rosiglitazone [Ligand Id: 1056] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
There should be some charts here, you may need to enable JavaScript!
  • carnitine palmitoyltransferase 1A/Carnitine O-palmitoyltransferase 1, liver isoform in Human [ChEMBL: CHEMBL1293194] [GtoPdb: 3249] [UniProtKB: P50416]
There should be some charts here, you may need to enable JavaScript!
  • carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • CDGSH iron-sulfur domain-containing protein 2 in Human [ChEMBL: CHEMBL4523399] [UniProtKB: Q8N5K1]
There should be some charts here, you may need to enable JavaScript!
  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
There should be some charts here, you may need to enable JavaScript!
  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
There should be some charts here, you may need to enable JavaScript!
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