rosiglitazone [Ligand Id: 1056] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL121 (Avandamet, Avandaryl, Avandia, BRL-49653, Gaudil, NSC-758698, Rezult, Rosiglitazone, Rosiglizole, Rosvel, TDZ-01) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] | ||||||||
| ChEMBL | 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 | B | 5.29 | pIC50 | 5100 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126623-126623 [PMID:31439379] |
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 5.19 | pIC50 | 6400 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
| ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.4 | pIC50 | 40000 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA)) | B | 5.39 | pIC50 | 4069 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| carnitine palmitoyltransferase 1A/Carnitine O-palmitoyltransferase 1, liver isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293194] [GtoPdb: 3249] [UniProtKB: P50416] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, liver isoform | B | 5 | pIC50 | >10000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, muscle isoform | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3238] [GtoPdb: 3252] [UniProtKB: P23786] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4037] [GtoPdb: 3252] [UniProtKB: P18886] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
| ChEMBL | 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 | B | 7.51 | pKi | 31 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| ChEMBL | 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 | B | 6.14 | pIC50 | 731 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| CDGSH iron-sulfur domain-containing protein 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308979] [UniProtKB: B0K020] | ||||||||
| ChEMBL | Displacement of [3H]rosiglitazone from rat liver mitochondrial mitoNEET by scintillation counting | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 819-823 [PMID:20064719] |
| CDGSH iron-sulfur domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523399] [UniProtKB: Q8N5K1] | ||||||||
| ChEMBL | Binding affinity to recombinant human N-terminal His6-tagged NAF1 expressed in Escherichia coli by scintillation proximity assay | B | 5.64 | pIC50 | 2290 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 901-904 [PMID:30770154] |
| FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] | ||||||||
| ChEMBL | Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation | B | 4.94 | pEC50 | 11481.54 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5330-5336 [PMID:25441945] |
| GtoPdb | - | - | 5.6 | pEC50 | - | - | - | Biochem Biophys Res Commun (2003) 301: 406-10 [PMID:12565875] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells by patch clamp assay | B | 4.53 | pIC50 | 29500 | nM | IC50 | Eur J Med Chem (2019) 162: 650-665 [PMID:30481687] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Competitive inhibition of human MAOA expressed in Pichia pastoris | B | 4.56 | pKi | 27600 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
| ChEMBL | Competitive inhibition of rat MAOA expressed in Pichia pastoris | B | 4.49 | pKi | 32600 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Competitive inhibition of human MAOB expressed in Pichia pastoris | B | 5.38 | pKi | 4200 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| ChEMBL | Inhibition of human recombinant MAO-B after 15 mins | B | 6.08 | pIC50 | 832 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5295-5298 [PMID:20650633] |
| Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | Competitive inhibition of rat MAOB expressed in Pichia pastoris | B | 5.24 | pKi | 5800 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | In vitro binding affinity towards human peroxisome proliferator activated receptor alpha (PPAR alpha) | B | 4.48 | pKi | >33300 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 931-935 [PMID:12617924] |
| ChEMBL | Inhibition of human Peroxisome proliferator activated receptor alpha | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2005) 48: 2248-2250 [PMID:15771468] |
| ChEMBL | Inhibition of human Peroxisome proliferator activated receptor alpha binding | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2005) 48: 2262-2265 [PMID:15801817] |
| ChEMBL | In vitro binding affinity against human PPAR alpha (peroxisome proliferator-activated alpha receptor) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | In vitro binding affinity against human Peroxisome proliferator activated receptor alpha | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | Inhibition of human PPARalpha receptor by scintillation proximity assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2009) 52: 4443-4453 [PMID:19530681] |
| ChEMBL | Displacement of [3H2]nTZD3 from human recombinant GST-fused PPARalpha expressed in Escherichia coli by scintillation proximity assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2009) 52: 3846-3854 [PMID:19507861] |
| ChEMBL | Displacement of [3H2]nTZD3 from GST-tagged human recombinant PPARalpha by scintillation proximity assay | B | 4.82 | pIC50 | >15000 | nM | IC50 | J Med Chem (2009) 52: 4631-4639 [PMID:19719236] |
| ChEMBL | In vitro binding affinity for human peroxisome proliferator activated receptor alpha using scintillation proximity assay (SPA) | B | 4.82 | pIC50 | >15000 | nM | IC50 | J Med Chem (2004) 47: 3255-3263 [PMID:15163205] |
| ChEMBL | Inhibition of PPARalpha | B | 4.82 | pIC50 | >15000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645] |
| ChEMBL | Mean inhibitory concentration against human peroxisome proliferator activated receptor alpha | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409] |
| ChEMBL | Displacement of tritium labeled ligand from human PPARalpha by SPA assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393] |
| ChEMBL | Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from hPPARalpha | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394] |
| ChEMBL | Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARalpha | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6744-6749 [PMID:18029178] |
| ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | 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 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Displacement of [3H]L-783483 from human PPAR alpha by SPA assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 1212-1216 [PMID:16451087] |
| ChEMBL | Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | In vitro binding affinity for human PPAR alpha in SPA | B | 8.3 | pIC50 | >5 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Effective concentration against human Peroxisome proliferator activated receptor alpha | B | 4.49 | pEC50 | >32000 | nM | EC50 | J Med Chem (2005) 48: 2248-2250 [PMID:15771468] |
| ChEMBL | Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay | F | 4.92 | pEC50 | >12000 | nM | EC50 | Bioorg Med Chem (2009) 17: 7113-7125 [PMID:19783444] |
| ChEMBL | Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay | F | 4.92 | pEC50 | >12000 | nM | EC50 | Bioorg Med Chem (2008) 16: 4883-4907 [PMID:18394907] |
| ChEMBL | Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay | F | 4.98 | pEC50 | 10580 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2605-2608 [PMID:20299214] |
| ChEMBL | Effective concentration against human Peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2005) 48: 2262-2265 [PMID:15801817] |
| ChEMBL | Agonist activity at human PPARalpha by luciferase reporter transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay | B | 5 | pEC50 | 10000 | nM | EC50 | Eur J Med Chem (2017) 137: 310-326 [PMID:28609708] |
| ChEMBL | Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 240-244 [PMID:21112784] |
| ChEMBL | Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6120-6123 [PMID:16973358] |
| ChEMBL | Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6116-6119 [PMID:16979341] |
| ChEMBL | Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2007) 50: 1495-1503 [PMID:17343371] |
| ChEMBL | Agonist activity at human PPARalpha by transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4144-4149 [PMID:17553681] |
| ChEMBL | Agonist activity at human PPARalpha by transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4625-4629 [PMID:17560785] |
| ChEMBL | Agonist activity at human PPARalpha by GAL4 transactivation assay | F | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1617-1622 [PMID:18255290] |
| ChEMBL | Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1581-1584 [PMID:20138762] |
| ChEMBL | Agonist activity at human PPARalpha receptor by cell based transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2009) 52: 2618-2622 [PMID:19301897] |
| ChEMBL | 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 | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963] |
| ChEMBL | In vitro effective concentration against human peroxisome proliferator activated receptor alpha/Gal4 in transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4421-4426 [PMID:16137885] |
| ChEMBL | Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay | F | 5.3 | pEC50 | >5000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645] |
| ChEMBL | Agonist activity at human PPARalpha by transactivation assay | F | 5.39 | pEC50 | 4100 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3198-3202 [PMID:17379517] |
| ChEMBL | In vitro activation of human peroxisome proliferator activated receptor alpha | B | 5.39 | pEC50 | 4100 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR alpha | F | 5.39 | pEC50 | 4100 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | Effective concentration for human peroxisome proliferator-activated receptor alpha | B | 5.39 | pEC50 | 4100 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1497-1500 [PMID:15713415] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha) | B | 5.39 | pEC50 | 4100 | nM | EC50 | J Med Chem (2003) 46: 4883-4894 [PMID:14584939] |
| ChEMBL | Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay | B | 5.46 | pEC50 | 3460 | nM | EC50 | J Med Chem (2008) 51: 6318-6333 [PMID:18826205] |
| ChEMBL | 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 | F | 5.46 | pEC50 | 3460 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 4993-4996 [PMID:18771917] |
| ChEMBL | Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs | F | 5.46 | pEC50 | 3460 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3595-3598 [PMID:17507225] |
| ChEMBL | Agonist activity at human PPARalpha transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 5.47 | pEC50 | 3390 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay | F | 5.52 | pEC50 | >3000 | nM | EC50 | J Med Chem (2009) 52: 4443-4453 [PMID:19530681] |
| ChEMBL | Displacement of radiolabeled GW-2331 from human PPAR alpha by SPA binding assay | B | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6120-6123 [PMID:16973358] |
| ChEMBL | In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | 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 | B | 6 | pEC50 | >1000 | nM | EC50 | Bioorg Med Chem (2011) 19: 6982-6988 [PMID:22051054] |
| ChEMBL | 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 | B | 6.62 | pEC50 | 240 | nM | EC50 | Eur J Med Chem (2016) 109: 157-172 [PMID:26774923] |
| ChEMBL | Effective concentration for human peroxisome proliferator-activated receptor gamma | B | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1497-1500 [PMID:15713415] |
| ChEMBL | In vitro transcription activation on human peroxisome proliferator activated receptor-alpha (PPAR alpha) | B | 6.85 | pEC50 | 140 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3507-3511 [PMID:15177462] |
| ChEMBL | Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | Bioorg Med Chem (2008) 16: 9498-9510 [PMID:18835719] |
| ChEMBL | Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,643 | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1617-1622 [PMID:18255290] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Activation of mouse liver PPARalpha | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay | F | 5.52 | pEC50 | >3000 | nM | EC50 | J Med Chem (2009) 52: 4443-4453 [PMID:19530681] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | In vitro binding affinity towards human peroxisome proliferator activated receptor delta (PPAR delta) | B | 4.48 | pKi | >33300 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 931-935 [PMID:12617924] |
| ChEMBL | In vitro binding affinity against human Peroxisome proliferator activated receptor delta | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro binding affinity against human PPAR delta (peroxisome proliferator-activated delta receptor) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | In vitro binding affinity for human Peroxisome proliferator activated receptor gamma using scintillation proximity assay (SPA) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2004) 47: 3255-3263 [PMID:15163205] |
| ChEMBL | Displacement of [3H]2-(4-{2-[3-(2,4-difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-butyric acid from human PPARdelta | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6744-6749 [PMID:18029178] |
| ChEMBL | In vitro binding affinity for human PPAR delta in SPA | B | 8.3 | pIC50 | >5 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | 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 | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963] |
| ChEMBL | Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 240-244 [PMID:21112784] |
| ChEMBL | Agonist activity at human PPARdelta receptor by cell based transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2009) 52: 2618-2622 [PMID:19301897] |
| ChEMBL | Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 5.05 | pEC50 | 8890 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Kinase Activity Assay: After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the supernatant was collected. The supernatant was reacted with a fluorescence assay kit (Promega) and counted by a fluorometer (Ascent Fluoroskan FL reader, Thermo Labsystems, Finland), and the relative intensity of luciferase was determined. For the assay of the β-galactosidase activity used in the experiment as the internal reference (the internal reference for calibrating the transfection efficiency), 50 μl of the supernatant was transferred into a fresh microplate, treated with a Promega kit, and the value was read with a microplate reader at a wavelength of 405 nm (Bio-tech Instruments Inc., Winooski, Vt., USA) (Sauerberg, P.; Olsen, G. S.; Jeppesen, L.; Mogensen, J. P. et al., J. Med. Chem., 2007, 50, 1495-1503). | B | 5.28 | pEC50 | 5248 | nM | EC50 | US-9346770-B2. Compounds having activating effect on subtypes of peroxisome proliferator-activated receptors and its preparation method and uses (2016) |
| ChEMBL | In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta) | B | 5.44 | pEC50 | 3620 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3507-3511 [PMID:15177462] |
| ChEMBL | In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis | B | 6 | pEC50 | >1000 | nM | EC50 | Bioorg Med Chem (2011) 19: 6982-6988 [PMID:22051054] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Binding affinity to human PPARgamma | B | 5.3 | pKd | 4980 | nM | Kd | Bioorg Med Chem Lett (2006) 16: 5913-5916 [PMID:17010604] |
| ChEMBL | Binding affinity to PPARgamma ligand binding domain by isothermal titration calorimetry | B | 6.92 | pKd | 120 | nM | Kd | J Med Chem (2012) 55: 37-54 [PMID:22081932] |
| ChEMBL | Binding affinity to PPARg (unknown origin) by SPR assay | B | 7.32 | pKd | 47.6 | nM | Kd | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| GtoPdb | - | - | 7.4 | pKd | - | - | - |
J Med Chem (1998) 41: 5020-36 [PMID:9836620]; J Biol Chem (1997) 272: 3406-10 [PMID:9013583]; J Pharmacol Exp Ther (1998) 284: 751-9 [PMID:9454824] |
| ChEMBL | Agonist activity at histidine-tagged PPARgamma ligand binding domain by cell free-coactivator recruitment assay | B | 7.83 | pKd | 14.8 | nM | Kd | J Biol Chem (2007) 282: 17314-17324 [PMID:17403688] |
| ChEMBL | Binding affinity to human PPARgamma (unknown origin) by competitive TR-FRET assay | B | 8.15 | pKd | 7 | nM | Kd | J Med Chem (2013) 56: 1535-1543 [PMID:23286787] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) assessed as thermodynamic dissociation constant by SPR assay | B | 8.92 | pKd | 1.2 | nM | Kd | Eur J Med Chem (2017) 127: 379-397 [PMID:28076827] |
| ChEMBL | Displacement of radiolabeled darglitazone from human PPAR gamma by SPA binding assay | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 6120-6123 [PMID:16973358] |
| ChEMBL | Displacement of radiolabeled darglitazone from human PPAR gamma by SPA assay | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 6116-6119 [PMID:16979341] |
| ChEMBL | In vitro binding affinity towards human peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 6.87 | pKi | 136 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 931-935 [PMID:12617924] |
| GtoPdb | - | - | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | 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 | B | 7.13 | pKi | 74 | nM | Ki | J Med Chem (2012) 55: 37-54 [PMID:22081932] |
| ChEMBL | Displacement of [3H]rosiglitazone from histidine-tagged PPARgamma ligand binding domain by scintillation proximity assay | B | 7.13 | pKi | 74 | nM | Ki | J Biol Chem (2007) 282: 17314-17324 [PMID:17403688] |
| ChEMBL | 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 | B | 7.23 | pKi | 59 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126664-126664 [PMID:31591015] |
| ChEMBL | Binding affinity for human peroxisome proliferator activated receptor gamma | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Binding affinity was determined by displacement of 20 nM [3H]- thiazolidinedione from 4 nM biotinylated human peroxisome proliferator-activated receptor (PPAR gamma) ligand binding domain | B | 7.31 | pKi | 49 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2491-2496 |
| ChEMBL | In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) | B | 7.33 | pKi | 46.77 | nM | Ki | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 7.33 | pKi | 46.77 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3329-3334 [PMID:10612594] |
| ChEMBL | Agonist activity at PPARgamma ligand binding domain (unknown origin) using fluormone Pan-PPAR green tracer by TR-FRET assay based competitive ligand binding method | B | 7.57 | pKi | 27.11 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 2579-2583 [PMID:25978962] |
| ChEMBL | Binding affinity to GST-tagged PPARG LBD (unknown origin) by Fluormone Pan-PPAR Green tracer based TR-FRET assay | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2021) 64: 1018-1036 [PMID:33423463] |
| ChEMBL | Displacement of [3H]-rosiglitazone from GST-tagged PPARgammaLBD (unknown origin) after 1 hr by scintillation proximity assay | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem (2013) 21: 979-992 [PMID:23294830] |
| ChEMBL | Displacement of [3H]Rosiglitazone from human PPARgamma | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1617-1622 [PMID:18255290] |
| ChEMBL | Binding affinity for human PPAR gamma construct expressed in bacteria with 3[H] rosiglitazone | B | 8.1 | pKi | 8 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4421-4426 [PMID:16137885] |
| ChEMBL | Binding affinity to human PPARgamma receptor by radioligand displacement assay | B | 8.24 | pKi | 5.8 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | 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 | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2776-2780 [PMID:28465099] |
| ChEMBL | Inhibition of PPARgamma (unknown origin) phosphorylation at pS273 residue | B | 5.36 | pIC50 | 4400 | nM | IC50 | ACS Med Chem Lett (2022) 13: 681-686 [PMID:35450368] |
| ChEMBL | 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 | B | 6.35 | pIC50 | 450 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | Displacement of fluormone-PPARgamma green from GST-tagged PPARgamma-LBD (unknown origin) by fluorescence polarization assay | B | 6.53 | pIC50 | 298 | nM | IC50 | Bioorg Med Chem (2017) 25: 4723-4744 [PMID:28720328] |
| ChEMBL | Displacement of fluormone-PPARgamma Green from recombinant human N-terminal GST-tagged PPARgamma-LBD by fluorescence polarization assay | B | 6.53 | pIC50 | 292 | nM | IC50 | Bioorg Med Chem (2017) 25: 1496-1513 [PMID:28117121] |
| ChEMBL | Displacement of [3H]darglitazone from human PPARgamma by scintillation proximity assay | B | 6.56 | pIC50 | 274 | nM | IC50 | Bioorg Med Chem (2008) 16: 4883-4907 [PMID:18394907] |
| ChEMBL | Displacement of [3H2]nTZD3 from GST-tagged human PPARgamma expressed in Escherichia coli by SPA | B | 6.56 | pIC50 | 274 | nM | IC50 | Bioorg Med Chem (2009) 17: 7113-7125 [PMID:19783444] |
| ChEMBL | Agonist activity at N-terminal His-tagged human PPARgamma ligand binding domain by fluorescence polarization assay | B | 6.57 | pIC50 | 267 | nM | IC50 | Eur J Med Chem (2010) 45: 193-202 [PMID:19879669] |
| ChEMBL | Displacement of fluorescein labeled ligand from PPARgamma receptor by fluorescence polarization assay | B | 6.59 | pIC50 | 256 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606] |
| ChEMBL | In vitro binding affinity against human PPAR gamma (peroxisome proliferator-activated gamma receptor) | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | In vitro binding affinity against human peroxisome proliferator activated receptor gamma | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | Inhibition of human peroxisome proliferator activated receptor gamma binding | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2437-2440 [PMID:15863293] |
| ChEMBL | Inhibition of human Peroxisome proliferator activated receptor gamma binding | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2005) 48: 2262-2265 [PMID:15801817] |
| ChEMBL | Inhibition of human Peroxisome proliferator activated receptor gamma | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2005) 48: 2248-2250 [PMID:15771468] |
| ChEMBL | Displacement of [3H2]nTZD3 from GST-tagged human recombinant PPARgamma by scintillation proximity assay | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2009) 52: 4631-4639 [PMID:19719236] |
| ChEMBL | Inhibitory concentration against human peroxisome proliferator activated receptor gamma in SPA assay | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5035-5038 [PMID:16153845] |
| ChEMBL | In vitro binding affinity for human PPAR gamma in SPA | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | Displacement of [3H]-rosiglitazone from GST-tagged PPARgammaLBD (unknown origin) after 1 hr by scintillation proximity assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2013) 21: 979-992 [PMID:23294830] |
| ChEMBL | Inhibition of human PPARgamma receptor by scintillation proximity assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2009) 52: 4443-4453 [PMID:19530681] |
| ChEMBL | In vitro binding affinity for human PPAR gamma receptor using scintillation proximity assay (SPA) | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2004) 47: 3255-3263 [PMID:15163205] |
| ChEMBL | Displacement of [3H2]nTZD3 from human recombinant GST-fused PPARgamma expressed in Escherichia coli by scintillation proximity assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2009) 52: 3846-3854 [PMID:19507861] |
| ChEMBL | Displacement of fluormone PPAR-green from N-terminal His-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay | B | 6.7 | pIC50 | 199 | nM | IC50 | Bioorg Med Chem (2010) 18: 8315-8323 [PMID:21030263] |
| ChEMBL | Displacement of fluormone from human PPARgamma LBD expressed in Escherichia coli BL21 DE3 by fluorescence polarization assay | B | 6.8 | pIC50 | 159 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5795-5802 [PMID:24075729] |
| ChEMBL | 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 | B | 6.95 | pIC50 | 112 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| ChEMBL | Inhibition of fluormone PPARgamma Green binding to recombinant N-terminal GST-tagged human PPARgamma LBD by fluorescence polarization assay | B | 6.99 | pIC50 | 103 | nM | IC50 | Eur J Med Chem (2017) 138: 830-853 [PMID:28735214] |
| ChEMBL | Displacement of [3H]rosiglitazone from human PPAR gamma by SPA assay | B | 7.04 | pIC50 | 92 | nM | IC50 | J Med Chem (2005) 48: 8194-8208 [PMID:16366601] |
| ChEMBL | Displacement of [3H]rosiglitazone from human PPAR gamma by SPA assay | B | 7.04 | pIC50 | 92 | nM | IC50 | J Med Chem (2006) 49: 1212-1216 [PMID:16451087] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) by lanthascreen TR-FRET assay | B | 7.05 | pIC50 | 90 | nM | IC50 | ACS Med Chem Lett (2022) 13: 681-686 [PMID:35450368] |
| ChEMBL | Displacement of Fluormone from PPAR gamma | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5659-5663 [PMID:16919947] |
| ChEMBL | 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 | B | 7.05 | pIC50 | 88.4 | nM | IC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | 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 | B | 7.12 | pIC50 | 76 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126664-126664 [PMID:31591015] |
| ChEMBL | Agonist activity at PPARgamma ligand binding domain (unknown origin) using fluormone Pan-PPAR green tracer by TR-FRET assay based competitive ligand binding method | B | 7.12 | pIC50 | 75.52 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2579-2583 [PMID:25978962] |
| ChEMBL | Mean inhibitory concentration against human peroxisome proliferator-activated receptor gamma | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409] |
| ChEMBL | 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 | B | 7.17 | pIC50 | 67 | nM | IC50 | J Med Chem (2006) 49: 5649-5652 [PMID:16970391] |
| ChEMBL | Displacement of [3H]2-methyl-2-(4-{3-propyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-pro-pyl}-phenoxy)-propionic acid from human PPARgamma | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394] |
| ChEMBL | Displacement of [3H]2-methyl-2-(4-{3-{propyl-(5-pyridin-2-yl-thiophene-2-sulfonyl)-amino}-propyl}-phenoxy)-propionic acid from human PPARgamma | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6744-6749 [PMID:18029178] |
| ChEMBL | Displacement of [3H]2-methyl-2-(4-{3-[porpyl-(5-pyridin-2yl-thiophene-2-sulfonyl)-amino]-propyl}-phenoxy)-propionic acid from human PPARgamma | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1052-1055 [PMID:17129725] |
| ChEMBL | Displacement of tritium labeled ligand from human PPARgamma by SPA assay | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393] |
| ChEMBL | Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma) | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | Inhibition of PPARgamma | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645] |
| ChEMBL | Binding affinity to GST-tagged human PPAR-gamma receptor by FRET assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2016) 108: 423-435 [PMID:26708109] |
| ChEMBL | Binding affinity to human PPARgamma receptor by radioligand displacement assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| ChEMBL | Binding affinity to human PPARgamma receptor by radioligand displacement assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]rosiglitazone from human recombinant PPAR-gamma receptor expressed in Escherichia coli measured after 120 mins by scintillation counting method | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Displacement of [3H]rosiglitazone from human recombinant PPARgamma receptor expressed in Escherichia coli | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | 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 | B | 8.11 | pIC50 | 7.7 | nM | IC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay | F | 2 | pEC50 | 10000000 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 3324-3327 [PMID:19423341] |
| ChEMBL | 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 | B | 4.36 | pEC50 | 43710 | nM | EC50 | Bioorg Med Chem (2013) 21: 766-778 [PMID:23265844] |
| ChEMBL | Agonist activity at human PPARgamma assessed as luciferase activity by transactivation assay | F | 4.36 | pEC50 | 43710 | nM | EC50 | J Med Chem (2009) 52: 6835-6850 [PMID:19807106] |
| ChEMBL | In vitro transcription activation on human peroxisome proliferator activated receptor-gamma (PPAR gamma) | B | 5.54 | pEC50 | 2880 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3507-3511 [PMID:15177462] |
| ChEMBL | 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 | F | 6.05 | pEC50 | 900 | nM | EC50 | J Nat Prod (2012) 75: 2076-2081 [PMID:23186307] |
| ChEMBL | Binding affinity at human PPAR gamma | B | 6.18 | pEC50 | 657 | nM | EC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | Displacement of tritium labeled ligand from human PPARgamma by SPA assay | B | 6.18 | pEC50 | 657 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6293-6297 [PMID:17005393] |
| ChEMBL | 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 | B | 6.32 | pEC50 | 480.6 | nM | EC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay | F | 6.35 | pEC50 | 450 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2468-2473 [PMID:19349176] |
| ChEMBL | Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay | B | 6.4 | pEC50 | 396 | nM | EC50 | Bioorg Med Chem (2018) 26: 5079-5098 [PMID:30241907] |
| ChEMBL | Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay | B | 6.4 | pEC50 | 396 | nM | EC50 | Bioorg Med Chem (2018) 26: 5099-5117 [PMID:30220602] |
| ChEMBL | Agonist activity at human PPARgamma LBD by cell based luciferase reporter gene assay | F | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
| ChEMBL | 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 | B | 6.48 | pEC50 | 332 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | 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 | B | 6.49 | pEC50 | 326 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay | F | 6.49 | pEC50 | 320 | nM | EC50 | J Med Chem (2006) 49: 4781-4784 [PMID:16854085] |
| ChEMBL | Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay | F | 6.49 | pEC50 | 320 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 5239-5244 [PMID:17624777] |
| ChEMBL | 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 | B | 6.5 | pEC50 | 316 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay | B | 6.51 | pEC50 | 310 | nM | EC50 | J Med Chem (2007) 50: 1495-1503 [PMID:17343371] |
| ChEMBL | Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay | F | 6.51 | pEC50 | 308 | nM | EC50 | J Med Chem (2006) 49: 5649-5652 [PMID:16970391] |
| ChEMBL | Activity at human PPARgamma in CV1 cells | B | 6.51 | pEC50 | 308 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6328-6333 [PMID:17005394] |
| ChEMBL | Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay | F | 6.51 | pEC50 | 308 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6744-6749 [PMID:18029178] |
| ChEMBL | Agonist activity at PPARgamma in CV1 cells by transactivation assay | F | 6.51 | pEC50 | 308 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 1052-1055 [PMID:17129725] |
| ChEMBL | Agonist activity at human PPARgamma by transactivation assay | F | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4144-4149 [PMID:17553681] |
| ChEMBL | Agonist activity at human PPARgamma by transactivation assay | F | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4625-4629 [PMID:17560785] |
| ChEMBL | 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 | B | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218] |
| ChEMBL | 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 | B | 6.53 | pEC50 | 296.9 | nM | EC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | 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 | B | 6.55 | pEC50 | 280 | nM | EC50 | J Med Chem (2020) 63: 2854-2876 [PMID:32096640] |
| ChEMBL | Mean effective concentration against human peroxisome proliferator-activated receptor gamma | B | 6.57 | pEC50 | 268 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 51-55 [PMID:15582409] |
| ChEMBL | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem (2016) 24: 5258-5269 [PMID:27591006] |
| ChEMBL | Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem (2016) 24: 5455-5461 [PMID:27622746] |
| ChEMBL | Transactivation of recombinant human N-terminal GAL4-DBD fused PPARgamma LBD expressed in reporter cells measured after 24 hrs by luciferase reporter gene assay | B | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 1595-1602 [PMID:29615345] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay | F | 6.65 | pEC50 | 223 | nM | EC50 | Bioorg Med Chem (2008) 16: 4883-4907 [PMID:18394907] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay | F | 6.65 | pEC50 | 223 | nM | EC50 | Bioorg Med Chem (2009) 17: 7113-7125 [PMID:19783444] |
| ChEMBL | Functional activity at human PPAR gamma in Huh7 cells by transactivation assay | F | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2005) 48: 8194-8208 [PMID:16366601] |
| ChEMBL | Activity at human PPAR gamma in Huh7 cells by transactivation assay | B | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2006) 49: 6421-6424 [PMID:17034149] |
| ChEMBL | Agonist activity at human PPARgamma receptor by cell based transactivation assay | F | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2009) 52: 2618-2622 [PMID:19301897] |
| ChEMBL | Effect on PPAR gamma transactivation activity in Huh7 cells | F | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2006) 49: 1212-1216 [PMID:16451087] |
| ChEMBL | 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 | B | 6.68 | pEC50 | 210 | nM | EC50 | J Med Chem (2020) 63: 4555-4561 [PMID:32267688] |
| ChEMBL | 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 | B | 6.7 | pEC50 | 200 | nM | EC50 | Eur J Med Chem (2018) 155: 736-753 [PMID:29940464] |
| ChEMBL | Partial agonist activity at human PPARgamma LBD assessed as activation of Src-1 by HTRF assay | F | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2011) 54: 8541-8554 [PMID:22070604] |
| ChEMBL | Agonist activity at human PPARgamma by transactivation assay | F | 6.7 | pEC50 | 200 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3198-3202 [PMID:17379517] |
| ChEMBL | Binding affinity to PPARgamma LBD by fluorescence polarization based competitive binding assay | B | 6.72 | pEC50 | 190 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
| ChEMBL | Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay | F | 6.72 | pEC50 | 190 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176] |
| ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 6.77 | pEC50 | 169 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
| ChEMBL | In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 6.8 | pEC50 | 160 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR gamma | F | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor gamma | B | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2003) 46: 4883-4894 [PMID:14584939] |
| ChEMBL | Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay | F | 6.8 | pEC50 | 158 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6120-6123 [PMID:16973358] |
| ChEMBL | Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay | F | 6.8 | pEC50 | 158 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 6116-6119 [PMID:16979341] |
| ChEMBL | Agonist activity at human PPARgamma transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 6.81 | pEC50 | 156 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
| ChEMBL | Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 6.84 | pEC50 | 144 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Effective concentration against human Peroxisome proliferator activated receptor gamma | B | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2005) 48: 2248-2250 [PMID:15771468] |
| ChEMBL | Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay | B | 6.92 | pEC50 | 120 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
| ChEMBL | Agonistic activity against PPAR (peroxisome proliferator activated receptor gamma) in Suarus chinesis | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2004) 47: 196-209 [PMID:14695833] |
| ChEMBL | Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction | F | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6773-6778 [PMID:18029176] |
| ChEMBL | Displacement of pan-PPAR fluormone from PPARgamma LBD by TR-FRET based LanthaScreen assay | B | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
| ChEMBL | Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay | B | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem (2012) 20: 1060-1075 [PMID:22197396] |
| ChEMBL | 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 | B | 6.93 | pEC50 | 117 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | 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 | B | 6.94 | pEC50 | 115 | nM | EC50 | J Med Chem (2020) 63: 4555-4561 [PMID:32267688] |
| ChEMBL | 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 | B | 6.94 | pEC50 | 114 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | Partial agonist activity at human PPARgamma LBD assessed as activation of PGC1 by HTRF assay | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2011) 54: 8541-8554 [PMID:22070604] |
| ChEMBL | Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 240-244 [PMID:21112784] |
| ChEMBL | Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay | F | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1581-1584 [PMID:20138762] |
| ChEMBL | Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay | F | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2010) 53: 5012-5024 [PMID:20527969] |
| ChEMBL | Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay | B | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2012) 55: 8303-8317 [PMID:22934537] |
| ChEMBL | Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem (2013) 21: 979-992 [PMID:23294830] |
| ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 7 | pEC50 | 100 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
| ChEMBL | Partial agonist activity at sGSF-PPARgamma (unknown origin) assessed as CBP-1 recruitment by HT-FRET assay | B | 7 | pEC50 | 100 | nM | EC50 | J Med Chem (2021) 64: 17259-17276 [PMID:34818007] |
| ChEMBL | 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 | B | 7.02 | pEC50 | 95 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | Transactivation of PPARgamma assessed as induction of alkaline phosphatase activity | B | 7.05 | pEC50 | 89.13 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 3344-3347 [PMID:20444603] |
| ChEMBL | Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells | F | 7.05 | pEC50 | 89.13 | nM | EC50 | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Transcriptional activation of peroxisome proliferator activated receptor gamma | F | 7.05 | pEC50 | 89.13 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 3329-3334 [PMID:10612594] |
| ChEMBL | Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay | B | 7.06 | pEC50 | 87 | nM | EC50 | J Med Chem (2015) 58: 6639-6652 [PMID:26226490] |
| ChEMBL | Agonist activity at human PPARgamma after 22 to 24 hrs by luciferase reporter gene assay | B | 7.08 | pEC50 | 83 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329] |
| ChEMBL | 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 cryptate labelled CBP recruitment measured after 2 hrs by HTRF assay | B | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (2021) 64: 2815-2828 [PMID:33620196] |
| ChEMBL | Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay | F | 7.09 | pEC50 | 82 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 937-941 [PMID:17157019] |
| ChEMBL | Transactivation of PPARgamma in CV1 cells | F | 7.12 | pEC50 | 76 | nM | EC50 | J Med Chem (2006) 49: 4072-4084 [PMID:16821769] |
| ChEMBL | 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 | B | 7.12 | pEC50 | 76 | nM | EC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | 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 | B | 7.28 | pEC50 | 52 | nM | EC50 | J Med Chem (2018) 61: 2246-2265 [PMID:29446942] |
| ChEMBL | Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem (2008) 16: 7117-7127 [PMID:18625559] |
| ChEMBL | Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay | F | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem (2009) 17: 5722-5732 [PMID:19574056] |
| ChEMBL | Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay | B | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3103-3109 [PMID:21450468] |
| ChEMBL | Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis | B | 7.32 | pEC50 | 48 | nM | EC50 | Bioorg Med Chem (2011) 19: 6982-6988 [PMID:22051054] |
| ChEMBL | Partial agonist activity at human PPARgamma LBD assessed as activation of CBP1-453 by HTRF assay | F | 7.34 | pEC50 | 46 | nM | EC50 | J Med Chem (2011) 54: 8541-8554 [PMID:22070604] |
| ChEMBL | Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay | F | 7.35 | pEC50 | 45 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 1939-1944 [PMID:18291645] |
| ChEMBL | Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay | B | 7.37 | pEC50 | 43 | nM | EC50 | J Med Chem (2011) 54: 331-341 [PMID:21128600] |
| ChEMBL | 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 | B | 7.37 | pEC50 | 43 | nM | EC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
| ChEMBL | Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. | F | 7.37 | pEC50 | 43 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 7.37 | pEC50 | 43 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | 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 | B | 7.4 | pEC50 | 40 | nM | EC50 | ACS Med Chem Lett (2019) 10: 545-551 [PMID:30996794] |
| ChEMBL | Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2008) 51: 7768-7776 [PMID:19053776] |
| ChEMBL | 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 | B | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2015) 90: 583-594 [PMID:25497132] |
| ChEMBL | Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay | B | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2017) 127: 379-397 [PMID:28076827] |
| ChEMBL | 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 | B | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2017) 138: 212-220 [PMID:28667876] |
| ChEMBL | Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2018) 61: 8282-8298 [PMID:30199253] |
| ChEMBL | Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | Medchemcomm (2015) 6: 1513-1517 |
| ChEMBL | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2009) 52: 6382-6393 [PMID:19775169] |
| ChEMBL | Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | Eur J Med Chem (2015) 89: 817-825 [PMID:25462281] |
| ChEMBL | Effective concentration against human PPARgamma expressed in HepG2 cells | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2005) 48: 5509-5519 [PMID:16107150] |
| ChEMBL | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2013) 56: 60-72 [PMID:23171045] |
| ChEMBL | Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay | F | 7.46 | pEC50 | 35 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 2312-2316 [PMID:17292606] |
| ChEMBL | Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay | F | 7.46 | pEC50 | 35 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2605-2608 [PMID:20299214] |
| ChEMBL | Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assay | F | 7.48 | pEC50 | 33 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 4993-4996 [PMID:18771917] |
| ChEMBL | Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2008) 51: 6318-6333 [PMID:18826205] |
| ChEMBL | Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1581-1584 [PMID:20138762] |
| ChEMBL | Partial agonist activity at human PPARgamma LBD assessed as activation of PBP by HTRF assay | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2011) 54: 8541-8554 [PMID:22070604] |
| ChEMBL | Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs | F | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3595-3598 [PMID:17507225] |
| ChEMBL | 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 | B | 7.57 | pEC50 | 27 | nM | EC50 | ACS Med Chem Lett (2022) 13: 681-686 [PMID:35450368] |
| ChEMBL | In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 357-362 [PMID:15603954] |
| ChEMBL | Effective agonist concentration for human PPAR gamma Gal4 construct in transactivation assay | F | 7.66 | pEC50 | 22 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 5035-5038 [PMID:16153845] |
| ChEMBL | Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor | F | 7.68 | pEC50 | 21 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 931-935 [PMID:12617924] |
| ChEMBL | In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | Effective concentration against human Peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2005) 48: 2262-2265 [PMID:15801817] |
| ChEMBL | Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivation | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2437-2440 [PMID:15863293] |
| ChEMBL | Agonist activity at human PPARgamma in U2OS cells by transactivation assay | F | 7.7 | pEC50 | 20 | nM | EC50 | Eur J Med Chem (2008) 43: 2428-2435 [PMID:18329751] |
| ChEMBL | In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells | F | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1801-1804 [PMID:12729668] |
| ChEMBL | Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2012) 55: 37-54 [PMID:22081932] |
| ChEMBL | Transactivation activity at Homo sapiens (human) PPARgamma | B | 7.7 | pEC50 | 20 | nM | EC50 | Med Chem Res (2011) 20: 1005-1014 |
| ChEMBL | In vitro potency of PPAR gene activation against human PPAR gamma receptor using chimeric Gal4-hPPAR transactivation assay (TA) | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2004) 47: 3255-3263 [PMID:15163205] |
| ChEMBL | 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 | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2009) 52: 3846-3854 [PMID:19507861] |
| ChEMBL | Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2009) 52: 4443-4453 [PMID:19530681] |
| ChEMBL | Agonist activity at GAL4-tagged human PPAR receptor | B | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay | B | 7.82 | pEC50 | 15 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963] |
| ChEMBL | Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1348-1351 [PMID:22225641] |
| ChEMBL | 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 | B | 7.96 | pEC50 | 11 | nM | EC50 | Eur J Med Chem (2012) 54: 522-533 [PMID:22727448] |
| ChEMBL | Agonist activity at PPARgamma assessed as transcriptional activation | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2095-2098 [PMID:20219371] |
| ChEMBL | Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay | B | 8 | pEC50 | 10 | nM | EC50 | Eur J Med Chem (2013) 63: 321-332 [PMID:23502212] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay | B | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay | F | 8 | pEC50 | 10 | nM | EC50 | Eur J Med Chem (2011) 46: 2513-2529 [PMID:21482446] |
| ChEMBL | Transcriptional activation by human PPAR gamma | B | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263] |
| ChEMBL | 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 | B | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| ChEMBL | Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Eur J Med Chem (2017) 137: 310-326 [PMID:28609708] |
| ChEMBL | In vitro effective concentration against human peroxisome proliferator activated receptor gamma/Gal4 in cell-based transactivation assay | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4421-4426 [PMID:16137885] |
| ChEMBL | Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2013) 56: 1535-1543 [PMID:23286787] |
| ChEMBL | 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 | B | 8.4 | pEC50 | 4 | nM | EC50 | J Nat Prod (2019) 82: 1802-1812 [PMID:31268307] |
| ChEMBL | Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay | B | 8.42 | pEC50 | 3.8 | nM | EC50 | J Biol Chem (2007) 282: 17314-17324 [PMID:17403688] |
| ChEMBL | Activation of wild type PPAR-gamma-mediated transcriptional activity assessed as luciferase reporter activity | B | 8.57 | pEC50 | 2.7 | nM | EC50 | J Biol Chem (2007) 282: 17314-17324 [PMID:17403688] |
| ChEMBL | Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
| ChEMBL | Kinase Activity Assay: After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the supernatant was collected. The supernatant was reacted with a fluorescence assay kit (Promega) and counted by a fluorometer (Ascent Fluoroskan FL reader, Thermo Labsystems, Finland), and the relative intensity of luciferase was determined. For the assay of the β-galactosidase activity used in the experiment as the internal reference (the internal reference for calibrating the transfection efficiency), 50 μl of the supernatant was transferred into a fresh microplate, treated with a Promega kit, and the value was read with a microplate reader at a wavelength of 405 nm (Bio-tech Instruments Inc., Winooski, Vt., USA) (Sauerberg, P.; Olsen, G. S.; Jeppesen, L.; Mogensen, J. P. et al., J. Med. Chem., 2007, 50, 1495-1503). | B | 9 | pEC50 | 1 | nM | EC50 | US-9346770-B2. Compounds having activating effect on subtypes of peroxisome proliferator-activated receptors and its preparation method and uses (2016) |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Agonist activity for murine PPAR gamma receptor in transcriptional activation assay | F | 7.12 | pEC50 | 76 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells | F | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (1996) 39: 665-668 [PMID:8576907] |
| ChEMBL | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay | B | 7.52 | pEC50 | 30 | nM | EC50 | J Nat Prod (2014) 77: 1594-1600 [PMID:24955889] |
| protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031] | ||||||||
| ChEMBL | Inhibition of PTB1B using pNPP as substrate after 30 mins | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2012) 20: 1060-1075 [PMID:22197396] |
| CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
| ChEMBL | DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) | B | 5.45 | pIC50 | 3560 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095] | ||||||||
| ChEMBL | Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hr | B | 9.64 | pKi | 0.23 | nM | Ki | Med Chem Res (2009) 18: 589-610 |
| TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 4.51 | pEC50 | - | - | - | Mol Pharmacol (2011) 79: 1023-30 [PMID:21406603] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
