 4 and 2 (Car4 and Car2), increases bicarbonate secretion and reduces mucus retention."	( Barrett, KE; Dennis, EA; Dong, H; Dumlao, DS; Glass, CK; Harmon, GS; Ng, DT, 2010)
"Rosiglitazone has several properties that may affect progression of atherosclerosis. "	( Cannon, CP; Fitzgerald, PJ; García-García, HM; Gerstein, HC; Huang, C; Kolatkar, NS; Kravitz, BG; Miller, DM; Nesto, RW; Ratner, RE; Serruys, PW; van Es, GA, 2010)
"Rosiglitazone (RSG) has been known to play a role in the modulation of inflammatory responses. "	( Cho, YS; Heo, JY; Kim, CH; Song, JS, 2010)
"Rosiglitazone has been shown to be efficacious in acute pancreatitis; thus, the present study was planned to evaluate the effect of rosiglitazone on pancreatic regeneration."	( Khanduja, KL; Malhotra, S; Pandhi, P; Sidhu, S; Vaiphei, K, 2011)
"Rosiglitazone (RSG) has a variety of actions on both insulin sensitization and anti-atherogenic effects. "	( Chen, CY; Chen, YL; Chuang, LM; Tsai, JS, 2010)
"Rosiglitazone (Ros) has been shown to attenuate CXCL8 and ICAM-1 overexpression in renal tubular cells exposed to glycated albumin. "	( Chan, LY; Cheng, AS; Lai, KN; Lan, HY; Leung, JC; Tang, SC, 2010)
"Yet, rosiglitazone has been linked to serious cardiovascular events."	( Gori, T; Parker, JD; Perampaladas, K, 2010)
"Rosiglitazone has been the focus of extensive discussion."	( Alessi, A; Baroncini, LA; Brofman, PR; França Neto, OR; Noronha, Ld; Précoma, DB; Prim, C; Silva, RF, 2010)
"Rosiglitazone has an ameliorative effect on the DRG and enhances the functional recovery after SNC in rats."	( Karbalay-Doust, S; Noorafshan, A; Omidi, A; Shariat, K, 2012)
"Rosiglitazone is a TZD that has been found to increase the risk of cardiovascular events, especially of myocardial ischemic events."	( Chang, YW; Chen, WL; Chou, CC; Kao, TW; Loh, CH; Wang, CC, 2011)
"Rosiglitazone has the potential to activate peroxisome proliferator-activated receptor-γ (PPARγ), which in turn can affect bone formation and resorption. "	( Cho, ES; Kim, MK; Lee, JC; Lee, KS; Park, SM; Son, YO, 2012)
"Rosiglitazone has been certified in Germany since July 2000. "	( Herrmann, A; Hesselbarth, N; Hippius, M; Hoffmann, A; Kuschel, U, 2002)
"Rosiglitazone has now been available in clinical practice for more than three years, so there is a large body of evidence supporting its efficacy and safety as an antihyperglycaemic agent in patients with type 2 diabetes."	( Viberti, GC, 2003)
"Rosiglitazone has been available since June 1999 and is still on the market."	( Cluxton, RJ; Heaton, PC; Hsu, VD; Li, Z; Moomaw, CJ; Rodriguez, EM; Weiss, SR; Zuckerman, IH, 2005)
"Rosiglitazone has minimal effect on flow-mediated dilation in HIV-infected lipoatrophic adults. "	( Carey, D; Carr, A; Cooper, DA; Emery, S; Feneley, MP; Kovacic, JC; Mallon, PW; Martin, A; Wand, H, 2005)
"Rosiglitazone has an anti-inflammatory effect in renal tubular epithelial cells through the inhibition of NF-kappaB activation."	( Kang, KP; Kim, DH; Kim, HJ; Kim, W; Lee, S; Moon, SO; Park, SK; Sung, MJ, 2005)
"Rosiglitazone (RGTZ) has protective effect against various types of injury. "	( Ahn, KO; Choi, YH; Chung, BH; Ito, S; Kim, J; Li, C; Lim, SW; Sugawara, A; Sun, BK; Yang, CW; Yang, JH; Yoon, KH, 2005)
"Rosiglitazone has protective effect on myocardial cells of diabetic rats, which seems to be independent of blood glucose levels."	( Lu, YL; Wang, NC; Wang, XF; Wang, YN; Wu, H; Yu, DL; Zhang, L; Zhao, JB; Zhu, L, 2006)
"Rosiglitazone (RGTZ) has a protective effect against various types of injury. "	( Ahn, KO; Bang, BK; Choi, BS; Kim, J; Kim, JY; Kim, SH; Kim, YS; Li, C; Lim, SW; Yang, CW; Yang, HJ, 2007)
"Rosiglitazone (RSG) has been reported to reduce blood pressure (BP) in patients with type-2 diabetes, but similar effects in non-diabetic people with insulin resistance is less clear. "	( Berglund, G; Donaldson, J; Hedblad, B; Nilsson, PM, 2007)
"Rosiglitazone, a drug that has an excellent safety profile, may offer a well tolerated systemic treatment option for AD. "	( Behshad, R; Cooper, KD; Korman, NJ, 2008)
"Rosiglitazone has been shown to be much safer than troglitazone, despite some reported cases of early-onset nonfatal hepatotoxicity."	( Al-Kadhi, Y; Al-Omary, M; El-Naggar, MH; Habib, B; Helmy, A; Moawad, M, 2008)
"Rosiglitazone has a low risk of gastrointestinal side effects and hypoglycemia, reduced insulin demand, potential sparing effects on beta-cells, and favorable drug interaction profile."	( Travaglini, MT; Werner, AL, 2001)

Excerpt	Reference
"Rosiglitazone can increase thrombin-induced microglial phagocytosis, by a mechanism possibly involved in the increase of PPARγ and CD36 through the PPARγ pathway, which may provide a new option for cerebral hemorrhage treatment."	( Hang, H; Liu, C; Mu, Q; Wang, L; Wu, G, 2017)
"Rosiglitazone abolished the increase in serum BCAA induced by adipocyte PPARγ deletion."	( Andrade, ML; Blanchard, PG; Caron, A; Castro, É; Côté, M; Deshaies, Y; Dias, FA; Festuccia, WT; Gélinas, Y; Guerra-Sá, R; Moreira, RJ; Oliveira, TE; Ortiz-Silva, M; Peixoto, AS, 2018)
"Rosiglitazone does not increase the risk of bladder cancer."	( Tseng, CH, 2013)
"Rosiglitazone can inhibit the expression of TNFα in serum of septic rats, reduce the inflammatory reaction, reduce kidney injury, improve the renal function. "	( Deng, J; Yu, J, 2015)
"The rosiglitazone-mediated increase in SIRT1 stability is accompanied by upregulation of mitogen-activated protein kinase phosphatase (MKP)-7, a JNK-specific phosphatase."	( Ham, SA; Hwang, JS; Kim, JH; Lee, CH; Lee, WJ; Paek, KS; Seo, HG; Yoo, T, 2016)
"Rosiglitazone-induced increase in glucose uptake correlated significantly with increased expression of GLUT4, whereas diminished MFAO correlated significantly with decreased expression of FATP-1 and MCAD."	( Finck, BN; Gropler, RJ; Herrero, P; Schechtman, KB; Sharp, T; Shoghi, KI; Welch, MJ, 2009)
"Rosiglitazone group had lower adhesion scores [median (min-max ranges)] regarding extent, severity, and degree of the adhesions [0 (0-3), 0 (0-3) and 0 (0-3), respectively], which were significantly different (P < 0.001, P < 0.05 and P < 0.01, respectively) from those of the controls [1 (0-3), 2 (0-2) and 2 (0-3), respectively]; however, there were no statistically significant differences between rosiglitazone versus melatonin groups [1 (0-4), 2 (0-3) and 1 (0-3), respectively] and melatonin versus control groups."	( Aksakal, O; Gungor, T; Inan, I; Kalyoncu, S; Mollamahmutoglu, L; Sirvan, L; Sut, N; Yilmaz, B, 2010)
"Rosiglitazone may increase cardiovascular risk in patients with type 2 diabetes. "	( Jelic-Ivanovic, Z; Koulouris, S; Manolis, AS; Mikhailidis, DP; Pastromas, S; Rini, GB; Rizzo, M; Sakellariou, D; Spasojevic-Kalimanovska, V; Vekic, J; Zeljkovic, A, 2010)
"Rosiglitazone may increase vascular leakage in insulin-treated patients with type 2 diabetes with autonomic neuropathy. "	( Rennings, AJ; Smits, P; Stewart, MW; Tack, CJ, 2010)
"Rosiglitazone can enhance this procedure in THP-1 macrophages derived foam cells which means that they can promote ABCA1 mediated cholesterol reverse transportation through improve ABCA1 protein expression."	( Chen, L; Gou, LP; Lü, Z; Qin, J; Xie, B, 2010)
"Rosiglitazone-mediated increase of A-FABP is closely associated with the elevation of NT-proBNP, a well-established marker of cardiac dysfunction. "	( Bao, Y; Jia, W; Lu, J; Zhou, J; Zhou, M, 2011)
"Rosiglitazone could suppress TGF-β1-induced collagen type I and fibronectin expression in ADPKD cyst-lining epithelia through modulation of the Smad2 pathway."	( Dai, B; Fu, L; Hua, Z; Liu, Y; Mei, C; Xu, C, 2011)
"Rosiglitazone did not increase subcutaneous fat in patients with HAART-associated lipodystrophy (HAL) in a randomized, double-blind, placebo-controlled trial, although it attenuated insulin resistance and decreased liver fat content."	( Ehrenborg, E; Fisher, RM; Funahashi, T; Hamsten, A; Kannisto, K; Korsheninnikova, E; Matsuzawa, Y; Nyman, T; Sutinen, J; Vidal, H; Virkamäki, A; Yki-Järvinen, H, 2004)
"Both rosiglitazone and metformin increase hepatic insulin sensitivity, but their mechanism of action has not been compared in humans. "	( Häkkinen, AM; Korsheninnikova, E; Mäkimattila, S; Nyman, T; Tiikkainen, M; Yki-Järvinen, H, 2004)
"Rosiglitazone did not increase PSADT or prolong the time to disease progression more than placebo in men with a rising PSA level after radical prostatectomy and/or radiation therapy. "	( George, D; Kantoff, PW; Kaufman, DS; Manola, J; Mueller, E; Oh, WK; Slovin, S; Small, E; Smith, MR; Spiegelman, B, 2004)
"Rosiglitazone can inhibit the expression of ICAM-1 and beta1 integrin in normal and high glucose treated GMCs, and the inhibition is stronger in high glucose treated-group, which is in a dose-dependent manner."	( Cai, WL; Fu, P; Huang, SM; Zeng, L; Zhou, L, 2006)
"Rosiglitazone reduced the increase in lipase and the level of edema and the increase in myeloperoxidase as well as the activation of NFkappaB and iNOS expression."	( Barthet, M; Closa, D; Folch-Puy, E; Granell, S; Iovanna, JL, 2006)
"Rosiglitazone may increase subcutaneous fat in some individuals."	( Alston-Smith, BL; Basar, MT; Fielding, RA; Grinspoon, S; Koletar, SL; Mulligan, K; Parker, RA; Schouten, JT; Wininger, DA; Yang, Y, 2007)
"Rosiglitazone mitigates the increase in FFA after infusion of triglyceride/heparin and prevents FFA-induced endothelial dysfunction. "	( Kapiotis, S; Krzyzanowska, K; Mittermayer, F; Pleiner, J; Roden, M; Schaller, G; Wolzt, M, 2007)
"Rosiglitazone failed to increase PPARgamma mRNA in cells with oxidative stress, but Western blots revealed an increase in cellular PPARgamma protein content in the presence of rosiglitazone and increasing concentrations of H2O2."	( Sommer, M; Wolf, G, 2007)
"Rosiglitazone was found to cause regression of experimental endometriosis in rats."	( Aytan, H; Aytan, P; Caliskan, AC; Demirturk, F; Koseoglu, DR, 2007)
"Rosiglitazone may increase total cholesterol compared to pioglitazone."	( Carson, S; Norris, SL; Roberts, C, 2007)
"Rosiglitazone and 15d-PGJ2 suppress Ang II-induced production of PAI-1 and ECM probably via interactions between PPAR-gamma and TGF-beta1/Smad2/3 and JNK signalling pathways. "	( Gao, DF; Hao, GH; Niu, XL; Wang, NP; Wei, J, 2008)
"Rosiglitazone stimulated an increase in the ADP/ATP ratio in endothelial cells, and LKB1 was essential for rosiglitazone-stimulated AMPK activity in HeLa cells."	( Boyle, JG; Cleland, SJ; Connell, JM; Ewart, MA; Logan, PJ; Reihill, JA; Ritchie, SA; Salt, IP, 2008)
"Rosiglitazone is able to increase serum adiponectin levels significantly in Type 2 diabetic patients. "	( Gong, ZC; Guo, ZW; Liu, HL; Liu, YZ; Liu, ZQ; Sun, H; Wu, J; Yin, JY; Zhou, HH, 2008)
"Rosiglitazone does not cause hypoglycaemia or gastrointestinal side effects."	( Huijberts, MS; Sels, JP; Wolffenbuttel, BH, 2001)

Excerpt	Reference
"Rosiglitazone treatment reduced the accumulation of saturated lipids and showed a concomitant increase in unsaturated TAG species in our inflammation-induced NAFLD model."	( Bhaskar, AK; Sachidanandan, C; Sengupta, S; Singh, MK; Yadav, R, 2023)
"Rosiglitazone pretreatment can alleviate APAP-induced ALI by suppressing three branches of ERS signaling."	( Cao, Y; He, W; Huang, J; Li, X; Wang, J, 2022)
"Rosiglitazone treatment significantly inhibited the proinflammatory polarization of microglia and rescued neuron loss in the temporal lobe and hippocampi of the brain after SE."	( Guan, Y; Hao, Y; Li, Y; Peng, J; Wang, K; Xiang, W, 2019)
"Rosiglitazone pre-treatment prevented the increases in ALT (and AST), soluble E-selectin concentration, red blood cells and platelet counts."	( Chen, MM; Jiang, ZL; Li, X; Peng, B; Wang, GH; Xu, LH, 2017)
"Rosiglitazone treatment did not induce hypoglycaemia nor significantly alter clinical, biochemical, haematological, or electrocardiographic parameters."	( Bassat, Q; Bila, R; Crowley, VM; Kain, KC; Madrid, L; Mayor, A; Mucavele, H; Serghides, L; Sitoe, A; Varo, R, 2017)
"Rosiglitazone pretreatment protected against liver IRI in wild type mice but not in FAM3A-deficient mice."	( Chen, J; Chen, Z; Cui, Q; Geng, B; Meng, Y; Wang, J; Yang, J; Yang, W, 2017)
"Rosiglitazone treatment in T2D subjects resulted in a reduction in serum ApoJ levels (before vs."	( Choe, C; Ciaraldi, TP; Farr, O; Henry, RR; Hwang, WM; Kang, MC; Kim, SS; Kim, YB; Lim, DM; Mantzoros, C; Park, KS; Seo, JA, 2018)
"Rosiglitazone treatment from days 14 to 20 ameliorated hypertension, improved renal function, decreased endothelin-1 (ET-1), angiotensin II (Ag II) and interleukin (IL-6), while it increases NO level and pup weight."	( Allam, HIG; Masri, AAA, 2018)
"Rosiglitazone treatment increased the insulin sensitization and altered these changes."	( Mahboob, T; Tabassum, A; Yasmeen, K; Zaidi, SNF, 2018)
"Rosiglitazone treatment restored these changes."	( Mahboob, T; Tabassum, A; Yasmeen, K; Zaidi, SNF, 2018)
"Rosiglitazone was used as treatment drug, and pancreatic inflammation was assessed."	( Cui, X; Guo, J; Li, S; Li, Y; Ma, X; Nie, S; Zhi, H, 2019)
"Rosiglitazone group was treated with rosiglitazone(0.2 mL, [20 mg/(kg.d)])and model group with normal saline(0.2 mL/d)."	( Ge, S; Qian, J; Shao, Z; Wang, J; Wang, L; Wang, W; Xie, Q; Zhang, C; Zhou, C; Zuo, L, 2018)
"Rosiglitazone treatment effectively decreased urine protein excretion and preserved renal function in the CRAD rats. "	( Deng, J; Shao, M; Shao, X; Wang, X; Xia, Y; Xiong, C; Zhou, Q; Zou, H, 2019)
"Rosiglitazone treatment did not induce adipogenesis or mitochondria biogenesis in Crif1 knockout ADSCs."	( Choi, MJ; Chung, HK; Jo, YS; Jung, SB; Kim, HJ; Kim, KS; Kim, SJ; Kim, YK; Kweon, GR; Lee, CH; Lee, MH; Lee, SE; Ryu, MJ; Shong, M, 2013)
"Rosiglitazone treatment of db/db mice normalized hyperglycemia, attenuated renal injury and decreased urinary ACE2 and renal ADAM17 protein expression."	( Chodavarapu, H; Elased, KM; Grobe, N; Madhu, M; Salem, ES; Somineni, HK, 2013)
"Rosiglitazone treatment led to an improvement in glycemic control and to an increase in paraoxonase activity and HDL-C levels."	( Atamer, A; Atamer, Y; Can, AS; Hekimoğlu, A; Ilhan, N; Koçyiğit, Y; Yenice, N, 2013)
"Rosiglitazone treatment attenuated casein-induced systemic inflammation, ER stress, deteriorated liver function, and increased apoptosis."	( Cha, BS; Huh, JH; Kang, ES; Kang, SB; Kim, HJ; Kim, HM; Lee, BW; Lee, HC; Seok, H, 2013)
"Rosiglitazone treatment induced volume expansion and CH in wild-type and PPARγ heterozygous knockout (Pparg(+/-)) mice, but not in mice defective for ligand binding (Pparg(P465L/+))."	( Chang, CS; Chen, JY; Ho, LC; Maeda, N; Pandya, K; Sung, JM; Tsai, PJ; Tsai, YS, 2014)
"Rosiglitazone-treated fetuses had a lower cardiac abundance of insulin-signaling molecules, including insulin receptor-β, insulin receptor substrate-1 (IRS-1), phospho-IRS-1 (Tyr-895), phosphatidylinositol 3-kinase (PI3K) regulatory subunit p85, PI3K catalytic subunit p110α, phospho-3-phosphoinositide-dependent protein kinase 1 (Ser-241), protein kinase B (Akt-1), phospho-Akt (Ser-273), PKCζ, phospho-PKCζ(Thr-410), Akt substrate 160 kDa (AS160), phospho-AS160 (Thr-642), and glucose transporter type-4."	( Botting, KJ; Dunn, SL; Hui, M; Lie, S; McMillen, IC; Morrison, JL; Muhlhausler, BS; Posterino, GS; Wang, KC, 2014)
"Rosiglitazone treatment significantly reduced the duration of induced AF in the treated rabbits (1.6 ± 0.4 s vs."	( Korantzopoulos, P; Li, G; Li, J; Liu, T; Zhao, H, 2014)
"Rosiglitazone treatment decreased WC-As lipid vacuoles significantly compared with the control cells."	( Anderson, JL; Keeley, MC; Smith, EC; Smith, SC; Taylor, RL, 2014)
"Rosiglitazone treatment significantly improved hepatic insulin sensitivity and inhibited the IKK-β, NF-κB, and Ser307p-IRS-1 expressions in the liver (P < 0.05)."	( You, S; Zhou, X, 2014)
"Rosiglitazone treatment resulted mainly in modulation via PPAR signaling and oxidative phosphorylation in WAT only."	( Meierhofer, D; Sauer, S; Weidner, C, 2014)
"Rosiglitazone treatment increased creatinine clearance and plasma transferrin, and decreased urinary ACR, HbA1c, plasma TNF-α, ICAM-1, and serum lipid peroxide levels without affecting the altered lipid profile. "	( Gad, HI, 2014)
"Rosiglitazone pretreatment significantly decreased peritoneal thickness."	( Wu, J; Yang, X; Yu, XQ; Zhang, YF; Zou, XL, 2015)
"Rosiglitazone treatment also reduced the numbers of Iba1(+)/CD16(+) M1 microglia and increased the numbers of Iba1(+)/CD206(+) M2 microglia after stroke."	( Cai, W; Chen, J; Han, L; Hu, X; Leak, RK; Li, P; Liu, J; Mao, L; Xu, Y, 2015)
"Rosiglitazone treatment improves long-term white matter integrity after cerebral ischemia, at least, in part, by promoting oligodendrogenesis and facilitating microglial polarization toward the beneficial M2 phenotype."	( Cai, W; Chen, J; Han, L; Hu, X; Leak, RK; Li, P; Liu, J; Mao, L; Xu, Y, 2015)
"Rosiglitazone treatment also significantly reduced mHtt aggregates that included ubiquitin (Ub) and heat shock factor 1 (HSF1), as assessed by a filter-retardation assay, and increased the levels of the functional ubiquitin-proteasome system (UPS), HSF1 and heat shock protein 27/70 (HSP27/70) in N2A cells."	( Chen, SJ; Cheng, YC; Chiang, MC; Huang, RN; Lin, KH; Nicol, CJ; Yen, CH, 2015)
"Rosiglitazone treatment significantly reduced the hypercholesterolemia of the Seipin(-/-)Ldlr(-/-) mice, and also alleviated the severity of atherosclerosis."	( Du, X; Gao, M; Li, L; Liao, J; Liu, G; Qi, Y; Wang, M; Wang, Y; Yang, H, 2016)
"Rosiglitazone-treated animals had improved performance on beam balance testing, but there was no difference in spatial memory function as determined by Morris water maze."	( Culver, S; Dixon, CE; Graham, SH; Liu, H; Ma, X; Rose, ME, 2016)
"Rosiglitazone co-treated hNSCs also showed significantly increased mitochondrial function (reflected by levels of adenosine triphosphate and Mit mass), and PPARγ-dependent mRNA upregulation of PGC1α and mitochondrial genes (nuclear respiratory factor-1 and Tfam)."	( Cheng, YC; Chiang, MC; Lin, CH; Lin, KH; Nicol, CJ; Yen, CH, 2016)
"Rosiglitazone treatment inhibited adrenal hypertrophy and hypercorticoidism observed in diabetic rats."	( Carvalho, VF; E Silva, PM; Magalhães, NS; Martins, MA; Torres, RC, 2016)
"MEHP/rosiglitazone-treated adipocytes exhibited increased levels of lipolysis, glucose uptake, and glycolysis; the gene expression profiles provided molecular basis for the functional changes."	( Chiang, HC; Chuang, WH; Kuo, YT; Liao, CW; Lin, WY; Lin, YH; Tsai, FY; Tsou, TC; Wang, CH; Yeh, SC, 2017)
"Rosiglitazone treatment restored insulin sensitivity in obese B6 mice, yet, surprisingly, had little effect on gene expression in eWAT."	( Benson, KK; Briggs, ER; Chen, ER; Damle, M; Dispirito, JR; Dzeng, RK; Emmett, MJ; Foong, YH; Jolivert, JF; Kissig, M; Lazar, MA; Li, Z; Lim, HW; Medina, CJ; Mullican, SE; Peed, LC; Rajapurkar, SR; Seale, P; Soccio, RE; Steger, DJ; Won, KJ, 2017)
"Rosiglitazone treatment in 3T3-L1 adipocytes promoted mitochondrial biogenesis, UCP1 expression, and mitochondrial uncoupling. "	( Gottlieb, RA; Taylor, D, 2017)
"Rosiglitazone treatment further increased adipose mass, reduced liver triglycerides, and changed adipose tissue morphology toward smaller adipocytes."	( Duval, C; Kersten, S; Keshtkar, S; Müller, M; Stienstra, R; van der Laak, J, 2008)
"Rosiglitazone treatment decreased PMNL priming."	( Farah, R; Lapin, O; Shurtz-Swirski, R, 2008)
"Rosiglitazone treatment decreased beta-cell apoptosis, preserved beta-cell mass and improved glucose tolerance in OLETF rats."	( Ahn, CW; Cha, BS; Choi, SE; Han, SJ; Hur, KY; Kang, ES; Kang, Y; Kim, HJ; Kim, SH; Lee, HC; Yun, CO, 2008)
"Rosiglitazone treatment reduced liver fat by 24.8% (P = .01 vs placebo) and increased HGU by 29.2% (P = .013 vs placebo)."	( Bergman, J; Borra, R; Hällsten, K; Iozzo, P; Komu, M; Lautamäki, R; Nuutila, P; Parkkola, R; Sijens, PE, 2008)
"Rosiglitazone-treated mice also showed significantly less number of TUNEL(+) apoptotic neurons and curtailed induction of caspase-3 and Bax, compared to vehicle control."	( Brooks, N; Lang, BT; Park, SW; Vemuganti, R; Yi, JH, 2008)
"Rosiglitazone-treated rats had restored systolic blood pressure (BP) and normalized plasma insulin level during oral glucose tolerance tests, whereas amlodipine-treated rats restored only systolic BP."	( Chen, HS; Juan, CC; Lin, HD; Wu, TE, 2009)
"Rosiglitazone treatment induced aortic expression of Bmal1 mRNA, and ChIP and promoter assays revealed that Bmal1 is a direct PPARgamma target gene."	( Aoyagi, T; Gonzalez, FJ; Jia, Z; Litwin, SE; Schnermann, JB; Soodvilai, S; Symons, JD; Wang, N; Yang, G; Yang, T; Zhang, H, 2008)
"Rosiglitazone treatment reduced the induction of the early-immediate transcription factor Egr-1 in situ without also blocking the activation of Smad2/3."	( Chang, E; Ghosh, AK; Melichian, DS; Varga, J; Warner-Blankenship, M; Wu, M, 2009)
"Rosiglitazone treatment resulted in improved peripheral insulin sensitivity with increased circulating adiponectin in HIV patients under HAART."	( Gmeinhardt, B; Haider, D; Ludvik, B; Pacini, G; Rieger, A; Schindler, K; Touzeau-Römer, V; Tura, A, 2009)
"Rosiglitazone treatment significantly reduced the expression of the inflammatory markers compared with control group."	( Cappetta, D; Capuano, A; Carnuccio, R; Domenici, L; Donniacuo, M; Filippelli, A; Pieri, L; Rinaldi, B; Romagnoli, P; Rossi, F, 2009)
"Rosiglitazone pre-treatment to cisplatin increases the expression of p38, PPAR-gamma in mammary tumours and shows maximum tumour reduction."	( Gupta, J; Kumar, P; Tikoo, K, 2009)
"Rosiglitazone treatment resulted in increased expression of LPL and adiponectin mRNA (P < 0.01) in fetal adipose tissue."	( McMillen, IC; Morrison, JL; Muhlhausler, BS, 2009)
"Rosiglitazone treatment prevented the reduction of collagen type IV in the ischemic injured brain by inhibiting the activation of matrix metallopeptidase-9 (MMP-9)."	( Ding, X; He, C; Noor, R; Pegg, C; Shuaib, A; Wang, CX, 2009)
"Rosiglitazone pretreatment attenuated cardiac apoptosis, as assessed by ELISA to determine cardiomyocyte DNA fragmentation."	( Dong, YG; Ma, H; Ma, YD; Tang, AL; Wu, JG; Xiong, ZB; Zhang, XJ, 2010)
"Rosiglitazone treatment has been shown to increase adipogenesis in bone marrow and to induce bone loss."	( Arnol, V; Cortizo, AM; Gangoiti, MV; McCarthy, AD; Molinuevo, MS; Schurman, L; Sedlinsky, C; Tolosa, MJ, 2010)
"Rosiglitazone treatment increased serum adiponectin, insulin sensitivity, and body weight, and decreased Atrogin-1 and MuRF-1 expression in the skeletal muscle of tumor-bearing mice."	( Asp, ML; Belury, MA; Tian, M; Wendel, AA, 2010)
"Rosiglitazone treatment after 2 wk of hypertension completely reversed the increased J(v)/S and L(p) that occurred during hypertension, whereas Tempol had no effect."	( Chapman, AC; Cipolla, MJ; Roberts, TJ, 2009)
"Rosiglitazone treatment reduced this effect by 23% (p < 0.01)."	( Böhm, M; Kilter, H; Kintscher, U; Reil, JC; Roggia, C; Schäfers, HJ; Werner, M, 2009)
"Rosiglitazone treatment (6 or 12 mg/kg, orally) significantly reduced plasma corticosterone levels in rats."	( Al-Rasheed, NM; Eissa Ahmed, AA, 2009)
"Rosiglitazone treatment was associated with durable reductions in CRP independent of changes in insulin sensitivity, A1C, and weight gain. "	( Haffner, SM; Herman, WH; Holman, RR; Kahn, SE; Kravitz, BG; Lachin, JM; Paul, G; Viberti, G; Yu, D; Zinman, B, 2010)
"Rosiglitazone-treated patients experienced a significant decrease in hs-CRP and systolic blood pressure compared with baseline values and those of the MET group (P < .05)."	( Kadoglou, NP; Kapelouzou, A; Karayannacos, PE; Liapis, CD; Sailer, N; Tsanikidis, H; Vitta, I; Vrabas, I, 2010)
"Rosiglitazone treatment improved glucose tolerance in P. "	( Chajut, A; Cooper, A; Lee, S; Leizerman, I; Molero, JC; Walder, K, 2010)
"Rosiglitazone treatment significantly improved E/A ratio in serial echocardiography assessment, and reduced LV collagen volume fraction as demonstrated by picrosirius red staining."	( Baek, SH; Chang, K; Ihm, SH; Kim, HY; Kim, JH; Seung, KB; Youn, HJ, 2010)
"Rosiglitazone enema treatment was well tolerated and reduced the Mayo ulcerative colitis score from 8.9 to 4.3 (P<0.01), similar to the effect of mesalazine."	( Brynskov, J; Pedersen, G, 2010)
"Rosiglitazone treatment inhibited cell proliferation in a dose- and time-dependent manner, and such effects were not associated with induction of cell death."	( Choi, IJ; Kim, SY; Kim, YK; Kwon, CH, 2010)
"Rosiglitazone treatment increased body weight and hip circumference and decreased WHR. "	( Bahia, LR; Bouskela, E; Domingues, RC; Geloneze, B; Godoy-Matos, AF; Kraemer-Aguiar, LG; Tambascia, M, 2010)
"Rosiglitazone treatment resulted in an improvement of insulin responsiveness in Type 2 diabetic subjects, which was associated with the redistribution of visceral and subcutaneous adipose tissue, an increase in TLDMA, and changes in serum adipocytokine levels. "	( Ahn, CW; Cha, BS; Cho, M; Kim, KR; Lee, EJ; Lee, HC; Lim, SK; Nam, JS; Nam, JY; Park, JS; Yoo, JS, 2010)
"Rosiglitazone treatment adversely affects bone formation over a 2-year period. "	( Berberoglu, Z; Demirag, NG; Yazici, AC, 2010)
"All rosiglitazone-treated rabbits had significantly improved laboratory parameters and plasma tumour necrosis factor-alpha levels."	( Chang, Y; Chen, YL; Chuang, HC; Hsieh, WC; Lan, BS; Su, IJ, 2010)
"Rosiglitazone treatment promoted pancreatic regeneration after acute injury."	( Khanduja, KL; Malhotra, S; Pandhi, P; Sidhu, S; Vaiphei, K, 2011)
"Rosiglitazone treatment prevented the hypoxia-induced reduction in PPARgamma expression, and restored ET-1 and VEGF expression almost to the levels of the normoxia group."	( Kim, EK; Lee, JH; Lee, SD; Lee, YS; Oh, YM, 2010)
"Rosiglitazone treated patients also displayed further improvements in glycemic control compared to placebo (HbA(1C): 6.4 + or - 0.7% vs."	( Alméras, N; Angel, J; Batalla, N; Bertrand, OF; Costerousse, O; De Larochellière, R; Després, JP; Dzavik, V; Natarajan, M; Poirier, P; Rinfret, S; Rodés-Cabau, J; Roy, L; Title, LM, 2010)
"Rosiglitazone treatment and exercise both led to significant improvements in insulin resistance at 6 months, whereas no change was observed in control patients."	( Blüher, M; de Waha, S; Desch, S; Eitel, I; Niebauer, J; Sareban, M; Schuler, G; Sixt, S; Sonnabend, M; Thiele, H, 2010)
"Rosiglitazone treatment stimulates the production of adiponectin, an insulin-sensitizing adipokine with hepatoprotective functions."	( Chan, L; Che, CM; Lam, KS; Lee, IK; Tam, PK; Wang, Y; Wu, D; Xu, A; Zhou, M, 2010)
"Rosiglitazone treatment prevented hepatic inflammation and reduced the expression of pro-inflammatory cytokines in livers of wild type mice. "	( Chan, L; Che, CM; Lam, KS; Lee, IK; Tam, PK; Wang, Y; Wu, D; Xu, A; Zhou, M, 2010)
"Rosiglitazone treatment significantly increased both total lipolysis (R(a) FFA(total) from 3.37 ± 0.40 to 4.57 ± 0.68 mmol FFA per kilogram fat per hour, P < .05) and adipocyte reesterification (1.25 ± 0.35 to 2.43 ± 0.65 mmol FFA per kilogram fat per hour, P < .05)."	( Balasubramanyam, A; D'Amico, S; Jahoor, F; Patel, SG; Rehman, K; Sekhar, RV; Shi, J; Visnegarwala, F, 2011)
"Rosiglitazone treatment maintains mitochondrial structure and function in the pancreas of rats that are prone to diabetes, as well as mitochondrial function in beta cell culture."	( Bruin, JE; Gerstein, HC; Holloway, AC; Hyslop, JR; Petrik, JJ; Raha, S; Tarnopolsky, MA, 2010)
"Rosiglitazone treatment reduced insulin resistance and partially restored β-cell mass in animals with reduced β-cell mass at birth. "	( Gerstein, HC; Hettinga, BP; Holloway, AC, 2011)
"The rosiglitazone treatment was started from one month after the start of cholesterol-rich diet plus methylthiouracil, and lasted five months."	( Li, Y; Liu, N; Ren, L; Sheng, Z; Tang, R; Zhi, H, 2011)
"Rosiglitazone treatment in patients with NAFLD is safe, well-tolerated and leads to a significant improvement in liver function and insulin sensitivity, without adversely affecting the lipid profile."	( Białkowska, J; Borkowska, A; Czupryniak, L; Ignaczak, A; Jabłkowski, M; Kwiecińska, E; Loba, J; Omulecka, A; Pawłowski, M; Saryusz-Wolska, M; Szymańska-Garbacz, E, 2011)
"Rosiglitazone treatment alone marginally increased long-term survival and reduced CD8 T-cell infiltration and vasculopathy in the grafts. "	( Chen, Y; Hui, K; Lamb, JR; Li, D; Lui, VC; Niu, N; Peng, J; Tam, PK; Tsang, JY; Xu, A; Zhu, J, 2011)
"Rosiglitazone treatment in the early phase of neuropathic pain significantly alleviated the development of tactile allodynia by regulating macrophage infiltration and production of proinflammatory molecules at the inflamed site. "	( Hasegawa-Moriyama, M; Inada, E; Sakurai, T; Takahashi, Y, 2011)
"Rosiglitazone treatment may decrease the expression of Galectin-9 and Tim-3."	( Feng, XX; Luan, B; Zhang, ZY, 2011)
"Rosiglitazone treatment (3 and 6 mg/kg) not only suppressed the activation of astrocytes and microglia markedly but also alleviated the impairment of memory and increased the synaptophysin level."	( Barut, F; Jakubowska-Dogru, E; Ozacmak, VH; Sayan-Ozacmak, H, 2011)
"Only rosiglitazone treatment caused a significant decrease in plasma OPG concentrations (p = 0.003), while no significant change was seen in the other treatment groups."	( Gram, J; Henriksen, JE; Juhl, HF; Nybo, M; Olesen, M; Preil, SR; Rasmussen, LM; Yderstraede, K, 2011)
"Rosiglitazone treatment significantly inhibited Ang II-induced rat aortic VSMC proliferation in a dose-dependent manner."	( Cha, MJ; Choi, E; Ham, O; Hwang, KC; Jang, Y; Kim, IK; Kim, JS; Lee, SY; Lim, S; Song, BW; Song, H, 2012)
"In rosiglitazone-treated rats the number of the A, B, and satellite cells decreased less, and was 38%, 34%, and 29% higher than in the SNC rats."	( Karbalay-Doust, S; Noorafshan, A; Omidi, A; Shariat, K, 2012)
"Rosiglitazone treatment not only inhibited the formation of tartrate-resistant acid phosphatase-positive cells, but also prevented pit formation by bone marrow cells in a dose- and time-dependent manner."	( Cho, ES; Kim, MK; Lee, JC; Lee, KS; Park, SM; Son, YO, 2012)
"Oral rosiglitazone treatment was applied for 6 months (4 mg per day for 2 weeks followed by 8 mg per day)."	( Bockisch, A; Freudenberg, LS; Jentzen, W; Nagarajah, J; Rosenbaum-Krumme, SJ, 2012)
"Rosiglitazone treatment provided both protective and harmful cardiovascular effects in nondiabetic postmenopausal women. "	( Chao, TH; Chen, IC; Chen, JY; Lee, WH; Li, YH; Pan, HA; Tsai, WC; Tseng, SY, 2012)
"Rosiglitazone treatment significantly attenuated the increased ratio of heart weight to body weight, and the increased expression of myocardial p22phox, Nox4, MCP-1 and CTGF in diabetic rats (P<0.05)."	( Guo, Z; Li, J; Qin, Z; Yin, Y; Zhang, R, 2012)
"Rosiglitazone treatment of diabetic rats abolished the increase in diastolic BP and significantly reduced the increased systolic BP without affecting the development of hyperglycaemia."	( Abo-Warda, SM; El-Bassossy, HM; Fahmy, A, 2012)
"Rosiglitazone treatment for 3 days induced GFP expression in more than 80% of cells."	( Case, N; Rowe, D; Rubin, J; Sen, B; Styner, M; Thomas, J; Xie, Z, 2013)
"Rosiglitazone treatments significantly lowered the contents of total cholesterol and free cholesterol (P<0.05), decreased the expression of ACAT-1 (P<0.05), and increased SR-BI expression (P<0.05) in the foam cells in a dose-dependent manner."	( Guo, W; Hu, H; Hu, X; Jia, J; Li, W; Meng, Y; Wang, Z; Xie, W; Xu, F, 2012)
"Rosiglitazone treatment also inhibits leptin-induced growth of breast cancer cells."	( Knight, BB; Nagalingam, A; Oberlick, E; Saxena, NK; Sharma, D; Taliaferro-Smith, L, 2013)
"Rosiglitazone treatment (10 mg/kg orally, 4 weeks) caused significant decreases in plasma insulin, blood glucose, and blood pressure while causing an increase in renal sodium excretion compared with untreated obese rats."	( Banday, AA; Hussain, T; Lokhandwala, MF; Umrani, DN, 2002)
"Rosiglitazone treatment caused a clear reduction of IMCL and hepatic fat despite increased body weight, and a marked improvement of insulin sensitivity."	( Belz, U; Herling, AW; Juretschke, HP; Kalisch, J; Kleinschmidt, E; Kramer, W; Kuhlmann, J; Neumann-Haefelin, C; Stein, M, 2003)
"Rosiglitazone treatment of nondiabetic hypertensive patients improves insulin sensitivity, reduces systolic and diastolic blood pressure, and induces favorable changes in markers of cardiovascular risk. "	( Bekins, SA; Raji, A; Seely, EW; Simonson, DC; Williams, GH, 2003)
"The rosiglitazone-treated mice, both diabetic and non-diabetic, had higher lipid levels."	( Cohen, H; Dvir, A; Gerber, Y; Harats, D; Levi, Z; Levkovitz, H; Ravid, M; Rhachmani, R; Shaish, A; Trestman, S; Yacov, N, 2003)
"Rosiglitazone-treated animals showed less atherosclerosis despite higher lipid levels and similar glucose levels. "	( Cohen, H; Dvir, A; Gerber, Y; Harats, D; Levi, Z; Levkovitz, H; Ravid, M; Rhachmani, R; Shaish, A; Trestman, S; Yacov, N, 2003)
"Rosiglitazone treatment, but not placebo, significantly reduced MMP-9 levels already after 2 weeks by -19.6% (-38.3% to 8.6%, P<0.05), and levels remained suppressed until the end of the study."	( Froehlich, J; Hombach, V; Ittner, J; Koenig, W; Marx, N; Scharnagl, H; Schmidt, A; Siam, L; Wierse, G, 2003)
"Rosiglitazone treatment exacerbated the fatty liver in ob/ob-PPARgamma(fl/fl)AlbCre(-) mice compared with livers from nonobese Cre(-) mice; there was no effect of rosiglitazone in ob/ob-PPARgamma(fl/fl)AlbCre(+) mice."	( Brewer, B; Gavrilova, O; Gonzalez, FJ; Haluzik, M; Lambert, G; Matsusue, K; Reitman, ML; Ward, JM; Yim, SH, 2003)
"Rosiglitazone treatment, but not placebo, significantly reduced sCD40L serum levels within the first 2 weeks by 8.1% (17.1 to -32.7) (median percentage [interquartile range]; P<0.05 compared with baseline), further decreasing it by 18.4% (-5.0 to -33.1) after 6 weeks (P<0.05 compared with baseline), and by 27.5% (8.2 to -70.5) after 12 weeks (P<0.05 compared with baseline and with 2 weeks of treatment)."	( Froehlich, J; Hombach, V; Imhof, A; Ittner, J; Koenig, W; Maerz, W; Marx, N; Schmidt, A; Siam, L; Wierse, G, 2003)
"Both rosiglitazone and metformin treatment were associated with an increase in HGU; versus placebo, the change reached statistical significance when controlling for sex (placebo-subtracted values = +0.008 +/- 0.004 micromol x min(-1) x kg(-1) x pmol/l(-1), P < 0.03, for metformin; and +0.007 +/- 0.004, P < 0.07, for rosiglitazone)."	( Ferrannini, E; Hallsten, K; Iozzo, P; Kemppainen, J; Knuuti, J; Lonnqvist, F; Nuutila, P; Oikonen, V; Parkkola, R; Solin, O; Virtanen, KA, 2003)
"Rosiglitazone treatment resulted in significantly higher body weight and decreased plasma levels of glucose, insulin, and triglyceride (TG)."	( Havekes, LM; Mensink, RP; Muurling, M; Pijl, H; Romijn, JA; Voshol, PJ, 2003)
"Rosiglitazone treatment increased insulin receptor expression and insulin-stimulated Tyr phosphorylation of insulin receptor beta-chain, but decreased insulin-stimulated Ser phosphorylation."	( Hernandez, R; Lorenzo, M; Teruel, T, 2003)
"Rosiglitazone treatment resulted in a significant reduction in E-selectin (p = 0.03), von Willebrand factor (p = 0.007), C-reactive protein (p < 0.001), fibrinogen (p = 0.003) and the homeostasis model of insulin resistance index (p = 0.02), compared with placebo. "	( Cowan, D; Kaski, JC; Sidhu, JS, 2003)
"Rosiglitazone treatment ameliorated the clinical signs on days 26-35 and improved the histologic findings in the joint and paw."	( Britti, D; Caputi, AP; Cuzzocrea, S; De Maio, M; Di Paola, R; Dugo, L; Genovese, T; Mazzon, E; Patel, NS; Serraino, I; Thiemermann, C, 2003)
"Rosiglitazone treatment resulted in restoration of G-protein coupling of D1A receptors and their recruitment by dopamine in obese rats similar to that seen in lean rats."	( Lokhandwala, M; Marwaha, A; Trivedi, M, 2004)
"Rosiglitazone treatment also reduced, but to a lesser extent, the intimal hyperplasia in the lean Zucker rats (0.57 +/- 0.10 vs 1.06 +/- 0.12 treated and untreated, respectively; P<.01); however, it had no effect on insulin, triglyceride, or glucose levels in this group."	( Desouza, CV; Diez, J; Dunne, B; Fonseca, VA; Matta, AS; McNamara, DB; Murthy, SN, 2003)
"Rosiglitazone treatment of R(+)A(+) mice did not alter the expression of genes, including endothelial nitric oxide synthase (eNOS), angiotensin 1 receptors, and preproendothelin-1, nor did it alter the levels of eNOS or soluble guanylyl cyclase protein."	( Didion, SP; Faraci, FM; Mathur, S; Ryan, MJ; Sigmund, CD, 2004)
"Rosiglitazone treatment attenuated neointimal formation (intima/media ratio: 0.98+/-0.12 [rosiglitazone] versus 3.1+/-0.5 [control]; P<0.001; n=10 per group)."	( Al-Omran, M; Cherng, WJ; Ciliberti, N; Fedak, PW; Li, RK; Li, SH; Stanford, WL; Szmitko, PE; Verma, S; Wang, CH; Weisel, RD, 2004)
"Rosiglitazone-treated patients showed reduced IMT progression compared with the placebo group, -0.012 mm/48 weeks versus 0.031 mm/48 weeks (P=0.03)."	( Kaposzta, Z; Kaski, JC; Markus, HS; Sidhu, JS, 2004)
"Rosiglitazone treatment resulted in partial normalization of apoB48-containing intestinal lipoprotein secretion."	( Adeli, K; Leung, N; Lewis, GF; Naples, M; Szeto, L; Uffelman, K, 2004)
"Rosiglitazone treatment resulted in a reduction in plasma MCP-1 and CRP in both groups (P < 0.05)."	( Al-Haddad, W; Aljada, A; Dandona, P; Dhindsa, S; Ghanim, H; Hofmeyer, D; Mohanty, P; Syed, T; Tripathy, D, 2004)
"Rosiglitazone treatment significantly reduced the insulin resistance index (HOMA-R) compared with placebo (P =.02)."	( Cowan, D; Kaski, JC; Sidhu, JS; Tooze, JA, 2004)
"Rosiglitazone treatment significantly reduced C-reactive protein (median 0.56 mg/L [interquartile range 0.33 to 1.02] to 0.33 mg/L [interquartile range 0.26 to 0.40], p <0.01), von Willebrand factor (139 +/- 47 to 132 +/- 44 IU/dl, p = 0.02), insulin resistance index (p = 0.05), and mean low-density lipoprotein (LDL) density (p <0.001) compared with placebo."	( Cowan, D; Kaski, JC; Sidhu, JS, 2004)
"Rosiglitazone treatment impaired TNF-alpha activation of p38 and p42/p44MAPK, restoring insulin signalling and leading to normalisation of glucose uptake."	( de Alvaro, C; Hernandez, R; Lorenzo, M; Teruel, T, 2004)
"Rosiglitazone treatment increased (P < 0.05) skeletal muscle diacylglycerol and ceramide levels by 65% and 100%, respectively, compared with obese rats, but elevated muscle diacylglycerol was not associated with changes in the total or membrane contents of the diacylglycerol-sensitive protein kinase C isoforms theta;, delta, alpha, and beta."	( Febbraio, MA; Hawley, JA; Lau, W; Lessard, SJ; Lo Giudice, SL; Reid, JJ; Turner, N; Watt, MJ, 2004)
"With rosiglitazone treatment of fructose-fed hamsters, there was approximately 50% reduction in apoB48 secretion from primary cultured enterocytes and amelioration of the elevated microsomal triglyceride transfer protein mass and activity in fructose-fed hamsters."	( Adeli, K; Haidari, M; Lewis, GF; Naples, M; Szeto, L; Uffelman, K, 2005)
"Rosiglitazone treatment for 6 months reduced fasting insulin concentration."	( Ahn, CW; Cha, BS; Choi, D; Choi, SH; Jang, Y; Kim, SK; Ko, YG; Lee, HC; Lim, SK, 2004)
"Rosiglitazone-treated mice had increased weight when compared with controls, with no significant alterations in serum levels of glucose, calcium or parathyroid hormone (PTH)."	( Bai, XY; Goltzman, D; Karaplis, AC; Miao, D; Sorocéanu, MA; Su, H, 2004)
"Rosiglitazone treatment significantly improved insulin resistance and reduced postchallenge glucose and insulin concentrations in patients with impaired glucose tolerance without remarkable effects on beta-cell secretory function."	( Fan, SC; He, CT; Hsieh, CH; Hung, YJ; Kuo, SW; Lee, CH; Lee, JT; Pei, D; Sheu, WH; Wu, LY, 2005)
"Rosiglitazone treatment (1, 5, and 10 micromol/L) also led to a dose-dependent increase (approximately 1.2-1.5-fold) in SERCA2 promoter activity."	( Abbott, A; Augustin, D; Caudillo, S; Golez, E; Gonzales, F; McDonough, PM; Morello, J; Paolini, PJ; Shah, RD; Shubeita, HE, 2005)
"In rosiglitazone-treated rats, the number of apoptotic cardiomyocytes and the myocardial infarct size were decreased by 58 and 46%, respectively, and the myocardial contractile dysfunction was improved."	( Bao, W; Cui, J; Gu, JL; Jucker, BM; Ma, XL; Ohlstein, EH; Tao, L; Yue, TL, 2005)
"Rosiglitazone treatment restored basal and agonist-induced coupling of D(1A) receptors to G(s) proteins and reduced basal serine phosphorylation of D(1A) receptors, GRK4 expression, and translocation of GRK2 to the plasma membrane in proximal tubules of OZRs."	( Lokhandwala, MF; Trivedi, M, 2005)
"Rosiglitazone treatment significantly ( P < .001) suppressed Hcy levels and increased the activity of the Hcy metabolizing enzyme, cystathionine-beta-synthase in the liver samples."	( Agrawal, KC; Chattergoon, NN; Diez, JG; Dunne, JB; Fonseca, NA; Fonseca, VA; Jeter, JR; Kadowitz, PJ; McNamara, DB; Mondal, D; Murthy, SN; Obregon, DF, 2005)
"Rosiglitazone treatment resulted in an increase in baseline GIR to 6.29 +/- 0.81 mg/kg.min (P = 0.03 vs."	( Aljada, A; Dandona, P; Dhindsa, S; Ghanim, H; Ravishankar, S; Sanalkumar, N; Tripathy, D, 2005)
"Rosiglitazone treatment increased adiponectin concentrations by 69%. "	( Debard, C; Frayn, KN; Funahashi, T; Humphreys, SM; Karpe, F; Matsuzawa, Y; Tan, GD; Vidal, H, 2005)
"Rosiglitazone treatment markedly increased GlyK expression in both fat depots, with a greater increase in the mesenteric fat."	( An, CS; Chung, MY; Kang, JS; Kang, SH; Lee, DH; Lee, YK; Oh, YS; Park, DB, 2005)
"Rosiglitazone treatment increased nuclear PPAR-gamma expression and activity in VSMC."	( Amiri, F; Benkirane, K; Diep, QN; El Mabrouk, M; Schiffrin, EL, 2006)
"Rosiglitazone treatment increased flow by 72% (P < 0.01) and GU by 23% (P < 0.05) and thereby decreased adipose tissue glucose extraction by 18% (P < 0.05); no changes were observed in the metformin or placebo-treated groups."	( Ferrannini, E; Hällsten, K; Iozzo, P; Järvisalo, MJ; Lönnqvist, F; Nuutila, P; Parkkola, R; Rönnemaa, T; Viljanen, AP; Virtanen, KA, 2005)
"Rosiglitazone treatment enhances GU and flow but decreases glucose extraction, suggesting that perfusion may contribute to adipose tissue insulin sensitization by rosiglitazone."	( Ferrannini, E; Hällsten, K; Iozzo, P; Järvisalo, MJ; Lönnqvist, F; Nuutila, P; Parkkola, R; Rönnemaa, T; Viljanen, AP; Virtanen, KA, 2005)
"Rosiglitazone treatment also results in up-regulation of the HSL gene in liver and skeleton muscle from an experimental obese rat model, accompanied by the decreased triglyceride content in these tissues."	( Cheng, J; Deng, T; Li, PP; Lu, XP; Ning, ZQ; Shan, S; Shen, ZF, 2006)
"Rosiglitazone-treated human umbilical vein endothelial cells were analyzed for growth rate by use of cell number counting, 3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay as well as 3H-thymidine incorporation."	( Chou, FP; Lin, TM; Ou, HC; Sheu, WH; Yang, CH, 2006)
"Rosiglitazone-treated participants (n = 10) had significantly improved VO(2max) (19.8 +/- 5.3 ml ."	( Bauer, TA; Regensteiner, JG; Reusch, JE, 2005)
"Rosiglitazone pretreatment significantly attenuated the increases in W/D ratio, MPO activity and MDA levels, and reduced pulmonary overproduction of TNF-alpha and CINC-1 as well as expression of ICAM-1 following endotoxemia. "	( Liu, D; Yao, SL; Zeng, BX; Zhang, SH, 2005)
"Rosiglitazone treatment for 8 wk significantly increased insulin sensitivity and muscle UCP3 content (from 53.2 +/- 29.9 to 66.3 +/- 30.9 arbitrary units; P < 0.05)."	( Blaak, EE; Hesselink, MK; Mensink, M; Moonen-Kornips, E; Russell, AP; Schaart, G; Schrauwen, P; Sels, JP, 2006)
"Rosiglitazone pretreatment resulted in significantly decreased proliferation, apoptosis and reduced responsiveness to A-II stimulation in cultures from controls, pregnant rats and non-pregnant diabetic animals. "	( Averbukh, Z; Berman, S; Efrati, S; Feldman, L; Rapoport, M; Weissgarten, J, 2006)
"The rosiglitazone group was treated daily for 12 weeks with 4 mg rosiglitazone."	( Baik, SH; Choi, DS; Choi, KM; Kim, HY; Kim, NH; Kim, SG; Lee, J; Lee, KW; Ryu, OH; Seo, JA, 2006)
"Rosiglitazone treatment significantly increased circulating adiponectin levels (P < 0.001) relative to the control group (P = 0.21). "	( Baik, SH; Choi, DS; Choi, KM; Kim, HY; Kim, NH; Kim, SG; Lee, J; Lee, KW; Ryu, OH; Seo, JA, 2006)
"Rosiglitazone treatment improved neurological function at 7 days after ischemia."	( Chen, J; Graham, SH; Hong, Z; Luo, Y; Signore, AP; Wang, S; Yin, W; Zhang, F, 2006)
"The rosiglitazone-treated group showed the enhanced neurologic improvement, the reduced infarction volume compared to the ischemia-vehicle group with dose dependency, and the reduced hemispheric atrophy."	( Chu, K; Jung, KH; Kim, EH; Kim, JM; Kim, M; Kim, SJ; Ko, SY; Koo, JS; Lee, ST; Roh, JK; Sinn, DI; Song, EC, 2006)
"Rosiglitazone treatment was well tolerated. "	( Feldt, T; Fritzen, R; Goebels, K; Häussinger, D; Kambergs, J; Kappert, G; Kroidl, A; Oette, M; Vogt, C; Wettstein, M, 2006)
"Rosiglitazone treatment reduced insulin resistance, fibrinogen, and CRP levels and improved endothelial function in non-diabetic subjects with metabolic syndrome. "	( Aguiar, LG; Bahia, L; Bottino, D; Bouskela, E; Godoy-Matos, AF; Villela, N, 2006)
"Rosiglitazone treatment, while enhancing adipogenesis, induces a more favourable pattern of adipocytokine expression in satellite-derived fat cells."	( Boldrin, L; Centobene, C; De Coppi, P; Gamba, P; Milan, G; Pagano, C; Piccoli, M; Pilon, C; Pozzobon, M; Scarda, A; Vettor, R, 2006)
"Rosiglitazone treatment could improve left ventricular +/-dp/dt(max), collagen volume fraction and perivascular circumferential area; reduce lung/body mass ratio and liver/body mass ratio; inhibit myocardial angiotensin II and aldosterone; and had no significant effects on myocardial AT1 and AT2 mRNA."	( Geng, DF; Jin, DM; Wang, JF; Wu, W; Wu, YM, 2006)
"Rosiglitazone treatment significantly improved flow-mediated dilation (p <0.001) and nitroglycerin-induced vasodilation (p = 0.001) of the right brachial artery."	( Chen, MF; Chen, WJ; Cheng, WC; Lee, YT; Lin, JW; Wang, TD, 2006)
"Rosiglitazone-treated rats also demonstrated improved neurological functions."	( Allahtavakoli, M; Djahanguiri, B; Parviz, M; Sadr, SS; Shabanzadeh, AP, 2006)
"Rosiglitazone treatment improved diabetes compensation, significantly reduced VCAM-1, PAI-1 and E-selectin concentrations and increased adiponectin levels, while it did not affect serum resistin concentrations."	( Bošanská, L; Doležalová, R; Haluzík, M; Haluzík, MM; Kasalová, Z; Lacinová, Z; Stulc, T, 2007)
"Rosiglitazone treatment significantly reduced the morphological alteration associated with TNBS administration and the UI with the highest dose."	( de la Lastra, CA; Martín, AR; Sánchez-Hidalgo, M; Villegas, I, 2007)
"Rosiglitazone treatment curtailed the post-ischemic expression of the pro-inflammatory genes interleukin-1beta, interleukin-6, macrophage inflammatory protein-1alpha, monocyte chemoattractant protein-1, cyclooxygenase-2, inducible nitric oxide synthase, early growth response-1, CCAAT/enhancer binding protein-beta and nuclear factor-kappa B, and increased the expression of the anti-oxidant enzymes catalase and copper/zinc-superoxide dismutase."	( Bowen, KK; Feinstein, DL; Kapadia, R; Liang, J; Satriotomo, I; Tureyen, K; Vemuganti, R, 2007)
"Rosiglitazone treatment reversed all these biochemical indices."	( Dülger, GA; Gedik, N; Sehirli, AO; Sener, G, 2007)
"Rosiglitazone treatment significantly increased insulin clearance (molar ratio of the C-peptide to insulin AUCs: 12.80 +/- 1.34 vs 11.38 +/- .33, p < 0.05) and the insulin sensitivity index (12.0 +/- 1.5 vs 8.5 +/- 1.1 micromol m(-2) min(-1) pmol(-1)l, p < 0.01)."	( Chevassus, H; Farret, A; Galtier, F; Petit, P; Roux, B, 2007)
"Rosiglitazone-treated mice had more diarrhea, weight of colon and spleen were increased, and length of colon was decreased."	( Mensink, RP; Plat, J; Ramakers, JD; Te Velde, AA; Thuijls, G; Verstege, MI, 2007)
"Rosiglitazone treatment during cell growth resulted in the reduction of colony formation and the effects were not immediately reversible in the cell culture."	( Bai, X; Chen, WC; Lin, MS; Wang, YD, 2007)
"Rosiglitazone treatment prevented glomerular injury in diabetic rats, which was closely related with its roles of reducing reactive oxygen species, NF-kappaB activation and MCP-1 expression in the early phase of diabetic nephropathy."	( Bao, Y; Jia, RH; Li, J; Yuan, J, 2007)
"Rosiglitazone treatment in patients with diabetes resulted in a lower serum RBP4 level (35.2 +/- 10.2 vs."	( Bao, Y; Jia, W; Lu, J; Wang, C; Wu, H; Xiang, K; Zhu, J, 2007)
"Rosiglitazone treatment of cells with oxidative stress preserved nuclear transactivation of PPARgamma."	( Sommer, M; Wolf, G, 2007)
"Rosiglitazone treatment increased liver steatosis, particularly microvesicular steatosis."	( Díaz-Sanjuán, T; García-Ruiz, I; Martínez, MA; Muñoz-Yagüe, T; Rodríguez-Juan, C; Solís-Herruzo, JA, 2007)
"Rosiglitazone treatment for 3 months improved the glycemic control. "	( Ahn, CW; Cha, BS; Cho, YW; Hur, KY; Kim, HJ; Kim, SK; Lee, HC; Lim, SK; Park, SW; Shim, WS, 2007)
"Rosiglitazone treatment had no effect on protein levels but reduced activity by 73% of the control (P<0.05)."	( Clancy, P; Golledge, J; Mangan, S, 2008)
"Rosiglitazone treatment lowered leptin levels in lean mice, but increased leptin levels in BAL fluid of obese mice (p < 0.01)."	( Hart, CM; Holguin, F; Rojas, M, 2007)
"Rosiglitazone treatment prevented the development of dysglycaemia in nicotine-exposed animals. "	( Bruin, JE; Gerstein, HC; Holloway, AC; Petrik, JJ, 2008)
"Rosiglitazone treatment abrogated augmented IL-6, A-II and TGF-beta synthesis and restored intrarenal NO availability in the remaining kidneys."	( Averbukh, Z; Berman, S; Chachashvili, A; Cohen, N; Efrati, S; Weissgarten, J, 2008)
"Rosiglitazone treatment attenuates the proinflammatory responses, represented by augmented IL-6, A-II and TGF-beta production, developing in the remaining kidney following contralateral nephrectomy. "	( Averbukh, Z; Berman, S; Chachashvili, A; Cohen, N; Efrati, S; Weissgarten, J, 2008)
"Rosiglitazone and glyburide treatment resulted in significant and equivalent decreases in glucose (p < 0.0001) and HbA1c (p < 0.0001), with a trend toward decreased HOMA (p = 0.09)."	( Bank, AJ; Gonzalez-Campoy, JM; Kaiser, DR; Kelly, AS; Thelen, AM, 2007)
"Rosiglitazone treatment in nonnephritic rats did not influence proteinuria, urea, or renal histology."	( den Ouden, K; Goldschmeding, R; Joles, JA; Nguyen, TQ; Verhaar, MC; Westerweel, PE, 2008)
"Rosiglitazone treatment was without effect on endothelium-dependent dilation, blood pressure, pulse-wave-velocity and plasma angiotensin peptide levels."	( Ahner, K; Boecking, W; Bramlage, P; Brosnihan, KB; Ferrario, CM; Jatzke, C; Kirch, W; Maywald, U; Oertel, R; Schindler, C, 2008)
"Rosiglitazone treatment improved insulin, glucose, triglyceride, and superoxide levels as well as NADHP oxidase activity in OZRs."	( Abram, SR; Carter, C; Dearman, J; Hester, RL; Xiang, L, 2008)
"Rosiglitazone treatment significantly increased VO2 peak (P < 0.0001), the duration of the exercise test (P < 0.0001), oxygen pulse (P = 0.010) and TIMP-2 levels (P = 0.008) in comparison with CG. "	( Alevizos, M; Angelopoulou, N; Iliadis, F; Kadoglou, NP; Liapis, CD; Perrea, D, 2008)
"Rosiglitazone treatment increases cardiorespiratory fitness and modulates favourably serum adiponectin, MMP-9 and TIMP-2 levels. "	( Alevizos, M; Angelopoulou, N; Iliadis, F; Kadoglou, NP; Liapis, CD; Perrea, D, 2008)
"Rosiglitazone treatment restored endothelium-dependent vasodilatory responses to pretransplantation levels."	( Boer, MW; Hillebrands, JL; Klatter, FA; Navis, G; Onuta, G; Rienstra, H; Roks, AJ; Rozing, J, 2008)
"Rosiglitazone treatment after allogeneic transplantation restores endothelial function but impairs vascular smooth muscle cell vasomotor activity. "	( Boer, MW; Hillebrands, JL; Klatter, FA; Navis, G; Onuta, G; Rienstra, H; Roks, AJ; Rozing, J, 2008)
"The rosiglitazone-treated tumor had reduced expression of ki-67 and lowered mitotic rate."	( Chan, KW; Dai, Y; Gu, Q; Lan, HY; Li, Z; Ma, J; Qiao, L; Wang, Y; Wong, BC; Wong, BL; Zou, B, 2008)
"In rosiglitazone-treated cultures, morphological signs of adipose differentiation and expression levels of the general adipogenic marker aP2 were manifested much earlier than in control cultures."	( Cannon, B; Nedergaard, J; Petrovic, N; Shabalina, IG; Timmons, JA, 2008)
"All rosiglitazone treatment groups showed significantly reduced peak postprandial glucose concentrations compared with baseline (p < 0.001) and with placebo (p < 0.0001) and reduced postprandial glucose excursion, without an increase in the area under the postprandial insulin concentration-time curve."	( Cole, ST; Freed, MI; Patwardhan, R; Rappaport, EB; Raskin, P; Yan, Y, 2000)
"Rosiglitazone treatment markedly enhanced weight gain compared with untreated ZDF rats (final weight 732+/-13 g vs."	( Arch, JR; Buckingham, RE; Cai, XJ; Lister, CA; Pickavance, L; Wilding, J; Williams, G; Wilson, S, 2000)
"Rosiglitazone treatment increased the triglyceride content of the steatotic livers of A-ZIP/F-1 and ob/ob mice, but not the "lean" livers of fat-transplanted A-ZIP/F-1 mice."	( Arioglu, E; Chao, L; Gavrilova, O; Marcus-Samuels, B; Mason, MM; Moitra, J; Reitman, ML; Vinson, C, 2000)
"Rosiglitazone treatment for 10-14 days, 10-day insulin treatment, and 60-h fasting reversed defects in PKC-zeta/lambda activation in GK muscles and adipocytes and increased glucose transport in GK adipocytes, without necessarily increasing IRS-1-dependent PI 3-kinase or PKB activation."	( Bandyopadhyay, G; Farese, RV; Kanoh, Y; Sajan, MP; Standaert, ML, 2001)
"rosiglitazone-treated, ad lib-fed dietary obese), despite unchanged FFAs."	( Buckingham, RE; Pickavance, LC; Wilding, JP, 2001)
"Rosiglitazone treatment decreased adiponectin and resistin mRNA levels by 57 and 72%, respectively (P < 0.001), with no effect on the level of TNFalpha or RELMalpha transcripts."	( Chapman, H; Clapham, JC; Holder, JC; Lister, CA; Moore, GB; Piercy, V; Smith, SA, 2001)
"Rosiglitazone treatment for 48 h significantly increased basal and insulin-stimulated glucose uptake and markedly increased the cellular expression of GLUT1 but not GLUT4."	( Chatterjee, VK; Nugent, C; O'Rahilly, S; Prins, JB; Savage, D; Wentworth, JM; Whitehead, JP, 2001)
"Rosiglitazone treatment for 5 months improved insulin sensitivity, lowered serum free testosterone, and resulted in spontaneous ovulation and conception."	( Abbasi, F; Cataldo, NA; Lamendola, C; McLaughlin, TL; Reaven, GM, 2001)
"Rosiglitazone treatment resulted in a 68% (P < 0.002) and a 20% (P < 0.016) improvement in insulin-stimulated glucose metabolism during the low- and high- dosage-insulin clamps, respectively, which was associated with approximately 40% reductions in plasma fatty acid concentration (P < 0.05) and hepatic triglyceride content (P < 0.05)."	( Befroy, D; Cline, GW; Dufour, S; Enocksson, S; Hundal, RS; Inzucchi, SE; Lebon, V; Mayerson, AB; Petersen, KF; Shulman, GI, 2002)
"Rosiglitazone treatment decreases insulin resistance in type 2 diabetic patients, but no data exist concerning rosiglitazone treatment of patients with syndromes of extreme insulin resistance."	( Lund, S; Pedersen, O; Vestergaard, H, 2001)
"Rosiglitazone treatment, in combination with insulin and metformin, of patients with severe primary insulin resistance due to IR mutations and diabetes mellitus, had no impact on the measured estimates of glucose and lipid metabolism. "	( Lund, S; Pedersen, O; Vestergaard, H, 2001)
"Rosiglitazone treatment normalized the insulin resistance and restored GLUT4 protein levels in obese rat hearts."	( Buckingham, RE; Clarke, K; Cole, MA; Desrois, M; Draper, NJ; Sidell, RJ, 2002)
"Rosiglitazone treatment led to normalization of the blunted insulin-mediated suppression of the glucose production rate and to a approximately 2-fold increase in whole body insulin-mediated glucose disappearance rate (p < 0.001)."	( Adeli, K; Buckingham, R; Carpentier, A; Leung, N; Lewis, GF; Szeto, L; Taghibiglou, C; Uffelman, KD; Van Iderstine, SC, 2002)
"Treatment with rosiglitazone (a peroxisome proliferator-activated receptor (PPAR)-γ agonist), GW501516 (a PPARδ agonist), and bone morphogenetic protein (BMP)-7 for 8 days efficiently increased Ucp1 expression in response to treatment with forskolin, an activator of the protein kinase A pathway."	( Diao, Z; Funaba, M; Matsui, T; Murakami, M; Shimokawa, F; Yamamoto, T, 2022)
"Pretreatment with rosiglitazone significantly prevented the progression of kindling in comparison with control group."	( Amini, A; Ayatollahi, AA; Chen, S; Koohsar, F; Li, J; Wang, F; Zeyghami, MA; Zhang, J, 2023)
"Treatment with rosiglitazone in vitro reduced the expression of NLRP3, and the NLRP3 activator monosodium urate (MSU) reversed the inhibition of IL-1β and TNF-α by rosiglitazone in macrophages."	( Chen, H; Feng, Z; Hu, L; Meng, Q; Zhang, H; Zhang, X, 2020)
"Pre-treatment with rosiglitazone ameliorated liver injury from severe DCS. "	( Chen, MM; Jiang, ZL; Li, X; Peng, B; Wang, GH; Xu, LH, 2017)
"Treatment with rosiglitazone (5 µM, 10 µM, and 20 µM) or metformin (1 mM and 10 mM) inhibited cell proliferation, and induced cell cycle arrest at G0/G1 or S phase, respectively, in a dose-dependent manner."	( Gao, H; Hong, T; Wang, H; Wei, R; Yang, J; Yu, F, 2018)
"Treatment with rosiglitazone dose-dependently upregulated anti-oxidative CAT and SOD2, and rescued hypoxic injury in first trimester villous explants and JEG-3 cells, strongly suggesting the involvement of the PPARγ in regulating their expressions."	( Armant, DR; Drewlo, S; Hertz, M; Johnson, E; Kadam, L; Kilburn, BA; Kohan-Ghadr, HR; Kolb, BL; Rodriguez-Kovacs, J, 2019)
"Treatment with rosiglitazone for 1 hour leads to acute transcriptional activation as well as repression of a number of genes as determined by genome-wide RNA polymerase II occupancy."	( Haakonsson, AK; Mandrup, S; Nielsen, R; Sandelin, A; Stahl Madsen, M, 2013)
"Pretreatment with rosiglitazone protects rats against PQ-induced acute lung injury by activating PPAR-γ, inducing Nrf2 expression and inhibiting NF-κB activation."	( Bai, SL; Hou, WJ; Liu, ZN; Zhao, HY; Zhao, M; Zheng, Q, 2013)
"Pretreatment of rosiglitazone prevents cisplatin induced nephrotoxicity which was, clearly evident from the renal biochemical parameters like reduced BUN, creatinine and TNFα levels, and increased albumin levels, which was also supported by histopathological studies of the kidneys."	( Barua, CC; Bezbaruah, B; Gaikwad, AB; Kumar, P; Prashanth, KS; Vij, M, 2013)
"Pretreatment with rosiglitazone (0.5-5 μM) for 24 h prevented the Aβ42-induced loss of dendritic filopodium and synapse in a dose-dependent manner."	( Anwyl, R; Bao, X; Li, S; Liu, G; Wang, Q; Wu, J; Xu, S; Zheng, B, 2014)
"Treatment with rosiglitazone, a peroxisome proliferator-activated receptor-γ agonist, in type 2 diabetic mellitus (T2DM) patients is under scrutiny because it affects adversely cardiovascular outcomes. "	( Ala-Korpela, M; Badeau, RM; Honka, MJ; Kangas, AJ; Lautamäki, R; Nuutila, P; Soininen, P; Stewart, M, 2014)
"Treatment with rosiglitazone (5, 10 mg/kg) and VPA (100, 200 mg/kg) for 21 days significantly attenuated these behavioral, biochemical, and cellular alterations as compared to control (QA 200 nmol) group."	( Chaudhary, T; Kumar, A; Mishra, J, 2014)
"Co-treatment with rosiglitazone diminished these changes."	( Dong, X; Gao, D; Hao, G; Liu, Z; Meng, Z; Ning, N; Niu, X; Yang, G, 2015)
"Treatment with rosiglitazone [5 mg/kg/day, per oral (PO)] was assessed for 21 days."	( Abduljawad, SH; El-Brairy, AI; El-Naa, MM; El-Readi, MZ; El-Refaei, MF; Nasif, WA, 2015)
"Treatment with Rosiglitazone, a PPARγ agonist, could overcome the differentiation inhibition imposed by R96Q mutant, suggesting the effect of FTO is mediated through PPARγ."	( Cao, Q; Chai, J; Guo, F; Ma, J; Zhang, M; Zhang, Y; Zhao, R; Zhao, W; Zhou, B, 2015)
"Treatment with rosiglitazone stimulated both AMPK and PPARγ in isolated rat platelets."	( Chang, KH; Huh, HJ; Lee, K; Lee, MY; Liu, Y; Park, JM, 2016)
"Treatment with rosiglitazone attenuated tubulointerstitial fibrosis and epithelial phenotype transition in WT but not proximal tubule PPAR-γ KO mice."	( Bai, M; Chen, Y; Ding, G; Huang, S; Jia, Z; Xu, Y; Zhang, A; Zhang, Y; Zhao, M, 2016)
"Treatment with rosiglitazone also resulted in significantly reduced first phase (-33%) and second phase (-20%) insulin release."	( Berry, EA; de Jong, SA; Manning, PJ; Sutherland, WH; Walker, RJ; Williams, SM, 2008)
"Treatment with rosiglitazone increased mitochondrial mass levels, suggesting a role for the PPARgamma pathway in mitochondrial function in striatal cells."	( Bronfman, M; Fuenzalida, K; Jin, YN; Johnson, GVW; Quintanilla, RA, 2008)
"Treatment with rosiglitazone caused a significant decrease of virus infection in macrophages. "	( Dou, H; Heilman, D; Knipe, B; Leibhart, J; Mercer, A; Morsey, B; Papugani, A; Persidsky, Y; Potula, R; Ramirez, SH; Schall, K, 2008)
"The treatment with rosiglitazone could be associated with increased risk for myocardial infarction (MI). "	( Mannucci, E; Marchionni, N; Monami, M, 2008)
"The treatment with Rosiglitazone inhibited all these derangements, i.e."	( Jain, S; Marotta, F; Prasad, GB; Sinha, PR; Yadav, H; Yadav, M, 2009)
"Dual treatment of rosiglitazone and losartan provided synergistic effect in reducing ICAM-1, IL-6 and ATR1 expression and NF-kappaB and ERK1/2 activation induced by the conditioned media when compared with monotherapy."	( Chan, LY; Lai, KN; Leung, JC; Tang, SC; Xiao, J, 2009)
"Pretreatment with rosiglitazone inhibited the Ang II-induced expression of angiotensin type 1a Ang II receptor while having no effect on the angiotensin type 2 Ang II receptor, in addition to reducing Ang II-induced expression of E-selectin, tumor necrosis factor-alpha, and interleukin-6."	( Cockerill, GW; Deb, R; Dunkley, M; Gaze, D; Gnaneswaran, Y; Howe, F; Jones, A; Loftus, IM; Nasr, H; Thompson, MM; Torsney, E, 2009)
"Treatment with rosiglitazone prevented the development of pulmonary hypertension at 3 weeks; reversed established pulmonary hypertension at 5 weeks; and attenuated CH-stimulated Nox4 expression and superoxide production, PDGFRbeta activation, and reductions in PTEN expression."	( Bland, JM; Hart, CM; Kleinhenz, DJ; Mitchell, PO; Nisbet, RE; Sutliff, RL; Walp, ER, 2010)
"Treatment with rosiglitazone reduced infarction and improved functional recovery; it also enhanced the neuroprotective action of tPA and lengthened the time window for initiating tPA treatment."	( Ding, X; He, C; Noor, R; Pegg, C; Shuaib, A; Wang, CX, 2009)
"Treatment with rosiglitazone over 1 year had no effect on progression of carotid atheroma in patients with type 2 diabetes mellitus compared to placebo."	( Chan, CF; Crowe, LA; Johnston, DG; Keenan, NG; Pennell, DJ; Varghese, A; Yee, MS, 2009)
"Treatment with rosiglitazone increased parasite clearance and decreased inflammatory biomarkers associated with adverse malaria outcomes."	( Boggild, AK; Kain, KC; Katz, K; Krudsood, S; Liles, WC; Looareesuwan, S; Patel, SN; Serghides, L; Tangpukdee, N; Wilairatana, P, 2009)
"Treatment with rosiglitazone increased proliferation, and decreased apoptosis, compared NV animals."	( Alfaidy, N; Cesta, CE; Gerstein, HC; Holloway, AC; Kellenberger, LD; Petrik, JJ, 2009)
"Treatment with rosiglitazone enhanced glucose utilization and diminished MFAO, thus reversing the metabolic phenotype of the diabetic heart."	( Finck, BN; Gropler, RJ; Herrero, P; Schechtman, KB; Sharp, T; Shoghi, KI; Welch, MJ, 2009)
"Treatment with rosiglitazone (RSG), an insulin sensitizer, for 2 weeks increased vascular PPARgamma expression and restored PI3-kinase/Akt/eNOS-mediated signaling pathway only in young SHRs."	( Gao, F; Huang, C; Huang, Y; Li, R; Wang, W; Wang, X; Zhang, H, 2010)
"Treatment with rosiglitazone and CC or LOD and CC resulted in increased ovulation (80.8 vs. "	( Baruah, J; Kachava, G; Karmakar, D; Kumar, S; Roy, KK; Sharma, A; Sharma, JB, 2010)
"Pretreatment with rosiglitazone also suppressed radiation-induced H2AX phosphorylation in response to DNA damage and AKT activation for cell survival; on the contrary, rosiglitazone pretreatment enhanced radiation-induced caspase-8, -9, and -3 activation and PARP cleavage in HT-29 cells."	( Chiu, SJ; Chuah, JQ; Hsaio, CH; Lee, JW; Shih, WL; Su, YH; Tseng, HH, 2010)
"The treatment with rosiglitazone (5 and 10 mg/kg per day orally) started from the first day of administration of L-methionine significantly abolished hyperhomocysteinemia-induced increase in left ventricular weight to body weight ratio, left ventricular wall thickness, cardiomyocyte diameter, collagen deposition, and oxidative stress without affecting serum homocysteine levels in rats."	( Kaur, T; Pal Singh, A; Singh Bedi, PM; Singh, N; SinghDahiya, R, 2010)
"Treatment with rosiglitazone (3 mg/kg/day, p.o., 2 weeks and 5 mg/kg/day, p.o., 2 weeks) significantly prevented sodium arsenite-induced VED by enhancing acetylcholine-induced endothelium dependent relaxation, improving the integrity of vascular endothelium, increasing the nitrite/nitrate concentration and decreasing the oxidative stress."	( Balakumar, P; Goel, RK; Kaur, T, 2010)
"Treatment with rosiglitazone significantly increased FMD after 6 h from 4.3% (3.3; 4.9) to 7.6% (5.6; 9.2) (p<0.0001 vs."	( Balletshofer, B; Böger, RH; Hetzel, J; Hombach, V; Koenig, W; Marx, N; Mielke, C; Rau, M; Rittig, K; Schwedhelm, E; Walcher, D; Walcher, T, 2010)
"Treatment with rosiglitazone increased baseline insulin sensitivity of OLETF rats and evoked an increase in CCK-1 receptor gene expression in LETO rats."	( Döbrönte, R; Drimba, L; Németh, J; Pázmány, T; Peitl, B; Sári, R; Szilvássy, Z; Varga, A, 2010)
"Treatment with rosiglitazone preserved salbutamol relaxant activity, mitigated carbachol hyperresponsiveness and partially restored β₂-adrenoceptor binding sites in tracheal tissues from homologously desensitized animals."	( Adinolfi, B; Bardelli, C; Betti, L; Breschi, MC; Brunelleschi, S; Fabbrini, L; Fogli, S; Giannaccini, G; Lucacchini, A; Mariotti, V; Melissari, E; Pellegrini, S; Stefanelli, F, 2011)
"Treatment with rosiglitazone significantly increased apoA-II production in subjects with metabolic syndrome and low HDL-C but had no effect on apoA-I metabolism."	( Bloedon, LT; Ikewaki, K; Millar, JS; Rader, DJ; Szapary, PO; Wolfe, ML, 2011)
"Pretreatment with rosiglitazone significantly increased the number of cells that stained for PPARγ and significantly decreased the number of cells that stained for inducible nitric oxide synthase."	( Fan, W; Han, J; Hong, Y; Hou, Y; Liu, Y; Wu, Z; Yin, Y; Zhu, H, 2010)
"Treatment with rosiglitazone decreased blood glucose levels to 80% at 1h after pretreatment of rosiglitazone (p<0.05)."	( Cheng, FC; Cheng, SM; Chou, CC; Chuang, HC; Lee, MR; Sheu, WH, 2011)
"Treatment with rosiglitazone has been associated with severe paradoxical HDL-c reductions. "	( Almeida, RL; Almeida, TS; Fedrizzi, D; Fedrizzi, P, 2010)
"Treatment with rosiglitazone prior to and during exposure to AM5.5 inhibited the H(2)O(2) generation whereas the specific PPARγ antagonist GW9662 offsets the inhibitory action of rosiglitazone."	( Park, SY; Sohn, UD, 2011)
"Treatment with rosiglitazone among patients with T2DM reduces the concentration of plasma OPG."	( Gram, J; Henriksen, JE; Juhl, HF; Nybo, M; Olesen, M; Preil, SR; Rasmussen, LM; Yderstraede, K, 2011)
"Treatment of rosiglitazone-supplemented VSMC cultures with the caloric restriction mimetic and antioxidant resveratrol diminished rosiglitazone-induced oxidative stress, osteoblast-like differentiation and mineralization."	( Bruedigam, C; Chiba, H; Eijken, M; Koedam, M; van Leeuwen, JP, 2011)
"Treatment with rosiglitazone improved survival rate, decreased the markers of organ injury, and suppressed the release of TNF-alpha, IL-6, and MCP-1 after HS in rats."	( Harn, HJ; Hsu, BG; Lee, CJ; Lee, RP; Peng, TC; Subeq, YM; Yang, FL, 2011)
"Treatment with rosiglitazone suppresses the release of serum TNF-alpha, IL-6 and MCP-1, and ameliorates HS-induced organ damage in rats."	( Harn, HJ; Hsu, BG; Lee, CJ; Lee, RP; Peng, TC; Subeq, YM; Yang, FL, 2011)
"Treatment with rosiglitazone restored mast cell numbers in the pleural cavity and mesenteric tissue of diabetic rats."	( Batista, MM; Carvalho, VF; Cordeiro, RS; E Silva, PM; Martins, MA; Pons, AH; Silva, AR; Torres, RC, 2012)
"Upon treatment with rosiglitazone, an agonist of PPARγ, intestine proinflammatory indicators were markedly decreased in wild-type mice, but to a much lesser degree in PFKFB3/iPFK2-disrupted mice."	( Chen, YE; Guo, X; Halim, V; Huo, Y; Li, H; Sturino, JM; Thomas, LN; Woo, SL; Wu, C; Xu, H, 2013)
"Mice treated with rosiglitazone were subjected to 60 minutes of focal ischemia followed by reperfusion."	( Chan, PH; Jung, JE; Kim, GS; Maier, CM; Narasimhan, P; Okami, N; Sakata, H; Yoshioka, H, 2013)
"Post-treatment (rosiglitazone/gastric banding) biopsies were also examined in adults."	( Baumann, U; Bhathal, PS; Brown, RM; Brunt, EM; Clouston, AD; Couper, RT; Dixon, JB; Ee, LC; Jonsson, JR; Manton, ND; Moschen, AR; Neuschwander-Tetri, BA; O'Brien, PE; Powell, EE; Richardson, MM; Skoien, R; Tilg, H; Weltman, M, 2013)
"Treatment with rosiglitazone resulted in a decrease in the production rates of T from, basal, 318 +/- 62 microg/h to 272 +/- 72 microg/h (P <.05)."	( Nowotny, P; Vierhapper, H; Waldhäusl, W, 2003)
"Treatment with rosiglitazone or with the natural PPARgamma agonist 15-deoxy-delta-(12,14) PGJ2 did not modify cell growth, but interestingly, activation of PPARgamma by this synthetic (rosiglitazone) or natural (15d-PGJ2) ligand markedly inhibited cell invasion in a concentration-dependent manner."	( Delouis, C; Evain-Brion, D; Fournier, T; Hermouet, A; Pavan, L; Tarrade, A; Thérond, P; Titeux, M; Vidaud, M, 2003)
"Treatment with rosiglitazone reduced hyperinsulinemia and improved small artery elasticity with a tendency to improve large artery elasticity, in hypertensive and in normotensive patients. "	( Gavish, D; Gavish, E; Leibovitz, E; Leibovitz, Z; Matas, D; Matas, Z; Shargorodsky, M; Wainstein, G; Wainstein, J; Zimlichman, R, 2003)
"Treatment with rosiglitazone at 30 mg/kg body weight for 24 and 48 h increased insulin signalling and decreased IRS1 S307 phosphorylation concomitantly."	( Biswas, S; Dallas-Yang, Q; Jiang, G; Li, Z; Zhang, BB, 2004)
"Treatment with rosiglitazone enhanced PPARgamma expression, improved endothelium-dependent vasodilatation, preserved P-VASP, suppressed gp91phox and iNOS expression, reduced superoxide and total NOx production, and inhibited nitrotyrosine formation."	( Batinic-Haberle, I; Christopher, TA; Gao, E; Liu, HR; Lopez, BL; Ma, XL; Ohlstein, EH; Tao, L; Teng, ZP; Willette, RN; Yue, TL, 2003)
"Upon treatment with rosiglitazone, an insulin-sensitizing drug, these macrophage-originated genes are downregulated."	( Barnes, GT; Chen, H; Chou, CJ; Nichols, A; Ross, JS; Sole, J; Tan, G; Tartaglia, LA; Xu, H; Yang, D; Yang, Q, 2003)
"Treatment with rosiglitazone or fenofibrate did not affect the serum estradiol level in the mice which received estradiol together with PPAR agonists for 30 days."	( Bitter, AD; Demakov, AB; Gunin, AG; Suslonova, NV; Vasilieva, EN, 2004)
"Treatment with rosiglitazone for 26 wk (study 1) produced significant dose-dependent decreases in both plasma PI concentrations (18-29%) and the PI:IRI ratio compared with baseline (7-14%) and placebo (19-29%) (P < 0.001)."	( Biswas, N; Freed, MI; Porter, LE; Smith, SA, 2004)
"Treatment with rosiglitazone was followed by a significantly improved mean glucose disposal rate (from 6.5 to 9.1 g/kg/min; P = 0.02) and a significant decline in fasting and 2 h plasma glucose (from 6.4 to 5.8 mmol/l, P = 0.01 and from 14.2 to 10.6 mmol/l, P = 0.03, respectively). "	( Asberg, A; Hartmann, A; Hjelmesaeth, J; Jenssen, T; Simonsen, C; Voytovich, MH, 2005)
"Treatment with rosiglitazone increased the production of thyroglobulin in some patients with thyroid cancers, but only rarely restored scintigraphically significant iodine trapping. "	( Buchegger, F; Meier, CA; Petite, C; Philips, JC; Willi, JP, 2004)
"Treatment with rosiglitazone increased food intake and body weight, and after 2 weeks, reduced daytime blood glucose, water intake and the area under the glucose tolerance curve."	( Arch, JR; Augstein, P; Cawthorne, MA; Demuth, HU; Heinke, P; Hoffmann, T; Meyer, A; Sennitt, MV; Stocker, C; Subramanian, A; Wargent, E, 2005)
"Treatment with rosiglitazone appears to be safe and effective in patients with NODM after renal transplantation."	( Herget-Rosenthal, S; Janssen, O; Kribben, A; Mann, K; Patschan, D; Philipp, T; Pietruck, F; Van, TN; Witzke, O, 2005)
"Pre-treatment with rosiglitazone reduced the infiltration of macrophages/monocytes in renal tissue."	( Kang, KP; Kim, DH; Kim, HJ; Kim, W; Lee, S; Moon, SO; Park, SK; Sung, MJ, 2005)
"Pretreatment with rosiglitazone also markedly suppressed lipopolysaccharide-induced expression of inducible nitric oxide synthase messenger RNA and protein in the lung, as demonstrated by reverse transcription-polymerase chain reaction or Western blot analysis."	( Geng, ZL; Liu, D; Wang, YL; Zeng, BX; Zeng, L; Zhang, SF; Zhang, SH, 2005)
"With treatment of rosiglitazone at 4 mg/day monotherapy for 3 months, hs-CRP levels decreased significantly by 26% (p <0.05) and adiponectin levels increased significantly by 192% (p <0.05), but no significant changes in levels of MMP-9 and sCD40L were demonstrated."	( Chu, CS; Lai, WT; Lee, KT; Lee, MY; Sheu, SH; Su, HM; Voon, WC, 2006)
"Treatment with rosiglitazone lead to improved insulin sensitivity which may predict longer term preservation of B-cell function."	( Kulenović, I, 2006)
"Pre-treatment with rosiglitazone reduced the systemic levels of TNF-alpha and down-regulated adhesion molecule expression in addition to the infiltration of inflammatory cells after cisplatin administration."	( Jang, KY; Jang, YB; Kang, KP; Kim, DH; Kim, W; Lee, JE; Lee, S; Moon, SO; Park, SK; Sung, MJ, 2006)
"Treatment with rosiglitazone in combination with metformin provides better glycaemic control over the remaining lifetime of patients than metformin and sulfonylurea combination therapy. "	( Bagust, A; Beale, S; Hulme, L; Martin, A; Shearer, AT, 2006)
"Treatment with rosiglitazone resulted in enhanced radioiodine uptake in areas of presumed metastatic disease in the neck that were previously only faintly seen, and serum thyroglobulin fell from a pretreatment level of 41 ng/mL to less than 2 ng/mL."	( Elias, AN; Lizotte, P, 2006)
"Cotreatment with rosiglitazone diminished these changes, whereas increased nuclear PPAR-gamma expression in VSMCs."	( Gao, DF; Hao, GH; Ning, N; Niu, XL; Peng, N; Wang, NP; Wei, J, 2007)
"Treatment with rosiglitazone resulted in increased serum adiponectin (P < 0.001), decreased insulin levels (P = 0.005), and increased insulin sensitivity (P = 0.004)."	( Eng, C; Farrar, WB; Johnson, MV; Lester, J; Povoski, SP; Suster, S; Walker, MJ; Wen, P; Williams, N; Yee, LD; Young, DC, 2007)
"Treatment with rosiglitazone reversed these effects and reduced BP to 133 +/- 7 mm Hg, insulin levels to 30 +/- 2.8 muU/mL, triglycerides to 116 +/- 9 mg/dL, and the OGTT to 15,415 +/- 372 mg/dL/min (P < .05 for all variables)."	( Avni, I; Grossman, E; Kamari, Y; Oron-Herman, M; Peleg, E; Shabtay, Z; Shamiss, A; Sharabi, Y, 2007)
"Treatment with rosiglitazone for 1-week significantly reduced aortic O(2)(-.) production and the expression of Nox-1, 2, and 4 but failed to increase Cu/Zn SOD or PPARgamma in aortic tissue from db(-)/db(-) mice."	( Campbell, AG; Hart, CM; Hwang, J; Kleinhenz, DJ; Rupnow, HL; Sutliff, RL; Thulé, PM, 2007)
"Treatment with rosiglitazone, a potent peroxisome proliferator-activated receptor (PPAR) gamma agonist, results in lipid storage coupled with reduced release of free fatty acids into the circulation. "	( Ahn, CW; Cha, BS; Jung, TW; Kang, ES; Kim, DJ; Kim, HJ; Lee, HC; Lee, KW, 2007)
"nontreated). Rosiglitazone reduced T cell alloreactivity which was not mediated through modulation of CD4+CD25+FoxP3+ regulatory T cells."	( Boer, MW; de Boer, JF; Hillebrands, JL; Klatter, FA; Navis, G; Onuta, G; Rienstra, H; Roks, AJ; Rozing, J; Uges, DR, 2007)
"Treatment with rosiglitazone increased BAL adiponectin levels in lean (p = 0.04) and to a lesser extent in obese mice (p = 0.07)."	( Hart, CM; Holguin, F; Rojas, M, 2007)
"Treatment with rosiglitazone can increase the NO production and improve the endothelial function through up-regulating the PI3K/PKB/eNOS signal pathways in cultured HUVECs."	( Feng, XL; Lei, MX; Wu, J; Xie, XY, 2007)
"Treatment with Rosiglitazone should be reconsidered because of a potential cardiovascular risk. "	( Erdmann, E; Hoppe, UC; Michels, G; Rottlaender, D, 2007)
"Treatment with rosiglitazone for 3 months resulted in a significant improvement in the index of hepatic insulin sensitivity (86.4+/-15% compared with 139+/-23; P=0.007) as well as peripheral insulin sensitivity (4.04+/-0.23 compared with 6.17+/-0.66 mg of glucose/kg of lean body mass per min; P<0.001)."	( Ahn, H; Ferris, R; Gelato, MC; McNurlan, MA; Mynarcik, DC; Qurashi, S, 2008)
"Co-treatment with rosiglitazone significantly decreased these levels and upregulated PPAR-gamma expression."	( Gao, DF; Hao, GH; Niu, XL; Wang, NP; Wei, J, 2008)
"Treatment with rosiglitazone was interrupted and the subject underwent a series of retinal photocoagulations for proliferative retinopathy."	( Arrigoni, F; Costanza, F; Di Blasi, P; Longobardi, A; Merante, D; Tatti, P, 2008)
"Treatment with rosiglitazone was associated with a reduction in mean TG of 13.34 mg/dL, an increase in TC of 4.81 mg/dL, a reduction in HDL-C of 0.12 mg/dL, and an increase in LDL-C of 3.56 mg/dL."	( Boyle, PJ; King, AB; Lau, H; Magar, R; Marchetti, A; Martin, J; Olansky, L, 2002)

Role	Description
pro-angiogenic agent	Any compound that promotes the growth of new blood vessels from pre-existing vessels.
radical scavenger	A role played by a substance that can react readily with, and thereby eliminate, radicals.
insulin-sensitizing drug	An agent which overcomes insulin resistance by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).
ferroptosis inhibitor	Any substance that inhibits the process of ferroptosis (a type of programmed cell death dependent on iron and characterized by the accumulation of lipid peroxides) in organisms.
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor	An EC 6.2.1.* (acid-thiol ligase) inhibitor that interferes with the action of a long-chain-fatty-acid--CoA ligase (EC 6.2.1.3).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
coumarins
acetate ester	Any carboxylic ester where the carboxylic acid component is acetic acid.
diester	A diester is a compound containing two ester groups.
aminopyridine	Compounds containing a pyridine skeleton substituted by one or more amine groups.
thiazolidinediones	A thiadiazolidine in which the 1,3-thiazolidine ring is substituted by two oxo groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathway	Proteins	Compounds
Rosiglitazone Metabolism Pathway	3	20

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, HADH2 protein	Homo sapiens (human)	Potency	31.6228	0.0251	20.2376	39.8107	AID893
Chain B, HADH2 protein	Homo sapiens (human)	Potency	31.6228	0.0251	20.2376	39.8107	AID893
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	28.1838	0.1778	14.3909	39.8107	AID2147
Luciferase	Photinus pyralis (common eastern firefly)	Potency	32.1968	0.0072	15.7588	89.3584	AID624030
USP1 protein, partial	Homo sapiens (human)	Potency	5.0119	0.0316	37.5844	354.8130	AID504865
TDP1 protein	Homo sapiens (human)	Potency	30.0534	0.0008	11.3822	44.6684	AID686978; AID686979
AR protein	Homo sapiens (human)	Potency	15.1891	0.0002	21.2231	8,912.5098	AID743036; AID743053
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	15.5567	0.0010	22.6508	76.6163	AID1224838; AID1224893
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	35.4813	0.0123	7.9835	43.2770	AID1346984
EWS/FLI fusion protein	Homo sapiens (human)	Potency	8.5547	0.0013	10.1577	42.8575	AID1259252; AID1259253
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	10.6822	0.0002	14.3764	60.0339	AID720692
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	6.3689	0.0002	29.3054	16,493.5996	AID743069; AID743075
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	0.8966	0.0010	19.4141	70.9645	AID743094; AID743140; AID743191
thyrotropin-releasing hormone receptor	Homo sapiens (human)	Potency	3.3786	0.1549	17.8702	43.6557	AID1346891
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	0.0007	0.0578	21.1097	61.2679	AID1159526
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1	Homo sapiens (human)	Potency	28.1838	0.0018	15.6638	39.8107	AID894
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	27.4822	0.0003	23.4451	159.6830	AID743065; AID743067
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	7.9433	0.0316	10.2792	39.8107	AID884; AID885
lamin isoform A-delta10	Homo sapiens (human)	Potency	0.0022	0.8913	12.0676	28.1838	AID1487
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Cellular tumor antigen p53	Homo sapiens (human)	Potency	13.3332	0.0023	19.5956	74.0614	AID651631
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	7.9433	1.0000	12.2248	31.6228	AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
CDGSH iron-sulfur domain-containing protein 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	1.1000	1.0000	1.0500	1.1000	AID458856
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	21.0000	0.2000	5.6774	10.0000	AID1473741
Bile salt export pump	Rattus norvegicus (Norway rat)	IC50 (µMol)	40.0000	0.4000	2.7500	8.6000	AID1209456
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	4.5853	0.1100	7.1903	10.0000	AID1209455; AID1443980; AID1443989; AID1449628; AID1473738; AID1674183
Carbonic anhydrase 2	Homo sapiens (human)	IC50 (µMol)	4.0690	0.0002	1.1060	8.3000	AID625236
Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)	IC50 (µMol)	215.0000	0.0005	3.4984	9.7600	AID440905; AID637349
Carnitine O-palmitoyltransferase 2, mitochondrial	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.3800	2.0933	5.1000	AID1207593
Amine oxidase [flavin-containing] B	Rattus norvegicus (Norway rat)	Ki	5.8000	0.0008	1.0927	6.0000	AID662859
Amine oxidase [flavin-containing] A	Rattus norvegicus (Norway rat)	Ki	32.6000	0.0019	0.5533	4.8000	AID662856
Amine oxidase [flavin-containing] A	Homo sapiens (human)	Ki	27.6000	0.0019	2.3797	10.0000	AID662857
Peroxisome proliferator-activated receptor alpha	Mus musculus (house mouse)	IC50 (µMol)	0.0800	0.0800	0.6150	1.1500	AID1546897
Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)	IC50 (µMol)	100.0000	0.1600	2.0300	3.9000	AID1207590
Thromboxane-A synthase	Homo sapiens (human)	IC50 (µMol)	3.5600	0.0009	1.2304	10.0000	AID625229
Amine oxidase [flavin-containing] B	Homo sapiens (human)	IC50 (µMol)	0.8320	0.0000	1.8914	9.5700	AID1917380; AID501302
Amine oxidase [flavin-containing] B	Homo sapiens (human)	Ki	4.2000	0.0006	1.7771	10.0000	AID662861
Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)	IC50 (µMol)	0.7109	0.0050	1.2051	10.0000	AID1204673; AID1272055; AID1285649; AID1336347; AID1339407; AID1419241; AID1466739; AID1488557; AID1499709; AID156377; AID1566178; AID156953; AID156955; AID156959; AID157294; AID1700087; AID1700088; AID1827895; AID1827920; AID223558; AID241843; AID242199; AID242406; AID242602; AID255009; AID256775; AID260320; AID270627; AID276054; AID276984; AID277004; AID304332; AID305542; AID306520; AID316707; AID354041; AID372041; AID382299; AID421047; AID422622; AID453564; AID476068; AID548200; AID733513; AID751861; AID752224; AID775854
Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)	Ki	0.0924	0.0000	0.3790	5.6000	AID1204673; AID1566178; AID157099; AID157107; AID157268; AID157275; AID1708004; AID1802948; AID238857; AID254528; AID276586; AID276710; AID314545; AID357423; AID712390; AID733513; AID751861
C-C chemokine receptor type 2	Homo sapiens (human)	Ki	32.6000	0.0020	0.8427	6.3096	AID662856
Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)	IC50 (µMol)	10.0000	1.0500	1.0500	1.0500	AID1207592
Mu-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0380	0.0002	0.6603	10.0000	AID1272055
Peroxisome proliferator-activated receptor delta	Homo sapiens (human)	IC50 (µMol)	32.0010	0.0010	0.8505	6.3100	AID156629; AID156630; AID156791; AID157292; AID304333
Peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Ki	33.3000	0.0000	0.5141	3.1623	AID156777
Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)	IC50 (µMol)	26.3892	0.0005	0.8269	6.3100	AID156152; AID156280; AID156281; AID156285; AID157290; AID223553; AID241842; AID242198; AID242373; AID260319; AID276983; AID277008; AID304331; AID316706; AID354040; AID372042; AID421048; AID422623
Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)	Ki	33.3000	0.0001	1.0189	4.5000	AID156295
ATP-binding cassette sub-family C member 8	Homo sapiens (human)	IC50 (µMol)	0.0480	0.0043	1.0703	8.2000	AID223558
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	29.5000	0.0009	1.9014	10.0000	AID1532824
ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)	IC50 (µMol)	0.0480	0.0043	1.3686	8.2000	AID223558
Sodium/bile acid cotransporter	Homo sapiens (human)	IC50 (µMol)	5.1000	1.0000	5.9267	9.6000	AID1600822
CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)	IC50 (µMol)	2.2900	2.2900	3.5450	4.8000	AID1572805
CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)	IC50 (µMol)	0.7310	0.7310	3.7994	9.0780	AID1323834
CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)	Ki	0.0310	0.0310	1.2054	7.2910	AID1323835
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Free fatty acid receptor 1	Homo sapiens (human)	EC50 (µMol)	11.4815	0.0003	0.7369	8.8000	AID1172631
Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	1.2737	2.8000	AID156799
Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	0.5105	1.0000	AID156799
Muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0760	0.0000	1.2626	10.0000	AID141913
Muscarinic acetylcholine receptor M3	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0760	0.0000	0.7646	10.0000	AID141913
Muscarinic acetylcholine receptor M4	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0760	0.0000	0.9905	10.0000	AID141913
Cytochrome P450 3A4	Homo sapiens (human)	EC50 (µMol)	0.0110	0.0001	0.2328	3.2000	AID666690
Muscarinic acetylcholine receptor M5	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0760	0.0000	1.0528	10.0000	AID141913
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0760	0.0000	1.1605	10.0000	AID141913
Cytochrome P450 2C9	Homo sapiens (human)	EC50 (µMol)	0.0110	0.0008	0.4170	2.3000	AID666690
Cytochrome P450 3A5	Homo sapiens (human)	EC50 (µMol)	0.0110	0.0110	0.0110	0.0110	AID666690
Catechol O-methyltransferase	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.2200	0.2200	0.2200	0.2200	AID256776
Peroxisome proliferator-activated receptor alpha	Mus musculus (house mouse)	EC50 (µMol)	3.0000	0.0002	1.3971	10.0000	AID421051
Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0210	0.0030	1.2903	8.3000	AID156799
Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)	EC50 (µMol)	70.3876	0.0000	0.9922	10.0000	AID1168705; AID1172119; AID1174867; AID1191335; AID1239207; AID1323522; AID1362843; AID1362964; AID1377503; AID1395948; AID1400346; AID1419242; AID1422537; AID1422550; AID1440537; AID1466737; AID1467409; AID1468737; AID1468738; AID1468739; AID1468740; AID1468741; AID1468742; AID1468745; AID1494541; AID1507887; AID1543219; AID1547182; AID1561662; AID1561663; AID156362; AID156788; AID156799; AID156931; AID156933; AID156934; AID156939; AID156941; AID156943; AID157124; AID157264; AID157293; AID1610432; AID1614971; AID1630673; AID1633575; AID1700072; AID1700089; AID1700090; AID1716437; AID1753552; AID1773584; AID1810339; AID1819935; AID1822057; AID1827896; AID1831359; AID1874139; AID1874147; AID1899747; AID1901244; AID1901641; AID1905822; AID223547; AID223555; AID240111; AID240232; AID240253; AID240268; AID240313; AID246567; AID246650; AID254642; AID255669; AID256776; AID260323; AID268111; AID268279; AID270628; AID273357; AID276590; AID276713; AID276984; AID277005; AID289933; AID299412; AID299623; AID304335; AID305545; AID306521; AID307132; AID308432; AID308927; AID311962; AID311963; AID316709; AID354043; AID357422; AID357425; AID365529; AID372044; AID382295; AID387492; AID391553; AID396054; AID413007; AID414708; AID417012; AID421049; AID431045; AID439369; AID440654; AID453567; AID465711; AID465712; AID475399; AID476882; AID484773; AID491669; AID551966; AID554248; AID569827; AID597761; AID599163; AID600729; AID610311; AID614594; AID635239; AID637345; AID642732; AID643835; AID643837; AID643839; AID643841; AID666690; AID675850; AID675851; AID675852; AID708121; AID712383; AID717961; AID722392; AID731518; AID733512; AID736343; AID744324; AID91246
Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)	Kd	1.2101	0.0012	0.9531	4.9800	AID1440532; AID1700083; AID1874137; AID277015; AID357434; AID712389; AID731519
Peroxisome proliferator-activated receptor gamma	Mus musculus (house mouse)	EC50 (µMol)	0.0553	0.0003	1.6542	10.0000	AID1180479; AID141913; AID157283
Cannabinoid receptor 2	Mus musculus (house mouse)	EC50 (µMol)	0.0330	0.0073	0.1546	0.7040	AID391553
Peroxisome proliferator-activated receptor delta	Homo sapiens (human)	EC50 (µMol)	6.1110	0.0002	0.8460	9.1000	AID1172119; AID156234; AID156612; AID157291; AID1810338; AID414709; AID417011; AID551967; AID597762; AID635240
Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	0.3585	1.0000	AID156799
Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)	EC50 (µMol)	6.7768	0.0006	1.6074	10.0000	AID1172119; AID1275405; AID1507885; AID156133; AID156143; AID156146; AID156218; AID157289; AID1810337; AID223541; AID240110; AID240119; AID240121; AID240252; AID255668; AID276587; AID276591; AID276714; AID280956; AID299410; AID299621; AID307130; AID308431; AID314546; AID314548; AID316708; AID344821; AID354042; AID382297; AID387491; AID391555; AID414707; AID417010; AID421050; AID453571; AID465709; AID475398; AID551965; AID597760; AID635238
Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	0.3242	1.0000	AID156799
Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	0.5170	1.0000	AID156799
Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	1.2403	2.7000	AID156799
Thrombin	Oryctolagus cuniculus (rabbit)	EC50 (µMol)	0.0110	0.0110	0.0110	0.0110	AID666690
Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)	EC50 (µMol)	0.0210	0.0210	0.5105	1.0000	AID156799
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)	Activity	0.1550	0.1200	2.0087	5.5000	AID156792; AID161302
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Free fatty acid receptor 1	Homo sapiens (human)
insulin secretion	Free fatty acid receptor 1	Homo sapiens (human)
negative regulation of interleukin-1 beta production	Free fatty acid receptor 1	Homo sapiens (human)
glucose homeostasis	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of calcium ion transport	Free fatty acid receptor 1	Homo sapiens (human)
response to fatty acid	Free fatty acid receptor 1	Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
ligand-gated ion channel signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
positive regulation of insulin secretion	Free fatty acid receptor 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Free fatty acid receptor 1	Homo sapiens (human)
startle response	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
brain development	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
adult locomotory behavior	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
calcium-mediated signaling	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of synaptic plasticity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of neuronal synaptic plasticity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of sensory perception of pain	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
calcium ion transmembrane import into cytosol	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
excitatory chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
regulation of monoatomic cation transmembrane transport	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
cellular response to L-glutamate	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
positive regulation of excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
excitatory postsynaptic potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
long-term synaptic potentiation	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
ionotropic glutamate receptor signaling pathway	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
protein insertion into membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of calcium ion transport	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
calcium ion transmembrane transport	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
modulation of chemical synaptic transmission	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
synaptic transmission, glutamatergic	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
morphogenesis of an epithelium	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of cellular pH reduction	Carbonic anhydrase 2	Homo sapiens (human)
angiotensin-activated signaling pathway	Carbonic anhydrase 2	Homo sapiens (human)
regulation of monoatomic anion transport	Carbonic anhydrase 2	Homo sapiens (human)
secretion	Carbonic anhydrase 2	Homo sapiens (human)
regulation of intracellular pH	Carbonic anhydrase 2	Homo sapiens (human)
neuron cellular homeostasis	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of dipeptide transmembrane transport	Carbonic anhydrase 2	Homo sapiens (human)
regulation of chloride transport	Carbonic anhydrase 2	Homo sapiens (human)
carbon dioxide transport	Carbonic anhydrase 2	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 2	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle G2/M phase transition	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
ER overload response	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
in utero embryonic development	Cellular tumor antigen p53	Homo sapiens (human)
somitogenesis	Cellular tumor antigen p53	Homo sapiens (human)
release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
T cell proliferation involved in immune response	Cellular tumor antigen p53	Homo sapiens (human)
B cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
T cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
response to ischemia	Cellular tumor antigen p53	Homo sapiens (human)
nucleotide-excision repair	Cellular tumor antigen p53	Homo sapiens (human)
double-strand break repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
protein import into nucleus	Cellular tumor antigen p53	Homo sapiens (human)
autophagy	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
Ras protein signal transduction	Cellular tumor antigen p53	Homo sapiens (human)
gastrulation	Cellular tumor antigen p53	Homo sapiens (human)
neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
protein localization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA replication	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
determination of adult lifespan	Cellular tumor antigen p53	Homo sapiens (human)
mRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
rRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
response to salt stress	Cellular tumor antigen p53	Homo sapiens (human)
response to inorganic substance	Cellular tumor antigen p53	Homo sapiens (human)
response to X-ray	Cellular tumor antigen p53	Homo sapiens (human)
response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of gene expression	Cellular tumor antigen p53	Homo sapiens (human)
cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
viral process	Cellular tumor antigen p53	Homo sapiens (human)
glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
cerebellum development	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell growth	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
mitotic G1 DNA damage checkpoint signaling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of telomere maintenance via telomerase	Cellular tumor antigen p53	Homo sapiens (human)
T cell differentiation in thymus	Cellular tumor antigen p53	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
regulation of tissue remodeling	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV	Cellular tumor antigen p53	Homo sapiens (human)
multicellular organism growth	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of mitochondrial membrane permeability	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
entrainment of circadian clock by photoperiod	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial DNA repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
transcription initiation-coupled chromatin remodeling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of proteolysis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
response to antibiotic	Cellular tumor antigen p53	Homo sapiens (human)
fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
circadian behavior	Cellular tumor antigen p53	Homo sapiens (human)
bone marrow development	Cellular tumor antigen p53	Homo sapiens (human)
embryonic organ development	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Cellular tumor antigen p53	Homo sapiens (human)
protein stabilization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of helicase activity	Cellular tumor antigen p53	Homo sapiens (human)
protein tetramerization	Cellular tumor antigen p53	Homo sapiens (human)
chromosome organization	Cellular tumor antigen p53	Homo sapiens (human)
neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic stem cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
type II interferon-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
cardiac septum morphogenesis	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of programmed necrotic cell death	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress	Cellular tumor antigen p53	Homo sapiens (human)
thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
necroptotic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to xenobiotic stimulus	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to ionizing radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV-C	Cellular tumor antigen p53	Homo sapiens (human)
stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to actinomycin D	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
replicative senescence	Cellular tumor antigen p53	Homo sapiens (human)
oxidative stress-induced premature senescence	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
oligodendrocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of G1 to G0 transition	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of miRNA processing	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of pentose-phosphate shunt	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
regulation of fibroblast apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
positive regulation of JUN kinase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein dephosphorylation	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
insulin receptor signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
regulation of signal transduction	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of signal transduction	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
actin cytoskeleton organization	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
regulation of endocytosis	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of vascular endothelial growth factor receptor signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
endoplasmic reticulum unfolded protein response	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
regulation of intracellular protein transport	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cellular response to unfolded protein	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
peptidyl-tyrosine dephosphorylation	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
IRE1-mediated unfolded protein response	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
insulin receptor recycling	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of MAP kinase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of insulin receptor signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
regulation of type I interferon-mediated signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STAT	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
positive regulation of protein tyrosine kinase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascade	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
regulation of hepatocyte growth factor receptor signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathway	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
positive regulation of IRE1-mediated unfolded protein response	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
negative regulation of PERK-mediated unfolded protein response	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
peptidyl-tyrosine dephosphorylation involved in inactivation of protein kinase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
positive regulation of receptor catabolic process	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A5	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A5	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A5	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A5	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A5	Homo sapiens (human)
biogenic amine metabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
positive regulation of signal transduction	Amine oxidase [flavin-containing] A	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] A	Homo sapiens (human)
long-chain fatty acid metabolic process	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
in utero embryonic development	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
fatty acid beta-oxidation	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
carnitine shuttle	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
carnitine metabolic process	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
prostaglandin biosynthetic process	Thromboxane-A synthase	Homo sapiens (human)
icosanoid metabolic process	Thromboxane-A synthase	Homo sapiens (human)
cyclooxygenase pathway	Thromboxane-A synthase	Homo sapiens (human)
intracellular chloride ion homeostasis	Thromboxane-A synthase	Homo sapiens (human)
response to ethanol	Thromboxane-A synthase	Homo sapiens (human)
positive regulation of vasoconstriction	Thromboxane-A synthase	Homo sapiens (human)
response to fatty acid	Thromboxane-A synthase	Homo sapiens (human)
response to xenobiotic stimulus	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to toxic substance	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to aluminum ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to selenium ion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
negative regulation of serotonin secretion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
phenylethylamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
substantia nigra development	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to lipopolysaccharide	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dopamine catabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to ethanol	Amine oxidase [flavin-containing] B	Homo sapiens (human)
positive regulation of dopamine metabolic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Amine oxidase [flavin-containing] B	Homo sapiens (human)
response to corticosterone	Amine oxidase [flavin-containing] B	Homo sapiens (human)
negative regulation of gene expression	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of cholesterol efflux	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
long-chain fatty acid transport	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of osteoblast differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of smooth muscle cell proliferation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of receptor signaling pathway via STAT	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of low-density lipoprotein receptor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of signaling receptor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of gene expression	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of BMP signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of MAP kinase activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of adiponectin secretion	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of miRNA transcription	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stress	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of connective tissue replacement involved in inflammatory response wound healing	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
placenta development	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
lipid metabolic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
signal transduction	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
response to nutrient	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
regulation of blood pressure	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of gene expression	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of gene expression	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
macrophage derived foam cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of cholesterol storage	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of lipid storage	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of sequestering of triglyceride	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of angiogenesis	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
monocyte differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
BMP signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
epithelial cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cellular response to insulin stimulus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
response to lipid	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
peroxisome proliferator activated receptor signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
glucose homeostasis	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
regulation of circadian rhythm	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
mRNA transcription by RNA polymerase II	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
lipoprotein transport	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of blood vessel endothelial cell migration	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
innate immune response	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cell fate commitment	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of fat cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of DNA-templated transcription	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of DNA-templated transcription	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
retinoic acid receptor signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cell maturation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
rhythmic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
white fat cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
lipid homeostasis	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of type II interferon-mediated signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of SMAD protein signal transduction	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
regulation of cholesterol transporter activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cellular response to hypoxia	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of mitochondrial fission	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
regulation of cellular response to insulin stimulus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of extracellular matrix assembly	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of miRNA transcription	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of miRNA transcription	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of cellular response to transforming growth factor beta stimulus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of adipose tissue development	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell apoptotic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of vascular endothelial cell proliferation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
positive regulation of fatty acid metabolic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
fatty acid metabolic process	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
negative regulation of inflammatory response	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cell differentiation	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
hormone-mediated signaling pathway	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cytokine-mediated signaling pathway	C-C chemokine receptor type 2	Homo sapiens (human)
blood vessel remodeling	C-C chemokine receptor type 2	Homo sapiens (human)
dendritic cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
monocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of T cell cytokine production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T-helper 1 type immune response	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of type 2 immune response	C-C chemokine receptor type 2	Homo sapiens (human)
intracellular calcium ion homeostasis	C-C chemokine receptor type 2	Homo sapiens (human)
chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
humoral immune response	C-C chemokine receptor type 2	Homo sapiens (human)
cellular defense response	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of adenylate cyclase activity	C-C chemokine receptor type 2	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	C-C chemokine receptor type 2	Homo sapiens (human)
response to wounding	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of vascular endothelial growth factor production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of angiogenesis	C-C chemokine receptor type 2	Homo sapiens (human)
sensory perception of pain	C-C chemokine receptor type 2	Homo sapiens (human)
cellular homeostasis	C-C chemokine receptor type 2	Homo sapiens (human)
hemopoiesis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of type II interferon production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of interleukin-2 production	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of tumor necrosis factor production	C-C chemokine receptor type 2	Homo sapiens (human)
monocyte extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
T-helper 17 cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
negative regulation of eosinophil degranulation	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of T cell differentiation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of alpha-beta T cell proliferation	C-C chemokine receptor type 2	Homo sapiens (human)
homeostasis of number of cells within a tissue	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of T cell activation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	C-C chemokine receptor type 2	Homo sapiens (human)
leukocyte adhesion to vascular endothelial cell	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine-mediated signaling pathway	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of monocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of immune complex clearance by monocytes and macrophages	C-C chemokine receptor type 2	Homo sapiens (human)
inflammatory response to wounding	C-C chemokine receptor type 2	Homo sapiens (human)
neutrophil clearance	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of leukocyte tethering or rolling	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of NMDA glutamate receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
macrophage migration	C-C chemokine receptor type 2	Homo sapiens (human)
regulation of macrophage migration	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of thymocyte migration	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of monocyte extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of CD8-positive, alpha-beta T cell extravasation	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of astrocyte chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of hematopoietic stem cell migration	C-C chemokine receptor type 2	Homo sapiens (human)
cell chemotaxis	C-C chemokine receptor type 2	Homo sapiens (human)
calcium-mediated signaling	C-C chemokine receptor type 2	Homo sapiens (human)
inflammatory response	C-C chemokine receptor type 2	Homo sapiens (human)
immune response	C-C chemokine receptor type 2	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	C-C chemokine receptor type 2	Homo sapiens (human)
response to hypoxia	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
long-chain fatty acid metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
glucose metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
fatty acid beta-oxidation	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
triglyceride metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
carnitine shuttle	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to nutrient	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to xenobiotic stimulus	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
carnitine metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
regulation of lipid storage	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to organic cyclic compound	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
epithelial cell differentiation	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
positive regulation of fatty acid beta-oxidation	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
eating behavior	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to alkaloid	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
positive regulation of innate immune response	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to ethanol	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
aflatoxin metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
regulation of insulin secretion	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
cellular response to fatty acid	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
liver regeneration	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
response to tetrachloromethane	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
fatty acid metabolic process	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
glucose metabolic process	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
generation of precursor metabolites and energy	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
lipid metabolic process	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
fatty acid beta-oxidation	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
apoptotic process	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
embryo implantation	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
cholesterol metabolic process	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
cell population proliferation	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
axon ensheathment	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
fatty acid catabolic process	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
positive regulation of gene expression	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
regulation of skeletal muscle satellite cell proliferation	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
fatty acid transport	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
intracellular receptor signaling pathway	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
cell-substrate adhesion	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
cellular response to nutrient levels	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
wound healing	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)

Process	via Protein(s)	Taxonomy
G protein-coupled receptor activity	Free fatty acid receptor 1	Homo sapiens (human)
lipid binding	Free fatty acid receptor 1	Homo sapiens (human)
bioactive lipid receptor activity	Free fatty acid receptor 1	Homo sapiens (human)
glutamate-gated receptor activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
voltage-gated monoatomic cation channel activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
monoatomic cation channel activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
neurotransmitter receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
arylesterase activity	Carbonic anhydrase 2	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
protein binding	Carbonic anhydrase 2	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 2	Homo sapiens (human)
cyanamide hydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
transcription cis-regulatory region binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
core promoter sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
TFIID-class transcription factor complex binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
protease binding	Cellular tumor antigen p53	Homo sapiens (human)
p53 binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity	Cellular tumor antigen p53	Homo sapiens (human)
mRNA 3'-UTR binding	Cellular tumor antigen p53	Homo sapiens (human)
copper ion binding	Cellular tumor antigen p53	Homo sapiens (human)
protein binding	Cellular tumor antigen p53	Homo sapiens (human)
zinc ion binding	Cellular tumor antigen p53	Homo sapiens (human)
enzyme binding	Cellular tumor antigen p53	Homo sapiens (human)
receptor tyrosine kinase binding	Cellular tumor antigen p53	Homo sapiens (human)
ubiquitin protein ligase binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase regulator activity	Cellular tumor antigen p53	Homo sapiens (human)
ATP-dependent DNA/DNA annealing activity	Cellular tumor antigen p53	Homo sapiens (human)
identical protein binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase binding	Cellular tumor antigen p53	Homo sapiens (human)
protein heterodimerization activity	Cellular tumor antigen p53	Homo sapiens (human)
protein-folding chaperone binding	Cellular tumor antigen p53	Homo sapiens (human)
protein phosphatase 2A binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Cellular tumor antigen p53	Homo sapiens (human)
14-3-3 protein binding	Cellular tumor antigen p53	Homo sapiens (human)
MDM2/MDM4 family protein binding	Cellular tumor antigen p53	Homo sapiens (human)
disordered domain specific binding	Cellular tumor antigen p53	Homo sapiens (human)
general transcription initiation factor binding	Cellular tumor antigen p53	Homo sapiens (human)
molecular function activator activity	Cellular tumor antigen p53	Homo sapiens (human)
promoter-specific chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
RNA binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein tyrosine phosphatase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
insulin receptor binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
zinc ion binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
enzyme binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein kinase binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
receptor tyrosine kinase binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cadherin binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
ephrin receptor binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein phosphatase 2A binding	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
non-membrane spanning protein tyrosine phosphatase activity	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A5	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A5	Homo sapiens (human)
protein binding	Cytochrome P450 3A5	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A5	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A5	Homo sapiens (human)
heme binding	Cytochrome P450 3A5	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A5	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A5	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] A	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] A	Homo sapiens (human)
carnitine O-palmitoyltransferase activity	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
protein binding	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
carnitine O-octanoyltransferase activity	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
acyltransferase activity	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
monooxygenase activity	Thromboxane-A synthase	Homo sapiens (human)
thromboxane-A synthase activity	Thromboxane-A synthase	Homo sapiens (human)
iron ion binding	Thromboxane-A synthase	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen	Thromboxane-A synthase	Homo sapiens (human)
heme binding	Thromboxane-A synthase	Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activity	Thromboxane-A synthase	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Thromboxane-A synthase	Homo sapiens (human)
protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
primary amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
electron transfer activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
identical protein binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
aliphatic amine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
monoamine oxidase activity	Amine oxidase [flavin-containing] B	Homo sapiens (human)
flavin adenine dinucleotide binding	Amine oxidase [flavin-containing] B	Homo sapiens (human)
transcription cis-regulatory region binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
transcription coregulator binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nucleic acid binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
chromatin binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
double-stranded DNA binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA-binding transcription factor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nuclear receptor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
prostaglandin receptor activity	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
protein binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
zinc ion binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
enzyme binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
peptide binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
identical protein binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
sequence-specific DNA binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nuclear retinoid X receptor binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
arachidonic acid binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA binding domain binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
LBD domain binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
alpha-actinin binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
R-SMAD binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
E-box binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
STAT family protein binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA-binding transcription factor binding	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
chemokine receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
protein binding	C-C chemokine receptor type 2	Homo sapiens (human)
CCR2 chemokine receptor binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 2 binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 12 binding	C-C chemokine receptor type 2	Homo sapiens (human)
chemokine (C-C motif) ligand 7 binding	C-C chemokine receptor type 2	Homo sapiens (human)
identical protein binding	C-C chemokine receptor type 2	Homo sapiens (human)
C-C chemokine binding	C-C chemokine receptor type 2	Homo sapiens (human)
C-C chemokine receptor activity	C-C chemokine receptor type 2	Homo sapiens (human)
carnitine O-palmitoyltransferase activity	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
protein-macromolecule adaptor activity	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
identical protein binding	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
palmitoleoyltransferase activity	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
transcription coactivator binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
DNA binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
DNA-binding transcription factor activity	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
nuclear steroid receptor activity	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
nuclear receptor activity	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
protein binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
zinc ion binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
lipid binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
linoleic acid binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
DNA-binding transcription factor binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calcium ion binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
calmodulin binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
protein-containing complex binding	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
signaling receptor activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
ligand-gated monoatomic ion channel activity	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription activator activity	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
transcription coactivator binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription factor activity	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
nuclear steroid receptor activity	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
nuclear receptor activity	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
protein binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
zinc ion binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
lipid binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
phosphatase binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
protein domain specific binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
mitogen-activated protein kinase kinase kinase binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
ubiquitin conjugating enzyme binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
sequence-specific DNA binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
protein-containing complex binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
NFAT protein binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
MDM2/MDM4 family protein binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
DNA-binding transcription factor binding	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
ATP-activated inward rectifier potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
sulfonylurea receptor activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP-activated inward rectifier potassium channel activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ADP binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
transmembrane transporter binding	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
zinc ion binding	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
amyloid-beta binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
zinc ion binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glutamate binding	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
voltage-gated potassium channel activity	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
protein binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
ATP binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
ATP-activated inward rectifier potassium channel activity	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
ATPase-coupled monoatomic cation transmembrane transporter activity	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
ankyrin binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
potassium ion binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
heat shock protein binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
transmembrane transporter binding	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
glutamate-gated calcium ion channel activity	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
virus receptor activity	Sodium/bile acid cotransporter	Homo sapiens (human)
protein binding	Sodium/bile acid cotransporter	Homo sapiens (human)
bile acid:sodium symporter activity	Sodium/bile acid cotransporter	Homo sapiens (human)
RNA binding	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
protein binding	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
protein homodimerization activity	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
metal ion binding	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
2 iron, 2 sulfur cluster binding	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
NMDA glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
calcium channel activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
protein binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glycine binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
identical protein binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
protein phosphatase 2A binding	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glutamate receptor activity	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
pyridoxal phosphate binding	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
identical protein binding	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
protein homodimerization activity	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
metal ion binding	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
L-cysteine transaminase activity	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
2 iron, 2 sulfur cluster binding	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Free fatty acid receptor 1	Homo sapiens (human)
plasma membrane	Free fatty acid receptor 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
presynaptic active zone membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
hippocampal mossy fiber to CA3 synapse	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
neuronal cell body	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
cytosol	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
myelin sheath	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
extracellular exosome	Carbonic anhydrase 2	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
nuclear body	Cellular tumor antigen p53	Homo sapiens (human)
nucleus	Cellular tumor antigen p53	Homo sapiens (human)
nucleoplasm	Cellular tumor antigen p53	Homo sapiens (human)
replication fork	Cellular tumor antigen p53	Homo sapiens (human)
nucleolus	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrion	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial matrix	Cellular tumor antigen p53	Homo sapiens (human)
endoplasmic reticulum	Cellular tumor antigen p53	Homo sapiens (human)
centrosome	Cellular tumor antigen p53	Homo sapiens (human)
cytosol	Cellular tumor antigen p53	Homo sapiens (human)
nuclear matrix	Cellular tumor antigen p53	Homo sapiens (human)
PML body	Cellular tumor antigen p53	Homo sapiens (human)
transcription repressor complex	Cellular tumor antigen p53	Homo sapiens (human)
site of double-strand break	Cellular tumor antigen p53	Homo sapiens (human)
germ cell nucleus	Cellular tumor antigen p53	Homo sapiens (human)
chromatin	Cellular tumor antigen p53	Homo sapiens (human)
transcription regulator complex	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cytoplasm	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
mitochondrial matrix	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
early endosome	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
endoplasmic reticulum	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cytosol	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
mitochondrial crista	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
endosome lumen	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
sorting endosome	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cytoplasmic side of endoplasmic reticulum membrane	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
protein-containing complex	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
endoplasmic reticulum	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
cytoplasm	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
early endosome	Tyrosine-protein phosphatase non-receptor type 1	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Cytochrome P450 3A5	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A5	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] A	Homo sapiens (human)
cytosol	Amine oxidase [flavin-containing] A	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] A	Homo sapiens (human)
nucleoplasm	Peroxisome proliferator-activated receptor alpha	Mus musculus (house mouse)
nucleoplasm	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
nucleolus	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
mitochondrion	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
mitochondrion	Carnitine O-palmitoyltransferase 2, mitochondrial	Homo sapiens (human)
endoplasmic reticulum	Thromboxane-A synthase	Homo sapiens (human)
endoplasmic reticulum membrane	Thromboxane-A synthase	Homo sapiens (human)
cytosol	Thromboxane-A synthase	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial envelope	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrial outer membrane	Amine oxidase [flavin-containing] B	Homo sapiens (human)
dendrite	Amine oxidase [flavin-containing] B	Homo sapiens (human)
neuronal cell body	Amine oxidase [flavin-containing] B	Homo sapiens (human)
mitochondrion	Amine oxidase [flavin-containing] B	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
nucleus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nucleus	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nucleoplasm	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
cytosol	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
intracellular membrane-bounded organelle	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
RNA polymerase II transcription regulator complex	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
chromatin	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
receptor complex	Peroxisome proliferator-activated receptor gamma	Homo sapiens (human)
nucleoplasm	Peroxisome proliferator-activated receptor gamma	Mus musculus (house mouse)
fibrillar center	C-C chemokine receptor type 2	Homo sapiens (human)
cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
cytosol	C-C chemokine receptor type 2	Homo sapiens (human)
plasma membrane	C-C chemokine receptor type 2	Homo sapiens (human)
membrane	C-C chemokine receptor type 2	Homo sapiens (human)
dendrite	C-C chemokine receptor type 2	Homo sapiens (human)
neuronal cell body	C-C chemokine receptor type 2	Homo sapiens (human)
perikaryon	C-C chemokine receptor type 2	Homo sapiens (human)
perinuclear region of cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
cytoplasm	C-C chemokine receptor type 2	Homo sapiens (human)
external side of plasma membrane	C-C chemokine receptor type 2	Homo sapiens (human)
mitochondrion	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
mitochondrial outer membrane	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
membrane	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
mitochondrion	Carnitine O-palmitoyltransferase 1, liver isoform	Homo sapiens (human)
plasma membrane	Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)
plasma membrane	Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)
nucleus	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
nucleus	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
nucleoplasm	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
chromatin	Peroxisome proliferator-activated receptor delta	Homo sapiens (human)
cytoplasm	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic vesicle	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
dendrite	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic cleft	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
terminal bouton	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
dendritic spine	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
excitatory synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)
nucleus	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
nucleoplasm	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
chromatin	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
nucleus	Peroxisome proliferator-activated receptor alpha	Homo sapiens (human)
plasma membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
inward rectifying potassium channel	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
synaptic vesicle membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
sarcolemma	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
potassium ion-transporting ATPase complex	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 8	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
synaptic vesicle	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cytoplasmic vesicle membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
presynaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
dendritic spine	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)
cytoplasm	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
lysosome	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
late endosome	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
cytoskeleton	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
cell surface	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic density	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
synaptic membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)
acrosomal vesicle	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
nuclear envelope	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
endosome	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
plasma membrane	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
inward rectifying potassium channel	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
intercalated disc	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
T-tubule	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
axolemma	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
presynaptic membrane	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
neuronal cell body	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
cell body fiber	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
glutamatergic synapse	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
plasma membrane	ATP-sensitive inward rectifier potassium channel 11	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
postsynaptic membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)
plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
basolateral plasma membrane	Sodium/bile acid cotransporter	Homo sapiens (human)
mitochondrial outer membrane	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
endoplasmic reticulum	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
endoplasmic reticulum membrane	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
membrane	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
perinuclear endoplasmic reticulum	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
protein-containing complex	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
mitochondrial outer membrane	CDGSH iron-sulfur domain-containing protein 2	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
neuron projection	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
neuronal cell body	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
synapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
presynapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
glutamatergic synapse	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
NMDA selective glutamate receptor complex	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
plasma membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
postsynaptic density membrane	Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)
mitochondrion	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
mitochondrial outer membrane	CDGSH iron-sulfur domain-containing protein 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1739)

Assay ID	Title	Year	Journal	Article
AID290104	Effect on TAase activity assessed as activation of liver microsomal NADPH cytochrome P450 at 5 uM	2007	European journal of medicinal chemistry, Apr, Volume: 42, Issue:4	Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: protein transacetylase.
AID393122	Inhibition of rat liver microsomal CRTAase catalyzed activation of NADPH cytochrome C reductase	2009	Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4	Specificities of calreticulin transacetylase to acetoxy derivatives of 3-alkyl-4-methylcoumarins: effect on the activation of nitric oxide synthase.
AID195383	Effect of compound on AFB1-induced micronuclei formation in rat bone marrow cells in the presence of AFB1 (Activity: Micronucleated cells/1000 cells)	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID195382	Effect of compound on AFB1-induced micronuclei formation in rat bone marrow cells (Activity: Micronucleated cells/1000 cells)	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID195226	Influence (2 uM) on transacetylase catalyzed time dependent activation of NADPH cytochrome C reductase at pre-incubation time being 20 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID290103	Effect on TAase activity assessed as inhibition of GST in liver microsome at 50 uM	2007	European journal of medicinal chemistry, Apr, Volume: 42, Issue:4	Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: protein transacetylase.
AID33223	The compound was evaluated for in Vitro binding of AFB1 to DNA in rat liver microsomes; Pre-incubation time being 30 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID33222	The compound was evaluated for in Vitro binding of AFB1 to DNA in rat liver microsomes; Pre-incubation time being 20 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID393121	Inhibition of rat liver microsomal CRTAase-mediated inhibition of cytosolic glutathione S-transferase activity	2009	Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4	Specificities of calreticulin transacetylase to acetoxy derivatives of 3-alkyl-4-methylcoumarins: effect on the activation of nitric oxide synthase.
AID393123	Increase in NO levels in citreated human platelet rich plasma assessed as enhancement of dichloro fluorescein fluorescence by flow cytometry	2009	Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4	Specificities of calreticulin transacetylase to acetoxy derivatives of 3-alkyl-4-methylcoumarins: effect on the activation of nitric oxide synthase.
AID290105	Inhibition of liver microsomal EROD at 25 uM	2007	European journal of medicinal chemistry, Apr, Volume: 42, Issue:4	Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: protein transacetylase.
AID33221	The compound was evaluated for in Vitro binding of AFB1 to DNA in rat liver microsomes; Pre-incubation time being 10 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID195227	Influence (2 uM) on transacetylase catalyzed time dependent activation of NADPH cytochrome C reductase at pre-incubation time being 30 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID195228	Influence (2 uM) on transacetylase catalyzed time dependent activation of NADPH cytochrome C reductase at pre-incubation time being 5 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID290106	Inhibition of micronuclei formation in benzene-induced in Wistar Albino rat bone marrow cells at 300 mg/ kg, ip after 1 hr	2007	European journal of medicinal chemistry, Apr, Volume: 42, Issue:4	Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: protein transacetylase.
AID195225	Influence (2 uM) on transacetylase catalyzed time dependent activation of NADPH cytochrome C reductase at pre-incubation time being 10 mins	2002	Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18	Comparison of the prevention of aflatoxin b(1)-induced genotoxicity by quercetin and quercetin pentaacetate.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID270629	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARdelta by SPA	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1566178	Displacement of fluormone PPAR green tracer ligand from recombinant GST-tagged PPARgamma ligand binding domain (unknown origin) incubated for 4 hrs by competitive fluorescence polarization binding assay	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID1499895	Toxicity in Zucker rat chronic ob/ob model assessed as food intake at 10 mg/kg, po qd for 28 days measured on day 1 to 28 during compound dosing (Rvb = 170.6 +/- 3 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1474029	AUC in human at 2 to 8 mg, po QD after 24 hrs	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1532812	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation at 16 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID357422	Activation of wild type PPAR-gamma-mediated transcriptional activity assessed as luciferase reporter activity	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID1494547	Antihyperglycemic activity in established high fat diet-induced obese mouse assessed as reduction in blood glucose level at 10 mg/kg, iv administered once daily for 14 days measured at 1 hr post dose on day 7 and 14 during compound dosing in presence of g	2018	Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9	Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
AID554248	Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1	Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.
AID1063318	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 24 hrs by ELISA (Rvb = 45.1 +/- 5.6 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1532805	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation at 8 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID289949	Decrease in plasma triglyceride level in db/db mouse at 10 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID453600	Antidiabetic effect in ob/ob mouse assessed as plasma triglycerides level at 20 mg/kg/day, po for 4 days (RVb = 344 +/- 31 mg/dL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID712387	Binding affinity to N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells assessed as change in denaturation temperature at 20 uM by differential scanning calorimetry	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID240313	Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay	2004	Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17	Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID637387	Hypotriglyceridemic activity in po dosed diabetic KK-Ay mouse model assessed as decrease in triglyceride level compound administered for 14 days	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID276590	Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID396055	Agonist activity at human PPARgamma in U2OS cells by transactivation assay relative to rosiglitazone	2008	European journal of medicinal chemistry, Nov, Volume: 43, Issue:11	Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.
AID365539	Hypolipidemic activity in Zucker diabetic fa/fa rat assessed as reduction in triglyceride level at 30 mg/kg/day, po for 14 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID705749	Binding affinity to mouse cytoplasmic malate dehydrogenase by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1858187	Antiproliferative activity against human UM-UC-9 cells measured after 7 days by IncuCyte live-cell imaging analysis	2022	Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21	Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists
AID745241	Antihyperglycemic activity in rat L6 cells assessed as increase in 2-deoxy-[3H]-D-glucose uptake at 50 uM after 18 hrs by liquid scintillation counting analysis relative to control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1422535	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in intracellular Ca2+ flux after 1 hr by Fluo4-AM dye based FLIPR assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID365528	Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID123422	In vivo triglyceride correction was determined in male db/db mice after administration at 5 mg/kg	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1191354	Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID440653	Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay relative to Wy-14643	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
AID1831360	Partial agonist activity at recombinant sGSF-PPARgamma (unknown origin) assessed as CBP-1 recruitment by HT-FRET assay relative to control	2021	Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23	Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
AID1767842	Induction of adipogenesis in mouse 3T3-L1 cells at 1 uM measured after 48 hrs by oil-O-red staining based inverted microscopic analysis	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID387497	Tmax in Sprague-Dawley rat at 3 mg/kg, po	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID712382	Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay relative to WY14643	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID666819	Toxicity in Zucker diabetic fatty rat assessed as increase in body weight at 0.1 mg/kg, po qd for 12 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1349994	Agonist activity at PPARgamma in mouse RAW264.7 cells assessed as increase in protein expression level in nuclear fractions at 10 uM after 24 hrs by Western blot assay relative to control	2018	Journal of natural products, 02-23, Volume: 81, Issue:2	An Anti-Inflammatory PPAR-γ Agonist from the Jellyfish-Derived Fungus Penicillium chrysogenum J08NF-4.
AID1468751	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PGC1alpha (196 to 221 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID751861	Binding affinity to human PPARgamma receptor by radioligand displacement assay	2013	European journal of medicinal chemistry, May, Volume: 63	Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID731520	Binding affinity to human PPARdelta (unknown origin) by competitive TR-FRET assay	2013	Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4	Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
AID637430	Effect on RBC count in Sprague-Dawley rat at 50 mg/kg after 28 days (Rvb = 832 +/- 25.2 x 10 ' 4/micro L)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID387506	Antihyperglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 3 mg/kg, po once daily after 28 days relative to non-fasting control	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID637380	Hypoglycemic activity in diabetic KK-Ay mouse model assessed as decrease in glucose level at 3 mg/kg, po qd for 14 days (Rvb = 648.4 +/- 77.1 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID714673	Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in blood glucose level at 30 mg/kg/day, po measured on day 6 post dose by postprandial oral glucose tolerance test relative to control	2012	Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6	Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice.
AID237607	Percent decrease in triglyceride level of wistar rat was determined at 30 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID678716	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1700130	Effect on perilipin mRNA expression in hMADS white adipocytes at 10 to 1000 nM by RT-PCR analysis
AID444053	Renal clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID387498	Cmax in Sprague-Dawley rat at 3 mg/kg, po	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID643909	Antidiabetic activity in db/db C57BLKS/J-m +/+ Leprdb mouse assessed as reduction of glucose level at 10 mg/kg, po qd for 10 days measured on 11 relative to control	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID656887	Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of triacylglycerol level at 50 mg/kg, po after 6 weeks (Rvb = 1.56 +/- 0.17 mmol/L)	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID750243	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of HbA1c level in blood at 50 mg/kg, po administered for 6 weeks (Rvb = 2.65 +/- 0.40%)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID199342	In vitro synergistic elevation of transcriptional activation in CV-1 cells expressing RAR and RXR with 3 nm TTNBP; No activity	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID372089	Toxicity in Sprague-Dawley rat assessed as brown adipose tissue weight at 150 mg/kg dosed daily for 2 weeks	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID643922	Antidiabetic activity in obese insulin resistant Zucker fa/fa rat assessed as decrease in free fatty acids level in plasma at 1 to 100 mg/kg qd for 7 days	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID693497	Antihyperglycemic activity in db/db mouse assessed as plasma glucose reduction at 5 mg/kg administered BID for 10 days relative to control	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis of N-(5-chloro-6-(quinolin-3-yloxy)pyridin-3-yl)benzenesulfonamide derivatives as non-TZD peroxisome proliferator-activated receptor γ (PPARγ) agonist.
AID1532835	Induction of membrane translocation of biotinylated human AQP2 expressed in rat IMCD cells at 10 to 50 uM after 30 mins by Western blot analysis	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID414712	Selectivity of EC50 for human PPARdelta receptor over EC50 for human PPARalpha receptor	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
AID1503451	Activation of AMPK in palmitate-induced insulin-resistant human HepG2 cells assessed as reduction in G6Pase mRNA expression at 12.5 uM incubated for 24 hrs by real-time PCR method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID705484	Binding affinity to Huntingtin-associated protein-interacting protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID750241	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of glycated serum protein level in blood at 50 mg/kg, po administered for 6 weeks (Rvb = 1.62 +/- 0.27 mmol/l)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID666689	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay relative to 5-(4-{[6-(4-hydroxy-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol- 2-y	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID610311	Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10	Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
AID637347	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay relative to farglitazar	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID444050	Fraction unbound in human plasma	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1156984	Cytotoxicity against human MKN74 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID705494	Binding affinity to mitochondrial ATP synthase alpha chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1827926	Toxicity in ob/ob diabetic C57BL/6J (B6.V Lepob/OlaHsd) mouse model assessed as tolerance at 10 to 100 micromol/kg, po dosed daily for 7 days	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID1507887	Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID1363014	Toxicity in Wistar-Imamichi rat assessed as elevation in ALT activity at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID156791	In vitro binding affinity for human Peroxisome proliferator activated receptor gamma using scintillation proximity assay (SPA)	2004	Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12	(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
AID331079	Reduction of glucose levels in DIO C57BL/6 mouse model at 5 mg/kg, po during insulin tolerance test	2007	Nature, Nov-29, Volume: 450, Issue:7170	Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.
AID1467410	Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay relative to rosiglitazone	2017	Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14	Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID175939	In vivo plasma triglyceride in Zucker diabetic fatty rat after 11 days at 30 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID453761	Antidiabetic in ZDF rat assessed as plasma insulin level at 3 mg/kg/day, po for 2 weeks (RVb = 20 +/- 3 mg/dL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID382296	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay relative to darglitazone	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1901678	Stabilization of human PPARgamma LBD assessed as change in melting temperature at 50 uM by thermal shift assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID276712	Displacement of radiolabeled GW-2331 from human PPAR alpha at 100 uM by SPA assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID157268	Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)	1999	Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23	Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
AID252367	Free fatty acid concentration was measured in male db/db mouse after 10 mpk/day for 14 days	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID252394	Triglycerides concentration in cell lysate of mouse fibroblast cell line (3T3L-1) incubated in the presence of 1.0 uM compound	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID705491	Binding affinity to sodium-dependent multivitamin transporter in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1323522	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	2016	Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21	Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity.
AID270633	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from murine PPARalpha by SPA	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID440652	Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
AID1543230	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using freshly i
AID189944	T4 level in rats at 24 hr r after 30 mg/kg oral dose	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID252583	Brown adipose tissue weight was determined in normal sprague-dawley rats at 150 mg/kg	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID1668561	Agonist activity at PPARgamma in mouse 3T3L1 adipocytes assessed as induction of FABP4 mRNA expression at 3 uM by qRT-PCR analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID444052	Hepatic clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1716466	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as increase in adipocyte-like multilocular morphology cells at 2 uM measured upto 12 days by oil-O-red staining based inverted microscopic analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID712384	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay relative to rosiglitazone	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID1760236	Anti-diabetic activity in high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as improved pathological changes in pancreas at 5 mg/kg, po by hematoxylin and eosin staining based histopathological analysis	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1700126	Induction of adipocyte browning in hMADS white adipocytes assessed as increase in UCP1 mRNA expression at 0.03 to 1 uM by RT-PCR analysis
AID276724	Reduction of plasma triglycerides in db/db mouse at 30 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID387512	Antihyperglycemic activity in po dosed db/db mouse assessed as reduction in glucose level after 28 days	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1700099	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in FABP4 mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID1251338	Antidiabetic activity in Wistar rat assessed as reduction in blood glucose level at 36 mg/kg, po dosed 30 mins before glucose challenge and measured 30 and 60 mins post glucose challenge by OGTT method	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1362908	Toxicity in F344/DuCrlCrlj rat assessed as effect on ovary weight at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1209456	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1410786	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as induction of adipocyte differentiation at 1 uM after 15 days by Oil Red O staining-based assay	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
AID1351162	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA (Rvb = 175.2 +/- 10.2 pg/m	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1440568	Binding affinity to PPARdelta (unknown origin) assessed as kinetic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID391556	Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay relative to gemfibrozil	2008	Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20	Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID714672	Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in postprandial hyperglycemia at 30 mg/kg, po measured for 10 days post dose relative to control	2012	Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6	Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice.
AID1440536	Transactivation of GAL4-fused human PPARalpa LBD expressed in human HepG2 cells up to 2 uM after 20 hrs by luciferase reporter gene assay relative to Wy-14,643	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1901644	Agonist activity at human PPARgamma expressed in HEK293 cells assessed as maximal activity by luciferase/beta-galactosidase reporter gene assay relative to rosiglitazone	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1217704	Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1266115	Agonist activity at PPAR in human THP1 cells assessed as induction of ABCA1 expression at 20 uM after 24 hrs by Western blot analysis relative to control	2015	Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24	Identification of dual PPARα/γ agonists and their effects on lipid metabolism.
AID156955	In vitro binding affinity for human PPAR gamma in SPA	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1760174	Antidiabetic activity in KK-Ay mouse assessed as reduction in fasting blood glucose level at 5 mg/kg, po for 50 days by glucose oxidase method (Rvb = 13.2 +/- 2.06 mM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1810333	Induction of adipogenesis differentiation in human Mesenchymal stem cells at 10 uM incubated for 21 days by Alizarin Red S staining-based microscopic analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID717056	Toxicity in db/db mouse type 2 diabetic model assessed as reduction of body weight at 10 mg/kg, po administered for 14 days	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
AID733513	Displacement of [3H]-rosiglitazone from GST-tagged PPARgammaLBD (unknown origin) after 1 hr by scintillation proximity assay	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID357438	Activation of PPARgamma Q286G mutant-mediated transcriptional activity assessed as Gal4 reporter activity	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1532825	Inhibition of human ERG expressed in CHO cells at 1.25 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID344821	Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay	2008	Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21	Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
AID1773599	Antidiabetic activity in ob/ob mouse assessed as reduction in polyphagia by measuring increase in food consumption at 10 mg/kg, po administered once daily for 30 days and measured daily	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID656885	Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of triacylglycerol level at 50 mg/kg, po after 2 weeks (Rvb = 1.24 +/- 0.12 mmol/L)	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID111555	In vivo blood glucose level in male db/db mice after administration of 0.33 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1174865	Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID731795	Induction of PPAR-gamma promoter activity in LPS-stimulated mouse CMT93 cells at 10 uM preincubated for 30 mins before LPS-challenge measured after 6 hrs post challenge by luciferase reporter gene assay	2013	European journal of medicinal chemistry, Apr, Volume: 62	Peroxisome proliferator-activated receptor-γ mediates the anti-inflammatory effect of 3-hydroxy-4-pyridinecarboxylic acid derivatives: synthesis and biological evaluation.
AID1760242	Increase in glucose consumption in human HepG2 cells at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID705506	Binding affinity to mouse Fanconi anemia group M protein homologue by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1323835	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis	2016	Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21	Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID662856	Competitive inhibition of rat MAOA expressed in Pichia pastoris	2011	ACS medicinal chemistry letters, Oct-15, Volume: 3, Issue:1	Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
AID1363008	Toxicity in Wistar-Imamichi rat assessed as reduction in RBC count at 100 mg/kg, po administered via gavage once daily for 28 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID277011	Activity at human PPARalpha in CV1 cells by CTF assay relative to 2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID276723	Reduction of plasma triglycerides in db/db mouse at 3 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID678715	Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1760232	Anti-diabetic activity in high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as reduction in microalbumin level in urine at 5 mg/kg, po measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID421153	Toxicity in Sprague-Dawley rat assessed as increase in brown adipose tissue weight at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1760247	Induction of glycolysis in rat L6 cells assessed as reduction in cellular ATP production at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID157293	In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1901246	Agonist activity at pBIND tagged human PPARalpha expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
AID240110	Effective concentration against human Peroxisome proliferator activated receptor alpha	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID124440	Maximum achieved blood glucose reduction relative to vehicle treated control group	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1716438	Cytotoxicity against African green monkey COS-1 cells assessed as cell viability at EC50 concentration for PPAR activation assay by LDH assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID123656	Compound was administered at a dose of 10 mg/kg/day to evaluate the percentage reduction in plasma triglyceride (TG) after 6 days of treatment in db/db mice via oral gavage.	1999	Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14	Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones.
AID1499755	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as fasting blood glucose level at 10 mg/kg, po qd for 31 days measured on day 29 post dose (Rvb = 163 +/- 9.2 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID712381	Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID705482	Binding affinity to mouse serine/threonine-protein kinase MAK by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1597807	Induction of adipocyte differentiation in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient assessed as lipid accumulation at 2 uM measured for 12 days by Oil red O staining based microscopic analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1570218	Antidiabetic activity in db/db mouse assessed as reduction in serum glucose level at 10 to 30 mg/kg, po after 1 week relative to control	2019	European journal of medicinal chemistry, 10-15, Volume: 180	An insight into the medicinal perspective of synthetic analogs of indole: A review.
AID453571	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID156943	In vitro transactivation of human Peroxisome proliferator activated receptor gamma	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID417011	Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Selective, potent PPARgamma agonists with cyclopentenone core structure.
AID548198	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 10 uM after 24 hrs by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.
AID1204673	Agonist activity at PPARgamma ligand binding domain (unknown origin) using fluormone Pan-PPAR green tracer by TR-FRET assay based competitive ligand binding method	2015	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12	Separation and peroxisome proliferator-activated receptor-γ agonist activity evaluation of synthetic racemic bavachinin enantiomers.
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1180480	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector assessed as fold activation after 24 hrs by dual-luciferase reporter assay	2014	Journal of natural products, Jul-25, Volume: 77, Issue:7	Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.
AID1499797	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as food intake at 10 mg/kg, po qd for 29 days measured on day 1 to 29 during compound dosing (Rvb = 969 +/- 18 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1744023	Agonist activity at RXR-alpha in mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB transcription by measuring NF-kappaB level at 0.01 to 10 uM incubated for 24 hrs by SEAP dependent NF-kappaB reporter assay	2021	Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1	Discovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.
AID705487	Binding affinity to mouse bullous pemphigoid antigen 1 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID705502	Binding affinity to septin-9 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID13178	Oral bioavailability in rat (dose 2 mg/kg)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1374659	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as final glucose level in plasma at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting (Rvb = 184 +/- 30 mg/dL)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID1427946	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in free diet blood glucose level at 10 mg/kg/day administered via oral gavage once daily measured on day 3 post dose	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID453564	Displacement of [3H2]nTZD3 from GST-tagged human PPARgamma expressed in Escherichia coli by SPA	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID750251	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of triglycerides level in blood at 50 mg/kg, po administered for 6 weeks measured on 2nd week (Rvb = 1.08 +/- 0.07 mmol/l)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID237606	Percent decrease in triglyceride level of wistar rat was determined at 10 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID705507	Binding affinity to mouse neurofibromin by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID705498	Binding affinity to mouse serine/threonine-protein kinase WNK1 by chromatographic analysis relative to rosiglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID429217	Antidiabetic activity in ob/ob mouse assessed as decrease in plasma triglyceride level at 10 mg, po measured on day 14	2009	European journal of medicinal chemistry, Aug, Volume: 44, Issue:8	Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents.
AID1063320	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 6 hrs by ELISA (Rvb = 7.2 +/- 0.9 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID1896155	Antiviral activity against HBV infected HepG2 2.2.15 cells assessed as reduction in HBsAg level at 50 microg/ml for 48 hrs by ELISA	2022	Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19	Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1773607	Reduction in plasma LDL level in ob/ob mouse at 10 mg/kg, po administered once daily for 30 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1901652	Agonist activity at human PPARgamma in mouse 3T3-L1 cells assessed as induction of LpI mRNA expression at 10 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID220375	Hypoglycemic activity in db/db mouse model after 7 days at 10 mg/kg/day oral dose	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID421165	Toxicity in Sprague-Dawley rat assessed as increase bilirubin levels at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID705322	Up-regulation of adiponectin expression in mouse 3T3L1 cells at 10 uM after 24 hrs by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Synthesis and biological evaluation of 5-benzylidenepyrimidine-2,4,6(1H,3H,5H)-trione derivatives for the treatment of obesity-related nonalcoholic fatty liver disease.
AID1899748	Agonist activity at human PPARdelta measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1222793	Dissociation constant, pKa of the compound	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Which metabolites circulate?
AID1532773	Induction of adipogenesis in mouse 3T3L1 preadipocytes assessed as increase in intracellular triglyceride level at 10 uM treated every other day up to day 14 by AdipoRed staining based confocal microscopic method	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID705477	Binding affinity to mouse transcription factor SOX-5 after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID364422	Antiglycemic activity in db/db mouse assessed as glucose correction at 10 mg/kg, po administered daily for 11 days	2008	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17	Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
AID175938	In vivo plasma triglyceride in Zucker diabetic fatty rat after 11 days at 10 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID387491	Agonist activity at human PPARalpha expressed in african green monkey CV-1 by co-transfected with GAL4 by by dual-glo luciferase reporter gene assay	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1543219	Agonist activity at human PPARgamma expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity by luciferase reporter gene assay relative to rosiglitazone
AID156612	In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID1827920	Inhibition of PPARgamma (unknown origin) phosphorylation at pS273 residue	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID1785322	Reduction in body weight change in high fat diet fed C57BL/6J DIO mouse measured at 15 mg/kg, po up to 6 days	2021	Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19	Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
AID705741	Binding affinity to Kinesin light chain 1 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID156607	Transcriptional activation by human PPAR delta	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1494546	Antihyperglycemic activity in established high fat diet-induced obese mouse assessed as reduction in body weight at 10 mg/kg, iv administered once daily for 14 days	2018	Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9	Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
AID1543234	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells at 1 uM treated for 28 hrs post 48 hrs after PPARalpha siRNA transfection fo
AID1507893	Anti-diabetic activity in ob/ob mouse assessed as change in serum glucose levels at 3 mg/kg administered via oral gavage daily for 4 days measured on day 5 relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID705508	Binding affinity to SECIS-binding protein 2 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID503296	Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	2006	Nature chemical biology, Jun, Volume: 2, Issue:6	Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID1633575	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.
AID372054	Agonist activity at mouse PPARalpha	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID240253	Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assay	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
AID1362983	AUC (0 to 24 hrs) in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administeration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1532769	Toxicity in spontaneous db/db BKS.Cg-Dock7m +/+ Leprdb/J mouse assessed as body weight gain at 27 umol/kg, po administered as daily dose via gavage treated for 18 days measured post last dose (Rvb = 5.6 +/- 2.1 g)	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID223547	In vitro transactivation using receptor transactivation assay against hPPAR gamma	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID382310	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as reduction in blood free fatty acid level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1172119	Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay	2014	Journal of natural products, Dec-26, Volume: 77, Issue:12	Sterol fatty acid esters from the mushroom Hericium erinaceum and their PPAR transactivational effects.
AID444051	Total clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1440537	Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID637428	Effect on RBC count in Sprague-Dawley rat at 12.5 mg/kg after 28 days (Rvb = 832 +/- 25.2 x 10 ' 4/micro L)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID280959	Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay relative to rosiglitazone	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID12364	Dose-normalized AUC was determined by po administration (10 mg/kg) in fasted male Sprague-Dawley rats	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID156223	In vitro transcription activation on human peroxisome proliferator activated receptor-alpha (PPAR alpha)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID1351160	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by ELISA (Rvb = 24216 +/- 498.	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1597852	Agonist activity at PPARalpha in human Huh7 cells assessed as PPARA mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID270631	Transactivation of human PPARalpha in CV1 cells by luciferase reporter gene assay relative to LG070660	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID1362843	Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1760212	Anti-diabetic activity in overnight fasted diabetic KK-Ay mouse assessed as increase in insulin responsiveness by measuring blood glucose at 5 mg/kg, po measured after 35 days by insulin tolerance test	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1494539	Transactivation of recombinant human N-terminal GAL4-DBD fused PPARgamma LBD expressed in reporter cells at 30 uM measured after 24 hrs by luciferase reporter gene assay relative to control	2018	Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9	Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
AID1532766	Antidiabetic activity in spontaneous db/db BKS.Cg-Dock7m +/+ Leprdb/J mouse assessed as decrease in fasting blood glucose level at 10 mg/kg, po administered as daily dose via gavage for 18 days measured on day 9 post last dose by glucometric analysis	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1499910	Toxicity in Zucker rat chronic ob/ob model assessed as serum cholesterol level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 195 +/- 5.5 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1503444	Stimulation of glucose consumption in palmitate-induced insulin-resistant human HepG2 cells at 12.5 uM incubated for 24 hrs by glucose oxidase based assay	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID733014	Antidiabetic activity in Zucker fatty rat assessed as body weight gain at 1 mg/kg/day, po measured after 14 days relative to vehicle-treated control	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID112794	Area under blood glucose time curve after oral glucose test in mice	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1400346	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID551965	Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1	Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.
AID1474030	Drug concentration at steady state in human at 2 to 8 mg, po QD after 24 hrs	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID268279	Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay	2006	Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15	Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.
AID418686	Antidiabetic activity in po dosed type 2 diabetes mellitus patient assessed as reduction in HbA1C level in skeletal muscle	2009	Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7	Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
AID1172788	Antidiabetic activity in Wistar rat model of streptozotocin-induced diabetes assessed as reduction in plasma glucose level at 36 mg/kg, po and dosage repeated for 15 days by GOD-POD method	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID29653	Oral bioavailability in rat	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID296176	Reduction in plasma glucose level in alloxan-induced diabetic mouse at 10 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID1700092	Binding affinity to PPARg in mouse 3T3-L1 cells assessed as reduction in CDK5-mediated phosphorylation of PPARg serine 273 residue at 5uM incubated for 60 mins by immunoblot analysis
AID503313	Antiproliferative activity against human PC3 cells at 15 uM after 120 hrs by MTT assay relative to DMSO	2006	Nature chemical biology, Jun, Volume: 2, Issue:6	Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID387500	Solubility at pH 6.8	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1217710	Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID421116	Antidiabetic activity in po dosed Zucker fa/fa rat assessed as insulin lowering activity treated once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID431132	Adipogenic activity in monosodium L-glutamate-treated obese Wistar rat assessed as increase in visceral fat weight at 5 mg/kg, po after 6 weeks relative to control	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID1760224	Effect on high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as total body weight gain at 5 mg/kg, po (Rvb = 43.5 +/- 5.24 g)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1374655	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as basal glucose level in plasma at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting (Rvb = 187 +/- 24 mg/dL)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID382308	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as reduction in blood insulin level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1503552	Cytotoxicity against human SCC15 cells assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay relative to control	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).
AID1532832	Toxicity in ICR mouse assessed mouse mortality at 500 mg/kg, po administered as single dose via gavage treated on day 1 and measured daily up to 14 days	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1055971	Increase in 2-NBDG uptake in mouse 3T3L1 cells at 400 ug/ml after 30 mins by fluorescence spectrophotometry relative to DMSO-treated control	2013	Journal of natural products, Nov-22, Volume: 76, Issue:11	Protein tyrosine phosphatase 1B (PTP1B) inhibitors from Morinda citrifolia (Noni) and their insulin mimetic activity.
AID1532841	Induction of superoxide dismutase level in TNF-alpha-induced insulin resistant mouse 3T3L1 cells at 10 uM after 48 hrs	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1785800	Agonist activity at human PPARgamma at 1 uM	2021	ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11	Synthesis of 2-Prenylated Alkoxylated Benzopyrans by Horner-Wadsworth-Emmons Olefination with PPARα/γ Agonist Activity.
AID382295	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID123671	Percentage reduction in plasma glucose after 6 days p.o. dosing at 30 mg/kg in db/db mice.	1999	Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14	Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones.
AID296185	Reduction in plasma triglyceride level in alloxan-induced diabetic mouse at 5 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID705324	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Synthesis and biological evaluation of 5-benzylidenepyrimidine-2,4,6(1H,3H,5H)-trione derivatives for the treatment of obesity-related nonalcoholic fatty liver disease.
AID240121	Effective concentration for human peroxisome proliferator-activated receptor gamma	2005	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5	Structure-activity relationships of dimeric PPAR agonists.
AID1468753	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled RIP140 (922 to 946 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1532797	Toxicity in spontaneous db/db BKS.Cg-Dock7m +/+ Leprdb/J mouse assessed as reduction in serum hematocrit value at 27 umol/kg, po administered as daily dose via gavage treated for 18 days	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1440546	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as inhibition of LiCl-stimulated Wnt/beta-catenin-mediated transcription at 1 uM treated for 24 hrs measured 48 hrs post transfection by TOPflash reporter gene assay relativ	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1899746	Agonist activity at human PPARalpha measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1716483	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as upregulation of fatty acid biosynthesis genes at 2 uM incubated for 8 days by Illumina sequencing method	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID276592	Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay relative to darglitazone	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID189064	Percent reduction in triglyceride (TG) after 9 days of dosing in db/db is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 200 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID1323834	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay	2016	Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21	Identification of small molecules that bind to the mitochondrial protein mitoNEET.
AID304338	Reduction in body weight gain in orally dosed ZDF rat after 7 days	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID1901646	Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of fabp1 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1351153	Inhibition of Pseudomonas aeruginosa PAO1 GFP-fused quorum sensing rhlA at 10 uM measured every 15 mins up to 12 hrs by GFP reporter gene assay relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1466737	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
AID157291	In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1608418	Inhibition of PPARgamma (unknown origin) at 10 uM after 24 hrs relative to control	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Role of sulphur-heterocycles in medicinal chemistry: An update.
AID678717	Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1532762	Inhibition of cellular glucose output in dexamethasone-induced insulin resistant human L02 cells assessed as insulin-stimulated glucose uptake at 10 uM preincubated for 24 hrs followed by insulin stimulation measured after 24 hrs by glucose oxidase method	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID236472	Area under plasma concentration time curve when administered to Sprague Dawley rats after once daily dosing for two weeks	2005	Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10	Selective PPARgamma modulators with improved pharmacological profiles.
AID745228	Insulin resistance reversal activity in db/db mouse assessed as decrease in plasma insulin level at 30 mg/kg, po qd administered 15 days measured on day 16 by ELISA relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1810339	Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID11908	Dose-normalized AUC measured in fasted male Sprague dawely rats when the compound was administered at a peroral dose of 2 mg/Kg	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID289946	Decrease in plasma glucose level in db/db mouse at 10 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID1668559	Agonist activity at PPARgamma in mouse 3T3L1 adipocytes assessed as induction of adiponectin mRNA expression at 3 uM by qRT-PCR analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID1810340	Agonist activity at human PPARalpha transfected in COS-7 cells assessed maximum luciferase activity measured after 24 hrs by cell based luciferase transactivation assay relative to gemfibrozil	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID157107	In vitro binding affinity towards human peroxisome proliferator activated receptor gamma (PPAR gamma)	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID666815	Antidiabetic activity in po dosed Zucker diabetic fatty rat assessed as improvement in plasma lipids profiles administered qd for 12 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID372117	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in plasma volume at 150 mg/kg, po once daily for 7 days by Evans blue dye dilution technique	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID240390	Effective concentration against human PPARalpha expressed in HepG2 cells; i.a = inactive at tested concentration	2005	Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17	Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
AID276716	Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay relative to GW-2331	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID678714	Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1351156	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1543214	Agonist activity at human PPARalpha expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity at 10 uM by luciferase reporter gene assay relative to WY-14643
AID1700124	Effect on adipocyte mitochondria content in mouse 3T3-L1 cells by Mito-tracker dye based flow cytometry
AID699165	Antidiabetic activity in Charles River ZDF rat assessed by improved glucose tolerance at 30 mg/kg, po qd for 29 days measured after 15 days by OGTT	2012	Journal of medicinal chemistry, May-10, Volume: 55, Issue:9	Discovery and characterization of an inhibitor of glucosylceramide synthase.
AID252270	Percent body weight gain in db/db mice at 10 mg/kg on day 11 of dosing	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID701826	Antihyperglycemic activity in diabetic C57BL/KsJ db/db mouse model assessed as improvement in glucose tolerance in hyperglycemia at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID1488558	Agonist activity at SUR in Wistar rat pancreatic islets assessed as increase in insulin secretion at 5 to 20 uM incubated for 1 hr followed by glucose addition for 30 mins by quantitative sandwich enzyme immunoassay	2017	Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.
AID491658	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID475407	Antidiabetic activity in db/db mouse assessed as serum leptin level at 10 mg/kg, po QD after 2 weeks (Rvb= 10.55 +/- 0.60 ng/ml)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID113925	In vivo glucose correction was determined in male db/db mice after administration at 5 mg/kg	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1547182	Agonist activity at human PPARgamma expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay	2020	Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6	Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders.
AID1440547	Agonist activity at PPARgamma in human HT-29 cells harboring APC mutant assessed as inhibition of Wnt/beta-catenin signaling pathway by measuring decrease in CyclinD1 level at 10 uM treated for 24 hrs by Western blot method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1773593	Improvement in glucose tolerance in high fat diet-fed C57BL/6 diabetic mouse model assessed as glucose lowering effect at 10 mg/kg, po administered once daily for 7 days and on day 7 treated at 30 mins prior to glucose challenge and measured up to 120 min	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID643924	Antidiabetic activity in obese insulin resistant Zucker fa/fa rat assessed as decrease in triglyceride level in plasma at 1 to 100 mg/kg qd for 7 days	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1543218	Agonist activity at human PPARalpha expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity by luciferase reporter gene assay relative to WY-14643
AID1377502	Agonist activity at GAL4-fused PPARalpha LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
AID485552	Antihyperglycemic activity in C57BL/KsBom-db db/db mouse assessed as decrease in blood glucose AUC level at 100 mg/kg measured on day 10 by oral glucose tolerance test (Rvb = 32480 +/- 5098 %)	2010	Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11	Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
AID357423	Displacement of [3H]rosiglitazone from histidine-tagged PPARgamma ligand binding domain by scintillation proximity assay	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID614594	Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay	2011	Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18	SAR studies of acidic dual γ-secretase/PPARγ modulators.
AID372082	Antihyperglycemic activity in db/db mouse assessed as plasma adiponectin level at 10 mg/kg, po administered once daily for 11 days by RIA	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID690961	Antihyperglycemic activity in streptozotocin-induced type 2 diabetic Wistar albino rat assessed as reduction in plasma glucose level at 10 mg/kg, po by glucometer	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20	Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents.
AID1773620	Downregulation of ADD1 gene expression in ob/ob mouse liver at 10 mg/kg, po administered once daily for 30 days by quantitative RT-PCR analysis	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID113924	In vivo glucose correction was determined in male db/db mice after administration at 10 mg/kg	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID26204	In vivo % reduction of blood glucose area under curve after oral glucose tolerance test in male db/db mice at 1 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID372085	Toxicity in Sprague-Dawley rat assessed as heart weight at 150 mg/kg dosed daily for 2 weeks	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1767822	Hypolipidemic activity against palmitic acid-induced hyperlipidemia in human HepG2 cells assessed as increase in insulin-induced Akt thr3O8 phosphorylation at 1 uM pretreated for 24 hrs followed by insulin challenge by Western blot analysis	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID1901661	In vivo agonist activity at human GFP-tagged PPARgamma in transgenic zebrafish assessed as increase in GFP expression in tail bud at 0.1 uM measured after 14 days by microscopy	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID690238	Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control	2011	Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18	Synthesis of a new [6]-gingerol analogue and its protective effect with respect to the development of metabolic syndrome in mice fed a high-fat diet.
AID1427956	Antidiabetic activity in KK-Ay diabetic mouse model assessed as increase in insulin sensitivity index at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID242198	Inhibition of human Peroxisome proliferator activated receptor alpha binding	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
AID91238	Agonist activity for Human PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID1819960	Induction of browning in human SGBS cells assessed as increase in UQCRC2 mRNA expression by qRT-PCR analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
AID643842	Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assay relative to L-796449	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1535247	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in Glut4 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4	Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1468741	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (671 to 695 residues) co-activator recruitment by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1427965	Hypolipidemic activity in KK-Ay diabetic mouse model assessed as reduction in serum NEFA level at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID1561673	Induction of adipogenesis in NHDF assessed as reduction in fibroblast differentiation into matured adipocytes at 2 uM administered on day 3 of differentiation 1 and day 5 of differentiation 2 followed by media refreshment at 2 days interval up to 13 days	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID1172631	Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Homology modeling and explicit membrane molecular dynamics simulation to delineate the mode of binding of thiazolidinediones into FFAR1 and the mechanism of receptor activation.
AID130064	Antihyperglycemic potency dose producing approximately 25% reduction in area under glucose tolerance curve	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID1499833	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum ALT level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 151 +/- 23 U/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID91246	Agonist activity for Human PPAR gamma receptor in transcriptional activation assay	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID1499841	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum BUN level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 28.3 +/- 1.1 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID637383	Hypoglycemic activity in po dosed diabetic KK-Ay mouse model assessed as decrease in glucose level compound administered for 14 days	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID255668	In vitro effective concentration against human peroxisome proliferator activated receptor alpha/Gal4 in transactivation assay	2005	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20	Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
AID372087	Toxicity in Sprague-Dawley rat assessed as liver weight at 150 mg/kg dosed daily for 2 weeks	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1276073	Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in LPL expression at 2 uM by qPCR method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID662851	Inhibition of human histone demethylase LSD1 up to 100 uM	2011	ACS medicinal chemistry letters, Oct-15, Volume: 3, Issue:1	Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
AID242406	Mean inhibitory concentration against human peroxisome proliferator-activated receptor gamma	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID354063	Antidiabetic activity in Zucker fa/fa rat assessed as HOMA-insulin resistance index at 3 mg/kg/day	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID666690	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1339405	Antihyperglycemic activity in Swiss albino rat model of streptozotocin-induced hyperglycemia assessed as reduction in blood glucose level at 2.7 mg/kg, po measured after 3 hrs by glucometer relative to control	2017	Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of novel quinoxaline derivatives as potential PPARγ and SUR agonists.
AID1467409	Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14	Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID111559	In vivo % reduction of blood glucose level in male db/db mice after administration of 0.33 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID714674	Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction in blood glucose level at 30 mg/kg/day, po measured day 10 post dose by postprandial oral glucose tolerance test relative to control	2012	Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6	Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice.
AID11226	Plasma clearance in fasted male Sprague dawely rats on administration of 0.5 mg/Kg i.v. of the compound	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID701824	Antidyslipidemic activity in diabetic C57BL/KsJ db/db mouse model assessed as increase in plasma HDL-cholesterol level at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1532824	Inhibition of human ERG expressed in CHO cells by patch clamp assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1700136	Toxicity in rat primary hepatocytes assessed as effect on ATP cellular content up to 10 uM
AID30162	Volume of distribution during steady state in rat	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID453588	Glucose lowering effect in ob/ob mouse assessed as plasma glucose level at 20 mg/kg/day, po for 4 days (RVb = 476 +/- 27 mg/dL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID1773622	Downregulation of FAS gene expression in ob/ob mouse liver at 10 mg/kg, po administered once daily for 30 days by quantitative RT-PCR analysis	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID223553	Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha)	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID372113	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in plasma volume at 100 mg/kg, po once daily for 7 days by Evans blue dye dilution technique	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID635239	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
AID1362889	Drug uptake in F344/DuCrlCrlj rat plasma administered via oral gavage measured on day 28 post dose	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1217707	Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID421117	Toxicity in Zucker fa/fa rat assessed as increase in plasma volume at 10 mg/kg, po treated once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID156629	In vitro binding affinity against human Peroxisome proliferator activated receptor delta	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID1532764	Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1700085	Induction of PPARg-LBD/GAL4-tagged RXRa (unknown origin) heterodimerization expressed in HEK293 cells at 0.01 to 10 uM incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
AID1315287	Activation of Akt-dependent signaling pathway in rat L6 myotubes assessed as increase in myc-tagged GLUT4-mediated 2-[3H]-deoxyglucose uptake at 10 uM incubated for 16 hrs measured for 5 mins by beta scintillation counting method relative to control	2016	Journal of natural products, 05-27, Volume: 79, Issue:5	Naturally Occurring Carbazole Alkaloids from Murraya koenigii as Potential Antidiabetic Agents.
AID311963	Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
AID156775	Binding affinity against Peroxisome proliferator activated receptor delta (PPAR delta); Not active	1999	Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23	Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
AID639491	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase of adiponectin expression at 10 uM after 8 to 12 days relative to control	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological activity of novel barbituric and thiobarbituric acid derivatives against non-alcoholic fatty liver disease.
AID639522	Cytotoxicity against human HepG2 cells assessed as glucose consumption at 10 uM by MTT assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological activity of novel barbituric and thiobarbituric acid derivatives against non-alcoholic fatty liver disease.
AID123674	Compound was administered at a dose of 30 mg/kg/day to evaluate the percentage reduction in plasma triglyceride (TG) after 6 days of treatment in db/db mice via oral gavage.	1999	Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14	Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones.
AID136643	Percent reduction in area under glucose10 umol/kg dose of diet in mice	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID599161	Insulin sensitizing activity in mouse 3T3L1 cells assessed as triglyceride accumulation at 1 uM by insulin-regulated cell differentiation assay relative to rosiglitazone	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
AID1700083	Binding affinity to PPARg (unknown origin) by SPR assay
AID637345	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1473835	Stimulation of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID440905	Inhibition of PTP1B	2009	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21	Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects.
AID701821	Antihyperglycemic activity in diabetic C57BL/KsJ db/db mouse model assessed as reduction in in plasma insulin level in hyperglycemia at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID1905824	Agonist activity at yeast Gal4-fused human PPARdelta transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID11393	Plasma clearance was determined in rat after intravenous administration (0.5 mg/kg)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID421119	Toxicity in Zucker fa/fa rat assessed as increase in heart weight at 10 mg/kg, po treated once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1167328	Growth inhibition of human MDA-MB-231 cells at 100 uM after 24 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Synthesis and anti-tumor activity of glycosyl oxadiazoles derivatives.
AID469775	Antidiabetic activity in BALB/c mouse type 2 diabetic model assessed as reduction of fasting blood glucose level at 2 mg/kg, po QD measured after 2 weeks by glucometry (Rvb=14.86 +/- 1.58 mmol/L)	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID372114	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in extracellular fluid volume at 100 mg/kg, po once daily for 7 days measured after 24 hrs by bioelectrical impedance analysis	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID244311	In vitro agonist activity against human PPAR-gamma in transactivation assay at 10 nM	2005	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14	6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-gamma activators.
AID639525	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase of adiponectin level at 10 uM after 8 to 12 days (Rvb = 843.78 +/- 20.61 ng/ml)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological activity of novel barbituric and thiobarbituric acid derivatives against non-alcoholic fatty liver disease.
AID1543220	Cytotoxicity against human neutrophils assessed as reduction in cell viability at 30 uM incubated for 24 hrs by MTT assay
AID1272055	Binding affinity to GST-tagged human PPAR-gamma receptor by FRET assay	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Design and synthesis of novel Y-shaped barbituric acid derivatives as PPARγ activators.
AID26203	In vivo % reduction of blood glucose area under curve after oral glucose tolerance test in male db/db mice at 0.33 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID372103	AUC in obese insulin-resistant Zucker fa/fa rat at 0.1 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1468749	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (607 to 631 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1819935	Agonist activity at recombinant N-terminal His6 -tagged GFP fused PPARgamma LBD (unknown origin) (203 to 477 residues) expressed in Escherichia cell Rosetta2 using biotinylated NLVPDAASKHKQLSELLRGGSGS peptide as substrate assessed as induction of Tb crypt	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
AID733019	Antidiabetic activity in KKAy diabetic mouse model assessed as body weight gain at 1 mg/kg/day administered through feeding for 3 days measured on day 4 relative to vehicle-treated control	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID276055	Induction of osteoblast differentiation assessed as stimulation of alkaline phosphatase in MC3T3-E1 cells	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
AID1315288	Activation of Akt-dependent signalling pathway in rat L6 myotubes assessed as increase in insulin-stimulated myc-tagged GLUT4-mediated 2-[3H]-deoxyglucose uptake at 25 uM incubated for 16 hrs followed by insulin stimulation for 20 mins measured for 5 mins	2016	Journal of natural products, 05-27, Volume: 79, Issue:5	Naturally Occurring Carbazole Alkaloids from Murraya koenigii as Potential Antidiabetic Agents.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID745232	Antidyslipidemic activity in db/db mouse assessed as decrease in plasma total cholesterol level at 30 mg/kg, po qd administered 15 days measured on day 16 by ELISA relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1532796	Metabolic stability in Sprague-Dawley rat plasma after 2 hrs by HPLC analysis	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID666818	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction of triglyceride level at 1 to 100 mg/kg, po qd for 12 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1266114	Cytotoxicity against human HEK293 cells assessed as inhibition of cell growth at 100 uM after 48 to 72 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24	Identification of dual PPARα/γ agonists and their effects on lipid metabolism.
AID237608	Percent decrease in plasma glucose level of wistar rat was determined at 3 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID276599	Reduction of plasma glucose in orally dosed db/db mouse at 30 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1785323	Reduction in body weight change in high fat diet fed C57BL/6J DIO mouse measured at 15 mg/kg, po up to 28 days	2021	Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19	Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
AID314546	Agonist activity at human PPARalpha by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID453575	Selectivity ratio of EC50 for human PPARgamma to EC50 for human PPARalpha	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID156799	Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID1468746	Displacement of N-terminal biotin-labeled SMRT-ID1 (2339 to 2363 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1760196	Antidiabetic activity in KK-Ay mouse assessed as effect on LDL level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 1.11 +/- 0.24 mM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID407776	Antihyperglycemic activity in C57BL/KsJ db/db mouse at 5 mg/kg, sc administered twice a day for 4 days once on day 5 after 60 mins of load injection by insulin suppression test relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
AID1657600	Agonist activity at GAL4-tagged PPARgamma (unknown origin) transiently expressed in HEK293T cells co-transfected with GAL4-tagged luc assessed as fold change at 1 uM incubated for 6 hrs by dual luciferase reporter gene assay	2020	Journal of natural products, 05-22, Volume: 83, Issue:5	The Oxidation of Phytocannabinoids to Cannabinoquinoids.
AID156281	In vitro binding affinity for human PPAR alpha in SPA	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID307136	Ratio of EC50 for human PPARalpha to human PPARgamma	2007	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11	Design of potent PPARalpha agonists.
AID678722	Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID483821	Antiobesity activity in diet-induced obese mouse assessed as decrease in body weight at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 13	2010	Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11	Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1362914	Agonist activity at recombinant human GAL4-TAD fused PPARgamma LBD assessed as induction of GAL4-DBD fused NCoA3 co-factor recruitment after 24 to 48 hrs by fluorescence assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1700119	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in COX7 mRNA expression by RT-PCR analysis
AID666825	Toxicity in po dosed Wistar-Imamichi rat assessed as increase heart weight administered qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1561670	Selective modulation of PPARgamma in human HepG2 cells assessed as induction of adiponectin mRNA expression at 1 uM measured after 12 hrs by qPCR analysis	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID1468754	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled SRC1 (619 to 643 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1901245	Agonist activity at human FFA1 expressed in CHO cells assessed as increase in calcium level measured by Fluo-4-AM staining based FLIPR assay	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
AID1874139	Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment by HTRF assay	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID476068	Agonist activity at N-terminal His-tagged human PPARgamma ligand binding domain by fluorescence polarization assay	2010	European journal of medicinal chemistry, Jan, Volume: 45, Issue:1	Identification of (beta-carboxyethyl)-rhodanine derivatives exhibiting peroxisome proliferator-activated receptor gamma activity.
AID304331	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARalpha	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID1198932	Induction of p53 protein level in human HepG2 cells at 50 uM upto 24 hrs by immunoblot analysis	2015	Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9	Structural insight of glitazone for hepato-toxicity: Resolving mystery by PASS.
AID174361	In vivo plasma glucose in Zucker diabetic fatty rat after 11 days at 30 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1878205	Transactivation of Gal4-fused human PPARalpha expressed in CHO cells co expressing pG5-Luc reporter at 1 uM	2022	Bioorganic & medicinal chemistry letters, 03-01, Volume: 59	Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
AID277013	Reduction of plasma glucose level in orally dosed Zucker diabetic fatty rat	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID1362894	Toxicity in F344/DuCrlCrlj rat assessed as body weight gain at 50 mg/kg, po administered via gavage once daily for 28 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID26205	In vivo % reduction of blood glucose area under curve after oral glucose tolerance test in male db/db mice at 3 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1532781	Inhibition of ROS production in TNF-alpha-induced insulin resistant mouse 3T3L1 cells at 10 uM after 48 hrs in presence of nitric oxide scavenger C-PTIO by DCFH-DA dye-based fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1499919	Toxicity in Zucker rat chronic ob/ob model assessed as serum BUN level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 28.3 +/- 1.1 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID387494	AUC (0 to 24 hrs) in Sprague-Dawley rat at 3 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID444057	Fraction escaping hepatic elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID357436	Activation of PPARgamma L469A mutant-mediated transcriptional activity assessed as Gal4 reporter activity	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID387496	Volume of distribution at steady state in Sprague-Dawley rat at 3 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID240252	Effective concentration against human Peroxisome proliferator activated receptor alpha in Gal4 transactivation assay	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
AID475418	Hypolipidemic activity in db/db mouse assessed as serum HDL level at 10 mg/kg, po QD after 14 days (Rvb= 1.99 +/- 0.13 m/mol)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID1827897	Agonist activity at Gal4-fused PPARgamma (unknown origin) expressed in human U2OS cells co-transfected with pSG5 expression vector assessed as maximum agonist effect at 50 uM preincubated for 40 hrs followed by substrate addition by microplate reader assa	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID276096	Lowering of plasma glucose level in DIO C57BL/6J mouse at 5 mg/kg, po after 4 hr fasting	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID276603	Reduction of plasma triglycerides in orally dosed db/db mouse at 3 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1822057	Agonist activity at PPARgamma (unknown origin)
AID643914	AUC in db/db C57BLKS/J-m +/+ Leprdb mouse at 10 mg/kg, po qd for 10 days measured on day 11	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID156149	In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1228168	Potentiation of insulin-induced 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM preincubated with cells followed by insulin induction for 30 mins by liquid scintillation counting analysis relative to control	2015	Journal of natural products, Apr-24, Volume: 78, Issue:4	Steroidal Alkaloids from Veratrum nigrum Enhance Glucose Uptake in Skeletal Muscle Cells.
AID290114	Agonist activity at human recombinant PPARgamma at 30 uM by GAL4 transactivation assay relative to control	2007	European journal of medicinal chemistry, Apr, Volume: 42, Issue:4	Synthesis and evaluation of N-acetyl-L-tyrosine based compounds as PPARalpha selective activators.
AID1716501	Agonist activity at human PPARgamma in 8 day differentiated human SGBS cells assessed as decrease in CXCL5 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1427958	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in blood glucose level at 10 mg/kg/day administered via oral gavage once daily for 21 days measured at 30 to 60 mins post glucose challenge by oral glucose tolerance test	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID123420	In vivo efficacy as percent triglyceride correction in male db/db mice at 10 mg/kg oral dose	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID1236824	Increase in body weight in C57BLKS/J-Lepr/Lepr db/db mouse at 10 mg/kg, po qd for 18 days administered via gavage measured on day 16 relative to untreated control	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists.
AID316707	Inhibition of PPARgamma	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
AID1773624	Hepatoprotective activity in ob/ob mouse assessed as reduction in plasma aspartate transaminase at 10 mg/kg, po administered once daily for 30 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID643840	Partial agonist activity at human PPARgamma LBD assessed as activation of Src-1 by HTRF assay relative to L-796449	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID733011	Antidiabetic activity in po dosed Zucker fatty rat assessed as reduction in blood glucose level measured after 14 days	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID637349	Inhibition of PTB1B using pNPP as substrate after 30 mins	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID548199	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.
AID554249	Transactivation of Gal4-fused human PPARalpha expressed in HEK293 cells at 10 uM after 16 to 20 hrs by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1	Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.
AID156152	In vitro binding affinity against human Peroxisome proliferator activated receptor alpha	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID417010	Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Selective, potent PPARgamma agonists with cyclopentenone core structure.
AID422626	Activation of human PPAR-gamma-dependent transcription expressed in human MCF7 cells assessed as induction of PPRE-reporter gene expression at 0.1 uM after 24 hrs by dual luciferase reporter gene assay relative to rosiglitazone	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
AID1251344	Increase in PPARgamma mRNA expression in mouse 3T3L1 cells at 10 uM incubated for 24 hrs by RT-PCR method	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1315291	Activation of Akt-dependent signalling pathway in rat L6 myotubes assessed as induction of myc-tagged GLUT4 translocation to cell surface at 10 uM incubated for 16 hrs by O-phenylenediamide based colorimetric assay relative to control	2016	Journal of natural products, 05-27, Volume: 79, Issue:5	Naturally Occurring Carbazole Alkaloids from Murraya koenigii as Potential Antidiabetic Agents.
AID1716439	Cytotoxicity against African green monkey COS-1 cells assessed as cell viability at EC50 concentration for PPAR activation assay by XTT assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID314547	Agonist activity at human PPARgamma by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID1468731	Toxicity in Sprague-Dawley rat assessed as increase in plasma volume at 30 mg/kg for 4 weeks by evans blue dye based assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1291847	Agonist activity at PPAR gamma (unknown origin) transfected in HEK293 cells at 1 uM after 24 hrs by dual-luciferase reporter gene assay	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	Pharmacophore elucidation of phosphoiodyn A - Potent and selective peroxisome proliferator-activated receptor β/δ agonists with neuroprotective activity.
AID453770	Toxicity in ZDF rat assessed as increase in body weight at 3 mg/kg/day, po for 2 weeks relative to untreated control	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID417012	Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay	2009	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7	Selective, potent PPARgamma agonists with cyclopentenone core structure.
AID157282	Displacement of [3H]-BRL 49653 from glutathione S-transferase-Peroxisome proliferator activated receptor gamma ligand binding domain in bacterial extracts	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
AID372105	AUC in obese insulin-resistant Zucker fa/fa rat at 10 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID637397	Effect on hematocrit level in Sprague-Dawley rat at 12.5 mg/kg after 28 days (Rvb = 47.5 +/- 0.6 %)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID484773	Transactivation of PPARgamma assessed as induction of alkaline phosphatase activity	2010	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11	Flexible ligand recognition of peroxisome proliferator-activated receptor-gamma (PPARgamma).
AID744326	Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay	2013	European journal of medicinal chemistry, May, Volume: 63	Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
AID1827895	Binding affinity to PPARgamma (unknown origin) by lanthascreen TR-FRET assay	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID307132	Agonist activity at human PPARgamma by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11	Design of potent PPARalpha agonists.
AID666826	Toxicity in Wistar-Imamichi rat assessed as increase plasma volume at 30 to 100 mg/kg, po qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID304332	Displacement of [3H]2-methyl-2-(4-{3-{propyl-(5-pyridin-2-yl-thiophene-2-sulfonyl)-amino}-propyl}-phenoxy)-propionic acid from human PPARgamma	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID239802	Mean percent of maximum efficacy against human peroxisome proliferator-activated receptor alpha	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID1597847	Upregulation of ADIPOQ gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID421147	AUC in Sprague-Dawley rat at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1905845	Reduction of lipid accumulation in oleic acid-induced steatosis in human HepaRG cells at 10 uM treated for 24 hrs by spectrophotometry	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID1674183	Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection method	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID690963	Antihyperglycemic activity in streptozotocin-induced type 2 diabetic Wistar albino rat assessed as reduction in plasma glucose level at 50 mg/kg, po by glucometer	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20	Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents.
AID1063325	Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID1700101	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in IRB mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID252307	Effect (150 mg/kg) on PPAR gamma- mediated effects measured as change in heart weight in rats	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
AID273357	Activity at human PPAR gamma in Huh7 cells by transactivation assay	2006	Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21	Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
AID114053	Nonfasting triglycerides after 7 days treatment in male db/db mice	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID276098	Effect on plasma triglyceride level in DIO C57BL/6J mouse at 5 mg/kg, po after 4hrs fasting	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID464095	Antidiabetic activity in Wistar rat hemidiaphragm assessed as glucose uptake at 2 mg after 45 mins by GOD/POD enzymatic method in absence of insulin	2010	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6	Novel glitazones: design, synthesis, glucose uptake and structure-activity relationships.
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AID1209455	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID156933	Transcriptional activation by human PPAR gamma	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1468748	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled LCOR (39 to 63 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID421159	Toxicity in Sprague-Dawley rat assessed as increase in liver weight at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID305545	Agonist activity at PPARgamma in CV1 cells by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID280961	Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay relative to carbacyclin	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID1362959	Metabolic stability in rat liver microsomes after 0.5 hrs	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1440528	Transactivation of GAL4-fused human PPARdelta LBD expressed in human HepG2 cells up to 2 uM after 20 hrs by luciferase reporter gene assay relative to L-165,041	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID289933	Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID1217705	Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID387510	Antihyperglycemic activity in db/db mouse assessed as increase in body weight at 1 mg/kg, po once daily after 28 days	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1503562	Downregulation of PPARgamma mRNA expression in human SCC15 cells at 10 uM after 4 hrs by RTqPCR analysis relative to control	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).
AID387495	Clearance in Sprague-Dawley rat at 3 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID705738	Binding affinity to mouse cell division protein kinase 7 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID123421	In vivo triglyceride correction was determined in male db/db mice after administration at 10 mg/kg	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1217708	Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID708114	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.
AID236414	Area under concentration curve for the compound was determined in sprague-dawley rat plasma at 150 mg/kg	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID1716484	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as upregulation of steroid biosynthesis genes at 2 uM incubated for 8 days by Illumina sequencing method	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID736343	Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay	2013	Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3	The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
AID1532780	Inhibition of ROS production in TNF-alpha-induced insulin resistant mouse 3T3L1 cells at 10 uM after 48 hrs by DCFH-DA dye-based fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID501302	Inhibition of human recombinant MAO-B after 15 mins	2010	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17	Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.
AID656881	Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction of plasma glucose level at 50 mg/kg, po after 2 to 6 weeks by glucometer relative to control	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID413008	Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay relative to rosiglitazone	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.
AID1339408	Agonist activity at SUR in Wistar rat islets of pancreas assessed as induction of glucose-stimulated insulin secretion preincubated for 1 hr followed by glucose addition measured after 30 mins by sandwich ELISA	2017	Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of novel quinoxaline derivatives as potential PPARγ and SUR agonists.
AID1532839	Induction of nitric oxide production in TNF-alpha-induced insulin resistant mouse 3T3L1 cells at 10 uM after 0.5 to 6 hrs by DAF-FM-2DA dye based fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID470059	Hypoglycemic effect in type 2 diabetic BALB/c mouse model assessed as reduction in blood glucose excursion at 2 mg/kg, po pretreated 60 mins before glucose challenge measured up to 3 hrs by one-touch glucometer relative to diabetic control	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID421051	Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID68772	Heart wt absolute in two week oral toxicity test in male F344/DuCrj rats after 50 mg/kg dose	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID1760216	Effect on high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as food intake at 5 mg/kg, po (Rvb = 5.67 +/- 0.55 g/day)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID421049	Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID23878	Clearance in rat	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID554250	Transactivation of Gal4-fused human PPARdelta expressed in HEK293 cells at 10 uM after 16 to 20 hrs by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1	Design, synthesis, and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.
AID1427977	Decrease in size of adipocytes in abdominal white adipose tissue in KK-Ay diabetic mouse model at 10 mg/kg/day administered via oral gavage once daily for 21 days by haematoxylin and eosin staining based microscopic or morphometric method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID1532827	Inhibition of human ERG expressed in CHO cells at 5 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID491659	Induction of adipogenesis in mouse mature 3T3L1 cells assessed as P2 mRNA expression level after 10 days by Oil red O staining	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID1363007	Toxicity in Wistar-Imamichi rat assessed as reduction in RBC count at 30 mg/kg, po administered via gavage once daily for 28 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1499805	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as brown adipose tissue weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 2.1 +/- 0.3 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1499922	Toxicity in Zucker rat chronic ob/ob model assessed as serum creatinine level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 0.55 +/- 0.018 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID124441	Maximum achieved insulin reduction relative to vehicle treated control group	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1716499	Agonist activity at human PPARgamma in 8 day differentiated human SGBS cells assessed as decrease in TNF gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID23875	Clearance after oral administration	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1266989	Antidyslipidemic activity in ZDF rat assessed as HDL level at 0.3 mg/kg for 9 days by FPLC analysis (Rvb = 48.3 mg/dL)	2015	Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24	Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
AID1668562	Agonist activity at PPARgamma in mouse 3T3L1 adipocytes assessed as induction of GLUT4 mRNA expression at 3 uM by qRT-PCR analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID439367	Agonist activity at human PPARgamma expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 5 uM after 48 hrs by reporter gene assay relative to control	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
AID421167	AUC in rat at 2 mg/kg, po	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1422538	Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID237612	Percent decrease in plasma glucose level of wistar rat was determined at 100 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID156286	Agonistic transcriptional activity in COS1 cells expressing GAL 4-PPAR alpha at 3 uM; Maximal percent	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID372110	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in plasma volume at 10 mg/kg, po once daily for 7 days by Evans blue dye dilution technique	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1810337	Agonist activity at human PPARalpha transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID114051	Nonfasting blood glucose after 7 days treatment in male db/db mice	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID431128	Hypolipidemic activity in monosodium L-glutamate-treated obese Wistar rat assessed as reduction in serum triglyceride level at 5 mg/kg, po for 6 weeks measured after 10 hrs post dose fasting	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID1377505	Agonist activity at GAL4-fused PPARgamma LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM after 18 hrs by dual luciferase reporter gene assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID439374	Cytotoxicity against HEK293 cells assessed as viable cells at 100 uM after 48 hrs by aqueous one solution cell proliferation assay relative to control	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
AID189062	Percent reduction in triglyceride (TG) after 9 days of dosing in db/db is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 10 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID136632	Percent reduction in area under glucose tolerance curve at 100 uM/kg dose in diet of mice.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
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AID705756	Binding affinity to L-lactate dehydrogenase B chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1419243	Antidiabetic activity in KKAy mouse model assessed as blood glucose level at 100 mg/kg/day, po administered for 4 days	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.
AID12365	Dose-normalized AUC was determined in rat after peroral administration (2 mg/kg)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID1362862	Cmax in Zucker diabetic fatty rat at 0.3 mg/kg, po administered once daily for 21 days followed by additional administration on day 22	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID491652	Antidiabetic activity in db/db mouse assessed as reduction of plasma glucose level at 10 mg/kg, po qd for 7 days	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID453572	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay relative to GW-9578	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID745236	Antihyperglycemic activity in db/db mouse assessed as inhibition of post prandial blood glucose level at 30 mg/kg, po qd administered 15 days by OGTT relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID666821	Toxicity in Wistar-Imamichi rat assessed as increase in body weight at 300 mg/kg, po qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID643926	Toxicity in obese insulin resistant Zucker fa/fa rat assessed as increase in plasma volume at >= 10 mg/kg	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1899745	Agonist activity at human FFA1 expressed in CHO cells measured by FLIPR assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID372046	Agonist activity at human recombinant PPARalpha expressed in COS1 cells coexpressing GAL4 assessed as transcriptional activity at 3000 nM after 48 hrs by luciferase reporter gene assay	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1716486	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as upregulation of fatty acid elongation genes at 2 uM incubated for 8 days by Illumina sequencing method	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1499860	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum adiponectin level at 10 mg/kg, po qd for 32 days by ELISA (Rvb = 10.7%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1063326	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release at 10 uM treated 2 hrs before LPS challenge measured after 48 hrs by Griess assay relative to control	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID156382	Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) alpha expressed in HEK 293T cells at 50 uM	2001	Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16	(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID238857	Binding affinity for human peroxisome proliferator activated receptor gamma	2004	Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17	Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID1507897	Toxicity in ob/ob mouse assessed as change in body weight at 3 mg/kg administered via oral gavage daily for 4 days measured on day 5 relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID26199	In vivo blood glucose area under curve after oral glucose tolerance test in male db/db mice at 0.33 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID243411	Efficacy against human PPARalpha expressed in HepG2 cells relative to Wy-14,643; i.a = inactive at tested concentration	2005	Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17	Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
AID354055	Antidiabetic activity in db/db mouse diabetic model assessed as reduction in post prandial blood glucose level at 0.3 mg/kg/day	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID744324	Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay	2013	European journal of medicinal chemistry, May, Volume: 63	Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
AID1905850	Reduction of lipid accumulation in oleic acid-induced steatosis in human HepaRG cells at 10 uM treated for 2 weeks with media replenishment along with compound and inducer for every 2 days by spectrophotometry	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID1419106	Binding affinity to recombinant human PPARgamma LBD at 40 uM by TR-FRET based green polar-screen PPAR competitor assay	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	Lobaric acid and pseudodepsidones inhibit NF-κB signaling pathway by activation of PPAR-γ.
AID424500	Metabolic stability in rat hepatocyte microsomes	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1156983	Cytotoxicity against HGC assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID306524	Displacement of fluorescein labeled ligand from PPARalpha receptor by fluorescence polarization assay	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID1700110	Induction of insulin-dependent glucose uptake in mouse 3T3-L1 cells at 0.1 uM incubated for 16 hrs before insulin stimulation by chemiluminescence based 2-deoxy-D-glucose uptake assay
AID1700123	Induction of mitochondrial biogenesis in mouse 3T3-L1 cells assessed as increase in UCP2 mRNA expression by RT-PCR analysis
AID305540	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl butyric acid from human PPARalpha	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID240268	Effective concentration against human PPARgamma expressed in HepG2 cells	2005	Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17	Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
AID552405	Antihyperlipidemic activity in db/db mouse assessed as reduction of serum triglyceride level at 30 mg/kg, po qd for 14 days relative to control	2011	Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2	Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
AID223543	Fold activation relative to maximum hPPAR alpha activation obtained with WY-14643	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1716463	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in UPC1 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1468734	Toxicity in Sprague-Dawley rat assessed as increase in heart weight at 30 mg/kg for 6 weeks	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID551877	Agonist activity at human PPARdelta in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of transactivation activity at 10 uM by luciferase reporter gene assay relative to control	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Modulation of PPAR subtype selectivity. Part 2: Transforming PPARα/γ dual agonist into α selective PPAR agonist through bioisosteric modification.
AID1532828	Inhibition of human ERG expressed in CHO cells at 10 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID439369	Agonist activity at human PPARgamma assessed as luciferase activity by transactivation assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
AID1532840	Induction of GSH level in TNF-alpha-induced insulin resistant mouse 3T3L1 cells 10 uM after 48 hrs	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID268281	Agonist activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay at 10 uM	2006	Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15	Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists.
AID246650	In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID656889	Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of total cholesterol level at 50 mg/kg, po after 2 weeks (Rvb = 9.8 +/- 0.7 mmol/L)	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID299623	Agonist activity at human PPARgamma by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15	Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
AID1503452	Activation of AMPK in palmitate-induced insulin-resistant human HepG2 cells assessed as reduction in GLUT2 mRNA expression at 12.5 uM incubated for 24 hrs by real-time PCR method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID189026	Percent reduction in blood glucose is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 10 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID240312	Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay	2004	Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17	Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID701823	Antidyslipidemic activity in diabetic C57BL/KsJ db/db mouse model assessed as reduction in plasma cholesterol level at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID1494541	Transactivation of recombinant human N-terminal GAL4-DBD fused PPARgamma LBD expressed in reporter cells measured after 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9	Synthesis, biological evaluation, and molecular docking investigation of benzhydrol- and indole-based dual PPAR-γ/FFAR1 agonists.
AID237611	Percent decrease in plasma glucose level of wistar rat was determined at 30 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID424498	Absorption in human Caco-2 cells	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID311962	Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
AID1668550	Agonist activity at PPARgamma in mouse 3T3L1 assessed as induction of lipid accumulation at 2 uM	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID1901614	Agonist activity at human PPARgamma in mouse 3T3-L1 cells assessed as induction of PPARgamma mRNA expression at 10 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID431047	Induction of adipogenesis in mouse 3T3L1 assessed as increase in triglyceride level at 0.1 uM after 5 days relative to control	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID1532806	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation at 16 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID372093	Effect on body weight in obese insulin-resistant Zucker fa/fa rat at 0.1 to 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID422623	Displacement of [3H2]nTZD3 from GST-tagged human recombinant PPARalpha by scintillation proximity assay	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
AID407778	Antihyperglycemic activity in C57BL/KsJ db/db mouse assessed as reduction in water consumption at 5 mg/kg, sc administered twice a day for 4 days and once on day 5 relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
AID421098	Antidiabetic activity in high fat diet-fed streptozotocin-treated mouse assessed as reduction in plasma glucose levels at 5 mg/kg, po once daily for 12 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1597854	Agonist activity at PPARalpha in C57BL/6N mouse primary hepatocytes assessed as activation of Srebf1 mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID421156	Toxicity in Sprague-Dawley rat assessed as hematocrit at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID12958	Oral bioavailability in rat (Sprague-Dawley) (fasted male) (dose 2 mg/kg)	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID1503445	Stimulation of glucose consumption in palmitate-induced insulin-resistant human HepG2 cells at 12.5 uM incubated for 24 hrs by glucose oxidase based assay relative to palmitate	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID1597839	Upregulation of ACSL1 gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1362906	Toxicity in F344/DuCrlCrlj rat assessed as effect on kidney weight at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID372042	Displacement of [3H2]nTZD3 from human recombinant GST-fused PPARalpha expressed in Escherichia coli by scintillation proximity assay	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1827896	Agonist activity at Gal4-fused PPARgamma (unknown origin) expressed in human U2OS cells co-transfected with pSG5 expression vector preincubated for 40 hrs followed by substrate addition by microplate reader assay	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID199648	In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay.	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID1362888	AUC (0 to 24 hrs) in F344/DuCrlCrlj rat at 50 mg/kg, po via gavage measured on day 28 post dose	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID637384	Hypotriglyceridemic activity in diabetic KK-Ay mouse model assessed as decrease in triglyceride level at 3 mg/kg, po qd for 14 days (Rvb = 819.9 +/- 135.5 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1468750	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (671 to 695 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1499845	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum creatinine level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 0.71 +/- 0.07 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1507889	Modulation of SGK1 mRNA expression in HCCD cells at 20 uM after 24 hrs by RT-PCR method relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID156232	In vitro transcriptional activation of peroxisome proliferator activated alpha-receptor (PPAR) expressed in CV-1 cells; Inactive	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
AID1362903	Toxicity in F344/DuCrlCrlj rat assessed as effect on hematocrit at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1597849	Upregulation of ANGPTL4 gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1532795	Metabolic stability in Sprague-Dawley rat plasma after 0.5 hrs by HPLC analysis	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1362853	Metabolic stability in rat liver microsomes after 0.5 hrs	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID354043	Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID223552	Transcriptional activation in CV-1 cells expressing hPPARalpha	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID199649	In vitro transcriptional activation in CV-1 cells expressing RXR-alpha and PPARgamma; No activity	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID1362859	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction in plasma glucose level administered orally once daily for 21 days measured on day 22	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID299411	Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs relative to gemfibrozil	2007	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13	Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
AID199624	In vitro transcriptional activation in CV-1 cells expressing RXR-alpha; No activity	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID503297	Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay	2006	Nature chemical biology, Jun, Volume: 2, Issue:6	Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID637385	Hypotriglyceridemic activity in diabetic KK-Ay mouse model assessed as decrease in triglyceride level at 10 mg/kg, po qd for 14 days (Rvb = 819.9 +/- 135.5 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID705757	Binding affinity to mitochondrial malate dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID270628	Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID305546	Efficacy at human Gal4-PPARalpha expressed in CV1 cells at 10 uM relative to control by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID1275402	Transactivation of N-terminal Gal4 DNA binding domain-linked human PPARalpha ligand binding domain at 30 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists.
AID705492	Binding affinity to mouse chloride channel protein 6 after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1532811	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation at 8 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID643838	Partial agonist activity at human PPARgamma LBD assessed as activation of PGC1 by HTRF assay relative to L-796449	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID548202	Ratio of compound IC50 to rosiglitazone IC50 for displacement of fluormone PPAR-green from N-terminal His-tagged human PPARgamma-LBD	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.
AID1901651	Agonist activity at human PPARgamma in mouse 3T3-L1 cells assessed as induction of aP2 mRNA expression at 10 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1217716	Time dependent inhibition of CYP2C8 (unknown origin) at 10 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1597822	Agonist activity at PPARalpha in human Huh7 cells assessed as SREBF1 mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1474031	Ratio of drug concentration at steady state in human at 2 to 8 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID161302	Functional potency was determined in pooled human preadipocytes by measurement of PPARg aP2 gene induction	2003	Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14	Benzoxazinones as PPARgamma agonists. part 1: SAR of three aromatic regions.
AID1443995	Hepatotoxicity in human assessed as drug-induced liver injury	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID252305	Heart weight was determined in normal sprague-dawley rats at 30 mg/kg	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID174360	In vivo plasma glucose in Zucker diabetic fatty rat after 11 days at 10 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID475404	Antidiabetic activity in db/db mouse assessed as serum insulin level at 10 mg/kg, po QD after 2 weeks (Rvb= 0.41 +/- 0.06 ng/ml)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID705483	Binding affinity to mouse importin-7 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID372041	Displacement of [3H2]nTZD3 from human recombinant GST-fused PPARgamma expressed in Escherichia coli by scintillation proximity assay	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID280957	Activity at human liver PPAR alpha expressed in HEK293 cells by GAL4 transactivation assay relative to NNC61-4655	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID475415	Hypolipidemic activity in db/db mouse assessed as serum total cholesterol level at 10 mg/kg, po QD after 14 days (Rvb= 5.56 +/- 0.60 m/mol)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID276608	Reduction of hematocrit in orally dosed db/db mouse at 3 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1266984	Antidyslipidemic activity in ZDF rat assessed as LDL/IgHDL level at 0.3 mg/kg for 9 days by FPLC analysis (Rvb = 17.8 mg/dL)	2015	Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24	Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
AID268118	Antiproliferative activity against human HT29 cell line	2006	Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14	Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
AID365529	Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID276614	Increase in body weight in orally dosed db/db mouse at 30 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1422550	Agonist activity at PPARgamma (unknown origin)	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID307130	Agonist activity at human PPARalpha by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11	Design of potent PPARalpha agonists.
AID662861	Competitive inhibition of human MAOB expressed in Pichia pastoris	2011	ACS medicinal chemistry letters, Oct-15, Volume: 3, Issue:1	Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
AID1572807	Binding affinity to NAF1 in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	2019	Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7	Binding of thiazolidinediones to the endoplasmic reticulum protein nutrient-deprivation autophagy factor-1.
AID1760240	Induction of glycolysis in human HepG2 cells assessed as reduction in cellular ATP production at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID156941	In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID733021	Antidiabetic activity in KKAy diabetic mouse model assessed as change in insulin level at 1 mg/kg/day administered through feeding for 3 days measured on day 4 relative to vehicle-treated control	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID1773610	Induction of hepatic steatosis in ob/ob mouse at 10 mg/kg, po administered once daily for 30 days by hematoxylin-eosin staining based histopathological analysis	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1275405	Transactivation of N-terminal Gal4 DNA binding domain-linked human PPARalpha ligand binding domain after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists.
AID429212	Antidiabetic activity in ob/ob mouse assessed as decrease in fasting whole blood glucose level at 10 mg, po measured on day 7	2009	European journal of medicinal chemistry, Aug, Volume: 44, Issue:8	Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents.
AID252306	Heart weight was determined in normal sprague-dawley rats at 150 mg/kg	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID439368	Agonist activity at human PPARgamma expressed in HEK293 cells co-transfected with PPRE assessed as beta-galactosidase signal at 25 uM after 48 hrs by reporter gene assay relative to control	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
AID1503553	Cytotoxicity against human SCC15 cells transfected with PPARalpha siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).
AID242602	Inhibition of human peroxisome proliferator activated receptor gamma binding	2005	Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10	Selective PPARgamma modulators with improved pharmacological profiles.
AID552195	Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity at 10 uM after 20 to 22 hrs by luciferase based transactivation assay relative to control	2011	Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2	Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
AID1063321	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 24 hrs by ELISA (Rvb = 38.3 +/- 3.3 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID1651578	Antidiabetic activity in mouse 3T3L1 preadipocytes assessed as increase in triglycerides level after 6 days
AID12665	Half life was measured in fasted male administration of compound 0.5 mg/Kg i.v.	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID246887	In vivo effective dose value in NIDDM animal model (ZDF rat)	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID157289	In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID277005	Activity at human PPARgamma in CV1 cells	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID372055	Agonist activity at hamster PPARalpha	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID276984	Displacement of tritium labeled ligand from human PPARgamma by SPA assay	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID1773584	Agonist activity at human PPARgamma transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1351163	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by ELISA (Rvb = 407.6 +/- 16.7 pg/m	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1499866	Antidiabetic activity in Zucker rat chronic ob/ob model assessed as fasting blood glucose level at 10 mg/kg, po qd measured on day 14 (Rvb = 337.5 +/- 17.9 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID465709	Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Acidic elements in histamine H(3) receptor antagonists.
AID1443989	Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID189027	Percent reduction in blood glucose is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 100 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID156280	In vitro binding affinity for human peroxisome proliferator activated receptor alpha using scintillation proximity assay (SPA)	2004	Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12	(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
AID1760208	Antidiabetic activity in KK-Ay mouse assessed as effect on BUN level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 12.8 +/- 2.97 mM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1700091	Binding affinity to PPARg (unknown origin) assessed as reduction in CDK5-mediated phosphorylation of PPARg serine 273 residue at 0.1 uM incubated for 3.5 hrs by ELISA
AID316711	Agonist activity at PPARgamma in HEK293 cells at 1 uM by GAL4 transactivation assay relative to rosiglitazone	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
AID731521	Binding affinity to human PPARalpha (unknown origin) by competitive TR-FRET assay	2013	Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4	Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
AID1610432	Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assay	2019	Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23	Novel berberine-based derivatives with potent hypoglycemic activity.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1566187	Induction of PPARgamma-mediated adipogenesis in mouse 3T3L1 cells assessed as upregulation of LPL mRNA expression at 10 uM by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID1773582	Agonist activity at human PPARalpha transfected in human HepG2 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1760248	Increase in glucose consumption in rat L6 cells at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID491673	Antidiabetic activity in db/db mouse assessed as reduction of plasma glucose level at 3 mg/kg, po qd for 7 days	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID705758	Binding affinity to mitochondrial long-chain specific acyl-CoA dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to rosiglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID372099	Antidiabetic activity in obese insulin-resistant Zucker fa/fa rat assessed as decrease in plasma insulin level at 0.1 to 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID157290	In vitro binding affinity against human PPAR alpha (peroxisome proliferator-activated alpha receptor)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID693499	Toxicity in db/db mouse assessed as body weight gain at 5 mg/kg administered BID relative to control	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis of N-(5-chloro-6-(quinolin-3-yloxy)pyridin-3-yl)benzenesulfonamide derivatives as non-TZD peroxisome proliferator-activated receptor γ (PPARγ) agonist.
AID772912	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose at 10 uM after 24 hrs in presence of insulin relative to control	2013	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20	Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.
AID1063323	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 6 hrs by ELISA (Rvb = 5.9 +/- 0.5 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID354059	Antidiabetic activity in Zucker fa/fa rat assessed as glucose infusion rate at 3 mg/kg/day after 7 days by hyperinsulinemic-euglycemic clamp study	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID354045	Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay relative to edaglitazone	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID1700114	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in PDK4 mRNA expression by RT-PCR analysis
AID1499829	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum cholesterol level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 295 +/- 91 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID254528	Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone	2005	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20	Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
AID705509	Binding affinity to mouse Rab11 family interacting protein 4 by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID136636	Percent reduction in area under glucose tolerance curve (AUC) was determined at 3 umol/kg dose of diet in mice	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID1443991	Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID661075	Antidiabetic activity in mouse 3T3L1 cells assessed as decrease in glucose consumption from cell culture medium using 450 mg/dL D-glucose at 30 ug/mL after 24 hrs (Rvb = 310 +/- 4 mg/dl)	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Synthesis of chalcone derivatives as potential anti-diabetic agents.
AID1339407	Displacement of fluormone-PPARgamma Green from recombinant human N-terminal GST-tagged PPARgamma-LBD by fluorescence polarization assay	2017	Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of novel quinoxaline derivatives as potential PPARγ and SUR agonists.
AID1546897	Activation of mouse liver PPARalpha	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10	The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID705742	Binding affinity to mouse norrin precursor by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID675850	Binding affinity to PPARgamma LBD by fluorescence polarization based competitive binding assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID1410785	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CD36 mRNA expression at 1 uM after 15 days by quantitative real-time PCR method	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
AID733051	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay relative to rosiglitazone	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID1874146	Stabilization of PPARgamma LBD (unknown origin) assessed as melting temperature in presence of SR16832 by differential scanning fluorimetry	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID1573760	Induction of insulin-stimulated 2-NBDG uptake in palmitic acid-induced insulin resistant human HepG2 cells at 1 umol/L preincubated for 24 hrs followed by insulin stimulation and measured after 30 mins by fluorescence assay	2019	Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2	BH3 mimetics derived from Bim-BH3 domain core region show PTP1B inhibitory activity.
AID413007	Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay	2008	Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24	Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.
AID254642	Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assay	2005	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22	Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
AID1566185	Induction of PPARgamma-mediated adipogenesis in mouse 3T3L1 cells assessed as upregulation of FABP4 mRNA expression at 10 uM by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID387499	AUC (0 to 24 hrs) in Sprague-Dawley rat at 3 mg/kg, po	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID253003	In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay at 3 uM	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID1760184	Antidiabetic activity in KK-Ay mouse assessed as effect on insulin level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 226 +/- 15.5 mU/l)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1700072	Agonist activity at GAL4-tagged PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay
AID276710	Displacement of radiolabeled darglitazone from human PPAR gamma by SPA assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1440525	Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells up to 2 uM after 20 hrs by luciferase reporter gene assay relative to rosiglitazone	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1440531	Binding affinity to PPARalpha (unknown origin) assessed as thermodynamic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID597761	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	2011	Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10	Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.
AID1256319	Increase in deoxy-D-glucose 2-[1.2-3H(N)] uptake in human Skeletal muscle cells at 10'-8 M after 72 hrs by scintillation counter relative to control	2015	Journal of natural products, Oct-23, Volume: 78, Issue:10	Cafestol, a Bioactive Substance in Coffee, Stimulates Insulin Secretion and Increases Glucose Uptake in Muscle Cells: Studies in Vitro.
AID1362912	Agonist activity at recombinant human GAL4-TAD fused PPARgamma LBD assessed as induction of GAL4-DBD fused CBP co-factor recruitment after 24 to 48 hrs by fluorescence assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID705489	Binding affinity to mouse voltage-dependent L-type calcium channel alpha-1F subunit by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID189028	Percent reduction in blood glucose is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 200 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID675852	Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID156774	Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR delta at 3 uM; Max %	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID307131	Agonist activity at human PPARalpha by transactivation assay relative to WY-14643	2007	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11	Design of potent PPARalpha agonists.
AID1700117	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in FGF21 mRNA expression by RT-PCR analysis
AID348506	Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity at 10 uM by transactivation assay	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID587347	Antidiabetic activity in rat hemidiaphragm assessed as glucose uptake at 1 mg after 45 mins in absence of insulin	2011	European journal of medicinal chemistry, Mar, Volume: 46, Issue:3	Synthesis, glucose uptake activity and structure-activity relationships of some novel glitazones incorporated with glycine, aromatic and alicyclic amine moieties via two carbon acyl linker.
AID637399	Effect on hematocrit level in Sprague-Dawley rat at 50 mg/kg after 28 days (Rvb = 47.5 +/- 0.6 %)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1507895	Anti-diabetic activity in ob/ob mouse assessed as change in serum insulin levels at 3 mg/kg administered via oral gavage daily for 4 days measured on day 5 relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID429214	Antidiabetic activity in ob/ob mouse assessed as decrease in fasting WBG at 10 mg, po measured on day 10 (Rvb= 139+/-8 mg/dl)	2009	European journal of medicinal chemistry, Aug, Volume: 44, Issue:8	Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents.
AID745240	Antihyperglycemic activity in db/db mouse assessed as reduction of blood glucose level at 30 mg/kg, po qd measured daily for 15 days relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID491662	Induction of adipogenesis in mouse blast 3T3L1 cells assessed as P2 mRNA expression level after 7 days by Oil red O staining	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID1351155	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 48 hrs by Griess method relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1362860	Antidiabetic activity in Zucker diabetic fatty rat assessed as plasma glucose level at >= 1 mg/kg, po administered once daily for 21 days measured on day 22 (Rvb >= 240 mg/dl)	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1315290	Activation of Akt-dependent signalling pathway in rat L6 myotubes assessed as increase in myc-tagged GLUT4-mediated 2-[3H]-deoxyglucose uptake incubated for 16 hrs measured for 5 mins by beta scintillation counting	2016	Journal of natural products, 05-27, Volume: 79, Issue:5	Naturally Occurring Carbazole Alkaloids from Murraya koenigii as Potential Antidiabetic Agents.
AID1668551	Agonist activity at PPARgamma in mouse 3T3L1 assessed as induction of adipocytes differentiation at 2 uM by Oil Red O staining based assay	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID1668560	Agonist activity at PPARgamma in mouse 3T3L1 adipocytes assessed as induction of LPL mRNA expression at 3 uM by qRT-PCR analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID1716459	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in ANGPTL4 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1363009	Toxicity in Wistar-Imamichi rat assessed as reduction in RBC count at 300 mg/kg, po administered via gavage once daily for 28 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID344820	Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay relative to rosiglitazone	2008	Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21	Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
AID469772	Antidiabetic activity in BALB/c mouse type 2 diabetic model assessed as reduction of fasting blood glucose level at 2 mg/kg, po QD measured after 1 week by glucometry (Rvb=14.89 +/- 1.37 mmol/L)	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID752224	Binding affinity to human PPARgamma receptor by radioligand displacement assay	2013	Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10	Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID1183853	Induction of Dectin-1 mRNA expression in mouse peritoneal macrophages isolated from PPARgamma -/- mouse treated at 5 uM for 5 hrs by qRT-PCR analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Protolichesterinic acid derivatives: α-methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors.
AID1905841	Cytotoxicity against oleic acid-induced steatosis in human HepaRG cells at 10 times of EC50	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID27582	Partition coefficient (logP)	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1315250	Transactivation of PPARgamma in mouse C2C12 cells assessed as increase in GLUT-4 mediated 2-NBDG uptake at 20 uM at 4 hrs by fluorescence assay	2016	Journal of natural products, 05-27, Volume: 79, Issue:5	Tadehaginosides A-J, Phenylpropanoid Glucosides from Tadehagi triquetrum, Enhance Glucose Uptake via the Upregulation of PPARγ and GLUT-4 in C2C12 Myotubes.
AID1819946	Induction of adipogenic differentiation in human SGBS cells assessed as increase in perilipin A mRNA expression A at 0.01 to 1 uM by RT-PCR analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPARγ Modulator.
AID705754	Binding affinity to glyceraldehyde 3-phosphate dehydrogenase in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID637429	Effect on RBC count in Sprague-Dawley rat at 25 mg/kg after 28 days (Rvb = 832 +/- 25.2 x 10 ' 4/micro L)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1362864	AUC (0 to 24 hrs) in Zucker diabetic fatty rat at 0.3 mg/kg, po administered once daily for 21 days followed by additional administration on day 22	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID136638	Percent reduction in area under glucose tolerance curve (AUC) was determined at 30 umol/kg dose of diet in mice	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID1532801	Cardioprotective activity in db/db BKS.Cg-Dock7m +/+ Leprdb/J mouse assessed as decrease in serum cTnI level at 27 umol/kg, po administered as daily dose via gavage for 18 days by ELISA	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID243396	Efficacy against human PPARgamma expressed in HepG2 cells relative to rosiglitazone	2005	Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17	Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
AID722392	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay	2013	Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1	New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.
AID1901248	Agonist activity at pBIND tagged human PPARdelta expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
AID1700135	Toxicity in rat primary hepatocytes assessed as effect on cell viability up to 10 uM by resazurin dye based assay
AID722376	Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells up to 10 uM after 20 hrs by luciferase reporter gene assay relative to WY-14643	2013	Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1	New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.
AID277010	Activity at human PPARalpha in CV1 cells at 10 uM relative to 2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID485554	Antihyperglycemic activity in C57BL/KsBom-db db/db mouse assessed as decrease in blood glucose AUC level at 100 mg/kg measured on day 5 by oral glucose tolerance test (Rvb = 30730 +/- 3687 %)	2010	Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11	Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
AID705486	Binding affinity to mouse cardiotrophin-like cytokine factor 1 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID299410	Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs	2007	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13	Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
AID1535246	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in CD36 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4	Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
AID1905851	Agonist activity at PPAR in oleic acid-induced steatosis in human HepaRG cells assessed as increase in FABP1 mRNA levels at 10 uM treated for 2 weeks with media replenishment along with compound and inducer for every 2 days by RT-qPCR analysis	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID156615	In vitro transactivation of human Peroxisome proliferator activated receptor delta (hPPARdelta); Not calculated for transactivation <25% at 30 uM	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1874138	Stabilization of PPARgamma LBD (unknown origin)/FITC-labeled PGC-1alpha (unknown origin) protein-protein interaction assessed as dissociation constant by fluorescence anisotropy assay	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID25996	Area under blood glucose time curve after OGTT on the 9th day of treatment	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1427974	Decrease in hepatocyte hypertrophy in KK-Ay diabetic mouse model at 10 mg/kg/day administered via oral gavage once daily for 21 days by haematoxylin and eosin staining based microscopic or morphometric method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID354040	Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARalpha expressed in Escherichia coli BL21 cells	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID244700	Effect (150 mg/kg) on PPAR gamma- mediated effects measured as change in brown adipose tissue weight in rats	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
AID317706	Inhibition of PPARgamma at 1 uM	2008	Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5	Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID483819	Antidiabetic activity in diet-induced obese mouse assessed as improvement of glucose tolerance at 5 mg/kg, ip QD for 13 days measured on day 14 after 12 hrs of fasting by glucose tolerance test	2010	Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11	Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1700094	Adipogenic activity in mouse 3T3-L1 cells assessed as increase in lipid content at 1 uM incubated for 6 days in presence of PPARg antagonist GW 9662 by Oil Red O dye fluorescence based assay
AID1874145	Stabilization of PPARgamma LBD (unknown origin) assessed as melting temperature in presence of GW9662 by differential scanning fluorimetry	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID637350	Hypoglycemic activity in diabetic KK-Ay mouse model assessed as decrease in glucose level at 10 mg/kg, po qd for 4 days relative to untreated control	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID722378	Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells up to 10 uM after 20 hrs by luciferase reporter gene assay	2013	Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1	New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression.
AID570001	Antidiabetic activity in ZDF fa/fa rat assessed as reduction of plasma glucose level at 10 mg/kg, po qd for 12 days by insulin tolerance test	2011	Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3	Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
AID414708	Agonist activity at human PPARgamma receptor by cell based transactivation assay	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
AID643916	Toxicity in po dosed db/db C57BLKS/J-m +/+ Leprdb mouse assessed as increase in water content of epididymal fat pad administered qd for 10 days measured on day 11 by vaccum drying method	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1708004	Binding affinity to GST-tagged PPARG LBD (unknown origin) by Fluormone Pan-PPAR Green tracer based TR-FRET assay
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1349993	Agonist activity at PPARgamma in mouse RAW264.7 cells assessed as increase in protein expression level in nuclear fractions at 30 uM after 24 hrs by Western blot assay relative to control	2018	Journal of natural products, 02-23, Volume: 81, Issue:2	An Anti-Inflammatory PPAR-γ Agonist from the Jellyfish-Derived Fungus Penicillium chrysogenum J08NF-4.
AID156132	Transcriptional activation by human PPAR alpha	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID306525	Agonist activity at PPARalpha receptor expressed in HEK293 cells by GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID1773623	Hepatoprotective activity in ob/ob mouse assessed as reduction in plasma alanine aminotransferase at 10 mg/kg, po administered once daily for 30 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID304337	Effect on glucose normalization in orally dosed ZDF rat after 7 days	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID1276075	Transactivation of PPARgamma in human primary preadipocytes assessed as increase in GTUT4 expression at 2 uM by qPCR method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID1400375	Induction of lipid accumulation in mouse 3T3L1 cells at 2 uM by Oil Red O staining-based assay	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID1700116	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in UCP1 mRNA expression by RT-PCR analysis
AID68774	Heart wt absolute in two week oral toxicity test in male F344/DuCrj rats after 50 mg/kg dose	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID276714	Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID727972	Toxicity in C57B6 DIO mouse assessed as body weight gain at 0.25 mg/g of food after 31 days	2013	ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1	Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes.
AID1395947	Agonist activity at human PPARdelta after 22 to 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16	Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.
AID1236828	Decrease in serum Hb1Ac level in C57BLKS/J-Lepr/Lepr db/db mouse at 10 mg/kg, po qd for 18 days administered via gavage by ELISA	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists.
AID705488	Binding affinity to afadin- and alpha-actinin-binding protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1543215	Agonist activity at human PPARgamma expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity at 10 uM by luciferase reporter gene assay relative to rosiglitazone
AID1440566	Binding affinity to PPARalpha (unknown origin) assessed as kinetic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1172127	Transactivation of human Gal4-PPARgamma LBD transfected in human HepG2 cells assessed as stimulation at 1 uM after 20 hrs by luciferase reporter gene assay relative to vehicle-treated control	2014	Journal of natural products, Dec-26, Volume: 77, Issue:12	Sterol fatty acid esters from the mushroom Hericium erinaceum and their PPAR transactivational effects.
AID637427	Effect on hematocrit level in Sprague-Dawley rat at 100 mg/kg after 28 days (Rvb = 47.5 +/- 0.6 %)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID421097	AUC in C57BLKS/J-m+/+Leprdb db/db mouse at 10 mg/kg, po once daily for 11 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1183852	Induction of Dectin-1 mRNA expression in mouse peritoneal macrophages isolated from PPARgamma -/- mouse treated at 1 uM for 5 hrs by qRT-PCR analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Protolichesterinic acid derivatives: α-methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors.
AID407777	Antihyperglycemic activity in C57BL/KsJ db/db mouse at 5 mg/kg, sc administered twice a day for 4 days once on day 5 immediately after load injection by insulin suppression test relative to control	2008	Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11	Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
AID280019	Reduction of blood glucose level in orally dosed db/db mouse at 1 mg/kg after 8 days	2007	Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5	Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
AID1905820	Agonist activity at yeast Gal4-fused human PPARalpha LBD transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID12878	Half-life was determined in rat after intravenous administration (0.5 mg/kg)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID68773	Relative wt in two week oral toxicity test in male F344/DuCrj rats after 50 mg/kg dose	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID1362855	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction in plasma glucose level at 3 mg/kg, po administered once daily for 14 days measured on day 15 relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID673437	Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16	Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists.
AID26202	In vivo blood glucose area under curve after oral glucose tolerance test in male db/db mice at 3 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID551967	Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1	Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.
AID276593	Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay relative to GW-2331	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID270627	Displacement of [3H]2-methyl-2-(4-{3-[propyl-(5-pyridin-2-yl-thiophene-2-sulfonyl)-amino]-propyl}-phenoxy)-propionic acid from human PPARgamma by SPA	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID1362901	Toxicity in F344/DuCrlCrlj rat assessed as reduction in RBC count at 50 mg/kg, po administered via gavage once daily for 28 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID277004	Displacement of [3H]2-methyl-2-(4-{3-propyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-pro-pyl}-phenoxy)-propionic acid from human PPARgamma	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID470058	Hypoglycemic effect in type 2 diabetic BALB/c mouse model assessed as reduction in blood glucose excursion at 100 to 200 mg/kg, po pretreated 60 mins before glucose challenge measured up to 3 hrs by one-touch glucometer relative to diabetic control	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID1507884	Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay relative to WY14643	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID678713	Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1901649	Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of Pdk4 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID223551	Binding affinity at human PPAR alpha	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID280963	Effect on fatty acid oxidation in rat L6 cells	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID260319	Displacement of [3H]L-783483 from human PPAR alpha by SPA assay	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
AID276990	Effect on glucose normalization in po dosed ZDF rat after 7 days	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID387511	Antihyperglycemic activity in db/db mouse assessed as increase in body weight at 3 mg/kg, po once daily after 28 days	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1156987	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID414709	Agonist activity at human PPARdelta receptor by cell based transactivation assay	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
AID453594	Antidiabetic effect in ob/ob mouse assessed as plasma insulin level at 20 mg/kg/day, po for 4 days (RVb = 21.28 +/- 7.5 ng/mL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID705504	Binding affinity to mouse cardiotrophin-like cytokine factor 1 precursor by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1561663	Partial agonist activity at recombinant N-terminal GFP-fused PPARgamma LBD (unknown origin) assessed as increase in biotinylated-SRC1 peptide recruitment measured after 2 hrs by HTRF assay	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID1597841	Upregulation of CD36 gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID705740	Binding affinity to mouse hepatocyte nuclear factor 6 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1285649	Displacement of [3H]rosiglitazone from human recombinant PPARgamma receptor expressed in Escherichia coli	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8	Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID745238	Antihyperglycemic activity in db/db mouse assessed as inhibition of post prandial blood glucose level at 30 mg/kg, po qd administered 15 days measured on day 10 by OGTT relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1466741	Cytotoxicity against HEK293 cells harboring beta-galactosidase expression plasmid assessed as effect on beta-galactosidase activity	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
AID115625	Minimum effective dose required for significant reduction in blood glucose in ob/ob mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
AID1499789	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as body weight at 10 mg/kg, po qd for 29 days measured on day 29 post last dose (Rvb = 533 +/- 10 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1488555	Antihyperglycemic activity in streptozotocin-induced diabetic Swiss albino rat assessed as decrease in blood glucose level at 2.7 mg/kg, po measured up to 3 hrs post dose relative to control	2017	Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.
AID475398	Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID1543216	Agonist activity at human PPARbeta/delta expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity at 10 uM by luciferase reporter gene assay relative to GW501516
AID372091	AUC in Sprague-Dawley rat at 150 mg/kg dosed daily for 2 weeks	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID662857	Competitive inhibition of human MAOA expressed in Pichia pastoris	2011	ACS medicinal chemistry letters, Oct-15, Volume: 3, Issue:1	Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
AID1874147	Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment in presence of GW9662 by HTRF assay	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID1427969	Hypoglycemic activity in KK-Ay diabetic mouse model assessed as increase in liver hepatic glycogen level at 10 mg/kg/day administered via oral gavage once daily for 4 weeks	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID431127	Hypolipidemic activity in KK-Ay mouse assessed as reduction in serum triglyceride level at 10 mg/kg, po for 6 weeks measured after 4 hrs post dose fasting	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID453566	Displacement of [3H2]nTZD3 from GST-tagged human PPARalpha at 10 uM expressed in Escherichia coli by SPA	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID240232	Mean effective concentration against human peroxisome proliferator-activated receptor gamma	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID236441	Area under plasma concentration time curve when administered to db/db mice at 10 mg/kg dose; Range = 250-700 uMh	2005	Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10	Selective PPARgamma modulators with improved pharmacological profiles.
AID731518	Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay	2013	Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4	Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
AID1700121	Induction of mitochondrial biogenesis in mouse 3T3-L1 cells assessed as increase in TFAM mRNA expression by RT-PCR analysis
AID236420	Area under concentration curve for the compound was determined in db/db mice plasma at 10 mg/kg on day 11	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID596764	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in triglyceride level at 1 uM after 8 days relative to control	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Isoprenylated flavonoids and adipogenesis-promoting constituents from Morus nigra.
AID1440543	Growth inhibition of human HT-29 cells assessed as cell vitality up to 10 uM up to 72 hrs by hemocytometry relative to control	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1224229	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	2014	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14	Thiazolidine-2,4-diones derivatives as PPAR-γ agonists: synthesis, molecular docking, in vitro and in vivo antidiabetic activity with hepatotoxicity risk evaluation and effect on PPAR-γ gene expression.
AID276993	Reduction of plasma triglyceride level in ZDF rat at 1 mg/kg, po after 7 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID1760204	Antidiabetic activity in KK-Ay mouse assessed as effect on serum Creatinine level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 124 +/- 35.1 uM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID28299	Maximum plasma concentration after oral administration at a dose 2.2 mg/kg	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1499817	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as triglyceride level per gram liver at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 163.4 +/- 8.3 mg)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1166248	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM by PPRE-driven luciferase reporter gene assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis, in silico molecular docking and biological evaluation of novel oxadiazole based thiazolidine-2,4-diones bis-heterocycles as PPAR-γ agonists.
AID1191334	Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay relative to Wy-14,643	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID91243	Agonist activity for Human PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID156237	In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID157111	In vitro Fold activation relative to maximum activation obtained with rosiglitazone (~ 120-fold corresponded to 100%) for human peroxisome proliferator activated receptor gamma	2003	Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2	Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID304335	Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID1499821	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as insulin level per gram pancreas at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 55.2 +/- 5.5 ug)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID705490	Binding affinity to mouse trace amine-associated receptor 7b by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID223558	Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma)	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID470057	Antidiabetic activity in BALB/c mouse type 2 diabetic model assessed as reduction of fasting blood glucose level at 2 mg/kg, po QD measured after 4 weeks by glucometry (Rvb=15.03 +/- 1.47 mmol/L)	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID675851	Displacement of pan-PPAR fluormone from PPARgamma LBD by TR-FRET based LanthaScreen assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID1700097	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in GLUT4 mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID1662159	Antidiabetic activity in C57 BL/Ks J-db/db mouse assessed as reduction in plasma triglyceride levels at 10 mg/kg after 6 days relative to control	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Anti-diabetic drugs recent approaches and advancements.
AID1716482	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as upregulation of PPAR signalling genes at 2 uM incubated for 8 days by Illumina sequencing method	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1422536	Agonist activity at human GAL4 fused PPARalpha-LBD expressed in human HepG2 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID635193	Induction of [14C]oleic acid oxidation in a human myotubes after 4 days by beta liquid scintillation counting	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
AID1901653	Agonist activity at human PPARgamma in mouse 3T3-L1 cells assessed as induction of cd36 mRNA expression at 10 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID156295	In vitro binding affinity towards human peroxisome proliferator activated receptor alpha (PPAR alpha)	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID1374676	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as change in plasma insulin level at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID156619	In vitro transactivation of human Peroxisome proliferator activated receptor delta (hPPARdelta)	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID599162	Insulin sensitizing activity in mouse 3T3L1 cells assessed as triglyceride accumulation by insulin-regulated cell differentiation assay	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
AID299413	Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs relative to rosiglitazone	2007	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13	Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
AID1535248	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4	Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
AID1440533	Binding affinity to PPARdelta (unknown origin) assessed as thermodynamic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID421048	Inhibition of human PPARalpha receptor by scintillation proximity assay	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID396054	Agonist activity at human PPARgamma in U2OS cells by transactivation assay	2008	European journal of medicinal chemistry, Nov, Volume: 43, Issue:11	Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.
AID1354477	Agonist activity at PPARgamma (unknown origin) expressed in human HepG2 cells cotransfected with PPREaP2-tk at 1.79 ug/ml after 24 hrs by luciferase reporter gene assay relative to control	2018	Journal of natural products, 05-25, Volume: 81, Issue:5	Bioactivity-Guided Isolation of Potential Antidiabetic and Antihyperlipidemic Compounds from Trigonella stellata.
AID141913	Agonist activity for murine PPAR gamma receptor in transcriptional activation assay	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID1572805	Binding affinity to recombinant human N-terminal His6-tagged NAF1 expressed in Escherichia coli by scintillation proximity assay	2019	Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7	Binding of thiazolidinediones to the endoplasmic reticulum protein nutrient-deprivation autophagy factor-1.
AID1374672	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as final insulin level in plasma at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting (Rvb = 7304 +/- 2967 pg/ml)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID1532830	Inhibition of human ERG expressed in CHO cells at 40 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1499927	Antidiabetic activity in Zucker rat chronic ob/ob model assessed as increase in plasma adiponectin level at 10 mg/kg, po qd for 31 days measured on day 32 by ELISA relative to control	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID277008	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from hPPARalpha	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID156285	Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID252361	Glucose concentration was measured in male db/db mouse after 10 mpk/day for 14 days	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID1874136	Stabilization of PPARgamma LBD (unknown origin) assessed as melting temperature at 14 uM by differential scanning fluorimetry	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID1611412	Transactivation of GAL4-fused human PPARalpha expressed in COS7 cells assessed as efficacy at 10 uM incubated for 24 hrs by luciferase reporter gene assay relative to WY-14643	2019	Bioorganic & medicinal chemistry, 12-15, Volume: 27, Issue:24	Synthesis of benzopyran derivatives as PPARα and/or PPARγ activators.
AID307135	Agonist activity at human PPARdelta by transactivation assay relative to carbacyclin	2007	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11	Design of potent PPARalpha agonists.
AID252362	Insulin concentration was measured in male db/db mouse after 10 mpk/day for 14 days	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID365541	Hypolipidemic activity in Zucker diabetic fa/fa rat assessed as reduction in total cholesterol level at 30 mg/kg/day, po for 14 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID268111	Transactivation of PPARgamma in CV1 cells	2006	Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14	Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1874148	Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment in presence of SR16832 by HTRF assay	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID1597845	Upregulation of PLIN1 gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1905844	Reduction of lipid accumulation in oleic acid-induced steatosis in human HepaRG cells at 10 uM treated for 24 hrs by Oil Red O staining based microscopy	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID1063322	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured after 12 hrs by ELISA (Rvb = 11.8 +/- 1.2 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID141910	Agonist activity for murine PPAR delta receptor in transcriptional activation assay; IA means inactive at 10 uM	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID156133	In vitro activation of human peroxisome proliferator activated receptor alpha	2003	Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2	Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID362019	Agonist activity at PPARgamma expressed in mouse NIH3T3 cells assessed as maximum activation at 10 uM after 16 hrs by reporter gene assay	2008	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16	Polychlorinated compounds with PPAR-gamma agonistic effect from the medicinal fungus Phellinus ribis.
AID1810338	Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID587346	Antidiabetic activity in rat hemidiaphragm assessed as glucose uptake at 1 mg after 45 mins in presence of insulin	2011	European journal of medicinal chemistry, Mar, Volume: 46, Issue:3	Synthesis, glucose uptake activity and structure-activity relationships of some novel glitazones incorporated with glycine, aromatic and alicyclic amine moieties via two carbon acyl linker.
AID1597806	Agonist activity at PPARalpha in C57BL/6N mouse primary hepatocytes assessed as activation of Scd1 mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1760238	Induction of glycolysis in human HepG2 cells assessed as reduction in lactate release at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID372056	Agonist activity at dog PPARalpha	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1217709	Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID276722	Reduction of plasma glucose in db/db mouse at 30 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1172789	Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID1351158	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 6 hrs by ELISA (Rvb = 11922 +/- 628.4	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID296182	Reduction in plasma triglyceride level in alloxan-induced diabetic mouse at 30 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID476882	Agonist activity at PPARgamma assessed as transcriptional activation	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID114052	Nonfasting insulin after 7 days treatment in male db/db mice	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1231389	Lipophilicity, log P of the compound	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.
AID276613	Increase in body weight in orally dosed db/db mouse at 3 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID768601	Agonist activity at LXRbeta in mouse RAW264.7 cells assessed as induction of ABCA1 promoter activation at 1 uM after 24 hrs by Dual-Glo luciferase reporter gene assay relative to vehicle-treated control	2013	Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15	Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation.
AID1499769	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as blood insulin AUC (0 to 120 min) at 10 mg/kg, po qd for 31 days measured on day 29 post dose (Rvb = 1503 +/- 160 ug.min/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID252205	Effect (150 mg/kg) on PPAR gamma- mediated effects measured as change in body weight in rats	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
AID1597843	Upregulation of FABP4 gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1532803	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation at 2 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1700111	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in ACOT2 mRNA expression by RT-PCR analysis
AID238856	Binding affinity for human peroxisome proliferator activated receptor alpha	2004	Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17	Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID421114	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 10 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID280958	Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID1156985	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID1174866	Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells assessed as maximum fold induction by luciferase reporter gene assay relative to Wy-14643	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID1363006	Toxicity in Wistar-Imamichi rat assessed as reduction in RBC count at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID475412	Hypolipidemic activity in db/db mouse assessed as serum triglyceride level at 10 mg/kg, po QD after 14 days (Rvb= 1.03 +/- 0.29 m/mol)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1239207	Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16	Novel Oxazolidinone-Based Peroxisome Proliferator Activated Receptor Agonists: Molecular Modeling, Synthesis, and Biological Evaluation.
AID111558	In vivo blood glucose level in male db/db mice after administration of 3 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1427948	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in HbA1C level at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID1532813	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID424501	Lipid lowering effect in po dosed C57BL/6J ob/ob mouse assessed as triglyceride level relative to untreated control	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID241843	Inhibition of human Peroxisome proliferator activated receptor gamma	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID1191353	Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID1760220	Effect on high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as water intake at 5 mg/kg, po (Rvb = 21.2 +/- 4.17 ml/day)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID588210	Human drug-induced liver injury (DILI) modelling dataset from Ekins et al	2010	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12	A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID642734	Agonist activity at human PPARgamma expressed in MG-63 cells at 2 times EC50 concentration by reporter gene-based transactivation assay relative to PPARgamma full agonist	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARγ partial agonists.
AID1362886	Cmax in F344/DuCrlCrlj rat at 50 mg/kg, po via gavage measured on day 28 post dose	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1172793	Effect on body weight in Wistar rat model of streptozotocin-induced diabetes at 36 mg/kg, po measured over 15 days	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID276983	Displacement of tritium labeled ligand from human PPARalpha by SPA assay	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID156949	In vitro transactivation of human Peroxisome proliferator activated receptor gamma	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1901641	Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID421111	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 3 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1760235	Anti-diabetic activity in high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed as improved pathological changes in kidney at 5 mg/kg, po by hematoxylin and eosin staining based histopathological analysis	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID387504	Antihyperglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 0.3 mg/kg, po once daily after 28 days relative to non-fasting control	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1532842	Inhibition of MDA level in TNF-alpha-induced insulin resistant mouse 3T3L1 cells 10 uM after 48 hrs	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID251616	Effect (150 mg/kg) on PPAR gamma- mediated effects measured as change in hematocrit weight in rats	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
AID1878209	Transactivation of Gal4-fused human PPARdelta expressed in CHO cells co expressing pG5-Luc reporter at 1 uM	2022	Bioorganic & medicinal chemistry letters, 03-01, Volume: 59	Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
AID422622	Displacement of [3H2]nTZD3 from GST-tagged human recombinant PPARgamma by scintillation proximity assay	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by nitroalkene fatty acids: importance of nitration position and degree of unsaturation.
AID270643	Lowering of glucose level in ZDF rat plasma at 1 mg/kg/day, po	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID1499892	Toxicity in Zucker rat chronic ob/ob model assessed as change in body weight at 10 mg/kg, po qd for 28 days measured on day 1 to 28 during compound dosing (Rvb = 9.9 +/- 1.27 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1561625	Inhibition of N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as S245 phosphorylation level at 10 uM by phospho gel stain method relative to control	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	Insights into PPARγ Phosphorylation and Its Inhibition Mechanism.
AID431045	Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID1488557	Displacement of fluormone-PPARgamma green from GST-tagged PPARgamma-LBD (unknown origin) by fluorescence polarization assay	2017	Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17	Design, synthesis, molecular modeling and anti-hyperglycemic evaluation of quinazolin-4(3H)-one derivatives as potential PPARγ and SUR agonists.
AID670832	Antidiabetic activity in rat L6 cells assessed as stimulation of glucose uptake at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Synthesis of novel imbricatolic acid analogues via insertion of N-substituted piperazine at C-15/C-19 positions, displaying glucose uptake stimulation in L6 skeletal muscle cells.
AID372104	AUC in obese insulin-resistant Zucker fa/fa rat at 1 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1362893	Toxicity in F344/DuCrlCrlj rat assessed as clinical abnormality at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID424502	Glucose lowering effect in po dosed C57BL/6J ob/ob mouse assessed as glycemia relative to untreated control	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1236827	Decrease in serum insulin level in C57BLKS/J-Lepr/Lepr db/db mouse at 10 mg/kg, po qd for 18 days administered via gavage by ELISA	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists.
AID475400	Agonist activity at human GAL4-tagged PPARdelta chimeric receptor expressed in HEK cells at 30 uM by transactivation assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID1351152	Inhibition of Pseudomonas aeruginosa PAO1 GFP-fused quorum sensing lasB at 10 uM measured every 15 mins up to 12 hrs by GFP reporter gene assay relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID610309	Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10	Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
AID414707	Agonist activity at human PPARalpha receptor by cell based transactivation assay	2009	Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8	Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
AID1251341	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1767825	Inhibition of osteoblast differentiation in rat UMR106-06 cells assessed as reduction in alkaline phosphatase activity measured by microplate reader analysis	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1700115	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in PGC1-alpha mRNA expression by RT-PCR analysis
AID1362858	AUC (0 to 24 hrs) in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1236826	Decrease in fasting blood glucose level in C57BLKS/J-Lepr/Lepr db/db mouse at 10 mg/kg, po qd for 18 days administered via gavage by ELISA	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists.
AID348508	Agonist activity at human PPARdelta ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity at 0.2 uM by transactivation assay	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID365526	Agonist activity at PPARgamma expressed in human HepG2 cells at 0.2 uM assessed as induction of receptor transactivation by reporter gene assay relative to control	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID1716493	Agonist activity at human PPARgamma in 8 day differentiated human SGBS cells assessed as decrease in IL-1 beta gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1427960	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in blood glucose level at 10 mg/kg/day administered via oral gavage once daily measured on day 19 at 30 to 60 mins post insulin challenge by insulin tolerance test	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID750247	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of total cholesterol level in blood at 50 mg/kg, po administered for 6 weeks measured on 2nd week (Rvb = 3.5 +/- 0.2 mmol/l)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID1546896	Binding affinity to mouse MPC	2020	Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10	The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.
AID28252	Oral half life was reported	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID708121	Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.
AID485563	Antiinflammatory activity against carrageenan-induced pleurisy in po dosed mouse assessed as inhibition of leukocyte infiltration administered 1 hr before carrageenan challenge measured after 6 hrs by hemocytometry relative to untreated control	2010	Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11	Synthesis and anti-inflammatory activity of new arylidene-thiazolidine-2,4-diones as PPARgamma ligands.
AID421050	Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1700131	Agonist activity at PPARg in hMADS white adipocytes assessed as increase in adiponectin mRNA expression at 10 to 1000 nM by RT-PCR analysis
AID599164	Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay relative to rosiglitazone	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
AID111561	In vivo % reduction of blood glucose level in male db/db mice after administration of 1 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID260320	Displacement of [3H]rosiglitazone from human PPAR gamma by SPA assay	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
AID220383	In vivo plasma triglyceride in db/db mouse after 11 days at 10 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID26200	In vivo blood glucose area under curve after oral glucose tolerance test in male db/db mice at 1 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1532834	Toxicity in po dosed ICR mouse administered as single dose via gavage treated on day 1 and measured daily up to 14 days	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID372079	AUC in db/db mouse at 10 mg/kg, po administered once daily for 11 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID673436	Binding affinity to GST-tagged PPARgamma LBD at 50 uM after 4 hrs by TR-FRET competitive binding assay	2012	Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16	Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists.
AID1166250	Antidiabetic activity in streptozotocin induced diabetic Albino Wistar rat model assessed as blood glucose level at 36 mg/kg, po by glucose oxidase method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis, in silico molecular docking and biological evaluation of novel oxadiazole based thiazolidine-2,4-diones bis-heterocycles as PPAR-γ agonists.
AID1174869	Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID635240	Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
AID331062	Reduction of fasting blood glucose in DIO C57BL/6 mouse model at 5 mg/kg, po assessed as glucose level by glucose tolerance test	2007	Nature, Nov-29, Volume: 450, Issue:7170	Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes.
AID357421	Activation of PPARgamma L465A mutant-mediated transcriptional activity assessed as Gal4 reporter activity	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID1351176	Anti-inflammatory activity in LPS-induced sepsis shock mouse model assessed as survival rate at 1 mg/kg, iv pretreated daily for 5 days followed LPS treatment on day 5 at 1 hr post last dose and measured after 7 days relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID733020	Antidiabetic activity in KKAy diabetic mouse model assessed as reduction in blood glucose level at 1 mg/kg/day administered through feeding for 3 days measured on day 4 relative to vehicle-treated control	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID1532831	Toxicity in ICR mouse assessed mouse mortality at 5000 mg/kg, po administered as single dose via gavage treated on day 1 and measured daily up to 14 days	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID637381	Hypoglycemic activity in diabetic KK-Ay mouse model assessed as decrease in glucose level at 10 mg/kg, po qd for 14 days (Rvb = 648.4 +/- 77.1 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1191333	Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID308431	Agonist activity at human PPARalpha by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16	Design of a partial PPARdelta agonist.
AID675856	Octanol-water partition coefficient, log P of the compound	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID354057	Antidiabetic activity in db/db mouse diabetic model assessed as reduction in post prandial blood glucose level at 3 mg/kg/day	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID701820	Reduction in body weight in diabetic C57BL/KsJ db/db mouse model in hyperglycemia at 25 mg/kg, po qd for 10 days relative to untreated control	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID491648	Antidiabetic activity in db/db mouse assessed as weight gain at 3 to 10 mg/kg, po qd for 7 days	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID28315	Maximum plasma concentration in rat after peroral administration	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1700095	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in SREBP mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID1172794	Increase in PPARgamma gene expression in mouse 3T3L1 cells at 10 uM incubated for 24 hrs by RT-PCR method	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID115316	In vivo nonfasting triglyceride in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID717961	Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay	2012	Journal of natural products, Dec-28, Volume: 75, Issue:12	PPARγ agonist from Chromolaena odorata.
AID1351175	Anti-inflammatory activity in LPS-induced sepsis shock mouse model assessed as survival rate at 20 mg/kg, iv pretreated daily for 5 days followed LPS treatment on day 5 at 1 hr post last dose and measured after 7 days relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID234402	Maximum achieved Nonfasted triglycerides reduction relative to vehicle treated control group	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID124442	Maximum achieved triglycerides reduction relative to vehicle treated control group	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID458856	Displacement of [3H]rosiglitazone from rat liver mitochondrial mitoNEET by scintillation counting	2010	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3	Structure-based design of a thiazolidinedione which targets the mitochondrial protein mitoNEET.
AID1767817	Antidiabetic activity in high fat diet-induced obese C57/B6 mouse model assessed as reduction in glucose level at 4 mg/kg, measured after 30 days by glucose tolerance test	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID1700090	Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as recruitment of MED1 incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
AID1734993	Hypoglycemic activity in Zucker fatty diabetes mellitus rat model assessed as increase in insulin levels in plasma at 3 mg/kg, po administered for 21 days and measured at 10 to 60 mins post glucose challenge on day 1 by OGTT	2016	Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24	The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
AID465712	Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Acidic elements in histamine H(3) receptor antagonists.
AID1449628	Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID639523	Cytotoxicity against human HepG2 cells assessed as glucose consumption at 10 uM by MTT assay in presence of insulin	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological activity of novel barbituric and thiobarbituric acid derivatives against non-alcoholic fatty liver disease.
AID1363011	Toxicity in Wistar-Imamichi rat assessed as effect on hemodilution by measuring increase in heart weight at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1532763	Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells at 10 uM preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID276094	Lowering of plasma insulin level in DIO C57BL/6J mouse at 5 mg/kg, po after 4 hr fasting	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID465711	Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Acidic elements in histamine H(3) receptor antagonists.
AID240119	Effective concentration for human peroxisome proliferator-activated receptor alpha	2005	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5	Structure-activity relationships of dimeric PPAR agonists.
AID29634	Oral bioavailability	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID476883	Agonist activity at PPARgamma assessed as transcriptional activation relative to GI262570	2010	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7	Discovery of a novel selective PPARgamma modulator from (-)-Cercosporamide derivatives.
AID258098	Decrease in blood glucose level in male db/db mice administered at 30 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 16, Issue:2	Substituted indanylacetic acids as PPAR-alpha-gamma activators.
AID597760	Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	2011	Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10	Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.
AID690962	Antihyperglycemic activity in streptozotocin-induced type 2 diabetic Wistar albino rat assessed as reduction in plasma glucose level at 30 mg/kg, po by glucometer	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20	Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents.
AID740611	Insulin sensitizing activity in po dosed high fat diet-induced insulin resistant obese mouse model assessed as reduction in glucose infusion rate by hyperinsulinemic-euglycemic clamp test (Rvb =12.8 mg/min/kg)	2013	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8	Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors.
AID156788	Agonistic activity against PPAR (peroxisome proliferator activated receptor gamma) in Suarus chinesis	2004	Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1	Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
AID387503	Antihyperglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 0.1 mg/kg, po once daily after 28 days relative to non-fasting control	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID199647	In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID1499869	Antidiabetic activity in Zucker rat chronic ob/ob model assessed as blood glucose AUC (0 to 120 min) at 10 mg/kg, po qd for 31 days measured on day 28 post dose by OGTT (Rvb = 62198 +/- 4121 mg.min/dL)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1905823	Agonist activity at yeast Gal4-fused human PPARgamma transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry relative to control	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID429216	Antidiabetic activity in ob/ob mouse assessed as decrease in plasma glucose level at 10 mg, po measured on day 14	2009	European journal of medicinal chemistry, Aug, Volume: 44, Issue:8	Synthesis and evaluation of some novel isochroman carboxylic acid derivatives as potential anti-diabetic agents.
AID1773621	Downregulation of ACC gene expression in ob/ob mouse liver at 10 mg/kg, po administered once daily for 30 days by quantitative RT-PCR analysis	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID750245	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of total cholesterol level in blood at 50 mg/kg, po administered for 6 weeks (Rvb = 3.3 +/- 0.5 mmol/l)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID1499907	Toxicity in Zucker rat chronic ob/ob model assessed as serum triglyceride level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 329 +/- 36 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1499856	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum adiponectin level at 10 mg/kg, po qd for 4 days by ELISA (Rvb = 9.1%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1532804	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation at 4 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID453765	Antidiabetic in ZDF rat assessed as plasma triglycerides level at 3 mg/kg/day, po for 2 weeks (RVb = 1579 +/- 244 mg/dL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID1499825	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum triglyceride level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 1382 +/- 268 mg/dl)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID444054	Oral bioavailability in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1499916	Toxicity in Zucker rat chronic ob/ob model assessed as serum AST level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 180 +/- 26 U/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID296177	Reduction in plasma glucose level in alloxan-induced diabetic mouse at 30 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID775854	Displacement of fluormone from human PPARgamma LBD expressed in Escherichia coli BL21 DE3 by fluorescence polarization assay	2013	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21	Structure-based identification of novel PPAR gamma ligands.
AID643839	Partial agonist activity at human PPARgamma LBD assessed as activation of Src-1 by HTRF assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1180479	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay	2014	Journal of natural products, Jul-25, Volume: 77, Issue:7	Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.
AID1878207	Transactivation of Gal4-fused human PPARgamma expressed in CHO cells co expressing pG5-Luc reporter at 1 uM	2022	Bioorganic & medicinal chemistry letters, 03-01, Volume: 59	Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
AID280006	Reduction of FFA level in ZDF rat at 10 mg/kg, po after 21 days	2007	Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5	Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
AID136640	Percent reduction in area under glucose tolerance curve at 300 uM/kg dose in diet of mice.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID678712	Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins	2012	Chemical research in toxicology, Oct-15, Volume: 25, Issue:10	Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID306522	Intrinsic activity at PPARgamma receptor expressed in HEK293 cells at 1 uM by GAL4 transactivation assay relative to rosiglitazone	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID639526	Induction of adipogenesis in mouse 3T3L1 cells assessed as decrease of leptin level at 10 uM after 24 hrs (Rvb = 3089.21 +/- 33.37 pg/ml)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological activity of novel barbituric and thiobarbituric acid derivatives against non-alcoholic fatty liver disease.
AID1419241	Competitive displacement of fluorescently labelled PPAR tracer ligand from GST-tagged human PPARgamma ligand binding domain after 1 hr in dark by TR-FRET competitive binding assay	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.
AID276604	Reduction of plasma triglycerides in orally dosed db/db mouse at 30 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID12877	Half-life was determined by iv administration (1.5 mg/kg) in fasted male Sprague-Dawley rats	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID712390	Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID1600822	Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method	2019	Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19	Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.
AID1677547	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 0.03 to 3 uM after 48 hrs by SRB assay	2020	Journal of natural products, 10-23, Volume: 83, Issue:10	CRISPR-Cas9 Genome-Wide Knockout Screen Identifies Mechanism of Selective Activity of Dehydrofalcarinol in Mesenchymal Stem-like Triple-Negative Breast Cancer Cells.
AID1156986	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID156377	In vitro binding affinity for human PPAR gamma receptor using scintillation proximity assay (SPA)	2004	Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12	(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
AID1716462	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in ADIPOQ gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID344819	Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay	2008	Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21	Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
AID1767824	Induction of osteoblast differentiation in rat UMR106-06 cells assessed as reduction in mineralization measured after 48 hrs by alizarin red S staining-based method	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID246567	Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivation	2005	Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10	Selective PPARgamma modulators with improved pharmacological profiles.
AID276588	Displacement of radiolabeled GW-2331 from human PPAR alpha by SPA assay at 100 uM	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID656883	Antihyperglycemic activity in C57BL/Ks db/db mouse assessed as reduction of glycosylated hemoglobin level using HbA1c reagent at 50 mg/kg, po after 2 to 6 weeks relative to control	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID1191336	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay relative to rosiglitazone	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID1760192	Antidiabetic activity in KK-Ay mouse assessed as effect on cholesterol level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 7.38 +/- 1.03 mM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID372044	Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1700088	Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as displacement of SMRT incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
AID239803	Mean percent of maximum efficacy against human peroxisome proliferator-activated receptor gamma	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID730956	Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay	2013	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3	Design, development and evaluation of novel dual PPARδ/PPARγ agonists.
AID1874137	Binding affinity to PPARgamma LBD (unknown origin) assessed as dissociation constant followed by heating for 3 mins by Bradford assay	2022	Bioorganic & medicinal chemistry, 08-15, Volume: 68	Indazole MRL-871 interacts with PPARγ via a binding mode that induces partial agonism.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1633588	Agonist activity at PPARgamma in human HepG2 cells assessed as increase in GLUT1 RNA expression at 10 uM incubated for 48 hrs by qRT-PCR analysis relative to control	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.
AID1760178	Antidiabetic activity in KK-Ay mouse assessed as effect on glycosylated haemoglobin level at 5 mg/kg, po for 50 days by glucose oxidase method (Rvb = 8.74 +/- 1.08%)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID354042	Agonist activity at human PPARalpha by luciferase reporter transactivation assay	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID276092	Effect on body weight in DIO C57BL/6J mouse at 5 mg/kg, po	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
AID243335	Activation of peroxisome proliferator-activated receptor gamma in reporter gene assay: most active	2005	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6	Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2.
AID1700138	Toxicity in rat primary hepatocytes assessed as induction of apoptosis up to 10 uM by caspase 3/7 activity detection based assay
AID587345	Antidiabetic activity in rat hemidiaphragm assessed as glucose uptake at 2 mg after 45 mins in presence of insulin	2011	European journal of medicinal chemistry, Mar, Volume: 46, Issue:3	Synthesis, glucose uptake activity and structure-activity relationships of some novel glitazones incorporated with glycine, aromatic and alicyclic amine moieties via two carbon acyl linker.
AID1700096	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in CEBPA mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID233277	Selectivity ratio for Antihyperglycemic potency dose and No significant effect dose	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID255009	Inhibitory concentration against human peroxisome proliferator activated receptor gamma in SPA assay	2005	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22	Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
AID276725	Reduction of hematocrit in db/db mouse at 3 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID156241	In vitro transcriptional activation of peroxisome proliferator activated delta-receptor (PPAR) expressed in CV-1 cells; Inactive	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
AID276586	Displacement of radiolabeled darglitazone from human PPAR gamma by SPA binding assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID268117	Antiproliferative activity against human keratinocytes	2006	Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14	Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
AID675862	Displacement of pan-PPAR fluormone from PPARalpha LBD at >= 100 uM by TR-FRET based LanthaScreen assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID1716498	Agonist activity at human PPARgamma in 8 day differentiated human SGBS cells assessed as decrease in IL-6 beta gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID308793	Reduction in blood glucose level in db/db mouse at 10 mg/kg, po	2007	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15	Indanylacetic acids as PPAR-delta activator insulin sensitizers.
AID1700112	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in FBXO31 mRNA expression by RT-PCR analysis
AID705510	Binding affinity to chorionic somatomammotropin hormone 2 precursor in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID421150	Toxicity in Sprague-Dawley rat assessed as increase in heart weight at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1468752	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PNRC1 (302 to 327 residues) co-activator recruitment by measuring Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID705503	Binding affinity to RasGTPase-activating protein SynGAP in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1610426	Increase in glucose consumption in human HepG2 cells assessed as glucose content in medium at 10'-6 M measured after 24 hrs by glucose oxidase method relative to control	2019	Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23	Novel berberine-based derivatives with potent hypoglycemic activity.
AID1231372	Activity at human PPARgamma transfected in HEK293 cells assessed as transactivation activity by reporter gene assay luciferase relative to rosiglitazone	2015	Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14	Peroxisome Proliferator-Activated Receptor γ (PPARγ) and Ligand Choreography: Newcomers Take the Stage.
AID305558	Reduction in glucose level in ZDF rat at 1 mg/kg, po after 7 days	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID1716476	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as increase in CEBPA mRNA expression at 2 uM measured on day 4 by qRT-PCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID157264	Transcriptional activation of peroxisome proliferator activated receptor gamma	1999	Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23	Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
AID316708	Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
AID643923	Antidiabetic activity in obese insulin resistant Zucker fa/fa rat assessed as decrease in insulin level in plasma at 1 to 100 mg/kg qd for 7 days	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1543221	Cytotoxicity against HUVEC assessed as reduction in cell viability at 30 uM incubated for 24 hrs by MTT assay
AID357437	Activation of PPARgamma I472A mutant-mediated transcriptional activity assessed as Gal4 reporter activity	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID306520	Displacement of fluorescein labeled ligand from PPARgamma receptor by fluorescence polarization assay	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID306521	Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID1700071	Agonist activity at GAL4-tagged PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation at 5 uM incubated for 16 hrs by luciferase reporter gene assay relative to control
AID1561635	Inhibition of N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as S245 phosphorylation level at 10 uM by phospho gel stain method relative to control	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	Insights into PPARγ Phosphorylation and Its Inhibition Mechanism.
AID157124	Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells	1998	Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25	N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
AID444055	Fraction absorbed in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID113349	In vivo nonfasting blood glucose in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1167329	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Synthesis and anti-tumor activity of glycosyl oxadiazoles derivatives.
AID1507885	Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1174870	Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells assessed as maximum fold induction by luciferase reporter gene assay relative to rosiglitazone	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID1716461	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in FABP4 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID643927	Toxicity in obese insulin resistant Zucker fa/fa rat assessed as increase in heart weight at >= 10 mg/kg	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID772913	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin	2013	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20	Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.
AID1499913	Toxicity in Zucker rat chronic ob/ob model assessed as serum ALT level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 127 +/- 9 U/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1716475	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as increase in PPARG mRNA expression at 2 uM measured on day 4 by qRT-PCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID666827	Toxicity in Wistar-Imamichi rat assessed as increase heart weight at 30 to 100 mg/kg, po qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1468737	Displacement of N-terminal biotin-labeled SMRT-ID1 (2339 to 2363 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1760246	Induction of glycolysis in rat L6 cells assessed as reduction in lactate release at 20 uM measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1362887	Tmax in F344/DuCrlCrlj rat at 50 mg/kg, po via gavage measured on day 28 post dose	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID643925	Antidiabetic activity in obese insulin resistant Zucker fa/fa rat assessed as decrease in insulin level in plasma administered qd for 7 days	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1543217	Agonist activity at human RXRalpha expressed in African green monkey COS7 cells assessed as increase in receptor transcriptional activity at 10 uM by luciferase reporter gene assay relative to 9-cis-retinoic acid
AID1349992	Agonist activity at full length human flag-tagged PPARgamma1 LBD expressed in rat Ac2F cells coexpressing PPRE-X3-TK at 5 uM after 6 hrs by one-glo luciferase reporter gene assay	2018	Journal of natural products, 02-23, Volume: 81, Issue:2	An Anti-Inflammatory PPAR-γ Agonist from the Jellyfish-Derived Fungus Penicillium chrysogenum J08NF-4.
AID305541	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl butyric acid from human PPARdelta	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID717059	Antidiabetic activity in db/db mouse type 2 diabetic model assessed as reduction of plasma triglyceride level at 10 mg/kg, po administered for 14 days	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
AID1572806	Binding affinity to NAF1 (unknown origin) expressed in human HepG2 cells assessed as inhibition of mitochondrial respiration at 30 uM	2019	Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7	Binding of thiazolidinediones to the endoplasmic reticulum protein nutrient-deprivation autophagy factor-1.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1468745	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled SRC1 (619 to 643 residues) co-activator recruitment by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID156939	In vitro potency of PPAR gene activation against human PPAR gamma receptor using chimeric Gal4-hPPAR transactivation assay (TA)	2004	Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12	(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
AID1251345	Solubility of the compound	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID712712	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation at 1 uM by oil red O staining based spectrophotometric analysis	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID1231390	Drug absorption in orally dosed human	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.
AID1700070	Adipogenic activity in mouse 3T3-L1 cells assessed as increase in lipid content at 0.1 uM incubated for 10 days by fluorescence based assay
AID1499809	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as liver weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 28 +/- 1.6 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID276721	Reduction of plasma glucose in db/db mouse at 3 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID705739	Binding affinity to mouse protein kinase C and casein kinase substrate in neurons protein 2 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID705501	Binding affinity to mouse membrane transport protein XK by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1217727	Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID705325	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Synthesis and biological evaluation of 5-benzylidenepyrimidine-2,4,6(1H,3H,5H)-trione derivatives for the treatment of obesity-related nonalcoholic fatty liver disease.
AID13633	Oral bioavailability in rat (Sprague-Dawley) (fasted male) (dose 10 mg/kg)	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID304334	Agonist activity at human PPARalpha expressed in CV1 cells by receptor transactivation assay	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID745234	Antidyslipidemic activity in db/db mouse assessed as decrease in plasma triglycerides level at 30 mg/kg, po qd administered 15 days measured on day 16 by ELISA relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID588209	Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset	2010	Chemical research in toxicology, Jul-19, Volume: 23, Issue:7	Developing structure-activity relationships for the prediction of hepatotoxicity.
AID344822	Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay relative to Wy-14,643	2008	Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21	Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.
AID156141	In vitro transcriptional activation by human PPAR alpha Gal4 chimera; Not active	2004	Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12	(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
AID431138	Adipogenic activity in monosodium L-glutamate-treated obese Wistar rat assessed as reduction in liver triglyceride content at 5 mg/kg, po after 6 weeks	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID260992	Effect on PPARgamma transactivation activity in U2OS cells	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
AID348772	Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Analogues of 2-phenyl-ethenesulfonic acid phenyl ester have dual functions of inhibiting expression of inducible nitric oxide synthase and activating peroxisome proliferator-activated receptor gamma.
AID1362904	Toxicity in F344/DuCrlCrlj rat assessed as increase in heart weight at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID680563	TP_TRANSPORTER: inhibition of estrone-3-sulfate uptake (Estrone-3-sulfate: 9.2 nM) by Rosiglitazone at a concentration of 10uM in OATP-C-expressing Xenopus oocytes	2004	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3	Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID156777	In vitro binding affinity towards human peroxisome proliferator activated receptor delta (PPAR delta)	2003	Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5	Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists.
AID1700128	Induction of adipocyte browning in hMADS white adipocytes assessed as increase in UCP1 protein expression at 0.1 uM by immunodetection analysis
AID1266977	Antidyslipidemic activity in ZDF rat assessed as VLDL level at 0.3 mg/kg for 9 days by FPLC analysis (Rvb = 35 mg/dL)	2015	Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24	Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
AID256776	Functional activity at human PPAR gamma in Huh7 cells by transactivation assay	2005	Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26	Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
AID1217706	Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1597815	Agonist activity at PPARalpha in C57BL/6N mouse primary hepatocytes assessed as activation of PPARalpha mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID1760231	Anti-diabetic activity in high fat diet-fed KK-Ay mouse model of obesity and diabetes assessed reduction in total protein level in urine at 5 mg/kg, po measured after 24 hrs	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID570002	Antidiabetic activity in ZDF fa/fa rat assessed as reduction of body weight at 10 mg/kg, po qd for 12 days	2011	Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3	Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
AID421085	Antidiabetic activity in ob/ob mouse assessed as reduction in plasma triglyceride levels at 1 mg/kg, po once daily for 5 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID599163	Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
AID1168705	Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
AID162627	Binding affinity against Peroxisome Proliferator activated receptor alpha (PPAR alpha); Not active	1999	Bioorganic & medicinal chemistry letters, Dec-06, Volume: 9, Issue:23	Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
AID1785798	Agonist activity at human PPARalpha at 10 uM	2021	ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11	Synthesis of 2-Prenylated Alkoxylated Benzopyrans by Horner-Wadsworth-Emmons Olefination with PPARα/γ Agonist Activity.
AID255669	In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay	2005	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20	Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
AID1543232	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells at 1 uM treated for 20 hrs post 48 hrs after control siRNA transfection foll
AID372076	Antihyperglycemic activity in db/db mouse assessed as reduction in blood glucose level at 10 mg/kg, po administered once daily for 11 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID387505	Antihyperglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 1 mg/kg, po once daily after 28 days relative to non-fasting control	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID775855	Binding affinity to human PPARgamma LBD expressed in Escherichia coli BL21 DE3 assessed as melting temperature at 33 uM after 2 hrs using SYPRO orange dye (Rvb = 48 degC)	2013	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21	Structure-based identification of novel PPAR gamma ligands.
AID94673	The hypoglycemic activity in diabetic KK mice, activity expressed as % decrease in blood glucose (21h)	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID270648	Increase in body weight in ZDF rat at 1 mg/kg, po relative to control	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID440654	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
AID156146	In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha)	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID270634	Transactivation of murine PPARalpha in CV1 cells by luciferase reporter gene assay	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID260995	Effect on PPARalpha transactivation activity in U2OS cells relative to reference	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
AID305547	Efficacy at human Gal4-PPARdelta expressed in CV1 cells at 10 uM relative to control by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID666814	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction of non-fasting plasma glucose level at >1 mg/kg, po qd for 12 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1362972	Toxicity in Zucker diabetic fatty rat assessed as body weight gain at 3 mg/kg, po administered once daily for 14 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1503447	Activation of AMPK in palmitate-induced insulin-resistant human HepG2 cells assessed as increase in AMPK phosphorylation at 12.5 uM incubated for 24 hrs by Western blot method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID1905822	Agonist activity at yeast Gal4-fused human PPARgamma transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID1276064	Transactivation of PPARgamma in human primary preadipocytes assessed as adipocyte differentiation at 2 uM by Oil Red O staining-based assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID1810342	Agonist activity at human PPARgamma transfected in COS-7 cells assessed maximum luciferase activity measured after 24 hrs by cell based luciferase transactivation assay relative to rosiglitazone	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID772910	Transactivation of GAL4 DNA binding domain-fused human PPAR-gamma ligand binding domain transfected in African green monkey CV1 cells at 1 uM after 24 hrs by luciferase reporter gene assay	2013	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20	Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.
AID1753552	Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay	2021	European journal of medicinal chemistry, Jun-05, Volume: 218	Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
AID666820	Toxicity in Wistar-Imamichi rat assessed as increase in body weight at 30 to 100 mg/kg, po qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID372095	Antidiabetic activity in obese insulin-resistant Zucker fa/fa rat assessed as plasma glucose level at 0.1 to 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID1362863	Tmax in Zucker diabetic fatty rat at 0.3 mg/kg, po administered once daily for 21 days followed by additional administration on day 22	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1899747	Agonist activity at human PPARgamma measured by dual luciferase reporter gene assay	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents.
AID1760181	Antidiabetic activity in KK-Ay mouse assessed as effect on AGE level at 5 mg/kg, po for 24 hrs by ELISA (Rvb 2.85 +/- 0.92 ug/ml)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID637398	Effect on hematocrit level in Sprague-Dawley rat at 25 mg/kg after 28 days (Rvb = 47.5 +/- 0.6 %)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID421110	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 0.3 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1901244	Agonist activity at pBIND tagged human PPARgamma expressed in human HEK293 cells incubated for 18 hrs by dual luciferase reporter assay relative to control	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold.
AID260993	Effect on PPARgamma transactivation activity in U2OS cells relative to reference	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
AID1152869	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells.
AID1753550	Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay	2021	European journal of medicinal chemistry, Jun-05, Volume: 218	Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
AID260994	Effect on PPARalpha transactivation activity in U2OS cells	2006	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4	Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
AID111557	In vivo blood glucose level in male db/db mice after administration of 1 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID299412	Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs	2007	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13	Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
AID156460	In vitro transactivation of rat Peroxisome proliferator activated receptor alpha	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID296181	Reduction in plasma triglyceride level in alloxan-induced diabetic mouse at 10 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID156792	Agonist activity determined in peroxisome proliferator activated receptor gamma using PPAR gamma-Gal4 Luciferase cotransfection assay	2003	Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14	Benzoxazinones as PPARgamma agonists. part 1: SAR of three aromatic regions.
AID1063317	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha release at 10 uM treated 2 hrs before LPS challenge measured by ELISA	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID308436	Agonist activity at human PPARdelta by transactivation assay relative to GW-501516	2007	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16	Design of a partial PPARdelta agonist.
AID1427975	Decrease in lipid droplet accumulation in liver in KK-Ay diabetic mouse model at 10 mg/kg/day administered via oral gavage once daily for 21 days by haematoxylin and eosin staining based microscopic or morphometric method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID1753551	Agonist activity at human Gal4 fused PPARdelta LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay	2021	European journal of medicinal chemistry, Jun-05, Volume: 218	Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
AID717060	Antidiabetic activity in db/db mouse type 2 diabetic model assessed as reduction of plasma glucose level at 10 mg/kg, po administered for 14 days	2012	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23	Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
AID156953	In vitro binding affinity against human peroxisome proliferator activated receptor gamma	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID111556	In vivo blood glucose level in male db/db mice after administration of 1 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1716458	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in CPT1A gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID708113	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.
AID1400366	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells up to 100 nM after 20 hrs in presence of 5 uM PPARgamma antagonist GW9662 by luciferase reporter gene assay	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID1700120	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in UCP1 mRNA expression by immunoblotting analysis
AID705480	Binding affinity to neuronal acetylcholine receptor subunit alpha-10 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID113348	In vivo insulin effect in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID220378	In vivo plasma glucose in db/db mouse after 11 days at 10 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID705481	Binding affinity to mouse multiple PDZ domain protein by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1677548	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability at 0.03 to 3 uM after 48 hrs by SRB assay	2020	Journal of natural products, 10-23, Volume: 83, Issue:10	CRISPR-Cas9 Genome-Wide Knockout Screen Identifies Mechanism of Selective Activity of Dehydrofalcarinol in Mesenchymal Stem-like Triple-Negative Breast Cancer Cells.
AID1499765	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as blood glucose AUC (0 to 120 min) at 10 mg/kg, po qd for 31 days measured on day 29 post dose by OGTT (Rvb = 41471 +/- 2451 mg.min/dL)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID276715	Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay relative to darglitazone	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID276987	Activity at human PPARgamma expressed in CV1 cells by cotransfection assay relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID1499793	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as change in body weight at 10 mg/kg, po qd for 29 days measured on day 1 to 29 during compound dosing (Rvb = 140 +/- 7 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1503450	Activation of AMPK in palmitate-induced insulin-resistant human HepG2 cells assessed as reduction in PEPCK mRNA expression at 12.5 uM incubated for 24 hrs by real-time PCR method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Baicalin and its metabolites suppresses gluconeogenesis through activation of AMPK or AKT in insulin resistant HepG-2 cells.
AID1276072	Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in FABP4 expression at 2 uM by qPCR method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID1427951	Toxicity in KK-Ay diabetic mouse model assessed as changes in body weight at 10 mg/kg/day administered via oral gavage once daily for 21 days measured every 3 days during compound dosing	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID453757	Glucose lowering effect in ZDF rat assessed as plasma glucose level at 3 mg/kg/day, po for 2 weeks (RVb = 433 +/- 37 mg/dL)	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID1700122	Induction of mitochondrial biogenesis in mouse 3T3-L1 cells assessed as increase in PGC1beta mRNA expression by RT-PCR analysis
AID29100	Oral half-life in rat after peroral administration	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID656891	Antidyslipidemic activity in C57BL/Ks db/db mouse assessed as reduction of total cholesterol level at 50 mg/kg, po after 6 weeks (Rvb = 9.2 +/- 1.2 mmol/L)	2012	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8	Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
AID68775	Relative wt in two week oral toxicity test in male F344/DuCrj rats after 50 mg/kg dose	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID1507891	Anti-diabetic activity in ob/ob mouse assessed as change in serum triglyceride levels at 3 mg/kg administered via oral gavage daily for 4 days measured on day 5 relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID552404	Antihyperglycemic activity in db/db mouse assessed as reduction of serum glucose level at 30 mg/kg, po qd for 14 days relative to control	2011	Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2	Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
AID712715	Reduction of visceral fat weight in high fat diet fed-induced obesity and insulin resistance C57Bl/6J mouse model at 10 mg/kg/day, po administered once daily for 2 weeks measured on day 12 by in vivo magnetic resonance imaging analysis	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID1440567	Binding affinity to PPARgamma (unknown origin) assessed as kinetic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1193220	Induction of glucose consumption in human HepG2 cells at 10'-5 M after 24 hrs by glucose oxidase method relative to control	2015	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7	Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity.
AID1561628	Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as induction of M348 cross-peak shift at 1 mol equiv by 2D 1H-15N HSQC NMR analysis	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	Insights into PPARγ Phosphorylation and Its Inhibition Mechanism.
AID1499898	Toxicity in Zucker rat chronic ob/ob model assessed as liver weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 2.77 +/- 0.16 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID712386	Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay relative to L165041	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID637382	Hypoglycemic activity in diabetic KK-Ay mouse model assessed as decrease in glucose level at 30 mg/kg, po qd for 14 days (Rvb = 648.4 +/- 77.1 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1362857	Tmax in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID431130	Adipogenic activity in monosodium L-glutamate-treated obese Wistar rat assessed as reduction in body weight at 5 mg/kg, po after 6 weeks	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID643841	Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID705748	Binding affinity to mouse mitochondrial dihydrolipoyl dehydrogenase by chromatographic analysis relative to rosiglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID237605	Percent decrease in triglyceride level of wistar rat was determined at 3 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID1532807	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1440535	Transactivation of GAL4-fused human PPARalpa LBD expressed in human HepG2 cells up to 2 uM after 20 hrs by luciferase reporter gene assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID11213	Clearance was determined by iv administration (1.5 mg/kg) in fasted male Sprague-Dawley rats	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID276989	Reduction of glucose level in db/db mouse at 30 mg/kg, po after 7 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID637432	Cmax in Sprague-Dawley rat at 10 mg/kg after 0.5 to 8 hrs by HPLC analysis	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1767823	Hypolipidemic activity against palmitic acid-induced hyperlipidemia in human HepG2 cells assessed as increase in insulin-induced Akt phosphorylation at 1 uM pretreated for 24 hrs followed by insulin challenge by Western blot analysis	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID475399	Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID1532808	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation at 1 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID372115	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in heart weight at 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID357425	Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID1466739	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
AID1760200	Antidiabetic activity in KK-Ay mouse assessed as effect on Triglycerides level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 4.01 +/- 1.83 mM)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1700100	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in IRA mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID597762	Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay	2011	Bioorganic & medicinal chemistry, May-15, Volume: 19, Issue:10	Biological evaluation of novel benzisoxazole derivatives as PPARδ agonists.
AID270649	Fat mass in ZDF rat	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID744758	Insulin sensitizing activity in mouse 3T3L1 cells assessed as increase in glucose uptake at 10 ug/mL after 50 hrs by ELISA relative to control	2013	European journal of medicinal chemistry, May, Volume: 63	Synthesis and biological evaluation of oleanolic acid derivatives as PTP1B inhibitors.
AID1408901	Transactivation of human PPARgamma expressed in human MCF7 cells harboring pPPRE3-tk-luc reporter at 10 uM after 24 hrs by luciferase reporter gene assay relative to control	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Synthesis and evaluation of new designed multiple ligands directed towards both peroxisome proliferator-activated receptor-γ and angiotensin II type 1 receptor.
AID1499759	Antidiabetic activity in Zucker rat sub-chronic fa/fa prediabetic model assessed as fasting blood insulin level at 10 mg/kg, po qd for 31 days measured on day 29 post dose (Rvb = 8.5 +/- 1.4 ug/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID156630	In vitro binding affinity for human PPAR delta in SPA	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID1499801	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as epididymal white adipose tissue weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 13.9 +/- 0.6 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1395948	Agonist activity at human PPARgamma after 22 to 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16	Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.
AID156234	In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID308434	Agonist activity at human PPARalpha by transactivation assay relative to NNC61-4655	2007	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16	Design of a partial PPARdelta agonist.
AID365543	Insulin sensitizing activity in Zucker diabetic fa/fa rat assessed as reduction in fasted insulin level at 30 mg/kg/day, po for 14 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID421113	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 1 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID637431	Effect on RBC count in Sprague-Dawley rat at 100 mg/kg after 28 days (Rvb = 832 +/- 25.2 x 10 ' 4/micro L)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1767821	Hypolipidemic activity against palmitic acid-induced hyperlipidemia in human HepG2 cells assessed as increase in insulin-induced Akt Akt Ser473 phosphorylation at 1 uM pretreated for 24 hrs followed by insulin challenge by Western blot analysis	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Design, synthesis, and biological evaluation of novel sulindac derivatives as partial agonists of PPARγ with potential anti-diabetic efficacy.
AID1395945	Agonist activity at human PPARalpha after 22 to 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16	Structure-guided evolution of a 2-phenyl-4-carboxyquinoline chemotype into PPARα selective agonists: New leads for oculovascular conditions.
AID382297	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1597851	Agonist activity at PPARalpha in human Huh7 cells assessed as SCD1 mRNA expression at 1 uM measured after 18 hrs by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID175790	In vivo plasma free fatty acid in Zucker diabetic fatty rat after 11 days at 30 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID175789	In vivo plasma free fatty acid in Zucker diabetic fatty rat after 11 days at 10 mg/kg/day	2003	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7	Phenylacetic acid derivatives as hPPAR agonists.
AID705505	Binding affinity to PX domain-containing protein kinase-like protein in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis relative to pioglitazone	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID637348	Transactivation of human full length PPARalpha expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay relative to WY14643	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1905849	Reduction of lipid accumulation in oleic acid-induced steatosis in human HepaRG cells at 10 uM treated for 2 weeks with media replenishment along with compound and inducer for every 2 days by Oil Red O staining based microscopy	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID387492	Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assay	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1700089	Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as recruitment of TIF2 incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
AID643833	Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID424503	Glucose lowering effect in po dosed C57BL/6J ob/ob mouse assessed as insulin level relative to untreated control	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1440527	Transactivation of GAL4-fused human PPARdelta LBD expressed in human HepG2 cells up to 2 uM after 20 hrs by luciferase reporter gene assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID431048	Induction of adipogenesis in mouse 3T3L1 assessed as increase in triglyceride level at 1 uM after 5 days relative to control	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID1566180	Partial agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as decrease in PPARgamma S273 phosphorylation at 10 uM preincubated for 1 hr followed by TNFalpha stimulation for 3 hrs by Western blotting analysis	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID157275	In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)	1998	Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25	N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
AID1193221	Agonist activity at human PPARgamma expressed in U2OS cells coexpressing human RXR assessed as luciferase activity at 10 uM after 24 hrs by transactivation assay relative to control	2015	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7	Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity.
AID600729	Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling.
AID256468	In vitro activity against human peroxisome proliferator activated alpha /Gal4 in cell-based transactivation assay	2005	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20	Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
AID1773601	Toxicity in ob/ob mouse assessed as weight gain at 10 mg/kg, po administered once daily for 30 days and measured every 5 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID365545	Hypoglycemic activity in Zucker diabetic fa/fa rat assessed as improvement in glucose AUC at 30 mg/kg/day, po for 14 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID1597835	Upregulation of PPARgamma gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1716460	Agonist activity at human PPARalpha in 8 day differentiated human SGBS cells assessed as increase in PLIN1 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID111560	In vivo % reduction of blood glucose level in male db/db mice after administration of 1 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID299622	Agonist activity at human PPARalpha by transactivation assay relative to NNC 61-4655	2007	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15	Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
AID1905838	Induction of glucose uptake in mouse C2C12 cells assessed as increase in GLUT4 expression at 10 uM incubated in starvation medium with replacement of fresh medium for every 24 hrs for 96 hrs by Western blotting analysis	2022	European journal of medicinal chemistry, May-05, Volume: 235	A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity.
AID382287	Selectivity ratio of EC50 for human PPARgamma to EC50 for human PPARalpha	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1827927	Toxicity in ob/ob diabetic C57BL/6J (B6.V Lepob/OlaHsd) mouse model assessed as effect on body weight at 10 to 100 micromol/kg, po dosed daily for 7 days	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID1363005	Toxicity in Wistar-Imamichi rat assessed as clinical abnormality at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1400347	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay relative to rosiglitazone	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID1191335	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID391554	Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay relative to rosiglitazone	2008	Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20	Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID733017	Antidiabetic activity in Zucker fatty rat assessed as reduction in blood glucose level at 1 mg/kg/day, po measured after 14 days by OGTT relative to vehicle-treated control	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID107484	Compound was tested in vivo for the measurement of triglyceride levels in db/db mice at a dose of 10 mg/kg	2003	Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20	Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
AID1566184	Induction of PPARgamma-mediated adipogenesis in mouse 3T3L1 cells assessed as increase in cell differentiation at 10 uM compound treatment renewed every 2 days and measured on day 7 by Oil-red O staining based assay	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID113923	In vivo efficacy as percent glucose correction in male db/db mice at 10 mg/kg oral dose	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1716467	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as increase in volume of lipid droplets at 2 uM measured upto 12 days by oil-O-red staining based inverted microscopic analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1597837	Upregulation of CEBPA gene expression in human preadipocyte derived from Simpson-Golabi-Behmel syndrome (SGBS) patient at 2 uM measured for 12 days by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18	Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPARα-selective agonist.
AID387509	Antihyperglycemic activity in db/db mouse assessed as increase in body weight at 0.3 mg/kg, po once daily after 28 days	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1422537	Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Nov-05, Volume: 159	Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ.
AID1468742	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PGC1alpha (196 to 221 residues) co-activator recruitment by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1193219	Induction of glucose consumption in human HepG2 cells at 10'-5 M after 24 hrs by glucose oxidase method (Rvb = 2 +/- 0.09 mM)	2015	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7	Design, synthesis and biological evaluation of GY3-based derivatives for anti-type 2 diabetes activity.
AID1700081	Binding affinity to PPARg (unknown origin) assessed as dissociation constant by SPR assay
AID1499904	Toxicity in Zucker rat chronic ob/ob model assessed as brown adipose tissue weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 0.59 +/- 0.05 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1063319	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured after 12 hrs by ELISA (Rvb = 13.9 +/- 2.6 pg/ml)	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID1700079	Binding affinity to PPARg (unknown origin) assessed as association constant by SPR assay
AID1507888	Activation of recombinant human SIRT1 at 10 uM using C-terminal AMC labeled Arg-His-Lys-Lys (Ac) as substrate after 30 mins by FLUOR DE LYS fluorescent assay relative to control	2017	European journal of medicinal chemistry, Sep-08, Volume: 137	Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
AID252990	Percent glucose correction of nonfasting hyperglycemia in vehicle control db/db mice relative to normal glucose levels in control db/lean mice at 10 mg/kg on day 11	2005	Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2	Benzoyl 2-methyl indoles as selective PPARgamma modulators.
AID1363015	Toxicity in Wistar-Imamichi rat assessed as elevation in AST activity at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID421047	Inhibition of human PPARgamma receptor by scintillation proximity assay	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1468740	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (607 to 631 residues) co-activator recruitment by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID244313	In vitro agonist activity against human PPAR-gamma receptor in transactivation assay at 1000 nM	2005	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14	6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-gamma activators.
AID1063316	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 release at 10 uM treated 2 hrs before LPS challenge measured by ELISA	2014	European journal of medicinal chemistry, Jan-24, Volume: 72	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
AID382311	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as reduction in blood total cholesterol level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1630673	Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	2016	Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21	Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID418682	Antidiabetic activity in po dosed type 2 diabetes mellitus patient assessed as reduction in HbA1C level in liver	2009	Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7	Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
AID1410796	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CPT1A mRNA expression at 1 uM after 15 days by quantitative real-time PCR method	2018	Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13	Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
AID1228166	Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis	2015	Journal of natural products, Apr-24, Volume: 78, Issue:4	Steroidal Alkaloids from Veratrum nigrum Enhance Glucose Uptake in Skeletal Muscle Cells.
AID26206	In vivo % reduction of blood glucose area under curve after oral glucose tolerance test in male db/db mice at 1 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1351154	Inhibition of Pseudomonas aeruginosa PAO1 GFP-fused quorum sensing pqsA at 10 uM measured every 15 mins up to 12 hrs by GFP reporter gene assay relative to control	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID223555	Binding affinity at human PPAR gamma	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID1183857	Activation of PPARgamma in mouse peritoneal macrophages assessed as increase in Dectin-1 mRNA expression treated for 5 hrs by qRT-PCR analysis	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Protolichesterinic acid derivatives: α-methylene-γ-lactones as potent dual activators of PPARγ and Nrf2 transcriptional factors.
AID348507	Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity at 0.2 uM by transactivation assay	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID1427945	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in blood glucose level after 4 hrs fasting at 10 mg/kg/day administered via oral gavage once daily measured on day 3 post dose	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID277015	Binding affinity to human PPARgamma	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).
AID1191352	Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.
AID1440532	Binding affinity to PPARgamma (unknown origin) assessed as thermodynamic dissociation constant by SPR assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
AID1419242	Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay	2018	Bioorganic & medicinal chemistry, 12-01, Volume: 26, Issue:22	PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.
AID268119	Antiproliferative activity against human MCF7 cell line	2006	Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14	Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
AID1532802	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation at 1 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1427971	Effect on serum AST level in KK-Ay diabetic mouse model at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID1901675	Stabilization of human PPARgamma LBD assessed as change in melting temperature at 25 uM by thermal shift assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1217729	Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID382298	Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay relative to GW-9578	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1716437	Agonist activity at recombinant human PPARgamma LBD (205 to 505 residues) expressed in African green monkey COS-1 cells incubated for 18 hrs by luciferase reporter gene assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID643836	Partial agonist activity at human PPARgamma LBD assessed as activation of CBP1-453 by HTRF assay relative to L-796449	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID156959	Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand	2003	Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8	Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID391555	Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay	2008	Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20	Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID1443992	Total Cmax in human administered as single dose	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID551702	Agonist activity at human PPARalpha in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of transactivation activity at 10 uM by luciferase reporter gene assay relative to control	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Modulation of PPAR subtype selectivity. Part 2: Transforming PPARα/γ dual agonist into α selective PPAR agonist through bioisosteric modification.
AID280964	Effect on increase in fatty acid oxidation in rat L6 cells relative to GW-501516	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID280956	Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay	2007	Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7	Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.
AID731800	Increase in PPAR-gamma mRNA transcript level in human macrophages at 10 uM by quantitative PCR analysis	2013	European journal of medicinal chemistry, Apr, Volume: 62	Peroxisome proliferator-activated receptor-γ mediates the anti-inflammatory effect of 3-hydroxy-4-pyridinecarboxylic acid derivatives: synthesis and biological evaluation.
AID1700078	Agonist activity at PPARg (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation at 0.1 uM incubated for 17 hrs by PPRE-driven luciferase reporter gene assay relative to control
AID551703	Agonist activity at human PPARgamma in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of transactivation activity at 0.2 uM by luciferase reporter gene assay relative to control	2011	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2	Modulation of PPAR subtype selectivity. Part 2: Transforming PPARα/γ dual agonist into α selective PPAR agonist through bioisosteric modification.
AID156934	In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)	2003	Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2	Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID372097	Antidiabetic activity in obese insulin-resistant Zucker fa/fa rat assessed as decrease in plasma triglyceride level at 0.1 to 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID453567	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID1499901	Toxicity in Zucker rat chronic ob/ob model assessed as epididymal white adipose tissue weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 3.92 +/- 0.14 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID276591	Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID156369	In vitro transcription activation on human peroxisome proliferator activated receptor-gamma (PPAR gamma)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID1734992	Hypoglycemic activity in Zucker fatty diabetes mellitus rat model assessed as reduction in blood glucose level at 3 mg/kg, po administered for 21 days and measured at 10 to 60 mins post glucose challenge on day 1 by OGTT	2016	Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24	The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
AID3424	Percentage of rosiglitazone response for insulin-sensitizing activity at 1 uM concentration in 3T3-L1 cells	2003	Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20	Synthesis and insulin-sensitizing activity of a novel kind of benzopyran derivative.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1810341	Agonist activity at human PPARdelta transfected in COS-7 cells assessed maximum luciferase activity measured after 24 hrs by cell based luciferase transactivation assay relative to GW0742	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID1362856	Toxicity in Zucker diabetic fatty rat assessed as body weight gain at 3 mg/kg, po administered once daily for 14 days relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID421109	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 0.03 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1172786	Antidiabetic activity in overnight fasted Wistar rat assessed as reduction in plasma glucose level at 36 mg/kg, po by oral glucose tolerance test	2014	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22	Novel benzenesulfonylureas containing thiophenylpyrazoline moiety as potential antidiabetic and anticancer agents.
AID1400376	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at >100 nM after 20 hrs in presence of 5 uM PPARgamma antagonist GW9662 by luciferase reporter gene assay	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID1827924	Anti-diabetic activity in ob/ob diabetic C57BL/6J (B6.V Lepob/OlaHsd) mouse model assessed as normalization of fasting plasma glucose level at 10 to 100 micromol/kg, po dosed daily for 7 days	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID609877	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in triglyceride content at 1 uM after 8 days by Oil red O staining relative to control	2011	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15	New isoprenylated flavonoids and adipogenesis-promoting constituents from Morus notabilis.
AID1810332	Induction of adipogenesis differentiation in human Mesenchymal stem cells at 1 uM incubated for 21 days by Alizarin Red S staining-based microscopic analysis	2021	Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10	Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
AID1532768	Antidiabetic activity in spontaneous db/db BKS.Cg-Dock7m +/+ Leprdb/J mouse assessed as decrease in blood glucose AUC at 10 mg/kg, po administered as daily dose via gavage for 18 days measured on day 12 up to 120 mins post glucose challenge by oral glucos	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID299621	Agonist activity at human PPARalpha by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15	Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
AID1499813	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as heart weight at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 1.19 +/- 0.04 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1773586	Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID491669	Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID26201	In vivo blood glucose area under curve after oral glucose tolerance test in male db/db mice at 1 mg/kg peroral dose of compound thrice a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID157292	In vitro binding affinity against human PPAR delta (peroxisome proliferator-activated delta receptor)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID372111	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in extracellular fluid volume at 10 mg/kg, po once daily for 7 days measured after 24 hrs by bioelectrical impedance analysis	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID382309	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as reduction in blood triglyceride level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID260323	Effect on PPAR gamma transactivation activity in Huh7 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
AID280020	Reduction of blood glucose level in orally dosed db/db mouse at 3 mg/kg after 8 days	2007	Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5	Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
AID701822	Antidyslipidemic activity in diabetic C57BL/KsJ db/db mouse model assessed as increase in plasma HDL-C/cholesterol ratio at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID675863	Displacement of pan-PPAR fluormone from PPARdelta LBD at >= 100 uM by TR-FRET based LanthaScreen assay	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
AID421112	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 15 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1662158	Antidiabetic activity in C57 BL/Ks J-db/db mouse assessed as reduction in plasma glucose levels at 10 mg/kg after 6 days relative to control	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Anti-diabetic drugs recent approaches and advancements.
AID469778	Antidiabetic activity in BALB/c mouse type 2 diabetic model assessed as reduction of fasting blood glucose level at 2 mg/kg, po QD measured after 3 weeks by glucometry (Rvb=14.89 +/- 1.42 mmol/L)	2009	Journal of natural products, Nov, Volume: 72, Issue:11	Hypoglycemic polysaccharides from the tuberous root of Liriope spicata.
AID705479	Binding affinity to 26S proteasome non-ATPase regulatory subunit 1 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1351161	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 6 hrs by ELISA (Rvb = 94.6 +/- 5.9 pg/ml)	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID453774	Toxicity in in ZDF rat assessed as decrease in hematocrit level at 3 mg/kg, po relative to untreated control	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID305542	Displacement of [3H]2-methyl-2-(4-{3-[porpyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-propyl}-phenoxy)-propionic acid from human PPARgamma	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	Design and synthesis of a novel class of dual PPARgamma/delta agonists.
AID444058	Volume of distribution at steady state in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID483816	Antidiabetic activity in diet-induced obese mouse assessed as decrease in fed blood glucose level at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 13 by glucose tolerance test	2010	Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11	Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1152868	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells at 10 uM after 16 hrs by scintillation counting analysis (Rvb = 0%)	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Design and synthesis of lupeol analogues and their glucose uptake stimulatory effect in L6 skeletal muscle cells.
AID276587	Displacement of radiolabeled GW-2331 from human PPAR alpha by SPA binding assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID431136	Adipogenic activity in monosodium L-glutamate-treated obese Wistar rat assessed as decrease in total fat mass at 5 mg/kg, po after 6 weeks	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID277007	Activity at human PPARgamma in CV1 cells by CTF assay relative to 2-methyl-2-(4-{3-propyl-(5-pyridin-2yl-thiophene-2-sulphonyl)-amino]-pro-pyl}-phenoxy)-propionic acid	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
AID1217728	Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID256469	In vitro activity against human peroxisome proliferator activated gamma/Gal4 in cell-based transactivation assay	2005	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20	Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.
AID357434	Agonist activity at histidine-tagged PPARgamma ligand binding domain by cell free-coactivator recruitment assay	2007	The Journal of biological chemistry, Jun-08, Volume: 282, Issue:23	Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
AID474857	Hypolipidemic activity in db/db mouse assessed as ratio of total serum cholesterol to total serum HDL at 10 mg/kg, po QD after 14 days	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID421091	Antidiabetic activity in ob/ob mouse assessed as insulin correction at 1 mg/kg, po once daily for 5 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1831359	Partial agonist activity at sGSF-PPARgamma (unknown origin) assessed as CBP-1 recruitment by HT-FRET assay	2021	Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23	Structure-Based Design of Dual Partial Peroxisome Proliferator-Activated Receptor γ Agonists/Soluble Epoxide Hydrolase Inhibitors.
AID372112	Toxicity in obese insulin-resistant Zucker fa/fa rat assessed as increase in heart weight at 10 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID643834	Binding affinity to human PPARgamma LBD Y473A mutant expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID548200	Displacement of fluormone PPAR-green from N-terminal His-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	1,3-Diphenyl-1H-pyrazole derivatives as a new series of potent PPARγ partial agonists.
AID240111	Effective concentration against human Peroxisome proliferator activated receptor gamma	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID111562	In vivo % reduction of blood glucose level in male db/db mice after administration of 3 mg/kg peroral dose of compound once in a day	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID731519	Binding affinity to human PPARgamma (unknown origin) by competitive TR-FRET assay	2013	Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4	Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ.
AID107482	Compound was tested in vivo for the measurement of glucose levels in db/db mice at a dose of 10 mg/kg	2003	Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20	Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists.
AID733512	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	2013	Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4	Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1466738	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay relative to pioglitazone	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.
AID1700133	Inhibition of oleic acid-induced lipid accumulation in rat primary hepatocytes at 1 uM incubated for 8 hrs before addition of oleic acid and measured after 24 hrs by Oil Red O staining based assay
AID1468747	Displacement of N-terminal biotin-labeled NCOR-ID1 (2253 to 2277 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as Emin/max ratio by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID276598	Reduction of plasma glucose in orally dosed db/db mouse at 3 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID252797	Percent intrinsic maximal response against peroxisome proliferator activated receptor gamma transactivation	2005	Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10	Selective PPARgamma modulators with improved pharmacological profiles.
AID157294	In vitro binding affinity against human PPAR gamma (peroxisome proliferator-activated gamma receptor)	2003	Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10	5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists.
AID157099	Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay	2001	Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24	Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
AID1773608	Reduction in hepatic total triglyceride level in ob/ob mouse at 10 mg/kg, po administered once daily for 30 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1700087	Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as displacement of NCoR incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
AID1261000	Antidiabetic activity in diet-induced obese C57BL/6J mouse assessed as increase in glucose disposal level at 5 mg/kg, po qd for 5 days by oral glucose tolerance test	2015	ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9	Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
AID712383	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID475401	Growth inhibition of HLF by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID649714	Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay	2012	Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6	Synthesis and antidiabetic performance of β-amino ketone containing nabumetone moiety.
AID705478	Binding affinity to mouse tyrosine-protein kinase transmembrane receptor ROR1 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1427966	Hypolipidemic activity in KK-Ay diabetic mouse model assessed as reduction in serum triglyceride level at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID314545	Displacement of [3H]Rosiglitazone from human PPARgamma	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID156931	Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.	2001	Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24	Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
AID1760188	Antidiabetic activity in KK-Ay mouse assessed as effect on HOMA-IR level at 5 mg/kg, po for 24 hrs by ELISA (Rvb = 137 +/- 18.4 No_unit)	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID252364	Triglycerides concentration was measured in male db/db mouse after 10 mpk/day for 14 days	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID1700113	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in OPLAH mRNA expression by RT-PCR analysis
AID276713	Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1468728	Toxicity in Sprague-Dawley rat assessed as reduction in hematocrit level at 30 mg/kg for 4 weeks	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID705485	Binding affinity to mouse dynactin-1 by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID276986	Activity at human PPARalpha expressed in CV1 cells using GAL4 chimeric system relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24	Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agents.
AID745230	Antidyslipidemic activity in db/db mouse assessed as increase in plasma HDL-cholesterol level at 30 mg/kg, po qd administered 15 days measured on day 16 by ELISA relative to vehicle-treated control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1674184	Toxicity in po dosed human assessed as maximum daily dose	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID440656	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay relative to rosiglitazone	2009	Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20	New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
AID223557	Transcriptional activation in CV- cells expressing hPPARgamma	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
AID365537	Hypolipidemic activity in db/db mouse assessed as reduction in triglyceride level at 30 mg/kg/day, po for 6 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID1700098	Induction of adipogenic differentiation in mouse 3T3-L1 cells assessed as increase in PLIN mRNA expression at 0.1 uM incubated for 7 days by RT-PCR analysis
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID157283	In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.
AID1156988	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Aug-18, Volume: 83	Synthesis and biological evaluation of new rhodanine analogues bearing 2-chloroquinoline and benzo[h]quinoline scaffolds as anticancer agents.
AID712385	Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID115313	Area under blood glucose time curve after oral glucose test in mice	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1209457	Unbound Cmax in human plasma	2012	Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1	In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1427955	Antidiabetic activity in KK-Ay diabetic mouse model assessed as reduction in serum insulin level at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID418685	Antidiabetic activity in po dosed type 2 diabetes mellitus patient assessed as reduction in HbA1C level in adipose tissue	2009	Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7	Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
AID242199	Inhibition of human Peroxisome proliferator activated receptor gamma binding	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Discovery of a novel series of peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes and dyslipidemia.
AID280021	Reduction of blood glucose level in orally dosed db/db mouse at 10 mg/kg after 8 days	2007	Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5	Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
AID252348	Effect (150 mg/kg) on PPAR gamma- mediated effects measured as change in liver weight in rats	2005	Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13	Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.
AID1716485	Induction of adipogenesis in 8 day differentiated human SGBS cells assessed as upregulation of unsaturated fatty acid biosynthesis genes at 2 uM incubated for 8 days by Illumina sequencing method	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID1700118	Induction of adipocyte browning in mouse 3T3-L1 cells assessed as increase in CIDEA mRNA expression by RT-PCR analysis
AID712389	Binding affinity to PPARgamma ligand binding domain by isothermal titration calorimetry	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID3422	Effective concentration for enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells	2003	Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20	Synthesis and insulin-sensitizing activity of a novel kind of benzopyran derivative.
AID156362	In vitro transcription activation on human peroxisome proliferator activated receptor-gamma (PPAR gamma)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID1499872	Antidiabetic activity in Zucker rat chronic ob/ob model assessed as HbA1C level at 10 mg/kg, po qd for 31 days measured on day 32 post dose (Rvb = 5.9 +/- 0.18%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1351159	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production by measuring TNF-alpha level at 10 uM preincubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA (Rvb = 21561.3 +/- 85	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	4-arylamidobenzyl substituted 5-bromomethylene-2(5H)-furanones for chronic bacterial infection.
AID156218	In vitro transcription activation on human peroxisome proliferator activated receptor-alpha (PPAR alpha)	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID750249	Antidyslipidemic activity in C57BL/KsJ db/db mouse assessed as reduction of triglycerides level in blood at 50 mg/kg, po administered for 6 weeks (Rvb = 1.05 +/- 0.11 mmol/l)	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID354065	Antidiabetic activity in Zucker fa/fa rat assessed as fasting plasma insulin level at 3 mg/kg/day	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID268114	Inhibition of PHA/PMA-induced IL2 production in human T lymphocytes	2006	Journal of medicinal chemistry, Jul-13, Volume: 49, Issue:14	Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists.
AID1377503	Agonist activity at GAL4-fused PPARgamma LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies.
AID372102	Antidiabetic activity in obese insulin-resistant Zucker fa/fa rat assessed as decrease in plasma free fatty acid level at 0.1 to 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID270632	Transactivation of human PPARdelta in CV1 cells by luciferase reporter gene assay relative to LG070660	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID276727	Increase in body weight in db/db mouse at 3 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID364055	Effect on insulin sensitizing activity in mouse 3T3-L1 cells assessed as increase in triglyceride accumulation at 10 uM after 7 days	2008	European journal of medicinal chemistry, Sep, Volume: 43, Issue:9	Insulin-releasing activity of a series of phenylalanine derivatives.
AID113350	In vivo nonfasting triglyceride in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID745226	Induction of adipogenesis in mouse 3T3L1 cells assessed as accumulation of lipid droplets at 10 uM measured on day 9 by Oil Red O staining method relative to control	2013	European journal of medicinal chemistry, May, Volume: 63	Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
AID1362910	Agonist activity at recombinant human GAL4-TAD fused PPARgamma LBD assessed as induction of GAL4-DBD fused RIP140e184b co-factor recruitment after 24 to 48 hrs by fluorescence assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1217711	Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1236833	Increase in triglyceride content in C57BLKS/J-Lepr/Lepr db/db mouse liver at 10 mg/kg, po administered via gavage by hematoxylin-eosin staining	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Design, synthesis, and biological evaluation of a series of alkoxy-3-indolylacetic acids as peroxisome proliferator-activated receptor γ/δ agonists.
AID237610	Percent decrease in plasma glucose level of wistar rat was determined at 10 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID1760164	Increase in glucose consumption in rat L6 cells cells at 20 uM after 24 hrs by glucose oxidase assay	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy.
AID474860	Hypolipidemic activity in db/db mouse assessed as serum free fatty acid level at 10 mg/kg, po QD after 14 days (Rvb= 2.17 +/- 0.23 m/mol)	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl) propanoic acid compounds: synthesis and biological evaluation of dual PPARalpha/gamma agonists.
AID1499889	Toxicity in Zucker rat chronic ob/ob model assessed as body weight at 10 mg/kg, po qd for 28 days measured on day 28 post last dose (Rvb = 47.3 +/- 1.06 g)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID1400357	Induction of lipid accumulation in mouse 3T3L1 cells at 5 uM by Oil Red O staining-based assay	2018	Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18	Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
AID1901648	Agonist activity at human PPARalpha in mouse hepatocytes assessed as induction of Fgf21 mRNA expression at 50 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1668558	Agonist activity at PPARgamma in mouse 3T3L1 adipocytes assessed as induction of CD36 mRNA expression at 3 uM by qRT-PCR analysis	2020	Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13	l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.
AID1362892	Toxicity in F344/DuCrlCrlj rat assessed as death at 50 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID25727	Area under plasma concentration time curve after oral administration at a dose 2.2 mg/kg	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID123654	Compound was administered at a dose of 10 mg/kg/day to evaluate the percentage reduction in plasma glucose(PG) after 6 days of treatment in db/db mice via oral gavage.	1999	Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14	Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones.
AID1362913	Agonist activity at recombinant human GAL4-TAD fused PPARgamma LBD assessed as induction of GAL4-DBD fused SRC1 co-factor recruitment after 24 to 48 hrs by fluorescence assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID256775	Displacement of [3H]rosiglitazone from human PPAR gamma by SPA assay	2005	Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26	Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
AID421053	Antidiabetic activity in C57BLKS/J-m+/+Leprdb db/db mouse assessed as reduction in plasma glucose levels at 10 mg/kg, po once daily for 11 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1827925	Anti-diabetic activity in ob/ob diabetic C57BL/6J (B6.V Lepob/OlaHsd) mouse model assessed as normalization of insulin level at 10 to 100 micromol/kg, po dosed daily for 7 days	2022	ACS medicinal chemistry letters, Apr-14, Volume: 13, Issue:4	Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation.
AID1917380	Inhibition of recombinant human MAO-B	2022	Bioorganic & medicinal chemistry letters, 11-15, Volume: 76	Design, synthesis, in-vitro, in-vivo and ex-vivo pharmacology of thiazolidine-2,4-dione derivatives as selective and reversible monoamine oxidase-B inhibitors.
AID382307	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as reduction in blood glucose level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID391553	Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay	2008	Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20	Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID431124	Hypoglycemic activity in monosodium L-glutamate-treated obese Wistar rat assessed as reduction in blood glucose level at 5 mg/kg, po for 4 weeks measured after 10 hrs post dose fasting	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID372106	AUC in obese insulin-resistant Zucker fa/fa rat at 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus w
AID491668	Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay relative to rosiglitazone	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazo
AID666824	Toxicity in po dosed Wistar-Imamichi rat assessed as increase plasma volume administered qd for 14 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1499709	Inhibition of fluormone PPARgamma Green binding to recombinant N-terminal GST-tagged human PPARgamma LBD by fluorescence polarization assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID276609	Reduction of hematocrit in orally dosed db/db mouse at 30 mg/kg after 8 days relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID156383	Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) gamma expressed in HEK 293T cells at 1 uM	2001	Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16	(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID1597636	Induction of glucose uptake in human HepG2 cells at 0.625 to 2.5 uM incubated for 24 hrs in low glucose medium relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Design and synthesis of novel xanthone-triazole derivatives as potential antidiabetic agents: α-Glucosidase inhibition and glucose uptake promotion.
AID115314	In vivo insulin effect in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID750254	Antidiabetic activity in C57BL/KsJ db/db mouse assessed as reduction of blood glucose level at 50 mg/kg, po administered for 6 weeks	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID382299	Displacement of [3H]darglitazone from human PPARgamma by scintillation proximity assay	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID123668	Compound was administered at a dose of 3 mg/kg/day to evaluate the percentage reduction in plasma triglyceride (TG) after 6 days of treatment in db/db mice via oral gavage.	1999	Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14	Novel euglycemic and hypolipidemic agents. 4. Pyridyl- and quinolinyl-containing thiazolidinediones.
AID365535	Hypoglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 30 mg/kg/day, po for 6 days	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID1716500	Agonist activity at human PPARgamma in 8 day differentiated human SGBS cells assessed as decrease in CXCL1 gene expression at 2 uM incubated for 24 hrs by SYBR-green based qPCR analysis	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Synthesis and biological evaluations of marine oxohexadecenoic acids: PPARα/γ dual agonism and anti-diabetic target gene effects.
AID276728	Increase in body weight in db/db mouse at 30 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1543238	Induction of RXRalpha/PPARgamma interaction in HUVEC at 1 uM pretreated for 20 hrs before TNFalpha stimulation by immunoprecipitation and Western blotting analysis
AID15885	Calculated partition coefficient (clogP)	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID1374668	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as basal insulin level in plasma at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting (Rvb = 16959 +/- 4943 pg/ml)	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID712713	Reduction of body weight in high fat diet fed-induced obesity and insulin resistance C57Bl/6J mouse model at 10 mg/kg/day, po administered once daily for 2 weeks relative to control	2012	Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1	Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
AID1362854	Cmax in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1532837	Induction of membrane translocation of biotinylated human AQP2 expressed in rat IMCD cells at 10 to 50 uM after 30 mins by FITC-staining based confocal fluorescence microscopic analysis	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1474032	Ratio of drug concentration at steady state in human at 2 to 8 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1532826	Inhibition of human ERG expressed in CHO cells at 2.5 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID453568	Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay relative to darglitazone	2009	Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20	Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
AID141904	Agonist activity for murine PPAR alpha receptor in transcriptional activation assay; IA means inactive at 10 uM	2000	Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4	The PPARs: from orphan receptors to drug discovery.
AID365527	Agonist activity at PPARdelta expressed in human HepG2 cells at 10 uM assessed as induction of receptor transactivation by reporter gene assay relative to control	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID255224	Percentage maximal activation against human PPAR gamma at 3 uM; partial agonist	2005	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22	Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID304336	Agonist activity at human PPARdelta expressed in CV1 cells by receptor transactivation assay	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID569827	Agonist activity at human PPARgamma LBD by cell based luciferase reporter gene assay	2011	Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3	Identification of diaryl ether-based ligands for estrogen-related receptor α as potential antidiabetic agents.
AID421054	Antidiabetic activity in C57BLKS/J-m+/+Leprdb db/db mouse assessed as reduction in plasma triglyceride levels at 10 mg/kg, po once daily for 11 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID705495	Binding affinity to mitochondrial ATP synthase beta chain in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID1700093	Adipogenic activity in mouse 3T3-L1 cells assessed as increase in lipid content at 1 uM incubated for 6 days by Oil Red O dye fluorescence based assay
AID1174867	Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID387493	Half life in Sprague-Dawley rat at 3 mg/kg, iv	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID1362911	Agonist activity at recombinant human GAL4-TAD fused PPARgamma LBD assessed as induction of GAL4-DBD fused TRAP220 co-factor recruitment after 24 to 48 hrs by fluorescence assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID635238	Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.
AID1276071	Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin expression at 2 uM by qPCR method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID191968	Triglyceride level in rats 24 hr r after 30 mg/kg oral dose	2003	Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19	Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
AID3421	Stimulation of adipogenesis in 3T3-L1 cells is expressed as concentration equivalent to the [ 1-14C] uptake counts after treatment with 0.2 ug/mL troglitazone	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID421162	Toxicity in Sprague-Dawley rat assessed as increase albumin/globulin levels at 150 mg/kg, po once daily for 14 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1427967	Hypolipidemic activity in KK-Ay diabetic mouse model assessed as reduction in serum total cholesterol level at 10 mg/kg/day administered via oral gavage once daily for 21 days	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	A novel class of α-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
AID156299	In vitro Fold activation relative to maximum activation obtained with WY-14643 (~ 20-fold corresponded to 100%) for human peroxisome proliferator activated receptor alpha	2003	Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2	Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID568211	Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control	2011	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4	Furoxan nitric oxide donor coupled chrysin derivatives: synthesis and vasculoprotection.
AID431131	Adipogenic activity in monosodium L-glutamate-treated obese Wistar rat assessed as increase in subcutaneous fat weight at 5 mg/kg, po after 6 weeks relative to control	2009	Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15	Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
AID587348	Antidiabetic activity in rat hemidiaphragm assessed as glucose uptake at 2 mg after 45 mins in absence of insulin	2011	European journal of medicinal chemistry, Mar, Volume: 46, Issue:3	Synthesis, glucose uptake activity and structure-activity relationships of some novel glitazones incorporated with glycine, aromatic and alicyclic amine moieties via two carbon acyl linker.
AID270645	Lowering of insulin level in po dosed ZDF rat plasma	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID237609	Percent decrease in triglyceride level of wistar rat was determined at 100 mg/kg dosage of the compound	2005	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4	Synthesis and pharmacological evaluation of substituted 5-[4-[2-(6,7-dimethyl-1,2,3,4-tetrahydro-2-oxo-4-quinoxalinyl)ethoxy]phenyl]methylene]thiazolidine-2,4-dione derivatives as potent euglycemic and hypolipidemic agents.
AID1532809	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation at 2 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID705493	Binding affinity to focal adhesion kinase 2 in Sprague-Dawley rat heart homogenate after 15 mins by chromatographic analysis	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
AID642732	Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPARγ partial agonists.
AID421094	Cmax in C57BLKS/J-m+/+Leprdb db/db mouse at 10 mg/kg, po once daily for 11 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID637386	Hypotriglyceridemic activity in diabetic KK-Ay mouse model assessed as decrease in triglyceride level at 30 mg/kg, po qd for 14 days (Rvb = 819.9 +/- 135.5 mg/dl)	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID1901650	Agonist activity at human PPARgamma in mouse 3T3-L1 cells assessed as induction of Cebpalpha-mRNA expression at 10 uM incubated for 16 hrs by quantitative real-time PCR analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic Diseases.
AID1266117	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase of triacylglycerol accumulation at 25 uM after 18 hrs by ORO staining	2015	Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24	Identification of dual PPARα/γ agonists and their effects on lipid metabolism.
AID276726	Reduction of hematocrit in db/db mouse at 30 mg/kg, po after 8 day	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
AID1276061	Transactivation of PPARgamma in mouse 3T3L1 cells assessed as adipocyte differentiation by measuring lipid accumulation at 2 uM by Oil Red O staining-based assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID1503554	Cytotoxicity against human SCC15 cells transfected with PPARbeta siRNA assessed as reduction in cell viability at 50 uM after 24 hrs by resazurin reduction assay	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).
AID304333	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARdelta	2007	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24	Design and synthesis of novel and potent amide linked PPARgamma/delta dual agonists.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID270644	Lowering of glucose level in ZDF rat plasma at 1 mg/kg/day, po by glucose tolerance test	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID750255	Antidiabetic activity in C57BL/KsJ db/db mouse assessed as reduction of blood glucose level at 50 mg/kg, po administered for 6 weeks measured on first week	2013	European journal of medicinal chemistry, Jun, Volume: 64	Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
AID1362964	Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID1543228	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in neutrophil adhesion to endothelial cells at 1 uM pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using fre
AID94672	The hypoglycemic activity in diabetic KK mice, activity expressed as % decrease in blood glucose (18 h)	2000	Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16	Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
AID1532829	Inhibition of human ERG expressed in CHO cells at 20 uM by patch clamp assay relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID30160	Volume of distribution during steady state	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1566186	Induction of PPARgamma-mediated adipogenesis in mouse 3T3L1 cells assessed as upregulation of Glut4 mRNA expression at 10 uM by qRT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 11-15, Volume: 29, Issue:22	Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor γ indole partial agonists.
AID424499	Metabolic stability in human hepatocyte microsomes	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID115315	In vivo nonfasting blood glucose in db/db mice after oral treatment	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1251343	Toxicity in STZ-induced diabetic Wistar rat model assessed as increase in body weight at 36 mg/kg, po repeated for 15 days by GOD-POD method	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1468739	Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled LCOR (39 to 63 residues) co-activator recruitment by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID666817	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction of free fatty acids level at >1 mg/kg, po qd for 12 days	2012	European journal of medicinal chemistry, Aug, Volume: 54	Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARγ modulators.
AID1535245	Agonist activity at PPARgamma in mouse 3T3L1 cells assessed as increase in AP1 mRNA expression at 10 uM after 24 hrs by SYBR green dye based RT-PCR analysis	2019	Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4	Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.
AID296180	Reduction in plasma glucose level in alloxan-induced diabetic mouse at 5 mg/kg/day, po after 15 days relative to control	2007	European journal of medicinal chemistry, Oct, Volume: 42, Issue:10	Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
AID365525	Agonist activity at PPARalpha expressed in human HepG2 cells at 10 uM assessed as induction of receptor transactivation by reporter gene assay relative to control	2008	Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15	Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID299626	Agonist activity at human PPARdelta by transactivation assay relative to carbacyclin	2007	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15	Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.
AID223549	Fold activation relative to maximum activation obtained with rosiglitazone	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID708112	Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells at 100 uM after 18 hrs by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor γ.
AID242373	Mean inhibitory concentration against human peroxisome proliferator activated receptor alpha	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents.
AID348509	Reduction of triglyceride level in Swiss albino mouse serum at 10 mg/kg/day, po for 6 days relative to control	2008	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20	Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID240120	Effective concentration for human peroxisome proliferator-activated receptor delta	2005	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5	Structure-activity relationships of dimeric PPAR agonists.
AID244312	In vitro agonist activity against human PPAR-gamma in transactivation assay at 100 nM	2005	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 15, Issue:14	6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-gamma activators.
AID421115	Antidiabetic activity in Zucker fa/fa rat assessed as decrease in triglyceride levels at 100 mg/kg, po once daily for 7 days	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID117720	In vivo effect on blood glucose level in mice at the dose of 5 mg/kg by oral administration after two week	2004	Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13	Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.
AID701827	Antihyperglycemic activity in diabetic C57BL/KsJ db/db mouse model assessed as reduction in hyperglycemia at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID1700137	Toxicity in rat primary hepatocytes assessed as effect on membrane integrity up to 10 uM by LDH release assay
AID270646	Lowering of insulin level in po dosed ZDF rat plasma by glucose tolerance test	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID663895	Adipogenic activity in mouse 3T3L1 cells assessed as increase in triglyceride level at 1 uM after 8 days relative to control	2012	Journal of natural products, Apr-27, Volume: 75, Issue:4	Isoprenylated flavonoid and adipogenesis-promoting constituents of Dodonaea viscosa.
AID1166259	Increase in PPARgamma gene expression in mouse 3T3L1 cells at 10 uM incubated for 24 hrs by real-time PCR method relative to untreated control	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis, in silico molecular docking and biological evaluation of novel oxadiazole based thiazolidine-2,4-diones bis-heterocycles as PPAR-γ agonists.
AID314548	Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643	2008	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID662859	Competitive inhibition of rat MAOB expressed in Pichia pastoris	2011	ACS medicinal chemistry letters, Oct-15, Volume: 3, Issue:1	Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
AID1362977	Cmax in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administeration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID316709	Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
AID241842	Inhibition of human Peroxisome proliferator activated receptor alpha	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and
AID596762	Induction of mouse 3T3L1 cell differentiation assessed as increase in accumulation of intracellular lipid droplet at 1 uM by Oil red O staining	2011	Journal of natural products, Apr-25, Volume: 74, Issue:4	Isoprenylated flavonoids and adipogenesis-promoting constituents from Morus nigra.
AID705321	Down-regulation of lectin expression in mouse 3T3L1 cells at 10 uM after 24 hrs by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Synthesis and biological evaluation of 5-benzylidenepyrimidine-2,4,6(1H,3H,5H)-trione derivatives for the treatment of obesity-related nonalcoholic fatty liver disease.
AID1362971	Glucose-lowering effect in Zucker diabetic fatty rat assessed as reduction in plasma glucose level at 3 mg/kg, po administered once daily for 14 days measured on day 14 post last dose relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID643835	Partial agonist activity at human PPARgamma LBD assessed as activation of CBP1-453 by HTRF assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID364050	Effect on insulin sensitizing activity in mouse 3T3-L1 cells assessed as increase in triglyceride accumulation at 1 uM after 7 days	2008	European journal of medicinal chemistry, Sep, Volume: 43, Issue:9	Insulin-releasing activity of a series of phenylalanine derivatives.
AID643837	Partial agonist activity at human PPARgamma LBD assessed as activation of PGC1 by HTRF assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
AID1251340	Antidiabetic activity in STZ-induced diabetic Wistar rat model assessed as reduction in blood glucose level at 36 mg/kg, po repeated for 15 days by GOD-POD method	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Antidiabetic effect of novel benzenesulfonylureas as PPAR-γ agonists and their anticancer effect.
AID1276070	Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in GTUT4 expression at 2 uM by qPCR method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
AID464094	Antidiabetic activity in Wistar rat hemidiaphragm assessed as glucose uptake at 2 mg after 45 mins by GOD/POD enzymatic method in presence of insulin	2010	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6	Novel glitazones: design, synthesis, glucose uptake and structure-activity relationships.
AID1543229	Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells at 1 uM pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using f
AID382312	Antihyperglycemic effect in Zucker diabetic fatty/Clr-Leprfa rat assessed as increase in body weight level at 10 mg/kg, po once daily for 4 weeks	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID382301	Displacement of [3H2]nTZD4 from human PPARalpha at 10 uM by scintillation proximity assay	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
AID1561662	Partial agonist activity at recombinant N-terminal GFP-fused PPARgamma LBD (unknown origin) assessed as increase in biotinylated-CBP peptide recruitment measured after 2 hrs by HTRF assay	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID444056	Fraction escaping gut-wall elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID701825	Antidyslipidemic activity in diabetic C57BL/KsJ db/db mouse model assessed as reduction in plasma triglyceride level at 25 mg/kg, po qd for 10 days	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Flavone-based novel antidiabetic and antidyslipidemic agents.
AID306523	Agonist activity at PPARgamma receptor expressed in 3T3L1 cells assessed as differentiation of preadipocytes by GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8	Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
AID280027	Effect on lipid level in fat fed hyperlipidemic Golden Syrian hamster at 10 mg/kg, po after 14 days	2007	Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5	Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
AID1512051	Agonist activity at full-length human RXR/PPARgamma expressed in HEK293T cells at 1 uM after 14 to 16 hrs by dual-glo luciferase reporter gene assay relative to untreated control	2019	ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9	A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.
AID276054	Displacement of Fluormone from PPAR gamma	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
AID1363004	Toxicity in Wistar-Imamichi rat assessed as death at 30 to 300 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID488389	Inhibition of glucose uptake in rat L6 myocyte at 50 uM after 24 hrs	2010	Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11	Insulinomimetic activity of two new gallotannins from the fruits of Capparis moonii.
AID354041	Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID25737	Area under the plasma concentration-time curve in rat after peroral administration	2003	Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23	Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.
AID1614971	Agonist activity at GAL4-tagged human PPAR receptor	2019	Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4	Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
AID1362980	Tmax in Zucker diabetic fatty rat at 3 mg/kg, po dosed once daily for 14 days and followed by additional administeration on day 15	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID308927	Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay	2007	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18	Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.
AID1499837	Toxicity in Zucker rat sub-chronic fa/fa prediabetic model assessed as serum AST level at 10 mg/kg, po qd for 31 days measured on day 32 (Rvb = 187 +/- 37 U/L)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.
AID637346	Transactivation of human full length PPARalpha expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor γ selective agonists with protein-tyrosine phosphatase 1B inhibition.
AID421088	Antidiabetic activity in ob/ob mouse assessed as reduction in plasma glucose levels at 1 mg/kg, po once daily for 5 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID421099	Antidiabetic activity in high fat diet-fed streptozotocin-treated mouse assessed as reduction in plasma glucose levels at 30 mg/kg, po once daily for 12 days relative to control	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.
AID1363013	Toxicity in Wistar-Imamichi rat assessed as effect on hemodilution by measuring increase in heart weight at 100 mg/kg, po administered via gavage once daily for 28 days	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part I: Lead identification.
AID156778	In vitro Fold activation relative to maximum activation obtained with carbacyclin (~ 250-fold corresponded to 100%) for human peroxisome proliferator activated receptor delta	2003	Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2	Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID270625	Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARalpha by SPA	2006	Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19	Design and synthesis of dual peroxisome proliferator-activated receptors gamma and delta agonists as novel euglycemic agents with a reduced weight gain profile.
AID1532810	Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation at 4 mM relative to control	2019	European journal of medicinal chemistry, Jan-15, Volume: 162	Design and synthesis of rosiglitazone-ferulic acid-nitric oxide donor trihybrids for improving glucose tolerance.
AID1174868	Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells assessed as maximum fold induction by luciferase reporter gene assay relative to rosiglitazone	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Structural development studies of PPARs ligands based on tyrosine scaffold.
AID387501	Oral bioavailability in Sprague-Dawley rat at 3 mg/kg	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID189063	Percent reduction in triglyceride (TG) after 9 days of dosing in db/db is evaluated in rat for euglycemic and hypolipidemic activities at a dose of 100 mg/kg	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Novel euglycemic and hypolipidemic agents. 1.
AID223541	In vitro transactivation using receptor transactivation assay against hPPAR alpha	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID234403	Maximum achieved Total cholesterol reduction relative to vehicle treated control group	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID551966	Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay	2011	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1	Synthesis of a novel human PPARδ selective agonist and its stimulatory effect on oligodendrocyte differentiation.
AID316706	Inhibition of PPARalpha	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
AID387508	Antihyperglycemic activity in db/db mouse assessed as increase in body weight at 0.1 mg/kg, po once daily after 28 days	2008	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18	Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID483817	Antidiabetic activity in diet-induced obese mouse assessed as decrease in plasma insulin level at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 13 by glucose tolerance test	2010	Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11	Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID223546	Fold activation relative to maximum activation obtained with carbacyclin	2002	Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4	Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1362861	Antidiabetic activity in Zucker diabetic fatty rat assessed as reduction in plasma glucose level at 0.3 mg/kg, po administered once daily for 21 days measured on day 22 relative to control	2018	Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18	Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization.
AID1336347	Displacement of [3H]rosiglitazone from human recombinant PPAR-gamma receptor expressed in Escherichia coli measured after 120 mins by scintillation counting method	2017	Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2	Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID308432	Agonist activity at human PPARgamma by transactivation assay	2007	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16	Design of a partial PPARdelta agonist.
AID1374663	Antiobesity activity in diet-induced obesity C57Bl6/J mouse model assessed as change in plasma glucose level at 3 mg/kg qd for 15 days measured on day 15 post 6 hrs fasting	2018	Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5	Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.
AID1561665	Partial agonist activity at recombinant PPARgamma LBD/N-terminal GFP-fused RXRalpha mutant LBD (unknown origin) assessed as increase in biotinylated-SRC1 peptide recruitment measured after 2 hrs by HTRF assay	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID127615	No significant effect dose level on blood hemoglobin.	1994	Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23	[[omega-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents.
AID1773609	Reduction in hepatic total cholesterol level in ob/ob mouse at 10 mg/kg, po administered once daily for 30 days	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome.
AID1561664	Partial agonist activity at recombinant PPARgamma LBD/N-terminal GFP-fused RXRalpha mutant LBD (unknown origin) assessed as increase in biotinylated-CBP peptide recruitment measured after 2 hrs by HTRF assay	2020	Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9	A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
AID1468738	Displacement of N-terminal biotin-labeled NCOR-ID1 (2253 to 2277 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli by TR-FRET assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID424504	Effect on bodyweight in po dosed C57BL/6J ob/ob mouse assessed as body weight gain relative to untreated control	2009	Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10	4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID540299	A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis	2010	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21	Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519	A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities	2011	Antiviral research, Sep, Volume: 91, Issue:3	High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1802948	Pharmacological In Vitro Assay from Article 10.3109/14756360903468171: \\Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.\\	2010	Journal of enzyme inhibition and medicinal chemistry, Oct, Volume: 25, Issue:5	Synthesis of new 8(S)-HETE analogs and their biological evaluation as activators of the PPAR nuclear receptors.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID493017	Wombat Data for BeliefDocking	2005	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22	Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARgamma partial agonists.
AID1346800	Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)	1998	Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25	N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
AID1346575	Human TRPC5 (Transient Receptor Potential channels)	2011	Molecular pharmacology, Jun, Volume: 79, Issue:6	Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels.
AID1346619	Human TRPM3 (Transient Receptor Potential channels)	2011	Molecular pharmacology, Jun, Volume: 79, Issue:6	Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels.
AID1346800	Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)	1997	The Journal of biological chemistry, Feb-07, Volume: 272, Issue:6	Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs.
AID1346800	Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)	2001	Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24	Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
AID1346800	Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)	1998	The Journal of pharmacology and experimental therapeutics, Feb, Volume: 284, Issue:2	Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
AID1345809	Human FFA1 receptor (Free fatty acid receptors)	2003	Biochemical and biophysical research communications, Feb-07, Volume: 301, Issue:2	A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
AID1159550	Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening	2015	Nature cell biology, Nov, Volume: 17, Issue:11	6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	115 (2.48)	18.2507
2000's	2323 (50.05)	29.6817
2010's	1936 (41.72)	24.3611
2020's	267 (5.75)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Trials	556 (11.71%)	5.53%
Reviews	1 (3.23%)	6.00%
Reviews	335 (7.05%)	6.00%
Case Studies	0 (0.00%)	4.05%
Case Studies	90 (1.90%)	4.05%
Observational	0 (0.00%)	0.25%
Observational	5 (0.11%)	0.25%
Other	30 (96.77%)	84.16%
Other	3,763 (79.24%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (196)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Randomized, Double-Blind, Placebo-Controlled Study of the Safety and Efficacy of Recombinant Human Growth Hormone and/or Rosiglitazone in the Treatment of Human Immunodeficiency Virus-Associated Visceral Adiposity and Insulin Resistance[NCT00130286]	Phase 1/Phase 2	77 participants (Actual)	Interventional	2005-03-31	Completed
Comparison of the Action of the Rosiglitazone-metformin Fixed-dose Combination and of a Metformin-sulfonylurea Free Combination on the B-cell Function in Type 2 Diabetic Patients Not Controlled With Metformin Alone.[NCT00367055]	Phase 4	84 participants (Actual)	Interventional	2004-10-31	Completed
Prescription Patterns, Resource Utilization & Costs - Add-on Therapy With Anti Dipeptidyl Peptidase-IVs vs Rosiglitazone[NCT01332370]		5,391 participants (Actual)	Observational	2009-12-31	Completed
Role of Insulin Action and Free Fatty Acids in Hyperandrogenism and Role of Metabolism of Inositols in Insulin Resistance of Women With Polycystic Ovary Syndrome[NCT01019356]		52 participants (Actual)	Interventional	2006-08-31	Completed
CSP #465 - Glycemic Control and Complications in Diabetes Mellitus Type 2 (VADT)[NCT00032487]	Phase 3	1,791 participants (Actual)	Interventional	2000-12-01	Completed
A Phase 1 Drug-Drug Interaction Study of the Effects of XL184 on the Pharmacokinetics of a Single Oral Dose of Rosiglitazone in Subjects With Solid Tumors[NCT01100619]	Phase 1	40 participants (Actual)	Interventional	2010-04-30	Completed
Comparison of Effects of Rosiglitazone and Metformin on Myocardial, Skeletal Muscle, Liver and Adipose Tissue Insulin Stimulated Glucose Uptake in Patients With Type 2 Diabetes Mellitus[NCT02526615]	Phase 4	48 participants (Actual)	Interventional	2000-10-31	Completed
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study[NCT02456428]		1,499,650 participants (Actual)	Observational	2014-03-31	Completed
A Phase I, Non-randomized Open-label Study to Evaluate the Effect of BAY73-4506 (Regorafenib) on Probe Substrates of CYP 2C9 (Warfarin), 2C19 (Omeprazole) and 3A4 (Midazolam) in a Cocktail Approach (Group A) and on a Probe Substrate of CYP 2C8 (Rosiglitaz[NCT01287598]	Phase 1	41 participants (Actual)	Interventional	2011-08-02	Completed
An Evaluation of the Metabolic Effects of Exenatide, Rosiglitazone, and Exenatide Plus Rosiglitazone in Subjects With Type 2 Diabetes Mellitus Treated With Metformin[NCT00135330]	Phase 3	137 participants (Actual)	Interventional	2005-10-31	Completed
Avandia™ + Amaryl™ or Avandamet™ Compared With Metformin: A 48-week Randomized, Open-label, Multicentre Phase IIIB Study to Compare the Effectiveness of Combination Therapy to Monotherapy in Type 2 Diabetes Mellitus Patients[NCT00131664]	Phase 3	391 participants (Actual)	Interventional	2005-09-30	Completed
A Methodological Study To Evaluate The Effects of Single Oral Doses Of Pioglitazone 45 mg And Rosiglitazone 8 mg On Sodium Balance In Healthy Male Volunteers[NCT01088594]	Phase 1	12 participants (Actual)	Interventional	2010-02-28	Completed
A Long Term, Open Label, Randomised Study in Patients With Type 2 Diabetes, Comparing the Combination of Rosiglitazone and Either Metformin or Sulfonylurea With Metformin Plus Sulfonylurea on Cardiovascular Endpoints and Glycaemia[NCT00379769]	Phase 3	4,447 participants (Actual)	Interventional	2001-04-30	Completed
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes[NCT02476760]		1,417,914 participants (Actual)	Observational	2014-03-31	Completed
Effects of Colesevelam HCl, Avandia® (Rosiglitazone Maleate), or JanuviaTM (Sitagliptin) on Glycemic Parameters and Lipid Profiles in Subjects With Type 2 Diabetes Mellitus Inadequately Controlled on Metformin Monotherapy[NCT00484419]	Phase 3	169 participants (Actual)	Interventional	2007-05-31	Completed
A Phase II Clinical Trial of Anti-PD-1 mAb Therapy Alone or With Metabolic Modulators to Reverse Tumor Hypoxia and Immune Dysfunction in Solid Tumor Malignancies[NCT04114136]	Phase 2	72 participants (Anticipated)	Interventional	2020-09-14	Recruiting
Effect of Inhaled Pre-Prandial Human Insulin Plus Metformin & Glimepiride Versus Rosiglitazone Plus Metformin & Glimepiride on HbA1c in Subjects With Type 2 Diabetes[NCT00427154]	Phase 3	227 participants (Actual)	Interventional	2007-01-10	Terminated(stopped due to See termination reason in detailed description)
Comparison of the Effects of Rosiglitazone and Glimepiride, Both Given in Combination With Metformin, on 24-Hour Glycemia in Type 2 Diabetes Patients Not Controlled With Metformin Alone. A 3-Month Multicentre, Randomized, Parallel-Group, Open-Label Study.[NCT00318656]	Phase 4	23 participants (Actual)	Interventional	2005-11-30	Completed
Rosiglitazone Adjunctive Therapy for Severe Malaria in Children[NCT02694874]		210 participants (Actual)	Interventional	2016-02-29	Active, not recruiting
A Meta Analysis of Malignancy Serious Adverse Events in the ADOPT, 49653/048, and RECORD, 49653/231, Studies, Comparing Metformin With Rosiglitazone.[NCT01195259]		1 participants (Actual)	Observational	2009-10-31	Completed
A 52 Week Randomized, Double-Blind, Multicenter, Mechanistic Study With a 24 Week Open-Label Follow-Up to Evaluate the Effect of AVANDIA TM on Bone in Postmenopausal Women With Type 2 Diabetes Mellitus[NCT00679939]	Phase 4	226 participants (Actual)	Interventional	2008-04-21	Completed
Effects of Simvastatin and Rosiglitazone Combination in Patients With the Metabolic Syndrome.[NCT00831129]	Phase 2/Phase 3	53 participants (Actual)	Interventional	2006-09-30	Completed
Influence of Glitazones on the Vasodilatory Effect of HDL Lipoproteins and on Phospholipase A2[NCT00953498]	Phase 4	40 participants (Actual)	Interventional	2007-10-31	Completed
An Open-label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Cytochrome P450 Probe Drugs in Healthy Adult Subjects[NCT00964106]	Phase 1	87 participants (Actual)	Interventional	2009-08-26	Completed
Effect of Rosiglitazone Versus Placebo on Cardiovascular Performance and Myocardial Triglyceride[NCT00424762]	Phase 4	150 participants (Actual)	Interventional	2005-02-28	Completed
Phase II Clinical Trial of Rosiglitazone, a Full-Agonist Ligand for the Peroxisome Proliferator-Activated Receptor Gamma (PPAR), as Differentiation Therapy for Patients With Liposarcoma[NCT00004180]	Phase 2	32 participants (Actual)	Interventional	1999-10-31	Completed
A Randomized, Placebo-controlled Trial of Rosiglitazone for Treatment of Ulcerative Colitis[NCT00065065]	Phase 2	105 participants (Actual)	Interventional	2002-09-30	Completed
An Open-label Extension to Study 49653/461, to Assess the Long-term Safety of Rosiglitazone (Extended Release Tablets) in Subjects With Mild to Moderate Alzheimer's Disease[NCT00381238]	Phase 2	33 participants (Actual)	Interventional	2006-06-20	Completed
Placebo Controlled Study of Rosiglitazone in HIV Lipoatrophy[NCT00367744]	Phase 2	71 participants (Actual)	Interventional	2006-07-31	Completed
Effects of Avandia on Cognition and Cerebral Glucose Utilisation in Subjects With Mild to Moderate Alzheimer's Disease (AD).[NCT00265148]	Phase 2	80 participants (Actual)	Interventional	2004-05-18	Completed
A Single Center, Single Sequence, Open-Label, Repeat-Dose Study to Investigate the Effect of GSK376501 on Hepatic Cytochrome P450 Activity in Healthy Adult Subjects[NCT00615212]	Phase 1	23 participants (Actual)	Interventional	2008-01-02	Completed
Gene Regulation by Thiazolidinediones[NCT00567593]	Phase 4	12 participants (Actual)	Interventional	2007-10-31	Completed
An Open-label Extension to Study AVA102670 and AVA102672, to Assess the Long-term Safety and Efficacy of Rosiglitazone (Extended Release Tablets) as Adjunctive Therapy on Cognition in Subjects With Mild to Moderate Alzheimer's Disease.[NCT00490568]	Phase 3	1,461 participants (Actual)	Interventional	2007-08-08	Terminated(stopped due to Based on preliminary parent study results)
A Multicenter, Double-Blind, Placebo and Active Controlled, Randomized Study to Evaluate the Safety and Efficacy of the Addition of Sitagliptin 100 mg Once Daily in Patients With Type 2 Diabetes With Inadequate Glycemic Control on Metformin Monotherapy[NCT00541775]	Phase 3	273 participants (Actual)	Interventional	2006-06-30	Completed
A 54-week, Double-blind, Randomized, Placebo-controlled, Parallel-group Study to Investigate the Effects of Rosiglitazone (Extended Release Tablets) as Adjunctive Therapy to Donepezil on Cognition and Overall Clinical Response in APOE ε4-stratified Subjec[NCT00348309]		1,496 participants (Actual)	Interventional	2006-07-06	Completed
A Phase III, 18 Month, Multicenter, Randomized, Double-Blind, Active-Controlled Clinical Trial to Compare Rosiglitazone Versus Glipizide on the Progression of Atherosclerosis in Subjects With Type 2 Diabetes Mellitus and Cardiovascular Disease (APPROACH)[NCT00116831]	Phase 3	672 participants (Actual)	Interventional	2005-01-31	Completed
Effects of Physical Exercise Versus Rosiglitazone on Endothelial Function in Coronary Artery Disease Patients With Prediabetes[NCT00675740]	Phase 4	45 participants (Actual)	Interventional	2004-01-31	Completed
Rosiglitazone Versus Rosiglitazone and Metformin (Avandamet) Versus Combination Rosiglitazone and Losartan in the Treatment of Nonalcoholic Steatohepatitis (NASH). A Prospective, Open-Label, Randomized Trial[NCT00699036]	Phase 2	165 participants (Anticipated)	Interventional	2007-04-30	Recruiting
A Phase I, Double Blind, Randomized, Two-Way Cross Over, Single- Centre Study in Healthy CYP2D6 Extensive Metabolizers and Poor Metabolizers to Investigate the Potential of AZD3480 to Inhibit Cytochrome P450 1A2, 2C19, 3A4, 2C8, 2B6 and UGT1A1 Activity[NCT00692510]	Phase 1	18 participants (Anticipated)	Interventional	2007-11-30	Completed
Randomized Clinical Trial, Effect of Metformin and Rosiglitazone Over Glucose Homeoastasis in no Diabetic With Metabolic Syndrome Patients.[NCT04148183]	Phase 2/Phase 3	30 participants (Actual)	Interventional	2004-01-01	Completed
Rosiglitazone and Exercise in Patients With Type 2 Diabetes Mellitus[NCT00306176]	Phase 4	100 participants	Interventional	2005-01-31	Completed
A 24-Week,Int.,Rand.,Double-blind,Parallel-group,Multi-centre, Plac.-Controlled Phase III Study With a 24-Wk Ext.Per.to Eval.the Efficacy and Safety of Dapagliflozin in Comb.With Glimepiride (a Sulphonylurea) in Subjects With Type2 Diab.Who Have Inadeq. G[NCT00680745]	Phase 3	597 participants (Actual)	Interventional	2008-04-30	Completed
A Phase Ib, Open-Label, Pharmacokinetic Drug Interaction Study of the Hedgehog Pathway Inhibitor GDC-0449 in Combination With Rosiglitazone or Combined Oral Contraceptive in Patients With Locally Advanced or Metastatic Solid Tumors That Are Refractory to [NCT01209143]	Phase 1	52 participants (Actual)	Interventional	2010-11-30	Completed
An Open Label Single Oral Dose Study in Patients With Mild Alzheimer's Disease to Assess the Pharmacokinetics of Extended Release Formulation of Rosiglitazone (RSG XR) in This Population[NCT00688207]	Phase 1	14 participants (Actual)	Interventional	2008-04-30	Completed
An Open-Label, Three-Part, Two Period, Single Sequence Study to Assess the Pharmacokinetic Interaction Between Repeat Doses of Oral Casopitant and Repeat Oral Doses of Dolasetron, Granisetron or Rosiglitazone When Co-Administered in Healthy Adult Subjects[NCT00511823]	Phase 1	16 participants (Actual)	Interventional	2007-07-23	Completed
Atherosclerotic Plaque Texture-Experimental and Clinical Study on the Diagnostic and Therapeutic Strategies of Atherosclerotic Plaque Vulnerability[NCT00636766]		300 participants (Actual)	Interventional	2005-09-30	Completed
An Open-Label, Single-Sequence Study to Assess the Effect of Multiple Doses of Tasimelteon on the Cytochrome P450 3A4 and 2C8 Enzymes Using Midazolam and Rosiglitazone as Substrates in Healthy Subjects[NCT01402076]	Phase 1	24 participants (Actual)	Interventional	2011-08-31	Completed
The Effect of Glitazone Treatment on Bone Marrow and Bone Marrow Cells[NCT00609362]	Phase 2	57 participants (Actual)	Interventional	2008-01-31	Completed
Insulin Resistance and Intramyocellular Lipid Content in Glucose Intolerant Subjects Receiving Rosiglitazone[NCT00746174]	Phase 4	24 participants (Actual)	Interventional	2004-02-29	Completed
Rosiglitazone And Fenofibrate Additive Effects on Lipids (RAFAEL)[NCT00819910]	Phase 4	41 participants (Actual)	Interventional	2008-09-30	Terminated(stopped due to Slow recruitment and increase in deployment overseas limiting follow up)
The Impact of Obesity and Obesity Treatments on Breast Cancer: A Phase I Trial of Exemestane With Metformin and Rosiglitazone for Postmenopausal Obese Women With ER+ Metastatic Breast Cancer[NCT00933309]	Phase 1	25 participants (Actual)	Interventional	2009-07-31	Completed
A Phase III Randomized, Placebo-Controlled Clinical Trial to Study the Safety and Efficacy of the Addition of Sitagliptin (MK0431) in Patients With Type 2 Diabetes Mellitus Who Have Inadequate Glycemic Control on Combination Therapy With Metformin and a P[NCT00350779]	Phase 3	262 participants (Actual)	Interventional	2006-06-12	Completed
A Single-Blind, Placebo-Controlled, Randomized First Time in Human Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Repeat Dose Escalation of GSK932121 in Healthy Adult Subjects[NCT00811356]	Phase 1	12 participants (Actual)	Interventional	2008-12-11	Terminated(stopped due to safety issues (toxicity))
Treatment With Rosiglitazone for the Prevention of Glucose Intolerance in Patients Treated With Corticosteroids[NCT00240604]	Phase 3	100 participants (Anticipated)	Interventional	2005-04-30	Recruiting
Obesity, Insulin Resistance, and Bone Metabolism in Adolescents With PCOS: Effects of Insulin Sensitizers Versus Oral Contraceptives[NCT00640224]	Phase 4	65 participants (Actual)	Interventional	2005-03-31	Completed
EMPOWIR: Enhance the Metabolic Profile of Women With Insulin Resistance: Carbohydrate Modified Diet Alone and in Combination With Metformin or Metformin Plus Avandia in Non-diabetic Women With Midlife Weight Gain and Documented Insulin Elevations (Syndrom[NCT00618072]	Phase 2	46 participants (Actual)	Interventional	2008-01-31	Completed
A Randomized, Double-Blind, Placebo-Controlled Study of Metformin and Rosiglitazone, Alone or in Combination, in HIV-Infected Subjects With Hyperinsulinemia and Elevated Waist/Hip Ratio[NCT00015691]		105 participants	Interventional		Completed
Insulin, Neurogenetics and Memory in Alzheimer's Disease: A Novel Therapeutic Approach[NCT00018382]	Phase 2	0 participants	Interventional	1999-10-31	Completed
The Impact of Rosiglitazone on Regression of Atherosclerosis: A Serial 18F-Fluorodeoxyglucose Positron Emission Tomography Study[NCT00166803]		60 participants (Anticipated)	Interventional	2005-06-30	Suspended(stopped due to no fund)
Insulin Resistance in Non-alcoholic Fatty Liver Disease[NCT00252499]		13 participants (Actual)	Interventional	2005-10-31	Terminated(stopped due to Protocol drug change required new clinicaltrails.gov entry)
An Open Label, Multicenter Study Evaluating the Safety and Efficacy of Short Term (6 Weeks) Rosiglitazone Treatment in Patient's With Cushing's Disease[NCT00612066]	Phase 2	2 participants (Actual)	Interventional	2007-04-30	Terminated(stopped due to Low accrual and funding term ended)
Rosiglitazone (Avandia) vs. Placebo for Androgen Dependent Prostate Cancer: A Randomized Double-Blind, Placebo Controlled Phase III Study[NCT00182052]	Phase 3	100 participants (Actual)	Interventional	2000-09-30	Completed
Effects of Rosiglitazone on Renal Hemodynamics and Proteinuria of Type 2 Diabetic Patients With Renal Insufficiency Due to Overt Diabetic Nephropathy[NCT00324675]		28 participants (Actual)	Interventional	2006-08-31	Completed
A 24-week, Double-blind, Double-dummy, Randomized, Parallel-group Study to Investigate the Effects of Rosiglitazone (Extended Release Tablets), Donepezil, and Placebo as Monotherapy on Cognition and Overall Clinical Response in APOE ε4-stratified Subjects[NCT00428090]	Phase 3	862 participants (Actual)	Interventional	2007-02-27	Completed
Comparison Fenofibrate, Rosiglitazone, or Weight Loss to Decrease Cardiovascular Risk in Insulin Resistant Dyslipidemic Individuals.[NCT00186537]		47 participants (Actual)	Interventional	2003-09-30	Completed
A 54 Week, Double-blind, Randomised, Placebo-controlled, Parallel Group Study to Investigate the Effects of Rosiglitazone (Extended Release Tablets) as Adjunctive Therapy to Acetylcholinesterase Inhibitors on Cognition and Overall Clinical Response in APO[NCT00348140]	Phase 3	1,468 participants (Actual)	Interventional	2006-07-12	Completed
A Pilot Trial of Combination Therapy With Interferon Alfacon1, Ribavirin, & Rosiglitazone in a Group of Insulin Resistant, Chronic Hepatitis C, GT 1 Patients Who Are Previous Relapsers or Nonresponders to Pegylated Interferon and Ribavirin[NCT00207402]	Phase 4	34 participants (Actual)	Interventional	2005-10-31	Completed
A Single-centre, Randomised, Double-blind, Placebo Controlled, Two 12 Week Period, Cross-over Phase III Study to Investigate the Effect of Rosiglitazone 4mg bd on the Vasodilator Response to Hyperinsulinaemia in Obese Insulin Resistant Subjects.[NCT00197132]	Phase 3	18 participants (Actual)	Interventional	2002-10-31	Completed
Rosiglitazone and Plaque Study: A 12 Month Randomised, Double-blind, Placebo-controlled, Magnetic Resonance Imaging Study to Evaluate the Effect of Rosiglitazone on the Structure and Composition of Carotid Atherosclerotic Plaques in Subjects With Type 2 D[NCT00231387]	Phase 3	60 participants	Interventional	2002-09-30	Completed
Effect of Pioglitazone on Left Ventricular Diastolic Function in Type 2 Diabetes Mellitus[NCT00232362]	Phase 1	0 participants (Actual)	Interventional	2007-06-30	Withdrawn(stopped due to This study was not conducted as the Principal Investigator left the institution)
AVANDAMET Compared to Metformin Evaluation Trial (ACME): A 48-week Randomized, Open-label, Multicenter Study to Compare the Efficacy and Tolerability of AVANDAMET to Metformin Monotherapy in Subjects With Type 2 Diabetes Mellitus Who Are Not Achieving Gly[NCT00241605]	Phase 4	600 participants	Interventional	2003-06-25	Completed
An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance to Monitor the Safety and/or Efficacy of Avandamet® Administered in Korean Diabetic Patients According to the Prescribing Information[NCT01294553]		717 participants (Actual)	Observational	2004-06-30	Completed
[NCT00006493]	Phase 2	0 participants	Interventional		Completed
A Pilot Study to Determine the Effects of Short-term Thiazolidinedione Treatment on Vascular Risk Markers in Type 2 Diabetes Patients[NCT00571506]	Phase 4	25 participants (Actual)	Interventional	2004-05-31	Completed
An Open-Label, Randomized, Crossover Study to the Dose Proportionality of RSG XR in Healthy Volunteers in Fasting Conditions[NCT00733785]	Phase 1	60 participants (Actual)	Interventional	2008-08-13	Completed
An Open-Label Drug-Drug Interaction Study to Investigate the Effects of Steady State Quinine on the Single-Dose Pharmacokinetics of Rosiglitazone Maleate in Healthy Volunteers[NCT00785213]	Phase 1	23 participants (Actual)	Interventional	2008-09-30	Completed
Rosiglitazone (Peroxisome Proliferating Activating Receptor-gamma {PPAR-y} Ligand) Treatment of Pituitary Tumors[NCT00616642]	Phase 2	1 participants (Actual)	Interventional	2006-10-31	Terminated(stopped due to low patient recruitment)
A Multicenter, Randomized, Double Blind, Placebo Controlled, Phase III Trial to Evaluate the Efficacy and Safety of Saxagliptin (BMS477118) in Combination With Thiazolidinedione Therapy in Subjects With Type 2 Diabetes Who Have Inadequate Glycemic Control[NCT00295633]	Phase 3	565 participants (Actual)	Interventional	2006-03-31	Completed
The Effects of the PPARy Agonist Rosiglitazone on Airway Hyperreactivity[NCT00614874]	Phase 2	16 participants (Actual)	Interventional	2008-12-31	Completed
Evaluation of the Duration of Oral Combination Therapy in Type 2 Diabetes, Prior to the Initiation of Insulin in the UK[NCT00995995]		7,641 participants (Actual)	Observational	2008-10-31	Completed
Rosiglitazone Therapy In The Prevention Of Coronary Artery Disease In Patients With Impaired Glucose Tolerance[NCT00733174]	Phase 4	60 participants (Anticipated)	Interventional	2004-03-31	Recruiting
AVANDIA CV Outcomes Study: Thiazolidinedione Intervention With Vitamin D Evaluation (TIDE) A Multicenter Randomized Double-Blind Placebo-Controlled Trial of a Thiazolidinedione or Placebo and of Vitamin D or Placebo In People With Type 2 Diabetes at Risk [NCT00879970]	Phase 4	1,332 participants (Actual)	Interventional	2009-05-31	Terminated(stopped due to FDA has placed the trial on full clinical hold.)
Effects of Rosiglitazone and Alpha-lipoic Acid on the Patients With Pathologically Proved NASH (Non-alcoholic Steato-hepatitis)[NCT01406704]	Phase 4	26 participants (Actual)	Interventional	2004-01-31	Terminated(stopped due to because of withdrawal of Avandia sale due to its risks outweigh its benefits)
A PHASE I, SINGLE-CENTER, OPEN-LABEL, CROSSOVER STUDY OF THE EFFECT OF AVANAFIL ON THE PHARMACOKINETICS OF OMEPRAZOLE, DESIPRAMINE AND ROSIGLITAZONE IN HEALTHY MALE SUBJECTS[NCT01415128]	Phase 1	60 participants (Actual)	Interventional	2010-04-30	Completed
Pioglitazone Versus Rosiglitazone in Subjects With Type 2 Diabetes Mellitus and Dyslipidemia[NCT00331487]	Phase 3	719 participants (Actual)	Interventional	2000-09-30	Completed
A Double-blind, Randomised, Placebo-controlled, Parallel-group Study to Investigate the Effects of Rosiglitazone (Extended Release Tablets) on Cerebral Glucose Utilisation and Cognition in Subjects With Mild to Moderate Alzheimers Disease (AD)[NCT00334568]	Phase 2	12 participants (Actual)	Interventional	2004-12-31	Terminated(stopped due to Slow recruitment)
Cellular Mechanisms for Metabolic Dysfunction in HIV[NCT00006185]	Phase 1	0 participants	Interventional	1999-09-30	Completed
A Multicenter Randomized Double-Blind Trial Comparing Rosiglitazone to Placebo for the Prevention of Atherosclerosis Progression After Coronary Bypass Surgery in Diabetic Patients[NCT00169832]	Phase 3	193 participants (Actual)	Interventional	2003-06-30	Completed
[NCT00409097]	Phase 3	30 participants	Interventional	2006-04-30	Recruiting
A Randomised, Double-Blind, Placebo-Controlled, Cardiovascular Magnetic Resonance (CMR) Study to Evaluate the Effect of Rosiglitazone on Carotid Atherosclerotic Plaques in Type 2 Diabetics With Vascular Disease or Hypertension[NCT00123227]	Phase 3	60 participants	Interventional	2002-10-31	Active, not recruiting
The Effect of CYP2C8 E274Q, a Novel 23452 G>T SNP, on the Disposition of Rosiglitazone in Healthy Subjects: The Genetic Polymorphisms of CYP2C8 in a Korean Population[NCT01872780]	Phase 1	11 participants (Actual)	Interventional	2008-08-31	Completed
Phase IIA Trial of Rosiglitazone (Avandia) for Oral Leukoplakia[NCT00369174]	Phase 2	25 participants (Actual)	Interventional	2006-06-30	Completed
A Randomized, Double-Blind, Placebo-Control, Clinical Evaluation of Insulin Plus Rosiglitazone Compared to Insulin Plus Placebo for 24 Weeks in Subjects With Type 2 Diabetes Mellitus Who Are Inadequately Controlled On Insulin[NCT00349427]	Phase 3	256 participants (Actual)	Interventional	2005-10-31	Completed
Ppar-Gamma EliminAtes Restenosis Longevity Study: PEARLS[NCT00465296]	Phase 3	200 participants (Anticipated)	Interventional	2006-01-31	Terminated(stopped due to Funding Discontinued)
A 24-Week Randomized, Double-blind, Double-Dummy, Multicenter Study to Compare the Efficacy of AVANDIA When Added to Submaximal Doses of Metformin and to Compare the Tolerability of the Combination to Metformin Monotherapy When Administered to Subjects Wi[NCT00501020]	Phase 4	750 participants	Interventional	2001-06-05	Completed
[NCT00501488]		42 participants (Actual)	Observational	2006-03-31	Completed
Effects of Rosiglitazone on Serum Ghrelin and Peptide YY Levels in Diabetic Women[NCT00522470]	Phase 4	0 participants	Interventional		Completed
Clinical Evaluation of Rosiglitazone Malate (BRL49653C) in Patients With Type 2 Diabetes Mellitus -Long-term Study of Rosiglitazone Maleate-[NCT00523913]	Phase 3	70 participants (Actual)	Interventional	2005-11-30	Completed
A Single-Center, Non-Randomized, Open-Label, Comparative Study to Assess the Utility of Novel Technologies and Biomarkers as Methods for Measuring Human Pharmacodynamic Response to 8 Weeks of Administration of Rosiglitazone Maleate 4mg BID in Healthy Norm[NCT00551564]	Phase 1	36 participants (Actual)	Interventional	2007-07-31	Completed
Attenuating Insulin Resistance as a Therapeutic Target in the Management of Heart Failure[NCT00064727]	Phase 2	50 participants	Interventional	2003-07-09	Completed
The Effects of Rosiglitazone on Cognition in Patients With MCI[NCT00242593]	Phase 2	120 participants (Anticipated)	Interventional	2006-06-30	Active, not recruiting
A 24 Week, Randomised, Double Blind, Parallel Study to Compare the Change in HbA1c With AVANDAMET® (8.0mg / 2.0g) Plus Insulin to Placebo Plus Insulin, in Subjects With Type 2 Diabetes Starting Insulin Therapy[NCT00069836]	Phase 3	272 participants (Actual)	Interventional	2003-10-31	Completed
Randomized Placebo-Control Pilot Study Evaluating the Efficacy and Safety of Rosiglitazone Combined With Pegylated Interferon Plus Ribavirin Versus Pegylated Interferon Plus Ribavirin Alone in Genotype 1 Hepatitis C With Steatosis[NCT00274495]	Phase 4	30 participants (Anticipated)	Interventional	2006-01-31	Terminated
Assessment of the Effect of Rosiglitazone on Insulin Secretion in Healthy Volunteers[NCT00285142]		12 participants	Interventional	2004-06-30	Completed
The Influence of Rosiglitazone on the Diuretic Effect of Furosemide and Amiloride. A Double-blind Placebo Controlled Cross Over Study.[NCT00285805]		13 participants (Actual)	Interventional	2006-02-28	Completed
A Clinical Study to Investigate the Effect of Rosiglitazone, Theophylline and Inhaled Corticosteroid, Inflammation and Pulmonary Function in Asthmatic Smokers[NCT00119496]	Phase 2/Phase 3	79 participants (Actual)	Interventional	2005-07-31	Completed
Study of Niacin and Rosiglitazone in Dysmetabolic Dyslipidemia[NCT00304993]	Phase 4	30 participants	Interventional	2001-01-31	Completed
Endometriosis: Immunomodulation[NCT00121953]	Phase 2/Phase 3	0 participants (Actual)	Interventional	2005-07-31	Withdrawn(stopped due to Due to the recent meta-analysis about CV adverse effects.)
A Randomized Trial of Celecoxib and Rosiglitazone, Alone and in Combination, in Patients With Early Stage Non-Invasive Bladder Carcinoma Undergoing Cystoscopic Surveillance and in Patients With Muscle-Invasive Bladder Cancer Undergoing Radical Cystectomy[NCT00084578]		0 participants (Actual)	Interventional	2004-03-31	Withdrawn(stopped due to Withdrawn due to drug toxicity)
Effect on Glycemic Control of Liraglutide in Combination With Rosiglitazone Plus Metformin Versus Rosiglitazone Plus Metformin in Subjects With Type 2 Diabetes[NCT00333151]	Phase 3	576 participants (Actual)	Interventional	2006-05-31	Completed
The DREAM (Diabetes Reduction Assessment With Ramipril and Rosiglitazone Medication) Trial[NCT00095654]	Phase 3	5,000 participants	Interventional	2001-07-31	Completed
A Pilot Study of Rosiglitazone in Patients With Incurable Differentiated Thyroid Cancer[NCT00098852]	Phase 2	25 participants (Anticipated)	Interventional	2004-10-31	Active, not recruiting
A Randomized, Blinded, Placebo-controlled Study to Investigate the Safety, and Pharmacokinetics of Single and Repeat Dose Escalation of the Oral YAK3/DYRK3 Inhibitor GSK626616AC in Healthy Subjects[NCT00443170]	Phase 1	90 participants (Actual)	Interventional	2006-11-30	Completed
Efficacy and Safety of Inhaled Pre-prandial Human Insulin Plus Metformin Versus Rosiglitazone Plus Metformin in Type 2 Diabetes[NCT00348712]	Phase 3	301 participants (Actual)	Interventional	2006-10-30	Terminated(stopped due to See termination reason in detailed description)
Treatment of Endometriosis Pain With Rosiglitazone: A Prospective Phase 2 Clinical Trial[NCT00115661]	Phase 2	25 participants (Anticipated)	Interventional	2005-07-31	Terminated(stopped due to Due to the meta-analysis about CV adverse effects of rosiglitazone.)
The Effect of Rosiglitazone on Ischemia-reperfusion-injury Using Annexin A5 Scintigraphy. A Double Blind Placebo- Controlled Cross-over Study in Subjects With the Metabolic Syndrome[NCT00405015]	Phase 2	13 participants (Actual)	Interventional	2007-04-30	Completed
CAnadian Normoglycemia Outcomes Evaluation Study[NCT00116922]	Phase 3	207 participants (Actual)	Interventional	2004-06-30	Completed
Evaluation of Predictive Markers of Glitazone Efficacy in Diabetic Patients - Pilot Study[NCT00481429]		0 participants (Actual)	Observational	2007-05-31	Withdrawn(stopped due to Unable to recruit enough participants)
Effects of ROSIglitazone on Inflammatory Markers and Adipokines in Diabetic Patients Using an Angiotensin Receptor Blocker (TELmisartan) - The ROSITEL Study[NCT00486187]		103 participants (Actual)	Interventional	2006-04-30	Completed
Studies on Diabetic and Pre Diabetic Vascular Disease and the Effect of Selected Therapeutic Modalities on Associated Vasculopathy[NCT00489229]	Phase 3	66 participants (Actual)	Interventional	2002-10-31	Completed
A One-Year, Randomized, Double-Blind, Placebo-Controlled Trial of Rosiglitazone in Non-Alcoholic Steatohepatitis[NCT00492700]	Phase 2	63 participants (Actual)	Interventional	2003-01-31	Completed
Characterization of Vascular Effects of Rosiglitazone.[NCT00154011]		24 participants	Interventional	2005-09-30	Completed
Effect of Rosiglitazone Maleate (Avandia®) on Carotid Intima Media Thickness, Brachial Artery Reactivity, Glucose Metabolism, Blood Lipid Concentrations, Body Fat Distribution, and Biochemical Markers of Cardiovascular Risk in Patients With the HIV Metabo[NCT00143624]		50 participants (Anticipated)	Interventional	2003-06-30	Completed
Cyclotron Produced Isotopes in Biology and Medicine, Project 3: Specific Aim 1A and 1B Effects of Fatty Acid Delivery on Myocardial Metabolism and Function in Type 2 Diabetes (T2DM)[NCT00577590]		78 participants (Actual)	Interventional	2003-10-31	Completed
Targeting Peroxisome Proliferator-activated Receptor-gamma in Peritoneal Dialysis Patients - Will it Reduce Inflammation, Atherosclerosis, Calcification and Improve Survival of Peritoneal Dialysis Patients?[NCT00516880]		160 participants (Anticipated)	Interventional	2006-03-31	Recruiting
Anti-Inflammatory Effects of Rosiglitazone in Patients With Stage 4 and 5 Chronic Kidney Disease[NCT00169923]	Phase 2/Phase 3	200 participants (Anticipated)	Interventional	2007-04-30	Withdrawn(stopped due to it was not possible to recruit any patient in the study)
Effect of Rosiglitazone on Myocardial Blood Flow Regulation in Type 2 Diabetes[NCT00549874]		27 participants (Actual)	Interventional	2002-02-28	Completed
Rosiglitazone-Induced Weight Gain[NCT00225225]		45 participants (Actual)	Interventional	2002-10-31	Terminated(stopped due to due to published data on Rosiglitazone)
Effects of Rosiglitazone and Sulphonylureas on Ischaemic Burden, Blood Pressure and Novel Risk Markers Inclusive of Vascular Function in Patients With Chronic Stable Angina and Type 2 Diabetes Mellitus: A Randomised, Double-Blinded Study.[NCT00225342]	Phase 4	60 participants	Interventional		Withdrawn
A Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Control, Clinical Evaluation of Insulin Plus Rosiglitazone (2mg and 4mg) Compared to Insulin Plus Placebo for 24 Weeks in Subjects With Type 2 Diabetes Mellitus Who Are Inadequately Controll[NCT00329225]	Phase 4	630 participants (Actual)	Interventional	2002-09-30	Completed
Rosiglitazone and Insulin Resistance in Renally Impaired Patients[NCT00452166]	Phase 3	30 participants (Anticipated)	Interventional	2007-04-30	Terminated(stopped due to it was not possible to recruit new patients anymore)
Comparison of Rosiglitazone Versus Glyburide on Vascular Structure and Function in Type 2 Diabetic Patients[NCT00123643]	Phase 4	36 participants (Actual)	Interventional	2003-05-31	Completed
Defining the Role of Insulin Resistance in 'Idiopathic' Dilated Cardiomyopathy[NCT00466713]		0 participants	Interventional	2007-03-31	Terminated(stopped due to concern over safety of rosiglitazone in heart failure)
[NCT00440375]	Phase 4	82 participants	Interventional	2005-06-30	Completed
A Randomized, Double-blind Trial to Evaluate the Efficacy and Safety of Fixed Dose Rosiglitazone/Metformin Combination Therapy Compared to Both Rosiglitazone and Metformin Monotherapies in Drug Naive Type 2 Diabetes Mellitus Subjects[NCT00499707]	Phase 3	453 participants (Actual)	Interventional	2003-10-08	Completed
A Study to Evaluate the Efficacy of Rosiglitazone (BRL-049653) on Reduction of Microalbuminuria in Subjects With Type 2 Diabetes Mellitus[NCT00500955]	Phase 3	336 participants	Interventional	2000-04-30	Completed
[NCT00483392]		0 participants	Interventional		Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Multicenter Study of the Effects of PN2034 in Type 2 Diabetes Patients on Concomitant Rosiglitazone and Metformin (or Avandamet) Therapy[NCT00110851]	Phase 2	90 participants (Anticipated)	Interventional	2005-04-30	Completed
South Danish Diabetes Study: A Prospective Randomised Multi-Centre Study for the Evaluation of the Optimal Pharmacological Antidiabetic Treatment of Type 2 Diabetes Mellitus[NCT00121966]	Phase 4	400 participants	Interventional	2003-01-31	Completed
Rosiglitazone and Exercise Training: Effects on HIV-Infected People With Insulin Resistance, Hypertriglyceridemia, and Adipose Tissue Maldistribution[NCT00025753]		0 participants	Interventional		Completed
Action to Control Cardiovascular Risk in Diabetes (ACCORD)[NCT00000620]	Phase 3	10,251 participants (Actual)	Interventional	1999-09-30	Completed
An Open-label Trial to Evaluate the Safety and Efficacy of Fixed Dose Rosiglitazone/Metformin Combination Therapy in Poorly-controlled Subjects With Type 2 Diabetes Mellitus[NCT00067951]	Phase 3	190 participants (Actual)	Interventional	2003-10-17	Completed
The Study of Atherosclerosis With Ramipril and Rosiglitazone[NCT00140647]	Phase 3	1,200 participants	Interventional	2001-07-31	Completed
A Clinical Trial to Prevent the Complications of Insulin Resistance (Including Type-2 Diabetes)[NCT00015626]	Phase 2	300 participants	Interventional		Completed
Endothelial Dysfunction as a Risk Factor in HIV Study[NCT00039663]	Phase 1	75 participants	Interventional	2002-05-31	Completed
A Multi-center, Randomized, Open-label, Active Controlled, Parallel Arm Study to Compare the Efficacy of 12 Weeks of Treatment With Vildagliptin 100 mg, qd to Thiazolidinedione (TZD) as add-on Therapy in Patients With Type 2 Diabetes Inadequately Controll[NCT00396227]	Phase 3	2,665 participants (Actual)	Interventional	2006-10-31	Completed
The Addition of Rosiglitazone to Insulin in Adolescents With Type 1 Diabetes and Poor Glycaemic Control: a Randomized, Placebo Controlled Trial[NCT00372086]	Phase 4	32 participants	Interventional	2003-08-31	Completed
A Trial of the Effect of Rosiglitazone as Add on to Metformin Therapy on Endothelial Function in Subjects With Type II DM[NCT00203632]	Phase 3	40 participants (Actual)	Interventional	2003-09-30	Terminated(stopped due to Terminated at 50% enrollment due to recent concerns about rosiglitazone)
A Multi-center, Randomized, Double-blind, Parallel-group Study to Compare the Efficacy and Safety of Fixed-dose Rosiglitazone/Glimepiride Combination Therapy With Glimepiride Monotherapy for 24 Weeks in Drug Naive Subjects With Type 2 Diabetes[NCT01453049]	Phase 3	86 participants (Actual)	Interventional	2010-04-30	Terminated(stopped due to US FDA/EMA/SFDA decisions to rosiglitazone-containing medicines, ethic)
Repaglinide and Metformin Combination Tablet (NN4440) in a TID Regimen Compared to a BID Regimen and BID Avandamet in Subjects With Type 2 Diabetes: A Twenty-Six Week, Open-Label, Multicenter, Randomized, Parallel Group Trial to Investigate Efficacy and S[NCT00399711]	Phase 3	560 participants (Actual)	Interventional	2006-11-30	Completed
A Randomized, Double-blind, Placebo-controlled Trial of Rosiglitazone as Adjunctive Therapy for P.Falciparum Infection[NCT00149383]	Phase 1/Phase 2	140 participants (Actual)	Interventional	2004-12-31	Completed
A 24-week Randomized, Double-Blind, Parallel-Group, Multicenter Study to Demonstrate the Efficacy and Safety of Two Different Rosiglitazone Dosing Regimens, 4mg OD and 8mg OD, in Poorly-Controlled Drug Naive Patients With Type 2 Diabetes Mellitus[NCT00044460]	Phase 4	142 participants	Interventional	2002-05-31	Completed
Novel Therapies for Resistant FSGS[NCT00193648]	Phase 1	21 participants (Actual)	Interventional	2005-07-31	Completed
Insulin Sensitisation as a Novel Mechanism to Lessen Ischaemic Burden in Overweight Non-Diabetic Patients With Chronic Stable Angina: A Pilot Study[NCT00225355]	Phase 4	80 participants (Anticipated)	Interventional	2006-02-28	Terminated
Effects of Rosiglitazone on the Metabolic Phenotype of Impaired Glucose Tolerance in Youth[NCT00413335]		21 participants (Actual)	Interventional	2005-11-30	Completed
Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study[NCT05220917]		781,430 participants (Anticipated)	Observational	2021-08-01	Active, not recruiting
Free Fatty Acid-Induced Hypertension in Obese Subjects With Type 2 Diabetes[NCT00738023]	Phase 4	36 participants (Actual)	Interventional	2004-03-31	Completed
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes[NCT02475499]		886,172 participants (Actual)	Observational	2014-03-31	Completed
Analyzing Beta Cell Function Tests Over Time In Patients With Type 2 Diabetes Mellitus Randomized To Metformin Or Rosiglitazone[NCT00282945]		29 participants (Actual)	Interventional	2006-01-31	Terminated(stopped due to See statement in Detailed Description.)
A Randomized, Double-Blind Study to Compare the Durability of Glucose Lowering and Preservation of Pancreatic Beta-Cell Function of Rosiglitazone Monotherapy Compared to Metformin or Glyburide/Glibenclamide in Patients With Drug-Naive, Recently Diagnosed [NCT00279045]	Phase 3	4,426 participants (Actual)	Interventional	2000-01-03	Completed
CSP #465D - Markers And Mechanisms of Vascular Disease in Type II Diabetes[NCT00256646]		298 participants (Actual)	Observational	2007-06-30	Completed
Study of PPAR Gamma Agonist-Rosiglitazone in Normotensive Type 2 Diabetics With Ambulatory Blood Pressure Monitoring[NCT00290394]	Phase 4	25 participants	Interventional	2004-03-31	Completed
Effect of Diet, Exercise and Rosiglitazone on Regional Fat and Insulin Resistance in HIV-Infected and Uninfected Men and Women[NCT00264251]		48 participants (Anticipated)	Interventional	2005-07-31	Completed
A Randomised Study Examining the Effect of Different Diuretics on Fluid Balance in Diabetics Treated With Avandia[NCT00306696]	Phase 4	388 participants (Actual)	Interventional	2002-10-31	Completed
A Prospective, Longitudinal Study to Assess the Metabolic and Renal Effects of Rosiglitazone in Albuminuric Kidney Transplant Recipients[NCT00309309]	Phase 2	10 participants (Actual)	Interventional	2005-04-30	Completed
[NCT00309660]	Phase 1/Phase 2	20 participants	Interventional	2005-11-30	Recruiting
A Randomised Double-blind Two-period Crossover Study to Investigate the Effect of Treatment With Repeat Doses of a PPAR Gamma Agonist on the Allergen-induced Late Asthmatic Response in Subjects With Mild Asthma Compared With Repeat Doses of Placebo[NCT00318630]	Phase 1	26 participants (Actual)	Interventional	2005-07-22	Completed
A Study of PPAR-Gamma Agonist-Rosiglitazone for Determining Cardiac Adverse Effects in Type 2 Diabetic Patients[NCT00300911]	Phase 4	45 participants	Interventional	2005-12-31	Completed
A 24-Week Randomized, Double-blind Study to Evaluate the Efficacy, Safety and Tolerability of AVANDIA (8mg Once Daily) in Combination With Glyburide in African American and Hispanic Patients With Type 2 Diabetes Mellitus Who Are Inadequately Controlled on[NCT00333723]	Phase 4	245 participants (Actual)	Interventional	2000-07-28	Completed
Effect of Rosiglitazone and Placebo on Carotid Intima Media Thickness in Patients With Insulin Resistance Syndrome and/or Type 2 Diabetes[NCT00306644]	Phase 4	556 participants (Actual)	Interventional	2002-05-31	Completed
Safety and Efficacy of Inhaled Pre-prandial Human Insulin Plus Glimepiride Versus Rosiglitazone Plus Glimepiride in Type 2 Diabetes[NCT00343980]	Phase 3	363 participants (Actual)	Interventional	2006-10-10	Terminated(stopped due to See termination reason in detailed description)
The Effect of Pioglitazone and Rosiglitazone on Atherosclerotic and Inflammatory Markers in Patients With Metabolic Syndrome: A Prospective, Randomized, Open-label, Crossover Trial[NCT00314561]	Phase 4	40 participants	Interventional	2006-05-31	Completed
A Double-blind, Placebo Controlled, Parallel Group Comparative Study to Evaluate the Efficacy and Safety of BRL 49653C With Concurrent Sulphonylurea Therapy, When Administered to Patients With Non-insulin Dependent Diabetes Mellitus.[NCT01706211]	Phase 3	77 participants (Actual)	Interventional	1998-10-31	Completed
The Effect of Rosiglitazone on Adipocyte-derived Cytokines in Nondiabetics With the Metabolic Syndrome[NCT00364221]	Phase 4	0 participants	Interventional	2004-11-30	Completed
The Pathogenic Role of 11ß-hydroxysteroid Dehydrogenase in the Metabolic Syndrome - the Effect of Rosiglitazone[NCT00370305]	Phase 2	24 participants (Actual)	Interventional	2004-05-31	Completed
A 16-week, Randomised, Double-blind, Placebo-controlled, Single-centre Study to Investigate Fluid Retention in Insulin-treated Subjects With Type 2 Diabetes Mellitus and Varying Degrees of Autonomic Neuropathy When Administered Rosiglitazone 4mg Twice Dai[NCT00422955]	Phase 3	36 participants (Actual)	Interventional	2003-11-30	Completed
Clinical Evaluation of Rosiglitazone Malate (BRL49653C) in Patients With Type 2 Diabetes Mellitus (Monotherapy) - Double-Blind Comparative Study of Rosiglitazone Maleate vs. Pioglitazone Hydrochloride and Placebo -[NCT00297063]	Phase 3	350 participants (Actual)	Interventional	2006-01-11	Completed
A Randomised, Double-blind, Placebo-controlled, Parallel Group Study to Investigate the Anti-inflammatory and Metabolic Effects of Rosiglitazone XR, 8mg Once Daily, in Subjects With Rheumatoid Arthritis[NCT00379600]	Phase 2	96 participants (Actual)	Interventional	2004-11-30	Completed
Effect of Rosiglitazone on In-vivo Angiogenic Potential of Human Adipose Tissue[NCT01150981]	Phase 2	35 participants (Actual)	Interventional	2006-11-30	Completed
Dietary Fatty Acids as Complementary Therapy in Type 2 Diabetes Mellitus[NCT00607945]	Phase 1	48 participants (Actual)	Interventional	2008-01-31	Completed
Open Label Pilot Study of Combination Therapy With Rosiglitazone and Bexarotene to Investigate a Possible Synergism in the Treatment of Cutaneous T-Cell Lymphoma[NCT00178841]	Phase 2	4 participants (Actual)	Interventional	2005-06-30	Completed
Role of Rosiglitazone Treatment and Secondary Prevention of Cardiovascular Events in Patients With Pre-Diabetes Mellitus and Coronary Artery Disease[NCT01574820]	Phase 3	105 participants (Actual)	Interventional	2006-11-30	Completed
A Randomized Controlled Trial Evaluating the Effects of Electroacupuncture and Rosiglitazone Combined Therapy on Patients With Type 2 Diabetes Mellitus[NCT01577095]	Phase 2	49 participants (Actual)	Interventional	2006-04-30	Completed
A Double-Blind, Placebo-Controlled Trial of Rosiglitazone for Clozapine Induced Glucose Metabolism Impairment: Bergman's Minimal Model Analysis[NCT00337350]	Phase 4	20 participants (Actual)	Interventional	2003-09-30	Completed
Liraglutide Effect and Action in Diabetes (LEAD-1): Effect on Glycaemic Control After Once Daily Administration of Liraglutide in Combination With Glimepiride Versus Glimepiride Monotherapy Versus Glimepiride and Rosiglitazone Combination Therapy in Subje[NCT00318422]	Phase 3	1,041 participants (Actual)	Interventional	2006-05-31	Completed
Rosiglitazone Add-On in Treatment of Depressed Patients With Insulin Resistance: a Pilot Study[NCT00242619]		12 participants (Actual)	Interventional	2007-07-31	Completed
[NCT00358124]	Phase 4	220 participants	Interventional	2001-01-31	Completed
A Randomized, Double-Blind Trial Comparing the Efficacy and Safety of a Fixed Combination of Fenofibrate and Metformin vs Rosiglitazone in Patients With Type 2 Diabetes Mellitus and Dyslipidemia[NCT00361868]	Phase 3	88 participants (Anticipated)	Interventional	2006-06-30	Terminated(stopped due to The study was discontinued prematurely at the end of March 2007 due to slow enrolment.)
Effect of Atazanavir Administered With and Without Ritonavir on the Pharmacokinetics of the Cytochrome P450 2C8 Substrate Rosiglitazone in Healthy Subjects[NCT00362726]	Phase 1	14 participants	Interventional	2006-09-30	Completed
Metabolic Effects of Treatment in Patients With Recently Diagnosed Type 2 Diabetes[NCT00373178]	Phase 4	100 participants (Actual)	Interventional	2005-01-31	Completed
Clinical Evaluation of Rosiglitazone Maleate (BRL49653C) in Patients With Type 2 Diabetes Mellitus (Combination Therapy With Sulfonyl Urea) - A Placebo-Controlled Double-Blind Study -[NCT00432679]	Phase 3	149 participants (Actual)	Interventional	2006-05-24	Completed
Studies to Treat Or Prevent Pediatric Type 2 Diabetes (STOPP-T2D) Treatment Options for Type 2 Diabetes in Adolescents and Youth (TODAY) Clinical Trial[NCT00081328]	Phase 3	699 participants (Actual)	Interventional	2004-05-31	Completed
Rosiglitazone Intervention Study in Patients With Type 1.5 Diabetes[NCT00194896]		64 participants (Actual)	Interventional	2000-02-29	Completed
An Open-label Extension to Study AVA105640, to Assess the Long-term Safety and Efficacy of Rosiglitazone (Extended Release Tablets) on Cognition in Subjects With Mild to Moderate Alzheimer's Disease.[NCT00550420]	Phase 3	331 participants (Actual)	Interventional	2007-10-01	Terminated(stopped due to Based on preliminary parent study results)
Assessment of Relative Bioavailability of Avandamet 4 mg + 1000 mg (GSK) in the Form of Film Coated Tablets Versus Avandamet 2 mg + 500 mg (GSK) in the Form of Film Coated Tablets, in Healthy Volunteers After Feeding Standardized, Using Liquid Chromatogra[NCT01332071]	Phase 1	26 participants (Actual)	Interventional	2009-11-24	Completed
A Pilot Study of Rosiglitazone in the Treatment of GH Secreting Pituitary Adenomas[NCT03309319]		24 participants (Anticipated)	Interventional	2016-10-16	Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Change in Insulin Sensitivity

"Change in insulin sensitivity value from baseline to week 12 by frequently sampled intravenous glucose tolerance test~This assessment was only conducted at baseline and week 12; therefore the change reflects the difference between these two time points." (NCT00130286)
Timeframe: 12 weeks

Intervention	uU10^-4min*ml^-1 (Median)
rhGH + Rosi	0.20
rhGH Placebo + Rosi	1.44
rhGH + Rosi Placebo	-0.63
Double Placebo	0.14

Change in Subcutaneous Adipose Tissue Volume

"Change in subcutaneous adipose tissue volume from baseline to week 12 by whole body MRI~Data are presented only for subjects who had MRI scans done at both time points." (NCT00130286)
Timeframe: 12 weeks

Intervention	L (Mean)
rhGH + Rosi	-0.11
rhGH Placebo + Rosi	0.74
rhGH + Rosi Placebo	-0.38
Double Placebo	-0.03

Change in Visceral Adipose Tissue Volume

"Change in visceral adipose tissue volume from baseline to week 12 measured by whole body MRI~Data are presented only for subjects who had MRI scans done at both time points." (NCT00130286)
Timeframe: 12 weeks

Intervention	L (Mean)
rhGH + Rosi	-1.13
rhGH Placebo + Rosi	-0.19
rhGH + Rosi Placebo	-1.15
Double Placebo	-0.04

Mean Change From Baseline in FBG at Month 36

Change from baseline was calculated as the Month 36 value minus the baseline value. FBG levels were measured by blood draw. (NCT00367055)
Timeframe: Baseline and Month 36

Intervention	millimoles per Liter (mmol/L) (Mean)
Rosiglitazone + Metformin 4 mg/2 g/Day	-1.6
Gliclazide + Metformin 80 mg/2 g/Day	-0.2

Mean Change From Baseline in HbA1c at Month 36

Change from baseline was calculated as the Month 36 value minus the baseline value. HbA1c levels were measured by blood draw. (NCT00367055)
Timeframe: Baseline and Month 36

Intervention	percent change (Mean)
Rosiglitazone + Metformin 4 mg/2 g/Day	-0.22
Gliclazide + Metformin 80 mg/2 g/Day	0.3

Mean Change From Baseline in Insulin Sensitivity Index at Months 18 and 36

Change from baseline was calculated as the Month 18 and 36 values minus the baseline value. Insulin sensitivity is measured as the quantity of glucose metabolized per unit of plasma insulin concentration. (NCT00367055)
Timeframe: Baseline and Months 18 and 36

Intervention	micromoles (umol)/kilogram/min/pmol/L (Mean)
	Month 18	Month 36
Gliclazide + Metformin 80 mg/2 g/Day	-0.02045	-0.01702
Rosiglitazone + Metformin 4 mg/2 g/Day	-0.00511	0.00040

Median Change From Baseline in the Insulin Secretion Capacity After an 18-month Treatment

Change from baseline was calculated as the Month 18 value minus the baseline value. Insulin secretion capacity is measured in blood (blood level of insulin) and is a response of the pancreatic beta-cells to hyperglycemia induced by a glucose IV bolus, then infusion. Hyperglycemic clamp (HC) is a reference technique to evaluate the initial and the secondary phases of insulin secretion. (NCT00367055)
Timeframe: Baseline and Month 18

Intervention	pmol/L*min (Median)
	HC, Total AUC(0-10min), n=30, 31	HC, Incremental AUC(0-10min), n=27, 26	HC, Total AUC(10-180min), n=26, 30	HC, Incremental AUC(10-180min), n=26, 29	Arginine (Arg) test, Total AUC(0-30min), n=25, 25	Arg test, Incremental AUC(0-30min), n=25, 25	Arg test, Incremental Conc. peak(0-30 min),n=26,29
Gliclazide + Metformin 80 mg/2 g/Day	-32.3	60.7	-7.6	14.6	10.9	-8.0	-111.1
Rosiglitazone + Metformin 4 mg/2 g/Day	18.3	22.3	55.9	72.9	38.4	15.1	23.3

Median Change From Baseline in the Insulin Secretory Capacity After a 36-month Treatment

Change from baseline in the insulin secretory capacity was measured by the assesment of blood insulin concentrations (conc.) using the hyperglycaemic clamp (HC) technique, per intravenous glucose perfusion by a catheter. Change from baseline for insulin conc peaks (highest conc level) was calculated as the Month 36 value minus the baseline value. Insulin secretion was assessed by calculating AUC during the first 10 minutes of HC (incremental and total AUC0-10 min) and the AUC after the first 10 minutes of the HC (10-180min). (NCT00367055)
Timeframe: Baseline and Month 36

Intervention	picomoles/L per minute (pmol/L*min) (Median)
	Total AUC(0-10 min), n=24, 26	Incremental AUC(0-10 min), n=22, 23	Total concentration peak(0-10 min), n=25, 26	Incremental concentration peak(0-10 min), n=24, 26	Total AUC(10-180 min), n=20, 24	Incremental AUC(10-180 min), n=19, 24	Total concentration peak(10-180 min), n=27, 29	Incremental concentation peak(10-180 min), n=25,29
Gliclazide + Metformin 80 mg/2 g/Day	-75.3	74.6	3.6	10.8	-21.2	13.6	-9.3	11.5
Rosiglitazone + Metformin 4 mg/2 g/Day	-3.9	7.0	-8.6	-1.8	40.6	67.0	7.9	10.8

Primary Major Macrovascular Events

Myocardial infarction (MI), intervention for coronary artery or Peripheral Vascular Disease (PVD), severe inoperable Coronary Artery Disease (CAD), new or worsening Congestive Heart Failure (CHF), stroke, Cardiovascular (CV) death, or amputation for ischemic gangrene. (NCT00032487)
Timeframe: Post baseline time to the first major macrovascular event up to 82 months

Intervention	participants (Number)
Arm 1	264
Arm 2	235

Secondary Endpoint

New or worsening angina, new transient ischemic attack (TIA), new intermittent claudication or critical limb ischemia with Doppler evidence or total mortality. (NCT00032487)
Timeframe: Post baseline time to first event up to 82 months

Intervention	participants (Number)
Arm 1	283
Arm 2	312

Hypoglycemia Rate Per 30 Days Per Patient

Average number of episodes of hypoglycemia per 30 days per patient (NCT00135330)
Timeframe: 20 weeks

Intervention	hypoglycemia events / 30 days / patient (Mean)
Exenatide	0.391
Exenatide Plus Rosiglitazone	0.594
Rosiglitazone	0.853

Incidence of Hypoglycemia Events

Number of subjects experiencing hypoglycemia at any point during the study (NCT00135330)
Timeframe: 20 weeks

Intervention	participants (Number)
Exenatide	8
Exenatide Plus Rosiglitazone	9
Rosiglitazone	6

Change in ASIiAUC During a Hyperglycemic Clamp Test.

Change in insulin incremental area under the concentration-time curve (ASIiAUC) from baseline to week 20. ASIiAUC is a measure of beta-cell function. (NCT00135330)
Timeframe: 20 weeks

Intervention	uIU-min/ml (Least Squares Mean)
	Baseline ASIiAUC	Change in ASIiAUC at week 20
Exenatide	643.40	747.26
Exenatide Plus Rosiglitazone	686.41	194.68
Rosiglitazone	786.12	-99.85

Change in AUC for C-peptide During a Meal Challenge Test (MCT).

Ratio (value at endpoint divided by value at baseline) of AUC(15-180 min) for C-peptide (nmol-min/L) during a MCT from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	nmol-min/L (Geometric Mean)
	Baseline C-peptide during a MCT	Ratio(endpoint/baseline) of C-peptide during a MCT
Exenatide	319.77	0.908
Exenatide Plus Rosiglitazone	310.51	0.804
Rosiglitazone	325.65	0.854

Change in AUC for Glucose During a Meal Challenge Test (MCT).

Change in AUC(15-180 min) for glucose during a MCT baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol-min/L (Least Squares Mean)
	Baseline glucose AUC during MCT	Change in glucose AUC during MCT at week 20
Exenatide	1782.86	-560.12
Exenatide Plus Rosiglitazone	1799.68	-635.24
Rosiglitazone	1741.87	-425.59

Change in Body Fat Mass During a Meal Challenge Test (MCT)

Change in body fat mass form baseline to week 20, as assessed during an MCT (NCT00135330)
Timeframe: 20 weeks

Intervention	kg (Least Squares Mean)
	Baseline body fat mass	Change in body fat mass at week 20
Exenatide	32.05	-2.76
Exenatide Plus Rosiglitazone	32.55	-1.06
Rosiglitazone	30.54	-1.99

Change in Body Weight

Change in body weight from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	kg (Least Squares Mean)
	Baseline body weight	Change in body weight at week 20
Exenatide	93.05	-2.82
Exenatide Plus Rosiglitazone	93.76	-1.21
Rosiglitazone	91.78	1.48

Change in Fasting HDL Cholesterol

Change in fasting high-density lipoprotein (HDL) cholesterol from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline HDL	Change from baseline HDL at week 20
Exenatide	1.13	0.022
Exenatide Plus Rosiglitazone	1.17	0.046
Rosiglitazone	1.17	0.055

Change in Fasting Insulin

Change in fasting insulin from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	uIU/ml (Geometric Mean)
	Baseline fasting insulin	Ratio (wk20/baseline)of fasting insulin
Exenatide	12.84	0.980
Exenatide Plus Rosiglitazone	10.96	0.599
Rosiglitazone	12.77	0.755

Change in Fasting LDL Cholesterol

Change in fasting low-density lipoprotein (LDL) cholesterol from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline LDL	Change from baseline LDL at week 20
Exenatide	2.59	-0.049
Exenatide Plus Rosiglitazone	2.57	0.096
Rosiglitazone	2.71	0.334

Change in Fasting Proinsulin

Ratio (endpoint value divided by baseline value) for fasting proinsulin, comparing endpoint (week 20) to baseline (NCT00135330)
Timeframe: Week 20

Intervention	pmol/L (Geometric Mean)
	Baseline fasting proinsulin	Ratio(wk20/baseline)of fasting proinsulin
Exenatide	4.32	0.663
Exenatide Plus Rosiglitazone	3.80	0.538
Rosiglitazone	3.56	0.623

Change in Fasting Serum Glucose Concentration.

Change in fasting serum glucose concentration from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline fasting serum glucose	Change fr baseline fasting serum glucose at wk 20
Exenatide	8.42	-1.46
Exenatide Plus Rosiglitazone	8.43	-1.60
Rosiglitazone	8.48	-1.80

Change in Fasting Total Cholesterol.

Change in fasting total cholestrol from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline total cholesterol	Change fr baseline total cholesterol at week 20
Exenatide	4.42	-0.128
Exenatide Plus Rosiglitazone	4.41	0.258
Rosiglitazone	4.62	0.438

Change in Fasting Triglycerides

Ratio (endpint value divided by baseline value) of fasting triglycerides from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Geometric Mean)
	Baseline triglyceride	Ratio (endpoint/baseline) for triglycerides
Exenatide	1.56	0.861
Exenatide Plus Rosiglitazone	1.67	0.977
Rosiglitazone	1.76	0.992

Change in HbA1c

Change in HbA1c from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	Percentage (Least Squares Mean)
	Baseline HbA1c	Change from baseline HbA1c at week 20
Exenatide	7.79	-0.908
Exenatide Plus Rosiglitazone	7.84	-1.31
Rosiglitazone	7.92	-0.968

Change in Hip Circumference

Change in hip circumference form baseline to week 20 (NCT00135330)
Timeframe: 20 weeks

Intervention	cm (Least Squares Mean)
	Baseline hip circumference	Change in hip circumference at week 20
Exenatide	113.29	-1.28
Exenatide Plus Rosiglitazone	112.12	0.147
Rosiglitazone	111.90	1.51

Change in Incremental for Postprandial C-peptide During Meal Challenge Test (MCT).

Change in incremental for postprandial C-peptide (mmol/L) during MCT from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline C-peptide at 15 min	Change fr baseline C-peptide at 15 min at week 20	Baseline C-peptide at 30 min	Change fr baseline C-peptide at 30 min at week 20	Baseline C-peptide at 60 min	Change fr baseline C-peptide at 60 min at week 20	Baseline C-peptide at 90 min	Change fr baseline C-peptide at 90 min at week 20	Baseline C-peptide at 120 min	Change fr baseline C-peptide at 120 min at week 20	Baseline C-peptide at 150 min	Change fr baseline C-peptide at 150 min at week 20	Baseline C-peptide at 180 min	Change fr baseline C-peptide at 180 min at week 20
Exenatide	0.238	-0.006	0.521	-0.071	0.818	-0.148	0.895	-0.185	0.817	-0.259	0.843	-0.251	0.610	-0.075
Exenatide Plus Rosiglitazone	0.259	0.016	0.517	-0.036	0.871	-0.025	0.953	-0.117	0.828	-0.134	0.651	-0.254	0.482	-0.238
Rosiglitazone	0.206	0.087	0.560	0.099	0.881	0.054	1.03	-0.052	0.972	-0.016	0.813	-0.093	0.619	-0.092

Change in Incremental for Postprandial Glucose During a Meal Challenge Test (MCT).

Change in incremental for postprandial glucose (mmol/L) during a MCT from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline glucose at 15 min	Change fr baseline glucose at 15 min at wk 20	Baseline glucose at 30 min	Change fr baseline glucose at 30 min at wk 20	Baseline glucose at 60 minutes	Change fr baseline glucose at 60 min at wk 20	Baseline glucose at 90 minutes	Change fr baseline glucose at 90 min at wk 20	Baseline glucose at 120 minutes	Change fr baseline glucose at 120 min at wk 20	Baseline glucose at 150 minutes	Change fr baseline glucose at 150 min at wk 20	Baseline glucose at 180 minutes	Change fr baseline glucose at 180 min at wk 20
Exenatide	0.950	-0.651	2.39	-1.46	3.59	-2.56	3.24	-2.87	2.49	-2.24	1.62	-1.42	0.461	-0.583
Exenatide Plus Rosiglitazone	1.12	-0.286	2.54	-1.06	3.88	-2.46	3.36	-2.91	2.24	-2.52	1.14	-1.95	0.036	-0.995
Rosiglitazone	0.828	0.150	2.23	-0.066	3.48	-0.720	3.48	-0.952	2.31	-0.912	1.25	-0.830	0.279	-0.481

Change in Incremental for Postprandial Insulin During Meal Challenge Test (MCT).

Change in incremental for postprandial insulin (mmol/L) during meal challenge test (MCT) from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mmol/L (Least Squares Mean)
	Baseline insulin at 15 min	Change fr baseline insulin at 15 min at wk 20	Baseline insulin at 30 min	Change fr baseline insulin at 30 min at wk 20	Baseline insulin at 60 min	Change fr baseline insulin at 60 min at wk 20	Baseline insulin at 90 min	Change fr baseline insulin at 90 min at wk 20	Baseline insulin at 120 min	Change fr baseline insulin at 120 min at wk 20	Baseline insulin at 150 min	Change fr baseline insulin at 150 min at wk 20	Baseline insulin at 180 min	Change fr baseline insulin at 180 min at wk 20
Exenatide	9.97	-1.71	19.81	-3.00	27.92	-11.04	26.06	-9.42	19.56	-11.26	15.67	-7.48	10.58	0.031
Exenatide Plus Rosiglitazone	8.09	-1.84	14.79	-2.63	27.67	-7.47	21.85	-9.27	17.52	-8.69	12.74	-8.13	8.18	-5.26
Rosiglitazone	7.53	-0.455	18.83	-1.04	32.09	-7.42	32.25	-6.19	25.47	-6.43	18.11	-5.57	10.74	-4.04

Change in Insulin AUC in the First Stage From Baseline to Endpoint.

"Change in insulin AUC in the first stage(uIU-min/ml) from baseline to week 20. First stage represents the first 10 minutes after reaching a steady state during a hyperglycemic clamp test." (NCT00135330)
Timeframe: Week 20

Intervention	uIU-min/ml (Least Squares Mean)
	Baseline insulin AUC	Change from baseline insulin AUC at week 20
Exenatide	200.50	134.88
Exenatide Plus Rosiglitazone	136.84	32.12
Rosiglitazone	157.49	-50.81

Change in Insulin iAUC From Baseline to Endpoint.

"Change in insulin iAUC in the first stage(uIU-min/ml) from baseline to week 20. First stage represents the first 10 minutes after reaching a steady state during a hyperglycemic clamp test." (NCT00135330)
Timeframe: Week 20

Intervention	uIU-min/ml (Least Squares Mean)
	Baseline insulin iAUC	Change from baseline insulin iAUC at week 20
Exenatide	5.98	99.08
Exenatide Plus Rosiglitazone	-9.92	53.71
Rosiglitazone	23.09	11.51

Change in Insulin Sensitivity Index as Measured by M-value.

Change of M-Value (mg/kg-min) during hyperinsulinemic euglycemic clamp test from baseline to week 20. (NCT00135330)
Timeframe: Week 20

Intervention	mg/kg-min (Least Squares Mean)
	M-Value at baseline	Change in M-Value from baseline at week 20
Exenatide	3.89	0.477
Exenatide Plus Rosiglitazone	2.49	2.07
Rosiglitazone	4.02	1.42

Change in Lean Body Mass During a Meal Challenge Test (MCT)

Change in lean body mass from baseline to week 20, as assessed during an MCT (NCT00135330)
Timeframe: 20 weeks

Intervention	kg (Least Squares Mean)
	Baseline lean body mass	Change in lean body mass at week 20
Exenatide	64.62	-2.99
Exenatide Plus Rosiglitazone	60.94	0.532
Rosiglitazone	61.09	1.23

Change in Percent Body Fat During a Meal Challenge Test (MCT)

Change in percent body fat from baseline to week 20, as assessed during an MCT (NCT00135330)
Timeframe: 20 weeks

Intervention	percentage (Least Squares Mean)
	Baseline percent body fat	Change in percent body fat at week 20
Exenatide	33.42	-1.40
Exenatide Plus Rosiglitazone	34.07	-0.347
Rosiglitazone	32.50	-1.18

Change in Waist Circumference

Change in waist circumference from baseline to week 20 (NCT00135330)
Timeframe: 20 weeks

Intervention	cm (Least Squares Mean)
	Baseline waist circumference	Change in waist circumference at Week 20
Exenatide	105.98	-2.95
Exenatide Plus Rosiglitazone	106.85	-2.38
Rosiglitazone	105.34	-0.225

Change in Waist-to-hip Ratio

Change in waist-to-hip ratio (waist circumference divided by hip circumference) from baseline to week 20 (NCT00135330)
Timeframe: 20 weeks

Intervention	ratio (cm/cm) (Least Squares Mean)
	Baseline waist-to-hip ratio	Change in waist-to-hip ratio at week 20
Exenatide	0.939	-0.016
Exenatide Plus Rosiglitazone	0.957	-0.022
Rosiglitazone	0.943	-0.016

Pedal Edema Score

"Pedal edema scores experienced by each patient throughout the study (1+ indicates a patient experienced a pedal edema score of 1 , 2, or 3; 2+ indicates a patient experienced a pedal edema score of 2 or 3, etc.)~Scale:~Slight pitting, no visible distortion, disappears rapidly~A somewhat deeper pit than in 1+, but again no readily detectable distortion, and it disappears in 10 - 15 seconds~The pit is noticeably deep and may last more than a minute; the dependent extremity looks fuller and swollen~The pit is very deep, lasts as long as 2 - 5 minutes, and the dependent extremity is grossly distorted" (NCT00135330)
Timeframe: 20 weeks

Intervention	participants (Number)
	No edema	Edema score: 1+	Edema score: 2+	Edema score: 3+
Exenatide	37	7	1	0
Exenatide Plus Rosiglitazone	34	11	3	0
Rosiglitazone	30	14	6	1

Ratio (Value at Endpoint Divided by Value at Baseline) of AUC for Insulin During a Meal Challenge Test (MCT).

Ratio (value at endpoint divided by value at baseline) of AUC (15-180 min) for insulin (uIU-min/ml) during MCT. (NCT00135330)
Timeframe: Week 20

Intervention	uIU-min/ml (Geometric Mean)
	Baseline AUC for insulin during MCT	Ratio(endpoint/baseline) of insulin AUC during MCT
Exenatide	5171.40	0.806
Exenatide Plus Rosiglitazone	4324.13	0.664
Rosiglitazone	5816.83	0.722

Mean Change From Baseline in 5 Year UKPDS Risk Scores at Month 12

"Change from baseline was calculated as the Month 12 value minus the baseline value, with LOCF from Month 2. The UKPDS (U.K. Prospective Diabetes Study) risk engine calculated was based on 5 years risk using gender, race, age at diagnosis of diabetes, duration of diabetes, smoking status, A1C, systolic blood pressure and total cholesterol to HDL ratio at a specified visit.~The UKPDS cardiovascular disease (CVD) risk engine is used to estimate the risk of having coronary heart disease in type II diabetes according to the UKPDS model. The possible risk scores can range from 0 to 100% and hence lower scores would predict a person is less likely to have an event." (NCT00131664)
Timeframe: Baseline and Month 12

Intervention	percent (Mean)
Avandia and Amaryl	-0.72
Avandamet	-0.62
Metformin	-1.11

Mean Change From Baseline in 5 Year UKPDS Risk Scores at Month 6

"Change from baseline was calculated as the Month 6 value minus the baseline value, with LOCF from Month 2. The UKPDS (United Kingdom Prospective Diabetes Study) risk engine calculated was based on 5 years risk using gender, race, age at diagnosis of diabetes, duration of diabetes, smoking status, A1C, systolic blood pressure and total cholesterol to high-density lipoprotein (HDL) ratio at a specified visit.~The UKPDS cardiovascular disease (CVD) risk engine is used to estimate the risk of having coronary heart disease in type II diabetes according to the UKPDS model. The possible risk scores can range from 0 to 100% and hence lower scores would predict a person is less likely to have an event." (NCT00131664)
Timeframe: Baseline and Month 6

Intervention	percent (Mean)
Avandia and Amaryl	-1.09
Avandamet	-1.05
Metformin	-1.54

Mean Change From Baseline in A1C at Month 12

Change from baseline was calculated as the Month 12 value minus the baseline value, with last on-treatment observation carried forward (LOCF) from Month 2 for withdrawn subjects or missing values. (NCT00131664)
Timeframe: Baseline and Month 12

Intervention	percent (Mean)
Avandia and Amaryl	-1.50
Avandamet	-1.56
Metformin	-1.14

Mean Change From Baseline in A1C at Month 4

Change from baseline was calculated as the Month 4 value minus the baseline value, with last on-treatment observation carried forward (LOCF) from Month 2 for withdrawn subjects or missing values. (NCT00131664)
Timeframe: Baseline and Month 4

Intervention	percent (Mean)
Avandia and Amaryl	-1.44
Avandamet	-1.28
Metformin	-0.94

Mean Change From Baseline in Adiponectin at Month 12

Change from baseline was calculated as the Month 12 value minus the baseline value, with LOCF from Month 6. Adiponectin was only done at baseline, months 6 and 12. The test was optional and performed only by participating sites. (NCT00131664)
Timeframe: Baseline and Month 12

Intervention	µg/mL (Mean)
Avandia and Amaryl	4.95
Avandamet	8.21
Metformin	1.453

Mean Change From Baseline in Adiponectin at Month 6

Change from baseline was calculated as the Month 6 value minus the baseline value. LOCF was not used for this analysis. Adiponectin was only done at baseline, months 6 and 12. The test was optional and performed only by participating sites. (NCT00131664)
Timeframe: Baseline and Month 6

Intervention	microgram per millilitre (µg/mL) (Mean)
Avandia and Amaryl	5.73
Avandamet	6.37
Metformin	0.23

Mean Change From Baseline in C-reactive Protein (CRP) at Month 12

Change from baseline was calculated as the Month 12 value minus the baseline value, with LOCF from Month 6. CRP was only done at baseline, months 6 and 12. The test was optional and performed only by participating sites. (NCT00131664)
Timeframe: Baseline and Month 12

Intervention	mg/dL (Mean)
Avandia and Amaryl	-0.40
Avandamet	-1.52
Metformin	-1.52

Mean Change From Baseline in C-reactive Protein (CRP) at Month 6

Change from baseline was calculated as the Month 6 value minus the baseline value. LOCF was not used for this analysis. CRP was only done at baseline, months 6 and 8. The test was optional and performed only by participating sites. (NCT00131664)
Timeframe: Baseline and Month 6

Intervention	milligram per decilitre (mg/dL) (Mean)
Avandia and Amaryl	-1.20
Avandamet	-1.68
Metformin	-1.25

Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Month 12

Change from baseline was calculated as the Month 12 value minus the baseline value, with LOCF from Month 2 for withdrawn subjects or missing values. (NCT00131664)
Timeframe: Baseline and Month 12

Intervention	millimoles per litre (mmol/L) (Mean)
Avandia and Amaryl	-2.71
Avandamet	-2.76
Metformin	-2.12

Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Month 4

Intervention	millimoles per litre (mmol/L) (Mean)
Avandia and Amaryl	-2.86
Avandamet	-2.33
Metformin	-1.75

Mean Change From Baseline in Fasting Plasma Glucose (FPG) at Month 6

Change from baseline was calculated as the Month 6 value minus the baseline value, with last on-treatment observation carried forward (LOCF) from Month 2 for withdrawn subjects or missing values. (NCT00131664)
Timeframe: Baseline and Month 6

Intervention	millimoles per litre (mmol/L) (Mean)
Avandia and Amaryl	-2.98
Avandamet	-2.55
Metformin	-1.86

Number of Subjects Achieving A1C Target at Month 12

A1C responders were described as subjects having achieved A1C less than 7 percent at Month 12 with LOCF from Month 2. (NCT00131664)
Timeframe: Month 12

Intervention	participants (Number)
Avandia and Amaryl	95
Avandamet	111
Metformin	82

Number of Subjects Achieving A1C Target at Month 4

A1C responders were described as subjects having achieved A1C less than 7 percent at Month 4, with LOCF from Month 2. (NCT00131664)
Timeframe: Month 4

Intervention	participants (Number)
Avandia and Amaryl	83
Avandamet	96
Metformin	69

Number of Subjects Achieving A1C Target at Month 6

A1C responders were described as subjects having achieved A1C less than 7 percent at Month 6, with LOCF from Month 2. (NCT00131664)
Timeframe: Month 6

Intervention	participants (Number)
Avandia and Amaryl	94
Avandamet	98
Metformin	69

Number of Subjects Achieving FPG Target at Month 12

FPG responders were described as subjects having achieved FPG less than 7 mmol/L at Month 12 with LOCF from Month 2. (NCT00131664)
Timeframe: Month 12

Intervention	participants (Number)
Avandia and Amaryl	64
Avandamet	86
Metformin	51

Number of Subjects Achieving FPG Target at Month 4

FPG responders were described as subjects having achieved FPG less than 7 mmol/L at Month 4 with LOCF from Month 2. (NCT00131664)
Timeframe: Month 4

Intervention	participants (Number)
Avandia and Amaryl	58
Avandamet	65
Metformin	38

Number of Subjects Achieving FPG Target at Month 6

FPG responders were described as subjects having achieved FPG less than 7 mmol/L at Month 6 with LOCF from Month 2. (NCT00131664)
Timeframe: Month 6

Intervention	participants (Number)
Avandia and Amaryl	61
Avandamet	76
Metformin	43

Mean Change From Baseline in A1C at Month 6

Intervention	percent (Mean)
	Baseline	Change from baseline
Avandamet	7.96	-1.39
Avandia and Amaryl	8.14	-1.61
Metformin	7.90	-1.02

Independent Re-adjudication (IR) Outcome: Number of Participants With a First Occurrence of a Major Adverse Cardiovascular Event (MACE) Defined as CV (or Unknown) Death, Non-fatal MI, and Non-fatal Stroke Based on Original RECORD Endpoint Definitions

IR was based on original RECORD endpoint definitions. CV death= no unequivocal non-CV cause (sudden death, death from acute vascular events, heart failure, acute MI, other CV causes, and deaths adjudicated as unknown cause). MI event=hospitalization + elevation of specific cardiac biomarkers above the upper limit of normal + cardiac ischemia symptoms/new pathological electrocardiogram findings. Stroke event=hospitalization + rapidly developed clinical signs of focal/global disturbance of cerebral function for more than 24 hours, with no apparent cause other than a vascular origin. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	181
Combined MET/SU	188

Independent Re-adjudication Outcome: Number of Participants (Par.) With an Event of Stroke (Fatal and Non-fatal), Based on Original RECORD Endpoint Definitions

Par. with a stroke (fatal or non-fatal) event as determined by independent re-adjudication using the original RECORD endpoint definitions was recorded. A stroke event=hospitalization plus rapidly developed clinical signs of focal (or global) disturbance of cerebral function lasting more than 24 hours (unless interrupted by thrombolysis, surgery, or death), with no apparent cause other than a vascular origin, including par. presenting clinical signs/symptoms suggestive of subarachnoid haemorrhage/intracerebral haemorrhage/cerebral ischemic necrosis or cause of death adjudicated as stroke. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	50
Combined MET/SU	63

Independent Re-adjudication Outcome: Number of Participants Who Died Due to Any Cause

All deaths identified during the original record study and discovered after the re-adjudication efforts began were included. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	139
Combined MET/SU	160

Independent Re-adjudication Outcome: Number of Participants With a CV (or Unknown) Death, Based on Contemporary Endpoint Definitions

The number of participants with a CV (or unknown) death as determined by independent re-adjudication using the Standard Data Collection for Cardiovascular Trials Initiative (draft October 2011) endpoint definitions was recorded. CV death included death resulting from an acute myocardial infarction (MI), sudden cardiac death, death due to heart failure, death due to stroke, and death due to other CV causes. Deaths of unknown cause were counted as CV deaths. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	88
Combined MET/SU	96

Independent Re-adjudication Outcome: Number of Participants With a CV (or Unknown) Death, Based on Original RECORD Endpoint Definitions

"The number of participants with a CV death (or unknown) as determined by independent re-adjudication using the original RECORD endpoint definitions was recorded. CV death was defined as any death for which an unequivocal non-CV cause could not be established. CV death included death following heart failure, death following acute myocardial infarction (MI), sudden death, death due to acute vascular events, and other CV causes. Deaths due to unknown causes were classified as unknown deaths, but were counted as CV deaths for the analysis of this endpoint." (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	88
Combined MET/SU	96

Independent Re-adjudication Outcome: Number of Participants With a First Occurrence of a Major Adverse Cardiovascular Event (MACE) Defined as CV (or Unknown) Death, Non-fatal MI, and Non-fatal Stroke Based on Contemporary Endpoint Definitions

Independent re-adjudication was based on the Standard Data Collection for Cardiovascular Trials Initiative (draft October 2011) endpoint definitions. CV death included death resulting from an acute MI; sudden cardiac death and death due to heart failure, stroke, and to other CV causes. Deaths of unknown cause were counted as CV deaths. MI was defined as evidence of myocardial necrosis in a clinical setting consistent with myocardial ischemia. Stroke was defined as an acute episode of neurological dysfunction caused by focal or global brain, spinal cord, or retinal vascular injury. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	186
Combined MET/SU	191

Independent Re-adjudication Outcome: Number of Participants With an Event of Myocardial Infarction (Fatal and Non-fatal), Based on Contemporary Endpoint Definitions

The number of participants with an MI (fatal or non-fatal) event as determined by independent re-adjudication using the Standard Data Collection for Cardiovascular Trials Initiative (draft October 2011) endpoint definitions was recorded. An event of MI was defined as evidence of myocardial necrosis in a clinical setting consistent with myocardial ischemia. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	72
Combined MET/SU	62

Independent Re-adjudication Outcome: Number of Participants With an Event of Myocardial Infarction (Fatal and Non-fatal), Based on Original RECORD Endpoint Definitions

The number of participants with an MI (fatal or non-fatal) event as determined by independent re-adjudication using the original RECORD endpoint definitions was recorded. An event of MI was defined as hospitalization plus elevation of cardiac biomarkers troponin (TN) I and/or TNT above the upper limit of normal (ULN) or creatinine kinase (CK) MB (M=muscle type; B=brain type) isoenzyme >= 2x the ULN or CK > 2x the ULN plus typical symptoms of cardiac ischemia or new pathological electrocardiogram findings, or cause of death adjudicated as MI. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	68
Combined MET/SU	60

Independent Re-adjudication Outcome: Number of Participants With an Event of Stroke (Fatal and Non-fatal), Based on Contemporary Endpoint Definitions

The number of participants with a stroke (fatal or non-fatal) event as determined by independent re-adjudication using the Standard Data Collection for Cardiovascular Trials Initiative (draft October 2011) endpoint definitions was recorded. An event of stroke was defined as an acute episode of neurological dysfunction caused by focal or global brain, spinal cord, or retinal vascular injury. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	53
Combined MET/SU	64

Model Adjusted Change From Baseline in Alanine Aminotransferase at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in alanine aminotransferase was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	U/L (Units/Liter) (Mean)
RSG in Addition to Background MET	-37.43
SU in Addition to Background MET	-21.73
RSG in Addition to Background SU	-30.17
MET in Addition to Background SU	-24.00

Model Adjusted Change From Baseline in Body Weight at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in body weight was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	kilograms (Mean)
RSG in Addition to Background MET	3.93
SU in Addition to Background MET	-0.54
RSG in Addition to Background SU	4.72
MET in Addition to Background SU	-2.16

Model Adjusted Change From Baseline in Fasting Plasma Glucose at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in fasting plasma glucose was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment period

Intervention	mmol/L (millimoles/Liter) (Mean)
RSG in Addition to Background MET	-1.38
SU in Addition to Background MET	-0.29
RSG in Addition to Background SU	-2.00
MET in Addition to Background SU	-0.94

Model Adjusted Change From Baseline in HbA1c at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in HbA1c was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline and Month 60 of randomised dual therapy treatment period

Intervention	Percent (Mean)
RSG in Addition to Background MET	-0.14
SU in Addition to Background MET	0.17
RSG in Addition to Background SU	-0.24
MET in Addition to Background SU	-0.10

Model Adjusted Change From Baseline in Waist Circumference at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in waist circumference was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	cm (centimeters) (Mean)
RSG in Addition to Background MET	2.70
SU in Addition to Background MET	0.65
RSG in Addition to Background SU	3.00
MET in Addition to Background SU	-0.60

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Apolipoprotein B (Apo-B) at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in Apo-B was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment period

Intervention	percent change (Geometric Mean)
RSG in Addition to Background MET	-13.77
SU in Addition to Background MET	-11.63
RSG in Addition to Background SU	-9.68
MET in Addition to Background SU	-12.09

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for C-Reactive Protein at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in C-Reactive Protein was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	percent change (Geometric Mean)
RSG in Addition to Background MET	-57.40
SU in Addition to Background MET	-28.92
RSG in Addition to Background SU	-56.50
MET in Addition to Background SU	-36.29

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Fibrinogen at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in fibrinogen was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	percent change (Geometric Mean)
RSG in Addition to Background MET	2.12
SU in Addition to Background MET	5.74
RSG in Addition to Background SU	-0.23
MET in Addition to Background SU	3.14

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Plasminogen Activator Inhibitor-1 (PAI-1) Antigen at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in plasminogen activator inhibitor-1 (PAI-1) antigen was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	percent change (Geometric Mean)
RSG in Addition to Background MET	-9.85
SU in Addition to Background MET	15.01
RSG in Addition to Background SU	-7.79
MET in Addition to Background SU	-0.64

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Urinary Albumin Creatinine Ratio at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in urinary albumin creatinine ratio was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

Intervention	percent change (Geometric Mean)
RSG in Addition to Background MET	8.31
SU in Addition to Background MET	15.17
RSG in Addition to Background SU	-3.43
MET in Addition to Background SU	11.91

Number of Participants With an Event of Death Due to a Bone Fracture-related Event: Main Study + Observational Follow-up Combined

Intervention	participants (Number)
Combined RSG: Main Study and Observational Follow-up	0
Combined MET/SU: Main Study and Observational Follow-up	0

Number of Participants With Cardiovascular Death/Cardiovascular Hospitalisation Events

The number of participants with cardiovascular death events (death due to cardiovascular causes or deaths with insufficient information to rule out a cardiovascular cause) and cardiovascular hospitalisation events (hospitalisation for a cardiovascular event, excluding planned admissions not associated with a worsening of the disease/condition of the participant) was recorded. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
Combined RSG	321
Combined MET/SU	323

Number of Participants With First Cardiovascular Hospitalisations/Cardiovascular Deaths by Stratum

Participants with first cardiovascular death (death due to cardiovascular causes or deaths with insufficient information to rule out a cardiovascular cause) and cardiovascular hospitalisation (hospitalisation for a cardiovascular event, excluding planned admissions not associated with a worsening of the disease/condition of the participant) were recorded by study stratum. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	partcipants (Number)
RSG in Addition to Background MET	158
SU in Addition to Background MET	154
RSG in Addition to Background SU	163
MET in Addition to Background SU	169

Number of Participants With Glycaemic Failure Events

Failure of glycaemic control was defined as two consecutive HbA1c values of ≥8.5 percent, or HbA1c ≥8.5percent at a single visit, after which the subject was either moved to the post-randomised treatment phase or triple therapy was started. (NCT00379769)
Timeframe: Baseline through to end of randomised dual therapy

Intervention	participants (Number)
RSG in Addition to Background MET	281
SU in Addition to Background MET	451
RSG in Addition to Background SU	365
MET in Addition to Background SU	424

The Number of Participants Starting Insulin at Any Time During the Study

The number of participants starting insulin at any time during the study was recorded. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
RSG in Addition to Background MET	126
SU in Addition to Background MET	276
RSG in Addition to Background SU	168
MET in Addition to Background SU	259

Model Adjusted Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within treatment groups) change from baseline in SBP and DBP was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

,,,

Intervention	mmHg (millimeters of mercury) (Mean)
	SBP	DBP
MET in Addition to Background SU	-0.6	-2.3
RSG in Addition to Background MET	-1.9	-3.6
RSG in Addition to Background SU	-2.3	-3.6
SU in Addition to Background MET	-2.2	-3.4

Model Adjusted Mean Change From Baseline in Insulin and Pro-insulin at Month 60

Model adjusted (adjusted for any imbalances in the baseline values between within stratum treatment groups) change from baseline in insulin and pro-insulin was calculated as the value at Month 60 minus the Baseline value. (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment period

,,,

Intervention	picamoles/liter (pmol/L) (Mean)
	Insulin, Adjusted Change from Baseline	Pro-insulin, Adjusted Change from Baseline
MET in Addition to Background SU	-12.1	-3.0
RSG in Addition to Background MET	-18.6	-2.4
RSG in Addition to Background SU	-16.9	-3.2
SU in Addition to Background MET	3.7	4.2

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Total Cholesterol (TC), Low-density Lipoprotein (LDL) Cholesterol, High-density Lipoprotein (HDL) Cholesterol, Triglycerides, and Free Fatty Acids (FFAs) at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in TC, LDL cholesterol, HDL cholesterol, triglycerides, and FFAs was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

,,,

Intervention	percent change (Geometric Mean)
	Total cholesterol	HDL-cholesterol	LDL-cholesterol	Triglycerides	Free fatty acids
MET in Addition to Background SU	-9.68	6.14	-17.80	-2.50	4.47
RSG in Addition to Background MET	-5.49	9.95	-12.70	-7.97	-16.46
RSG in Addition to Background SU	-2.91	7.73	-8.99	-2.68	-11.58
SU in Addition to Background MET	-9.09	2.57	-17.68	-1.95	2.79

Model Adjusted Ratio to Baseline (Expressed as a Percentage) for Total Cholesterol (TC):High-density Lipoprotein (HDL) Cholesterol and Low-density Lipoprotein (LDL) Cholesterol:HDL Cholesterol Ratios at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in TC:HDL cholesterol and LDL cholesterol:HDL cholesterol was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment period

,,,

Intervention	percent change (Geometric Mean)
	Total Cholesterol: HDL Cholesterol Ratio	LDL Cholesterol: HDL-Cholesterol Ratio
MET in Addition to Background SU	-15.01	-22.53
RSG in Addition to Background MET	-14.20	-20.89
RSG in Addition to Background SU	-9.93	-15.85
SU in Addition to Background MET	-11.33	-20.04

Model Adjusted Ratio to Baseline (Expressed as a Percentage) Homeostasis Model Assessment (HOMA) Beta Cell Function and Insulin Sensitivity at Month 60

The model adjusted (adjusted for any imbalances in the baseline [BL] values between within stratum treatment groups) ratio to BL in HOMA beta-cell function and insulin sensitivity was calculated as the ratio of the Month 60 value to the BL value and was expressed as percent change from BL. For each treatment group, the model-adjusted mean change from BL at Month 60 was determined on the log scale. This mean was then back transformed to give a geometric mean (GM) of the ratio of the Month 60 value to BL on the original scale. The GM was expressed as a percentage (100*[GM^-1]). (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment phase

,,,

Intervention	percent change (Geometric Mean)
	Beta cell function	Insulin sensitivity
MET in Addition to Background SU	12.43	23.90
RSG in Addition to Background MET	20.54	42.57
RSG in Addition to Background SU	32.35	42.07
SU in Addition to Background MET	19.28	-3.45

Number of Bone Fracture Events With the Indicated Outcome: Main Study + Observational Follow-up Combined

"The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. The indicated fracture outcome was pre-specified in the CRF and included Unknown as a category. Fracture events with missing outcome data were reported as Data unavailable." (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	bone fracture events (Number)
	Number of bone fracture events	Unknown	Normal healing with standard management	Complication	Additional therapeutic measures required	Data unavailable
Combined MET/SU: Main Study and Observational Follow-up	174	5	142	13	9	5
Combined RSG: Main Study and Observational Follow-up	299	7	250	14	16	12

Number of Bone Fracture Events With the Indicated Outcome: Observational Follow-up

"The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. The indicated fracture outcome was pre-specified in the CRF and included Unknown as a category. Fracture events with missing outcome data were reported as Data unavailable." (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	bone fracture events (Number)
	Number of bone fracture events	Unknown	Normal healing with standard management	Complication	Additional therapeutic measures required	Data unavailable
Combined MET/SU: Observational Follow-up	41	1	33	4	2	1
Combined RSG: Observational Follow-up	70	1	51	7	3	8

Number of HbA1c and Fasting Plasma Glucose (FPG) Responders at Month 60

Number of responders, i.e., participants meeting glycaemic targets (HbA1c less than or equal to 7 percent, FPG less than or equal to 7 mmol/L) (NCT00379769)
Timeframe: Baseline to Month 60 of the randomised dual therapy treatment period

,,,

Intervention	participants (Number)
	HbA1c Responders	FPG Responders
MET in Addition to Background SU	180	154
RSG in Addition to Background MET	265	300
RSG in Addition to Background SU	235	257
SU in Addition to Background MET	208	180

Number of Participants Who Died Due to the Indicated Cancer-related Event: Main Study + Observational Follow-up Combined

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	participants (Number)
	Any cancer-related death	Any gastrointestinal event	Pancreatic	Colon/rectal	Gastric	Liver	Gall bladder/biliary	Gastrointestinal event; not specified	Any genitourinary event	Renal	Uterine	Prostate	Bladder	Ovarian	Lung	Any hematologic event	Skin (melanoma)	Skin (non-melanomatous)	Metastases	Breast	Head and neck	Any neurologic event	Endocrine	Not specified
Combined MET/SU: Main Study and Observational Follow-up	72	34	12	11	3	4	3	1	15	3	5	2	3	2	11	0	0	0	4	3	2	2	0	1
Combined RSG: Main Study and Observational Follow-up	59	25	4	6	7	4	4	0	6	2	1	1	1	1	13	4	3	1	2	2	1	2	1	0

Number of Participants Who Died Due to the Indicated Cancer-related Event: Observational Follow-up

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	Any cancer-related death	Any gastrointestinal event	Pancreatic	Colon/rectal	Gastric	Liver	Gall bladder/biliary	Gastrointestinal event; not specified	Any genitourinary event	Renal	Uterine	Prostate	Bladder	Ovarian	Lung	Any hematologic event	Skin (melanoma)	Skin (non-melanomatous)	Metastases	Breast	Head and neck	Any neurologic event	Endocrine	Not specified
Combined MET/SU: Observational Follow-up	24	14	3	6	1	2	1	1	0	0	0	0	0	0	5	0	0	0	1	3	0	1	0	0
Combined RSG: Observational Follow-up	25	10	3	2	2	2	1	0	2	1	1	0	0	0	4	4	1	1	1	1	1	1	0	0

Number of Participants With a Bone Fracture Event - Overall and by Gender: Main Study and Observational Follow-up Combined

Intervention	participants (Number)
	Overall, n=2220, 2227	Male, n=1142, 1152	Female, n=1078, 1075
Combined MET/SU: Main Study and Observational Follow-up	151	60	91
Combined RSG: Main Study and Observational Follow-up	238	82	156

Number of Participants With a Bone Fracture Event - Overall and by Gender: Observational Follow-up

Intervention	participants (Number)
	Overall, n=1280, 1250	Male, n=665, 635	Female, n=615, 615
Combined MET/SU: Observational Follow-up	37	11	26
Combined RSG: Observational Follow-up	64	25	39

Number of Participants With a Bone Fracture Event Reported as the Indicated Serious Adverse Event (by Higher Level Group Term) or Death: Main Study + Observational Follow-up Combined

The OFU was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the OFU. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	participants (Number)
	Any event	Upper limb	Distal lower limb	Femur/hip	Spinal	Pelvic	Other
Combined MET/SU: Main Study and Observational Follow-up	57	17	16	11	9	3	4
Combined RSG: Main Study and Observational Follow-up	81	41	24	15	7	0	7

Number of Participants With a Bone Fracture Event Reported as the Indicated Serious Adverse Event (by Higher Level Group Term) or Death: Observational Follow-up

The OFU was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the OFU. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	Any event	Upper limb	Distal lower limb	Femur/hip	Spinal	Pelvic	Other
Combined MET/SU: Observational Follow-up	21	5	8	4	3	1	1
Combined RSG: Observational Follow-up	35	17	9	6	2	0	2

Number of Participants With Addition of Third Oral Agent/Switch to Insulin

The number of participants with addition of a third oral agent or switch to insulin from randomised dual combination treatment were recorded. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

,,,

Intervention	participants (Number)
	Participants with an event	First Event - Triple Therapy	First Event - Insulin
MET in Addition to Background SU	171	6	165
RSG in Addition to Background MET	295	257	38
RSG in Addition to Background SU	344	296	49
SU in Addition to Background MET	183	7	176

Number of Participants With Bone Fracture Events of the Indicated Cause: Main Study + Observational Follow-up Combined

Intervention	participants (Number)
	Any event	Non-traumatic event	Traumatic event	Pathologic	Unknown	Data unavailable
Combined MET/SU: Main Study and Observational Follow-up	151	55	77	4	19	3
Combined RSG: Main Study and Observational Follow-up	238	113	110	1	20	9

Number of Participants With Bone Fracture Events of the Indicated Cause: Observational Follow-up

"The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. The indicated fracture outcome was pre-specified in the CRF and included Unknown as a category. Fracture events with missing outcome data were reported as Data unavailable." (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	Any event	Non-traumatic event,	Traumatic event	Pathologic	Unknown	Data unavailable
Combined MET/SU: Observational Follow-up	37	14	17	2	4	1
Combined RSG: Observational Follow-up	64	36	24	1	1	3

Number of Participants With Cardiovascular Events and All-cause Deaths

Composites of participants with first cardiovascular (CV) hospitalisations and CV death or all-cause death and individual first events of acute myocardial infarction (MI) , stroke, congestive heart failure (CHF), CV death, and all-cause death. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
	CV death, acute MI, stroke	CV death, acute MI, stroke, unstable angina	CV death, acute MI, stroke, unstable angina, CHF	All-cause death,acuteMI,stroke,unstable angina,CHF	Acute MI (fatal or non-fatal)	Stroke (fatal or non-fatal)	CHF (fatal or non-fatal)	Death from CV causes	Death (all cause) during CV follow-up	Death (all-cause) including survival status
Combined MET/SU	165	184	206	268	56	63	29	71	139	157
Combined RSG	154	171	204	251	64	46	61	60	111	136

Number of Participants With CV/Microvascular Events

The number of participants with first cardiovascular or microvascular events (renal, foot, eye) were recorded. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	participants (Number)
	Participants with a CV/Microvascular event	Participants with any microvascular event	Participants with any eye event	Participants with any foot event	Participants with any renal event
Combined MET/SU	385	78	52	28	0
Combined RSG	363	59	42	19	0

Number of Participants With Potentially High Morbidity Fracture Events and Non-high Morbidity Fracture Events, in Participants With Prior Hand/Upper Arm/Foot Fractures (H/UA/FF): Main Study + Observational Follow-up Combined

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. The following bone fractures were grouped and were identified as potentially high morbidity bone fractures: hip, pelvis, upper leg, vertebral (lumbar spine, thoracic spine, cervical spine, spine - site unknown). (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	participants (Number)
	Any H/UA/FF event, overall, n=2220, 2227	Any H/UA/FF event, male, n=1142, 1152	Any H/UA/FF event, female, n=1078, 1075	High morbidity fractures, overall, n=2220, 2227	High morbidity fractures, male, n=1142, 1152	High morbidity fractures, female, n=1078, 1075	Non-high morbidity fractures, overall, n=2220, 222	Non-high morbidity fractures, male, n=1142, 1152	Non-high morbidity fractures, female, n=1078, 1075
Combined MET/SU: Main Study and Observational Follow-up	46	15	31	1	0	1	4	3	1
Combined RSG: Main Study and Observational Follow-up	86	28	58	5	0	5	15	2	13

Number of Participants With Potentially High Morbidity Fractures: Main Study + Observational Follow-up Combined

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. A bone fracture event is defined as one or more fractured bones occurring on the same date and that had the same Higher Level Group Term (HLGT) for fracture location, per participant. The following bone fractures were grouped and were identified as potentially high morbidity bone fractures: hip, pelvis, upper leg, vertebral (lumbar spine, thoracic spine, cervical spine, spine - site unknown). (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	participants (Number)
	Any event, overall, n=2220, 2227	Any event, male, n=1142, 1152	Any event, female, n=1078, 1075	Hip, overall, n=2220, 2227	Hip, male, n=1142, 1152	Hip, female, n=1078, 1075	Pelvis, overall, n=2220, 2227	Pelvis, male, n=1142, 1152	Pelvis, female, n=1078, 1075	Upper leg, overall, n=2220, 2227	Upper leg, male, n=1142, 1152	Upper leg, female, n=1078, 1075	Any vertebral event, overall, n=2220, 2227	Any vertebral event, male, n=1142, 1152	Any vertebral event, female, n=1078, 1075	Lumbar spine, overall, n=2220, 2227	Lumbar spine, male, n=1142, 1152	Lumbar spine, female, n=1078, 1075	Thoracic spine, overall, n=2220, 2227	Thoracic spine, male, n=1142, 1152	Thoracic spine, female, n=1078, 1075	Cervical spine, overall, n=2220, 2227	Cervical spine, male, n=1142, 1152	Cervical spine, female, n=1078, 1075
Combined MET/SU: Main Study and Observational Follow-up	31	13	18	7	1	6	5	4	1	6	0	6	13	8	5	4	3	1	8	4	4	1	1	0
Combined RSG: Main Study and Observational Follow-up	31	10	21	9	0	9	0	0	0	7	4	3	16	6	10	10	5	5	5	1	4	1	0	1

Number of Participants With the Indicated Bone Fracture by Fracture Site: Main Study + Observational Follow-up Combined

Intervention	participants (Number)
	Any event, overall; n=2220, 2227	Any event, male; n=1142, 1152	Any event, female; n=1078, 1075	Upper limb, any event, overall; n=2220, 2227	Upper limb, any event, male; n=1142, 1152	Upper limb, any event, female; n=1078, 1075	Distal lower limb, any event, overall; n=2220, 222	Distal lower limb, any event, male; n=1142, 1152	Distal lower limb, any event, female; n=1078, 1075	Femur/hip, any event, overall; n=2220, 2227	Femur/hip, any event, male; n=1142, 1152	Femur/hip, any event, female; n=1078, 1075	Spinal, any event, overall; n=2220, 2227	Spinal, any event, male; n=1142, 1152	Spinal, any event, female; n=1078, 1075	Pelvic, any event, overall; n=2220, 2227	Pelvic, any event, male; n=1142, 1152	Pelvic, any event, female; n=1078, 1075	Unclassified, any event, overall; n=2220, 2227	Unclassified, any event, male; n=1142, 1152	Unclassified, any event, female; n=1078, 1075	Other, any event, overall; n=2220, 2227	Other, any event, male; n=1142, 1152	Other, any event, female; n=1078, 1075
Combined MET/SU: Main Study and Observational Follow-up	151	60	91	70	22	48	40	14	26	13	1	12	14	9	5	5	4	1	0	0	0	26	16	10
Combined RSG: Main Study and Observational Follow-up	238	82	156	116	32	84	88	31	57	16	4	12	18	7	11	0	0	0	1	1	0	31	18	13

Number of Participants With the Indicated Bone Fracture by Fracture Site: Observational Follow-up

Intervention	participants (Number)
	Any event, overall; n=1280, 1250	Any event, male; n=665, 635	Any event, female; n=615, 615	Upper limb, any event, overall; n=1280, 1250	Upper limb, any event, male; n=665, 635	Upper limb, any event, female; n=615, 615	Distal lower limb, any event, overall; n=1280,1250	Distal lower limb, any event, male; n=665, 635	Distal lower limb, any event, female; n=615, 615	Femur/hip, any event, overall; n=1280, 1250	Femur/hip, any event, male; n=665, 635	Femur/hip, any event, female; n=615, 615	Spinal, any event, overall; n=1280, 1250	Spinal, any event, male; n=665, 635	Spinal, any event, female; n=615, 615	Pelvic, any event, overall; n=1280, 1250	Pelvic, any event, male; n=665, 635	Pelvic, any event, female; n=615, 615	Unclassified, any event, overall; n=1280, 1250	Unclassified, any event, male; n=665, 635	Unclassified, any event, female; n=615, 615	Other, any event, overall; n=1280, 1250	Other, any event, male; n=665, 635	Other, any event, female; n=615, 615
Combined MET/SU: Observational Follow-up	37	11	26	15	3	12	13	4	9	5	0	5	5	4	1	1	1	0	0	0	0	1	1	0
Combined RSG: Observational Follow-up	64	25	39	33	10	23	18	9	9	6	1	5	4	1	3	0	0	0	1	1	0	6	4	2

Number of Participants With the Indicated Serious Adverse Event: Observational Follow-up

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	Any event	Ankle fracture	Prostate cancer	Lung neoplasm malignant	Breast cancer	Basal cell carcinoma	Pancreatic carcinoma	Colon cancer	Humerus fracture	Upper limb fracture	Malignant melanoma	Uterine cancer	Gastric cancer	Wrist fracture	Hip fracture	Radius fracture	Forearm fracture	Hepatic neoplasm malignant	Rectal cancer	Renal cancer	Foot fracture	Renal cell carcinoma	Femur fracture	Femoral neck fracture	Lumbar vertebral fracture	Metastases to bone	Metastases to liver	Bladder cancer	Fall	Metastases to central nervous system	Rib fracture	Squamous cell carcinoma	Acute myocardial infarction	Brain neoplasm	Gastric neoplasm	Metastases to lung	Patella fracture	Death	Abdominal pain	Acute myeloid leukaemia	Acute respiratory failure	Anaemia	Benign salivary gland neoplasm	Biliary colic	Biliary neoplasm	Bone neoplasm malignant	Bronchial carcinoma	Cardiac failure acute	Chest pain	Chronic lymphocytic leukaemia	Colon neoplasm	Contusion	Drowning	Dysplasia	Endometrial cancer stage I	Leukaemia	Lower limb fracture	Lung squamous cell carcinoma stage unspecified	Lymphoma	Malignant neoplasm of pleura	Metastases to skin	Metastases to testicle	Metastatic renal cell carcinoma	Oesophageal carcinoma	Osteoarthritis	Pancreatic necrosis	Rectal cancer stage II	Spinal fracture	T-cell lymphoma	Urinary tract infection	Uterine leiomyosarcoma	Biliary cancer metastatic	Cervix carcinoma	Chronic obstructive pulmonary disease	Comminuted fracture	Craniocerebral injury	Gastrointestinal neoplasm	Hepatic lesion	Joint dislocation	Laryngeal cancer	Lip neoplasm malignant stage unspecified	Lung neoplasm	Metastases to lymph nodes	Metastasis	Musculoskeletal chest pain	Myocardial infarction	Non-Hodgkin's lymphoma	Pubis fracture	Pulmonary embolism	Rectal cancer recurrent	Rectal neoplasm	Skin cancer	Skin ulcer	Small cell lung cancer stage unspecified	Sternal fracture	Subdural haemorrhage	Sudden death	Thoracic vertebral fracture	Thyroid cancer	Vulval cancer
Combined MET/SU: Observational Follow-up	76	3	1	4	6	3	3	6	1	1	2	3	0	0	1	1	2	2	2	2	3	0	1	2	2	2	2	0	0	0	0	0	1	1	1	1	1	2	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	1	1	1	0	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1
Combined RSG: Observational Follow-up	99	6	7	4	2	4	4	1	5	5	3	2	4	4	3	3	2	2	2	2	1	3	2	1	1	1	1	2	2	2	2	2	1	1	1	1	1	0	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	1	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0	0

Number of Participants With the Indicated Type of Malignant Neoplasms/Cancer Events Reported as an SAE or Death by Location (Including Location of Special Interest): Main Study + Observational Follow-up Combined

The observational follow-up (OFU) was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the OFU. The neoplasms/cancer events of bladder, breast, colon, liver, pancreatic, prostate cancer, and melanoma were pre-specified as cancers of interest for the OFU. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the beginning of the main study through the end of the observational follow-up (up to 11.4 years)

Intervention	participants (Number)
	Any genitourinary	Prostate	Renal	Uterine	Bladder	Vaginal/vulvar	Ovarian	Any gastrointestinal	Colon/rectal cancer	Colon	Gastric	Pancreatic	Liver	Gall bladder/biliary	Gastrointestinal; not specified	Any hematologic	Lung	Skin (non-melanomatous)	Skin (melanomatous)	Metastases	Breast	Head and neck	Neurologic	Endocrine	Not specified	Other
Combined MET/SU: Main Study and Observational Follow-up	57	22	9	16	5	1	4	62	30	21	5	16	5	5	1	6	15	13	4	18	23	7	3	6	1	3
Combined RSG: Main Study and Observational Follow-up	57	22	12	11	8	1	5	48	22	14	13	5	4	4	0	12	19	19	6	12	12	4	3	3	0	0

Number of Participants With the Indicated Type of Malignant Neoplasms/Cancer Events Reported as an SAE or Death by Location (Including Location of Special Interest): Observational Follow-up

The observational follow-up (OFU) was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the OFU. The neoplasms/cancer events of bladder, breast, colon, liver, pancreatic, prostate cancer, and melanoma were pre-specified as cancers of interest for the OFU. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	Any genitourinary	Prostate	Renal	Uterine	Bladder	Vaginal/vulvar	Ovarian	Any gastrointestinal	Colon/rectal cancer	Colon	Gastric	Pancreatic	Liver	Gall bladder/biliary	Gastrointestinal; not specified	Any hematologic	Lung	Skin (non-melanomatous)	Skin (melanomatous)	Metastases	Breast	Head and neck	Neurologic	Endocrine	Not specified	Other
Combined MET/SU: Observational Follow-up	8	1	2	4	0	1	0	19	11	7	1	3	2	1	1	1	6	5	2	6	7	1	1	1	0	0
Combined RSG: Observational Follow-up	18	7	5	4	2	0	0	17	5	2	5	4	2	1	0	6	6	6	3	3	2	2	1	0	0	0

Number of Participants With the Indicated Type of Neoplasm/Cancer Event Reported as a Serious Adverse Event (SAE) or Death: Main Study + Observational Follow-up Combined

Intervention	participants (Number)
	All neoplasms/cancer (N/C) (benign/malignant)	Malignant (Mal.) N/C	Mal. N/C; excluding non-melanomatous skin cancers
Combined MET/SU: Main Study and Observational Follow-up	215	195	186
Combined RSG: Main Study and Observational Follow-up	196	179	164

Number of Participants With the Indicated Type of Neoplasm/Cancer Event Reported as a Serious Adverse Event (SAE) or Death: Observational Follow-up

The observational follow-up was designed to collect data concerning cancer and bone fractures in RECORD participants during a 4-year period after the end of the main RECORD study. At the end of the main study, all study medication was stopped. Participants were not provided with study medication in the observational follow-up; instead, anti-diabetic treatment was prescribed at the investigator's discretion. An SAE is defined as any event that is fatal; life threatening; disabling/incapacitating; results in hospitalization (excluding elective surgery or routine clinical procedures); prolongs a hospital stay; is associated with a congenital abnormality; cancer; is associated with an overdose. In addition, any event that the investigator regards as serious or that would suggest any significant hazard, contraindication, side effect, or precaution that may be associated with the study procedures should be reported as an SAE. (NCT00379769)
Timeframe: From the end of the RECORD study through the end of the observational follow-up (up to 4.0 years)

Intervention	participants (Number)
	All neoplasms/cancer (N/C) (benign/malignant)	Malignant (Mal.) N/C	Mal. N/C; excluding non-melanomatous skin cancers
Combined MET/SU: Observational Follow-up	51	51	46
Combined RSG: Observational Follow-up	60	59	55

Total Number of Cardiovascular Hospitalisations and Cardiovascular Deaths

The total number of events for individual components of cardiovascular (CV) hospitalisations and cardiovascular deaths were recorded. MI, myocardial infarction. (NCT00379769)
Timeframe: Baseline through End of Study (up to 7.5 years)

Intervention	Number of events (Number)
	CV deaths	Death due to acute MI	Death due to heart failure	Sudden death	Death due to acute vascular events	Other CV mortality	Death of presumed CV cause	Cardiovascular hospitalisation	Hospitalisation for acute MI	Hospitalisation for unstable angina	Hospitalisation for congestive heart failure	Hospitalisation for stroke	Hospitalisation for transient ischaemic attack	Hospitalisation for invasive CV procedure	Hospitalisation for amputation of extremities	Other CV hospitalisations
Combined MET/SU	71	10	2	12	10	4	33	490	57	28	36	67	10	116	23	153
Combined RSG	60	7	10	8	1	6	28	483	66	28	69	51	10	99	6	154

Change in Fasting Insulin From Week 0(Baseline) to Week 16 Least Squares Mean

change in fasting insulin from Week 0(baseline) to week 16 least squares mean and 95% confidence interval change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	uIU/mL (Least Squares Mean)
Colesevelam	-0.320
Rosiglitazone	-1.482
Sitagliptin	0.092

Change in Fasting Insulin From Week 0(Baseline) to Week 8 Least Squares Mean

change in fasting insulin from Week 0(baseline) to week 8 least squares mean and 95% confidence interval change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention	uIU/mL (Least Squares Mean)
Colesevelam	0.075
Rosiglitazone	-2.156
Sitagliptin	4.002

Change in Fasting Plasma Glucose (FPG) From Week 0(Baseline) to Week 8 Least Squares Mean

change in FPG from Week 0(baseline) to week 8 least squares mean and 95% confidence interval change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention	mg/dL (Least Squares Mean)
Colesevelam	-15.6
Rosiglitazone	-28.9
Sitagliptin	-17.4

Change in FPG From Week 0(Baseline) to Week 16 Least Squares Mean

change in FPG from Week 0(baseline) to week 16 least squares mean and 95% confidence interval change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Least Squares Mean)
Colesevelam	-17.3
Rosiglitazone	-31.4
Sitagliptin	-24.4

Change in Low-Density Lipoprotein-C(LDL-C) From Week 0(Baseline) to Week 16 Least Squares Mean

change in LDL-C from Week 0(baseline) to week 16 least squares mean with 95% confidence intervals change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Least Squares Mean)
Colesevelam	-19.5
Rosiglitazone	4.9
Sitagliptin	6.2

Change in Post-prandial Glucose From Week 0(Baseline) to Week 16 Least Squares Mean

change in post-prandial glucose from Week 0(baseline) to week 16 least squares mean with 95% confidence intervals change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Least Squares Mean)
Colesevelam	-17.7
Rosiglitazone	-53.6
Sitagliptin	-43.6

Mean Change in Fasting Insulin From Week 0(Baseline) to Week 16

mean change in fasting insulin from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	uIU/mL (Mean)
Colesevelam	-0.212
Rosiglitazone	-1.910
Sitagliptin	-0.419

Mean Change in Fasting Insulin From Week 0(Baseline) to Week 8

mean change in fasting insulin from Week 0(baseline) to week 8 with standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention	uIU/mL (Mean)
Colesevelam	0.107
Rosiglitazone	-2.213
Sitagliptin	4.028

Mean Change in FPG From Week 0(Baseline) to Week 16

change in FPG from Week 0(baseline) to week 16 mean and standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Mean)
Colesevelam	-15.8
Rosiglitazone	-34.0
Sitagliptin	-23.1

Mean Change in FPG From Week 0(Baseline) to Week 8

mean change in FPG from Week 0(baseline) to Week 8 with standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention	mg/dL (Mean)
Colesevelam	-12.5
Rosiglitazone	-30.8
Sitagliptin	-18.6

Mean Change in LDL-C From Week 0(Baseline) to Week 16

mean change in LDL-C from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Mean)
Colesevelam	-19.7
Rosiglitazone	5.5
Sitagliptin	5.7

Mean Change in Post-prandial Glucose From Week 0(Baseline) to Week 16

mean change in post-prandial glucose from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Mean)
Colesevelam	-20.1
Rosiglitazone	-54.0
Sitagliptin	-40.9

Mean Change in Post-prandial Insulin From Week 0(Baseline) to Week 16

mean change in post-prandial insulin from Week 0(baseline) to week 16 with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	mg/dL (Mean)
Colesevelam	3.898
Rosiglitazone	1.962
Sitagliptin	4.832

Mean Percentage of Change in Glycosylated Hemoglobin (HbA1c) From Week 0(Baseline) to Week 16 Endpoint Least Squares Mean

Change in HbA1c from Week 0(baseline)to Week 16 endpoint least squares mean with 95% confidence intervals, change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	% change in HbA1c (Least Squares Mean)
Colesevelam	-0.27
Rosiglitazone	-0.58
Sitagliptin	-0.38

Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 16 Endpoint

Change in HbA1c from Week 0(baseline) to Week 16 endpoint mean with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	% change HbA1c (Mean)
Colesevelam	-0.31
Rosiglitazone	-0.65
Sitagliptin	-0.56

Mean Percentage of Change in HbA1c From Week 0(Baseline) to Week 8

change in HbA1c from Week 0(baseline) to week 8 mean and standard deviation change = week 8 - week 0. (NCT00484419)
Timeframe: 8 weeks change = week 8- week 0.

Intervention	% change in HbA1c (Mean)
Colesevelam	-0.31
Rosiglitazone	-0.19
Sitagliptin	-0.48

Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16 (Least Squares Mean)

percent change in LDL-C levels from Week 0(baseline) to Week 16 (least squares mean with 95% confidence interval) (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	% change in LDL-C (Least Squares Mean)
Colesevelam	-16.24
Rosiglitazone	6.92
Sitagliptin	7.98

Mean Percentage of Change in LDL-C Levels From Week 0(Baseline) to Week 16

mean percent change in LDL-C levels from Week 0(baseline) to Week 16 mean with standard deviation change = week 16 - week 0. (NCT00484419)
Timeframe: 16 weeks change = week 16 - week 0.

Intervention	% change in LDL-C (Mean)
Colesevelam	-16.40
Rosiglitazone	7.41
Sitagliptin	7.61

8-Iso Prostaglandin F2α (8-iso PGF2α) Excretion Rate

8-Iso Prostaglandin F2α (8-iso PGF2α) excretion rate measured during the 24 hours preceding the CGM system removal. The nocturnal glycemia measured by CGM system will be defined as the average of glycemic values collected between midnight and breakfast time. (NCT00318656)
Timeframe: Baseline and 12 weeks

Intervention	pg/mL (Mean)
	Baseline	12 weeks
Avandamet® (Rosiglitazone/Metformin)	361.9	373.5
Glimepiride/Metformin	325.1	320.4