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)
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carnitine palmitoyltransferase 1A/Carnitine O-palmitoyltransferase 1, liver isoform in Human [ChEMBL: CHEMBL1293194] [GtoPdb: 3249] [UniProtKB: P50416]
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  • carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523]
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  • carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Human [ChEMBL: CHEMBL3238] [GtoPdb: 3252] [UniProtKB: P23786]
  • carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Rat [ChEMBL: CHEMBL4037] [GtoPdb: 3252] [UniProtKB: P18886]
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  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
  • CDGSH iron-sulfur domain-containing protein 1 in Rat [ChEMBL: CHEMBL3308979] [UniProtKB: B0K020]
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  • CDGSH iron-sulfur domain-containing protein 2 in Human [ChEMBL: CHEMBL4523399] [UniProtKB: Q8N5K1]
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  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
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  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
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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]
ChEMBL Inhibition of recombinant human MAO-B B 6.08 pIC50 832 nM IC50 Bioorg Med Chem Lett (2022) 76: 128994-128994 [PMID:36162779]
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 LBD (unknown origin) assessed as dissociation constant followed by heating for 3 mins by Bradford assay B 5.48 pKd 3300 nM Kd Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
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 Displacement of [3H]rosiglitazone from human PPAR-gamma incubated for 1 day by radioligand binding assay B 7.59 pKi 26 nM Ki Eur J Med Chem (2020) 187: 111969-111969 [PMID:31865018]
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 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 B 4.36 pEC50 44000 nM EC50 Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
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 Agonist activity at GAL4-fused human PPARgamma expressed in HepG2 cells B 6.14 pEC50 730 nM EC50 Eur J Med Chem (2017) 129: 218-250 [PMID:28231521]
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: 5099-5117 [PMID:30220602]
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 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 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 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 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 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 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 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 Binding affinity to PPARgamma (unknown origin) B 6.52 pEC50 300 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
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 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 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 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 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 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 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 human PPARgamma by transactivation assay F 6.7 pEC50 200 nM EC50 Bioorg Med Chem Lett (2007) 17: 3198-3202 [PMID:17379517]
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 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 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 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 (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 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 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 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 pBIND tagged human PPARgamma expressed in human HEK293 cells incubated for 18 hrs by dual luciferase reporter assay relative to control B 6.87 pEC50 134 nM EC50 Bioorg Med Chem (2022) 56: 116615-116615 [PMID:35051813]
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 Agonist activity at human PPARgamma measured by dual luciferase reporter gene assay B 6.92 pEC50 120 nM EC50 Eur J Med Chem (2022) 229: 114061-114061 [PMID:34954593]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 PPARgamma in CV1 cells F 7.12 pEC50 76 nM EC50 J Med Chem (2006) 49: 4072-4084 [PMID:16821769]
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 expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay B 7.31 pEC50 49 nM EC50 J Med Chem (2022) 65: 1961-1978 [PMID:35089724]
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 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 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 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 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 yeast Gal4-fused human PPARgamma transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry B 7.4 pEC50 40 nM EC50 Eur J Med Chem (2022) 235: 114240-114240 [PMID:35325635]
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 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-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 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 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 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 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 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 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 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 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 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 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 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 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 Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment by HTRF assay B 7.59 pEC50 26 nM EC50 Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
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 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 Transactivation activity at Homo sapiens (human) PPARgamma B 7.7 pEC50 20 nM EC50 Med Chem Res (2011) 20: 1005-1014
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 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 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 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 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 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 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 PPAR-gamma in human BMMSC cells assessed as induction of adiponectin production in presence of IDX adipogenic induction medium and measured on day 5 by ELISA B 7.85 pEC50 14 nM EC50 Eur J Med Chem (2020) 187: 111969-111969 [PMID:31865018]
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 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 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 Transcriptional activation by human PPAR gamma B 8 pEC50 10 nM EC50 Bioorg Med Chem Lett (2003) 13: 1277-1280 [PMID:12657263]
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 Agonist activity at human PPARgamma transfected in HEK293 cells assessed increase in luciferase activity incubated for 24 hrs B 8.05 pEC50 9 nM EC50 Eur J Med Chem (2017) 129: 218-250 [PMID:28231521]
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 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 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 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 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 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]