Rosiglitazone is a thiazolidinedione (TZD) drug used to treat type 2 diabetes. It works by increasing insulin sensitivity in the body. Rosiglitazone is synthesized through a multi-step process involving several chemical reactions. The drug was initially developed and marketed by GlaxoSmithKline under the brand name Avandia. Rosiglitazone was found to be effective in reducing blood glucose levels in patients with type 2 diabetes. However, it was also associated with an increased risk of cardiovascular events, leading to its restricted use and eventual withdrawal in several countries. Rosiglitazone continues to be studied due to its unique mechanism of action and its potential benefits for specific patient populations. Despite the controversy surrounding its cardiovascular safety, research continues to explore its potential role in diabetes management.'
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]
| 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.) |
Rosiglitazone (RSG) is a member of the thiazolidinedione family. It is reported to protect cells from cytotoxicity and endoplasmic reticulum (ER) stress in other cell types.
Rosiglitazone (RSG) has a variety of actions on both insulin sensitization and anti-atherogenic effects. The drug has an ameliorative effect on the DRG and enhances the functional recovery after SNC in rats.
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. It has been proven to enhance the glycolytic capability of stallion spermatozoa maintained at ambient temperature.
Rosiglitazone-mediated increase in SIRT1 stability is accompanied by upregulation of mitogen-activated protein kinase phosphatase (MKP)-7. Rosig litazone group had lower adhesion scores [median (min-max ranges)] regarding extent, severity, and degree of the adhesions.
Rosiglitazone treatment adversely affects bone formation over a 2-year period. All rabbits treated had significantly improved laboratory parameters and plasma tumour necrosis factor-alpha levels.
Rosiglitazone displays a robust hypoglycemic action in patients with type 2 diabetes mellitus (T2DM) and elicits serious adverse reactions, especially hepatotoxicity and cardiotoxicity. The aim is to investigate the usefulness of metric indices in post-marketing safety evaluations.
There were no measurable changes in glipizide (5 mg), metformin (500 mg) or rosiglitazone (2 mg) exposure parameters, maximum plasma concentration and the area under the concentration-time curve, or pharmacokinetic parameter, elimination half-life when coadministered with ISIS 113715. There were no significant differences between SLCO1B1 diplotype groups.
The purpose of this study was to determine the maximally tolerated dose, peak plasma concentrations and side effect profile of oral rosiglitazone when combined with carboplatin in dogs with cancer. We investigated the tolerability and pharmacokinetics of exemestane in combination with metformin and ros Giglita in nondiabetic overweight and obese postmenopausal women with hormone receptor-positive metastatic breast cancer.
The absorption of rosiglitazone was rapid and essentially complete, with absolute bioavailability estimated to be approximately 99% after oral tablet dosing. The proposed method enabled the unambiguous evaluation and quantitation for pharmacokinetic, bioavailability or drug-drug interaction studies.
Clinical data on more than 4500 patients with type 2 diabetes show that rosiglitazone is a safe, effective monotherapy or combination therapy, producing significant reductions in haemoglobin A1c and fasting plasma glucose under different dosing regimens.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dose-response relationships for both of the TZDs were also determined using the 24-h treatment time point." | ( A novel method for analysis of nuclear receptor function at natural promoters: peroxisome proliferator-activated receptor gamma agonist actions on aP2 gene expression detected using branched DNA messenger RNA quantitation. Burris, TP; Cryan, E; Demarest, KT; Osborne, MC; Pelton, PD; Zhou, L, 1999) | 0.3 |
| "These data support dosing guidelines that will permit the administration of rosiglitazone without regard to meals for treatment of type 2 diabetes mellitus." | ( Systemic exposure to rosiglitazone is unaltered by food. Allen, A; DiCicco, RA; Freed, MI; Jorkasky, DK, 1999) | 0.85 |
| "To examine the effects of repeat oral dosing of rosiglitazone on the pharmacokinetics of nifedipine, a prototype CYP3A4 substrate, a randomized, open-label, crossover study was performed with two treatment phases separated by a washout period of at least 14 days." | ( Rosiglitazone has no clinically significant effect on nifedipine pharmacokinetics. Finnerty, D; Freed, MI; Harris, RZ; Inglis, AM; Jorkasky, DK; Miller, AK; Patterson, S; Thompson, KA, 1999) | 2 |
| " dosing of rosiglitazone solution, and the disposition of nonradiolabeled rosiglitazone was determined after oral dosing of tablets in this open-label, three-part, semirandomized, crossover study." | ( Absorption, disposition, and metabolism of rosiglitazone, a potent thiazolidinedione insulin sensitizer, in humans. Cowley, H; Cox, PJ; Harris, AM; Hollis, FJ; Miller, AK; Ryan, DA; Vousden, M, 2000) | 0.96 |
| " PPAR-gamma ligands significantly inhibited VEGF-induced migration and proliferation in both cell types and tube formation of CEC in a dose-response manner." | ( Peroxisome proliferator-activated receptor-gamma ligands inhibit choroidal neovascularization. Hangai, M; He, S; Hinton, DR; Hsueh, WA; Ishibashi, T; Kim, S; Law, RE; Murata, T; Ryan, SJ; Xi, XP, 2000) | 0.31 |
| "In two independent studies, obese Zucker rats were dosed orally once daily for 14 days with one of the following treatments: LG 100268 (20 mg/kg), LG 100324 (20 mg/kg), BRL 49653 (3 mg/kg) or vehicle." | ( Retinoid X receptor agonists have anti-obesity effects and improve insulin sensitivity in Zucker fa/fa rats. Cawthorne, MA; Crombie, DL; Heyman, RA; Hislop, DC; Liu, YL; Sennitt, MV, 2000) | 0.31 |
| " The 5 h fasted plasma insulin concentration was significantly lower in the rexinoid-treated groups and the terminal insulin level (at the end of the clamp) tended to be lower in all treated groups compared with animals given the dosing vehicle." | ( Retinoid X receptor agonists have anti-obesity effects and improve insulin sensitivity in Zucker fa/fa rats. Cawthorne, MA; Crombie, DL; Heyman, RA; Hislop, DC; Liu, YL; Sennitt, MV, 2000) | 0.31 |
| " Clinical data on more than 4500 patients with type 2 diabetes show that rosiglitazone is a safe, effective monotherapy or combination therapy, producing significant reductions in haemoglobin A1c and fasting plasma glucose under different dosing regimens." | ( Rosiglitazone. Goldstein, BJ, 2000) | 1.98 |
| "This article reviews the pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and dosing of rosiglitazone, the second thiazolidinedione approved for the treatment of type 2 diabetes mellitus." | ( Rosiglitazone in the treatment of type 2 diabetes mellitus: a critical review. Bolesta, S; Malinowski, JM, 2000) | 1.96 |
| " To determine the specific effects of rosiglitazone (RSG) on beta-cell mass dynamics, male fa/fa (obese) and +/fa or +/+ (lean) rats age 6 weeks were fed either chow (control group [CN]) or chow mixed with rosiglitazone (RSG group) at a dosage of 10 micromol." | ( Beta-cell mass dynamics in Zucker diabetic fatty rats. Rosiglitazone prevents the rise in net cell death. Buckingham, RE; Finegood, DT; Kojwang, D; Leonard, T; McArthur, MD; Thomas, MJ; Topp, BG, 2001) | 0.83 |
| "Sixteen healthy volunteers (24-59-years old) received a single 8-mg dose of rosiglitazone on day 1, followed by 7 days of repeat dosing with acarbose [100 mg three times daily (t." | ( The effect of acarbose on the pharmacokinetics of rosiglitazone. Culkin, KT; Freed, MI; Inglis, AM; Jorkasky, DK; Miller, AK, 2001) | 0.79 |
| " A dosage of 4 mg twice/day significantly reduced fasting plasma glucose levels and produced comparable reductions in glycosylated hemoglobin compared with glyburide." | ( A review of rosiglitazone in type 2 diabetes mellitus. Travaglini, MT; Werner, AL, 2001) | 0.69 |
| " The effects of rosiglitazone treatment were studied using Zucker (fa/fa) rats after 7 days of oral dosing (3." | ( Insulin-sensitizing effect of rosiglitazone (BRL-49653) by regulation of glucose transporters in muscle and fat of Zucker rats. Adler, A; Bush, E; Kramer, D; Rondinone, CM; Shapiro, R, 2001) | 0.95 |
| " The percentage recoveries of Active Pharmaceutical Ingredient (API) from dosage forms ranged from 99." | ( LC determination of rosiglitazone in bulk and pharmaceutical formulation. Radhakrishna, T; Satyanarayana, A; Satyanarayana, J, 2002) | 0.64 |
| " We also document a PPAR gamma activator dose-response effect on reporter gene expression." | ( Efficient gene regulation by PPAR gamma and thiazolidinediones in skeletal muscle and heart. Caron, A; Darteil, R; Latta-Mahieu, M; Mahfoudi, A; Staels, B; Thuillier, V; Wang, M, 2002) | 0.31 |
| " Results of po dosed efficacy studies in the db/db mouse model of type 2 diabetes showed efficacy equal or superior to Rosiglitazone in correcting hyperglycemia and hypertriglyceridemia." | ( Amphipathic 3-phenyl-7-propylbenzisoxazoles; human pPaR gamma, delta and alpha agonists. Adams, AD; Berger, JP; Doebber, TW; Hu, Z; Jones, AB; MacNaul, KL; Moller, DE; Santini, C; Yuen, W, 2003) | 0.53 |
| " The prandial glucose regulator repaglinide has been studied in combination with metformin (an inhibitor of hepatic glucose production), neutral protamine Hagedorn (NPH)-insulin (which has a long duration of effect, but at the risk of early hypoglycaemia and late hyperglycaemia in the dosing interval) and three thiazolidinediones (TZDs--troglitazone, rosiglitazone and pioglitazone, which stimulate nuclear receptors to increase insulin sensitivity and reduce insulin resistance) in patients whose diabetes was inadequately controlled by previous monotherapy or combination therapy." | ( Repaglinide in combination therapy. Moses, R, 2002) | 0.48 |
| "This review examines the pharmacology, pharmacokinetics, drug-interaction potential, adverse effects, and dosing guidelines for metformin hydrochloride, a biguanide agent for the treatment of type 2 diabetes." | ( Metformin hydrochloride in the treatment of type 2 diabetes mellitus: a clinical review with a focus on dual therapy. Campbell, RK; Iltz, JL; Setter, SM; Thams, J, 2003) | 0.32 |
| "Following an open-label, lead-in phase to optimize the dosing of glyburide/metformin tablets, 365 patients randomly received additive therapy comprising rosiglitazone (4 mg once daily) or placebo for 24 weeks." | ( Glycemic control with glyburide/metformin tablets in combination with rosiglitazone in patients with type 2 diabetes: a randomized, double-blind trial. Bruce, S; Dailey, GE; Fiedorek, FT; Noor, MA; Park, JS, 2004) | 0.76 |
| " The initial daily dosage of rosiglitazone, 2 mg daily, was increased to 4 mg if their fasting plasma glucose concentrations were above 10 mmol/L after 4 weeks." | ( The metabolic effects of insulin and rosiglitazone combination therapy in Chinese type 2 diabetic patients with nephropathy. Chan, JC; Chan, NN; Chiu, CK; Leung, WY; So, WY; Tong, PC, 2004) | 0.89 |
| " Sensitivity analyses undertaken by the assessment team suggest that the cost per quality-adjusted life-year (QALY) of rosiglitazone is most sensitive to dosage and treatment effect, that is, the effect of rosiglitazone on beta-cell function and insulin sensitivity." | ( Clinical effectiveness and cost-effectiveness of pioglitazone and rosiglitazone in the treatment of type 2 diabetes: a systematic review and economic evaluation. Beverley, C; Chilcott, J; Cowan, J; Czoski-Murray, C; Psyllaki, MA; Warren, E, 2004) | 0.77 |
| " No published economic studies on either pioglitazone or rosiglitazone were found, although sensitivity analyses undertaken by the assessment team suggest that the cost per QALY of rosiglitazone is most sensitive to dosage and treatment effect." | ( Clinical effectiveness and cost-effectiveness of pioglitazone and rosiglitazone in the treatment of type 2 diabetes: a systematic review and economic evaluation. Beverley, C; Chilcott, J; Cowan, J; Czoski-Murray, C; Psyllaki, MA; Warren, E, 2004) | 0.81 |
| " The results indicated that MEKC can be used an alternative method to HPLC for the determination of rosiglitazone in pharmaceutical dosage form." | ( Determination of rosiglitazone in coated tablets by MEKC and HPLC methods. Gomes, P; Jablonski, A; Sippel, J; Steppe, M, 2004) | 0.88 |
| " Records were assessed for the diagnosis of CHF and documented patient complaints of CHF symptoms requiring a medical intervention (unscheduled primary care or emergency room visit, start or dosage adjustment of CHF pharmacotherapy, or hospitalization)." | ( Chronic heart failure-related interventions after starting rosiglitazone in patients receiving insulin. Biery, JC; Goins, JA; Lee, TA; Marceille, JR; Soni, R, 2004) | 0.57 |
| " Diabetics showed blunted dose-response curves to both SNP and ACh." | ( Haematocrit, type 2 diabetes, and endothelium-dependent vasodilatation of resistance vessels. Baldeweg, S; Baldi, S; Casolaro, A; Ferrannini, E; Natali, A; Sironi, AM; Toschi, E; Yudkin, JS, 2005) | 0.33 |
| "Ninety-five patients with type 2 diabetes for at least 6 months without glycemic control by diet and oral hypoglycemic agents to their maximum tolerated dosage and who also had metabolic syndrome." | ( Antithrombotic effects of rosiglitazone-metformin versus glimepiride-metformin combination therapy in patients with type 2 diabetes mellitus and metabolic syndrome. Ciccarelli, L; Cicero, AF; Derosa, G; Ferrari, I; Gaddi, AV; Ghelfi, M; Peros, E; Piccinni, MN; Salvadeo, S, 2005) | 0.63 |
| " Insulin regimen and dosage were modified in all subjects to achieve near-normal glycemic control." | ( The effect of rosiglitazone on overweight subjects with type 1 diabetes. Raskin, P; Strowig, SM, 2005) | 0.69 |
| " Bioequivalence between the fixed-dose combination tablet and coadministration of rosiglitazone with metformin at the same dosage has been established in a pharmacokinetic study." | ( Rosiglitazone/Metformin. Wellington, K, 2005) | 2 |
| "Compensatory hyperinsulinemia permitting insulin-resistant individuals to maintain normal glucose tolerance is associated with a left shift in the glucose-stimulated insulin secretion rate (GS-ISR) dose-response curve and decrease in the insulin metabolic clearance rate (I-MCR)." | ( Rosiglitazone reduces glucose-stimulated insulin secretion rate and increases insulin clearance in nondiabetic, insulin-resistant individuals. Abbasi, F; Chu, JW; Kim, SH; Lamendola, C; McLaughlin, TL; Polonsky, KS; Reaven, GM, 2005) | 1.77 |
| " Rats were dosed daily for 6 wk with either vehicle (0." | ( Chronic rosiglitazone treatment restores AMPKalpha2 activity in insulin-resistant rat skeletal muscle. Chen, ZP; Febbraio, MA; Hashem, M; Hawley, JA; Kemp, BE; Lessard, SJ; Reid, JJ; Watt, MJ, 2006) | 0.77 |
| " Patients from both groups continued to take the same dosage of metformin during the study period." | ( Rosiglitazone effects on blood pressure and metabolic parameters in nondipper diabetic patients. Dazzi, D; Hassan, H; Mangieri, T; Negro, R; Pezzarossa, A, 2005) | 1.77 |
| "An open-label randomized study was performed in which 52 patients with type 2 diabetes on peritoneal dialysis therapy administered a constant dosage of subcutaneous insulin with stable glycemic control were randomly assigned to the administration of either RSG (fixed dose, 4 mg) plus insulin or insulin alone." | ( Rosiglitazone reduces insulin requirement and C-reactive protein levels in type 2 diabetic patients receiving peritoneal dialysis. Chow, KM; Lam, CW; Leung, CB; Li, PK; Szeto, CC; Wong, TY, 2005) | 1.77 |
| " There was a significantly greater decrease in insulin dosage in the RSG than control group (-21." | ( Rosiglitazone reduces insulin requirement and C-reactive protein levels in type 2 diabetic patients receiving peritoneal dialysis. Chow, KM; Lam, CW; Leung, CB; Li, PK; Szeto, CC; Wong, TY, 2005) | 1.77 |
| " Rats were dosed orally for 16 days with bladder carcinogenic (ragaglitazar) as well as non-bladder carcinogenic (fenofibrate and rosiglitazone) PPAR agonists and protein changes were assayed in the urinary bladder urothelium by Western blotting." | ( Biomarkers for early effects of carcinogenic dual-acting PPAR agonists in rat urinary bladder urothelium in vivo. Egerod, FL; Iversen, L; Nielsen, HS; Oleksiewicz, MB; Storgaard, T; Thorup, I, ) | 0.34 |
| "Extending the residence time of a dosage form at a particular site and controlling the release of drug from the dosage form are useful especially for achieving controlled plasma level of the drug as well as improving bioavailability." | ( Formulation and evaluation of mucoadhesive dosage form containing rosiglitazone maleate. Krishna, SS; Ray, S; Thakur, RS, 2006) | 0.57 |
| " Another objective of the study was to determine the effect of staggered oral CSA dosing at 1, 2 and 4 h after oral RGL administration at 10 mg kg-1." | ( Influence of cholestyramine on the pharmacokinetics of rosiglitazone and its metabolite, desmethylrosiglitazone, after oral and intravenous dosing of rosiglitazone: impact on oral bioavailability, absorption, and metabolic disposition in rats. Mullangi, R; Muzeeb, S; Srinivas, NR; Venkatesh, P, 2006) | 0.58 |
| "To investigate the effect of multiple dosing with montelukast, a selective leukotriene-receptor antagonist, on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in humans." | ( Effect of multiple doses of montelukast on the pharmacokinetics of rosiglitazone, a CYP2C8 substrate, in humans. Kim, KA; Kim, KR; Park, JY; Park, PW, 2007) | 0.78 |
| " Insulin dosage was adjusted as necessary." | ( Rosiglitazone: safety and efficacy in combination with insulin in poorly controlled type 2 diabetes mellitus patients treated with insulin alone. Garg, R; Gopal, J; Jones, GR, ) | 1.57 |
| "0001), insulin dosage reduction 10 U (74+/-34 vs." | ( Rosiglitazone: safety and efficacy in combination with insulin in poorly controlled type 2 diabetes mellitus patients treated with insulin alone. Garg, R; Gopal, J; Jones, GR, ) | 1.57 |
| " However, in the absence of clinical data, it is prudent to reduce the dosage of each glitazone by half in patients treated with gemfibrozil." | ( Pharmacokinetic interactions with thiazolidinediones. Scheen, AJ, 2007) | 0.34 |
| "Plasma ACTH was measured before (0830 h) and 120 min after morning dosing with hydrocortisone (HC)." | ( Ineffectiveness of rosiglitazone therapy in Nelson's syndrome. Ince, P; Munir, A; Newell-Price, J; Ross, R; Song, F; Walters, SJ, 2007) | 0.67 |
| " By performing a dose-response assay, we determined that high concentrations of Rosi inhibit proliferation, while low concentrations of Rosi induce proliferation." | ( Transactivation of ERalpha by Rosiglitazone induces proliferation in breast cancer cells. Allred, CD; Kilgore, MW; Talbert, DR; Zaytseva, YY, 2008) | 0.63 |
| " RG was administered daily and increased to a maximum dosage of 24 mg daily, according to the response of ACTH and cortisol secretion." | ( Long-term treatment of central Cushing's syndrome with rosiglitazone. Becker, C; Bierhaus, A; Bode, H; Fohr, B; Hamann, A; Hammes, HP; Humpert, P; Kasperk, C; Morcos, M; Nawroth, PP; Pfisterer, F; Schilling, T; Schwenger, V; Tafel, J; Zeier, M, 2007) | 0.59 |
| " The dosage of insulin therapy could be adjusted at the investigator's discretion if required for hypoglycemia or additional glycemic control." | ( Low-dose rosiglitazone in patients with insulin-requiring type 2 diabetes. Chou, HS; Hollander, P; Yu, D, 2007) | 0.76 |
| "This study assessed the efficacy and safety of two different dosing regimens of fixed-dose combination (FDC) rosiglitazone (RSG) plus glimepiride (GLIM) compared with RSG or GLIM monotherapy in drug-naive subjects with type 2 diabetes mellitus (T2DM)." | ( Initial treatment with fixed-dose combination rosiglitazone/glimepiride in patients with previously untreated type 2 diabetes. Chou, HS; Ferreira-Cornwell, C; Goldstein, BJ; Jones, AR; Krebs, J; Palmer, JP; Waterhouse, B, 2008) | 0.82 |
| " They can be minimised through the use of an appropriate stepwise dosing regimen and careful choice of diet." | ( Cardiovascular benefits and safety profile of acarbose therapy in prediabetes and established type 2 diabetes. Hanefeld, M, 2007) | 0.34 |
| " The mean therapeutic dosage of insulin glargine in group A was 14." | ( Therapeutic options for elderly diabetic subjects: open label, randomized clinical trial of insulin glargine added to oral antidiabetic drugs versus increased dosage of oral antidiabetic drugs. Alagona, C; Chiavetta, A; Fedele, V; Leotta, C; Lorenti, I; Luca, S; Papa, G; Pezzino, V; Piro, S; Purrello, F; Rabuazzo, AM; Spadaro, L, 2008) | 0.35 |
| " PK assessment of potential novel therapies for resistant FSGS is necessary to define appropriate dosing regimens." | ( Phase I trial of rosiglitazone in FSGS: I. Report of the FONT Study Group. Cattran, D; Dike, M; Eddy, A; Fogo, AB; Gipson, DS; Joy, MS; Kopp, JB; Powell, L; Thompson, A; Trachtman, H; Vento, S, 2009) | 0.69 |
| " Whereas high dosage of full agonists may expose RA patients to cardiovascular adverse effects, the proof of concept that PPAR agonists have therapeutical relevance to OA may benefit from an epidemiological follow-up of joint lesions in diabetic or hyperlipidemic patients treated for long periods of time with glitazones or fibrates." | ( [Pathophysiological relevance of peroxisome proliferators activated receptors (PPAR) to joint diseases - the pro and con of agonists]. Bianchi, A; Jouzeau, JY; Koufany, M; Moulin, D; Netter, P; Sebillaud, S, 2008) | 0.35 |
| "Various approaches have been used to retain the dosage form in stomach as a way of increasing the gastric residence time, including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extensible, or swellable systems; and superporous hydrogel systems." | ( Development and in vitro evaluation of floating rosiglitazone maleate microspheres. Borate, SG; Parikh, GN; Ranpise, AA; Rao, MR; Thanki, KC, 2009) | 0.61 |
| "An efficient, sensitive, and simple method was developed for the simultaneous determination of rosiglitazone and metformin hydrochloride in a combination tablet dosage form by column high-performance liquid chromatography." | ( Column high-performance liquid chromatographic method for the simultaneous determination of rosiglitazone and metformin in a pharmaceutical preparation. Abu-Nameh, ES; Ali, AR; Duraidi, II; Saket, MM, ) | 0.57 |
| " Using the data collected with the USP II apparatus, the plasma profiles were simulated and compared with human plasma profiles obtained after administration of the same dosage forms to healthy fasted volunteers." | ( A comparative study of different release apparatus in generating in vitro-in vivo correlations for extended release formulations. Aivaliotis, A; Butler, J; Dressman, J; Fischbach, M; Fotaki, N; Hempenstall, J; Klein, S; Reppas, C, 2009) | 0.35 |
| " In contrast, Egr-1 was induced in the nuclei of bladder, as well as kidney pelvis, urothelia within one day (2 doses) of oral dosing of rats with a combination of 8 mg/kg rosiglitazone and 200 mg/kg fenofibrate (specific PPAR gamma and PPAR alpha agonists, respectively)." | ( PPAR alpha and PPAR gamma coactivation rapidly induces Egr-1 in the nuclei of the dorsal and ventral urinary bladder and kidney pelvis urothelium of rats. Bartels, A; Brünner, N; Egerod, FL; Hinley, J; Oleksiewicz, MB; Southgate, J; Svendsen, JE, 2009) | 0.55 |
| " According to the linear relationship between the peak current and the concentration, differential pulse and square wave voltammetric methods for rosiglitazone assay in pharmaceutical dosage forms and biological fluids were developed." | ( Anodic voltammetric behavior and determination of rosiglitazone in pharmaceutical dosage forms and biological fluids on solid electrode. Dogan-Topal, B; Ozkan, SA; Tuncel, S, 2010) | 0.81 |
| " Translation of these findings into clinical therapy will require careful assessment of dosing paradigms and effective time windows for treatment." | ( Extension of the neuroprotective time window for thiazolidinediones in ischemic stroke is dependent on time of reperfusion. Blankenship, DA; Gamboa, J; Hilow, E; Karl, M; Landreth, GE; Niemi, JP; Sundararajan, S, 2010) | 0.36 |
| " Heart weight was increased 10% after 7 days and 16% after 14 days of dosing at 80 mg/kg/day in the absence of microscopic changes." | ( Serum cardiac troponin I concentrations transiently increase in rats given rosiglitazone. Bachynsky, MO; Berkofsky-Fessler, W; Boyle, BW; Buness, A; Coluccio, D; Dick, LS; Dunn, M; Fernandes, R; Geng, W; Giron, M; Hilton, H; Hirkaler, G; Hoflack, JC; Kanwal, C; Mikaelian, I; Nicklaus, R; Sanders, M; Singer, T; Visalli, T, 2011) | 0.6 |
| "0%), even at maximal dosage levels of one or two oral agents, and are at increased risk for diabetes-related complications." | ( Cost-effectiveness of liraglutide versus rosiglitazone, both in combination with glimepiride in treatment of type 2 diabetes in the US. Conner, C; Hammer, M; Lee, WC, 2011) | 0.64 |
| " After establishing a dose-response curve for each drug, the drugs were orally administered for 3 weeks either alone or in combination." | ( Synergistic improvement in insulin resistance with a combination of fenofibrate and rosiglitazone in obese type 2 diabetic mice. Choi, WS; Kim, IS; Kim, Y; Lee, JJ; Myung, CS; Zhang, WY, 2011) | 0.59 |
| " Phenylephrine, ACh, and SNP dose-response curves were impaired to different extents in arteries of SHROBs." | ( Reactivity of the aorta and mesenteric resistance arteries from the obese spontaneously hypertensive rat: effects of glitazones. Llorens, S; Mendizábal, Y; Nava, E, 2011) | 0.37 |
| " Four weeks of dosing resulted in decreased plasma triglycerides and reduced hepatic fat deposition." | ( Discovery and characterization of an inhibitor of glucosylceramide synthase. Aay, N; Aoyama, R; Arcalas, A; Bentzien, F; Cancilla, B; Chan, V; Du, H; Finn, P; Galan, A; Hanel, A; Harrison, A; Kearney, P; Koltun, ES; Lamb, P; Larson, CJ; Mohan, R; Nachtigall, J; Nuss, J; Ogilvie, K; Plonowski, A; Qian, F; Richards, S; Rosen, J; Tam, D; Wang, T; Won, KA; Yakes, M; Zhang, J; Zhang, W, 2012) | 0.38 |
| " A probe of CYP2C8 that is easy to administer and interpret may be valuable for individualized dosing of paclitaxel." | ( Pilot study of rosiglitazone as an in vivo probe of paclitaxel exposure. Bridges, AS; Dees, EC; Herendeen, J; Hertz, DL; Hull, JH; Rollins, K; Walko, CM; Watkins, PB, 2012) | 0.73 |
| " The finding, that a single rosiglitazone plasma concentration after oral dosing may explain significant variance in paclitaxel exposure, suggests that rosiglitazone may satisfy the requirements of a clinically useful in vivo probe." | ( Pilot study of rosiglitazone as an in vivo probe of paclitaxel exposure. Bridges, AS; Dees, EC; Herendeen, J; Hertz, DL; Hull, JH; Rollins, K; Walko, CM; Watkins, PB, 2012) | 1.03 |
| " Patients were on a stable dosage of TZD (rosiglitazone or pioglitazone) and, if applicable, metformin." | ( Safety of exenatide once weekly in patients with type 2 diabetes mellitus treated with a thiazolidinedione alone or in combination with metformin for 2 years. Boardman, MK; Haber, H; Liutkus, JF; Norwood, P; Pintilei, E; Trautmann, ME, 2012) | 0.64 |
| "020) with less daily insulin dosage and was more powerful in lowering total cholesterol, increasing AIR and HOMA β-cell function, whereas reduction of IMCL in the soleus was more obvious in the rosiglitazone group but not in the metformin group." | ( Short-term continuous subcutaneous insulin infusion combined with insulin sensitizers rosiglitazone, metformin, or antioxidant α-lipoic acid in patients with newly diagnosed type 2 diabetes mellitus. Chen, A; Deng, W; Fang, D; Huang, Z; Li, H; Li, Y; Liu, J; Liu, L; Wan, X; Wei, G, 2013) | 0.8 |
| " Dose-response effects were evaluated by comparing the incidence rates among patients with different cumulative exposures to TZD." | ( Risk of stroke with thiazolidinediones: a ten-year nationwide population-based cohort study. Chen, PC; Chen, RC; Hsu, CY; Lu, CJ; Muo, CH; Sun, Y, 2013) | 0.39 |
| " The results also showed a significant dose-dependent effect of higher risk of ischemic stroke with increasing dosage of rosiglitazone, while there was no increased risk at any level of pioglitazone dosage." | ( Risk of stroke with thiazolidinediones: a ten-year nationwide population-based cohort study. Chen, PC; Chen, RC; Hsu, CY; Lu, CJ; Muo, CH; Sun, Y, 2013) | 0.6 |
| " However, since the inhibition of transporter is not specific to cancer cells, a decrease in the cytotoxic drug dosing may be needed to prevent excess toxicity, thus undermining the potential benefit brought about by a drug efflux inhibitor." | ( Targeting the ABCG2-overexpressing multidrug resistant (MDR) cancer cells by PPARγ agonists. To, KK; Tomlinson, B, 2013) | 0.39 |
| " Colesevelam (3750mg once daily) was dosed throughout the pharmacokinetic sampling period." | ( Lack of effect of colesevelam HCl on the single-dose pharmacokinetics of aspirin, atenolol, enalapril, phenytoin, rosiglitazone, and sitagliptin. He, L; Lee, J; Mendell-Harary, J; Tao, B; Walker, J; Wickremasingha, P; Wight, D, 2014) | 0.61 |
| " When orally dosed in C57/BL6 diet-induced obesity (DIO) mice, HSD-621 was efficacious and showed a significant reduction in both fed and fasting glucose and insulin levels." | ( Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes. Bard, J; Chenail, E; Hahm, S; Ipek, M; Johnson, CE; Li, HQ; Li, X; Mansour, TS; Panza, D; Perreault, M; Qadri, A; Saiah, E; Suri, V; Svenson, K; Tian, X; Tobin, JF; Wan, ZK; Wang, M; Xiang, J; Xu, X, 2013) | 0.39 |
| " In the spinal cord, catalase protection was showed by the lower rosiglitazone dosage without effect on the astrocyte density increase induced by oxaliplatin." | ( Oxaliplatin neurotoxicity involves peroxisome alterations. PPARγ agonism as preventive pharmacological approach. Cinci, L; Di Cesare Mannelli, L; Failli, P; Ghelardini, C; Micheli, L; Zanardelli, M, 2014) | 0.64 |
| " The preclinical ADME properties of LY2562175 were consistent with enabling once daily dosing in humans, and it was ultimately advanced to the clinic for evaluation in humans." | ( 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. Agejas Francisco, J; Bocchinfuso, WP; Bueno, AB; Cannady, EA; Cox, A; Genin, MJ; Jones, TM; Manninen, PR; Michael, LF; Michael, MD; Montrose-Rafizadeh, C; Raddad, E; Reidy, C; Stille, JR, 2015) | 0.42 |
| " Further study using an alternative dosage paradigm and more sensitive behavioral testing may be warranted." | ( Rosiglitazone attenuates inflammation and CA3 neuronal loss following traumatic brain injury in rats. Culver, S; Dixon, CE; Graham, SH; Liu, H; Ma, X; Rose, ME, 2016) | 1.88 |
| " Duration-response and dose-response relations were observed for pioglitazone but not for rosiglitazone." | ( Pioglitazone use and risk of bladder cancer: population based cohort study. Azoulay, L; Filion, KB; Platt, RW; Tuccori, M; Yin, H; Yu, OH, 2016) | 0.66 |
| " Generalized concentration addition (GCA) is one such method for predicting joint effects of coexposures to chemicals and has the advantage of allowing for mixture components to have differences in efficacy (ie, dose-response curve maxima)." | ( Generalized Concentration Addition Modeling Predicts Mixture Effects of Environmental PPARγ Agonists. Schlezinger, JJ; Watt, J; Webster, TF, 2016) | 0.43 |
| " Incidences for ever users, never users and subgroups of rosiglitazone dose-response parameters (tertile cutoffs of cumulative duration and cumulative dose) were calculated and hazard ratios estimated by Cox regression." | ( Rosiglitazone reduces breast cancer risk in Taiwanese female patients with type 2 diabetes mellitus. Tseng, CH, 2017) | 2.14 |
| " To examine clinically relevant effects of the potential interaction with SCY-078, this phase 1, open-label, 2-period crossover study evaluated the pharmacokinetic parameters of rosiglitazone, a sensitive substrate of CYP2C8 metabolism, in the absence and presence of SCY-078 dosed to therapeutically relevant SCY-078 concentration exposure after repeat dosing." | ( Lack of Impact by SCY-078, a First-in-Class Oral Fungicidal Glucan Synthase Inhibitor, on the Pharmacokinetics of Rosiglitazone, a Substrate for CYP450 2C8, Supports the Low Risk for Clinically Relevant Metabolic Drug-Drug Interactions. Angulo, D; Atiee, G; Corr, C; Hyman, M; Murphy, G; Willett, M; Wring, S, 2018) | 0.88 |
| " The dose-response relationship studies suggested that the pan agonist 15 suppressed the excursion of blood glucose levels in a dose-dependent manner." | ( Design, synthesis, and biological evaluation of novel pan agonists of FFA1, PPARγ and PPARδ. Deng, F; Li, Y; Li, Z; Zhang, D; Zhang, L; Zhou, Z, 2018) | 0.48 |
| " Compared with the plain drugs, given via the pulmonary or oral route as a single or dual combination, PLGA particles of the drugs, although given at a longer dosing interval compared with the plain drugs, caused more pronounced reduction in mPAP without affecting mean systemic pressure, improved cardiac function, slowed down right heart remodeling, and reduced arterial muscularization." | ( Inhaled combination of sildenafil and rosiglitazone improves pulmonary hemodynamics, cardiac function, and arterial remodeling. Ahsan, F; McMurtry, IF; Nozik-Grayck, E; Rashid, J; Stenmark, KR, 2019) | 0.78 |
| "A sensitive, rapid and cost-effective method based on HPTLC with UV detection was developed for the quantitation of Glibenclamide (GLIBEN), Rosiglitazone maleate (ROSI) and Metformin hydrochloride (MET) from a combined dosage form." | ( A Sensitive HPTLC Method for the Estimation of Glibenclamide, Rosiglitazone Maleate and Metformin Hydrochloride from a Multicomponent Dosage Form. Abbulu, K; Bhende, SD; Varanasi, MB, 2020) | 1 |
| 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) |
|---|---|---|---|---|---|---|---|
| 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] | |||||||
| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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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] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (60.41) All Compounds (24.57) |
| 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] | ||
| 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] | |||||||