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

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ChEMBL ligand: CHEMBL121 (BRL-49653, TDZ-01, Rosiglitazone, Avandamet, Avandaryl, Avandia)
  • Sodium/bile acid and sulphated solute cotransporter 1/Bile acid transporter in Human [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973]
  • This target only has 0 pki data point
  • 0
1 CHEMBL121_lig_chart_1 Bile acid transporter Human
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  • ABCB11/Bile salt export pump in Human [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
  • ABCB11/Bile salt export pump in Rat [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127]
  • This target only has 0 pki data point
  • 0
2 CHEMBL121_lig_chart_2 Bile salt export pump HumanRat
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
  • This target only has 0 pki data point
  • 0
3 CHEMBL121_lig_chart_3 Carbonic anhydrase II Human
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  • Carnitine O-palmitoyltransferase 1, liver isoform in Human [ChEMBL: CHEMBL1293194] [UniProtKB: P50416]
  • This target only has 0 pki data point
  • 0
4 CHEMBL121_lig_chart_4 Carnitine O-palmitoyltransferase 1, liver isoform Human
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  • Carnitine O-palmitoyltransferase 1, muscle isoform in Human [ChEMBL: CHEMBL2216739] [UniProtKB: Q92523]
  • This target only has 0 pki data point
  • 0
5 CHEMBL121_lig_chart_5 Carnitine O-palmitoyltransferase 1, muscle isoform Human
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  • Carnitine palmitoyltransferase 2 in Human [ChEMBL: CHEMBL3238] [UniProtKB: P23786]
  • Carnitine palmitoyltransferase 2 in Rat [ChEMBL: CHEMBL4037] [UniProtKB: P18886]
  • This target only has 0 pki data point
  • 0
6 CHEMBL121_lig_chart_6 Carnitine palmitoyltransferase 2 HumanRat
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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]
  • This target only has 1 pki data point
  • 0
7 CHEMBL121_lig_chart_7 CDGSH iron-sulfur domain-containing protein 1 HumanRat
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  • CDGSH iron-sulfur domain-containing protein 2 in Human [ChEMBL: CHEMBL4523399] [UniProtKB: Q8N5K1]
  • This target only has 0 pki data point
  • 0
8 CHEMBL121_lig_chart_8 CDGSH iron-sulfur domain-containing protein 2 Human
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  • FFA1 receptor/Free fatty acid receptor 1 in Human [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842]
  • This target only has 0 pki data point
  • 0
9 CHEMBL121_lig_chart_9 Free fatty acid receptor 1 Human
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
10 CHEMBL121_lig_chart_10 HERG Human
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11 CHEMBL121_lig_chart_11 Monoamine oxidase A HumanRat
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12 CHEMBL121_lig_chart_12 Monoamine oxidase B HumanRat
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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]
  • This target only has 1 pki data point
  • 0
13 CHEMBL121_lig_chart_13 Peroxisome proliferator-activated receptor alpha HumanMouse
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 1 pki data point
  • 4.48
14 CHEMBL121_lig_chart_14 Peroxisome proliferator-activated receptor delta Human
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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]
  • 0
15 CHEMBL121_lig_chart_15 Peroxisome proliferator-activated receptor gamma HumanMouse
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  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
  • This target only has 0 pki data point
  • 0
16 CHEMBL121_lig_chart_16 Protein-tyrosine phosphatase 1B Human
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  • CYP5A1/Thromboxane-A synthase in Human [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
  • This target only has 0 pki data point
  • 0
17 CHEMBL121_lig_chart_17 Thromboxane-A synthase Human
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  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
  • This target only has 1 pki data point
  • 9.64
18 CHEMBL121_lig_chart_18 Type-1A angiotensin II receptor Rat
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
  • This target only has 0 pki data point
  • 0
19 CHEMBL121_lig_chart_19 TRPC5 Human
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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 O-palmitoyltransferase 1, liver isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293194] [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 O-palmitoyltransferase 1, muscle isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216739] [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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3238] [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 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4037] [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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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