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!
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] 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!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] Monoamine oxidase A in Rat [ChEMBL: CHEMBL3358] [UniProtKB: P21396] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase B in Human [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] Monoamine oxidase B in Rat [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] 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!
CYP5A1/Thromboxane-A synthase in Human [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] 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]
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