GW501516 [Ligand Id: 2687] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38943 (Cardarine, GSK-516, GW-1516, Gw-501516, Gw501516, GW501516) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Displacement of radiolabeled ligand from human PPARalpha by competition-binding assay | B | 5.7 | pIC50 | 1995.26 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5018-5022 [PMID:18722772] |
| ChEMBL | Displacement of [3H]GW 2433 from human PPARalpha by scintillation proximity assay | B | 5.7 | pIC50 | 1995.26 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2345-2350 [PMID:21414782] |
| ChEMBL | Agonist activity at PPARalpha | F | 5.7 | pIC50 | 1995.26 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Displacement of [3H]2-(4-(2-(3-(2,4-difluorophenyl)-1-heptylureido)ethyl)phenoxy)-2-methylbutanoic acid from human PPARalpha after 30 mins by SPA | B | 6.33 | pIC50 | 463 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3630-3635 [PMID:17512197] |
| 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 | Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells | F | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| ChEMBL | Agonist activity at human PPARalpha by transactivation assay | F | 5.41 | pEC50 | 3900 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4144-4149 [PMID:17553681] |
| ChEMBL | Agonist activity at human PPARalpha by transactivation assay | F | 5.41 | pEC50 | 3900 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4625-4629 [PMID:17560785] |
| ChEMBL | Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay | B | 5.41 | pEC50 | 3900 | nM | EC50 | J Med Chem (2007) 50: 1495-1503 [PMID:17343371] |
| ChEMBL | Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay | F | 5.72 | pEC50 | 1888 | nM | EC50 | J Med Chem (2007) 50: 685-695 [PMID:17243659] |
| ChEMBL | Agonist activity at PPARalpha by transactivation assay | F | 5.91 | pEC50 | 1230 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4376-4380 [PMID:16750626] |
| ChEMBL | Maximum transcriptional activation of human PPAR alpha receptor | B | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| 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 | Effect on PPARalpha transactivation activity in HEK293 cells | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem (2007) 15: 5177-5190 [PMID:17532641] |
| ChEMBL | Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 6 | pEC50 | 990 | 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 | 6 | pEC50 | 990 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation of human PPARalpha expressed in monkey CV-1 cells coexpressing TK-PPRE-Luc after 24 hrs by luciferase reporter gene assay | B | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem (2018) 26: 4382-4389 [PMID:30054191] |
| ChEMBL | Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay | B | 6.64 | pEC50 | 229 | nM | EC50 | Eur J Med Chem (2012) 53: 190-202 [PMID:22534184] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Activity against murine PPAR alpha receptor | B | 5.6 | pEC50 | 2500 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Binding affinity to PPAR-delta (unknown origin) by TR-FRET assay | B | 8.22 | pKi | 6.08 | nM | Ki | J Med Chem (2020) 63: 16012-16027 [PMID:33325691] |
| ChEMBL | Binding affinity to PPARdelta (unknown origin) by TR-FRET assay | B | 9.09 | pKi | 0.82 | nM | Ki | Bioorg Med Chem (2019) 27: 2948-2958 [PMID:31128991] |
| ChEMBL | Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD by TR-FRET assay | B | 10.32 | pKi | 0.05 | nM | Ki | J Med Chem (2017) 60: 7459-7475 [PMID:28799755] |
| ChEMBL | Antagonist activity at human PPARdelta ligand binding domain-mediated transcriptional activity in CV1 cells by Gal4 chimera reporter assay | B | 6.9 | pIC50 | 125.89 | nM | IC50 | J Med Chem (2010) 53: 1857-1861 [PMID:20128594] |
| ChEMBL | Displacement of [3H]GW 2433 from human PPARdelta by competition-binding assay | B | 8.3 | pIC50 | 5.01 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5018-5022 [PMID:18722772] |
| ChEMBL | Displacement of [3H]GW 2433 from human PPARdelta by scintillation proximity assay | B | 8.3 | pIC50 | 5.01 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2345-2350 [PMID:21414782] |
| ChEMBL | Agonist activity at PPARdelta | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Displacement of [3H]2-(4-(3-(4-acetyl-3-hydroxy-2 propyl-phenoxy)propoxy)phenoxy)acetic acid from human PPARdelta after 30 mins by SPA | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3630-3635 [PMID:17512197] |
| ChEMBL | Binding affinity for human PPAR delta receptor | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at human Gal4 fused PPARdelta LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay | B | 5.98 | pEC50 | 1050 | nM | EC50 | Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603] |
| ChEMBL | Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay | F | 7.07 | pEC50 | 85 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4351-4357 [PMID:17524643] |
| ChEMBL | Binding affinity at human GST-tagged PPARdelta ligand binding domain after 1 hr by time-resolved FRET analysis | B | 7.62 | pEC50 | 24 | nM | EC50 | Eur J Med Chem (2012) 53: 190-202 [PMID:22534184] |
| 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 | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963] |
| ChEMBL | Agonist activity at human PPARdelta by transactivation assay | F | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4144-4149 [PMID:17553681] |
| ChEMBL | Agonist activity at human PPARdelta by transactivation assay | F | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4625-4629 [PMID:17560785] |
| ChEMBL | Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay | B | 8.1 | pEC50 | 7.9 | nM | EC50 | J Med Chem (2007) 50: 1495-1503 [PMID:17343371] |
| ChEMBL | Agonist activity at human PPARdelta ligand binding domain by FRET assay | B | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 8.23 | pEC50 | 5.9 | nM | EC50 | Bioorg Med Chem (2016) 24: 5258-5269 [PMID:27591006] |
| ChEMBL | Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 8.23 | pEC50 | 5.9 | nM | EC50 | Bioorg Med Chem (2016) 24: 5455-5461 [PMID:27622746] |
| ChEMBL | Agonist activity at human PPARdelta ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay | B | 8.36 | pEC50 | 4.4 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218] |
| ChEMBL | Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 3630-3635 [PMID:17512197] |
| ChEMBL | Partial agonist activity at human PPARdelta expressed in african green monkey CV1 cells transfected with Gal4 assessed as beta-galactosidase activity by transactivation assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2345-2350 [PMID:21414782] |
| ChEMBL | Agonist activity at human PPARdelta by Gal4 chimera cell-based reporter assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5018-5022 [PMID:18722772] |
| ChEMBL | Agonist activity at PPARdelta by transactivation assay | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4376-4380 [PMID:16750626] |
| 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 | 8.54 | pEC50 | 2.9 | nM | EC50 | Bioorg Med Chem (2011) 19: 6982-6988 [PMID:22051054] |
| ChEMBL | Transactivation of GAL4-fused human PPARdelta LBD expressed in African green monkey CV1 cells after 24 hrs by luciferase reporter gene assay | B | 8.59 | pEC50 | 2.6 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 533-536 [PMID:29275935] |
| ChEMBL | Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Eur J Med Chem (2012) 53: 190-202 [PMID:22534184] |
| ChEMBL | Transactivation of human PPARdelta expressed in monkey CV-1 cells coexpressing TK-PPRE-Luc after 24 hrs by luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem (2018) 26: 4382-4389 [PMID:30054191] |
| ChEMBL | Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 492-496 [PMID:21094606] |
| ChEMBL | Effect on PPARdelta transactivation activity in HEK293 cells | B | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem (2007) 15: 5177-5190 [PMID:17532641] |
| ChEMBL | Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 8.77 | pEC50 | 1.7 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 240-244 [PMID:21112784] |
| ChEMBL | Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 8.77 | pEC50 | 1.7 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Competitive binding affinity to GST-tagged human PPARdelta LBD incubated for 1 to 6 hrs by TR-FRET assay | B | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266] |
| ChEMBL | Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 4122-4126 [PMID:22579420] |
| ChEMBL | Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| GtoPdb | - | - | 9 | pEC50 | - | - | - | Proc Natl Acad Sci USA (2001) 98: 5306-11 [PMID:11309497] |
| ChEMBL | Maximum transcriptional activation of human PPAR delta receptor | B | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| ChEMBL | Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2007) 50: 685-695 [PMID:17243659] |
| ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2020) 63: 10109-10134 [PMID:32539376] |
| ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
| ChEMBL | Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay | B | 9.3 | pEC50 | 0.5 | nM | EC50 | Eur J Med Chem (2015) 94: 229-236 [PMID:25768705] |
| ChEMBL | Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay | B | 9.74 | pEC50 | 0.18 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] | ||||||||
| ChEMBL | Agonist activity at mouse PPARdelta by FRET assay | F | 7.11 | pEC50 | 77 | nM | EC50 | J Med Chem (2010) 53: 77-105 [PMID:19928766] |
| ChEMBL | Transactivation of mouse PPARdelta by cell-based luciferase reporter gene assay | B | 7.15 | pEC50 | 70 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 533-536 [PMID:29275935] |
| ChEMBL | Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay | F | 7.27 | pEC50 | 54 | nM | EC50 | J Med Chem (2007) 50: 1495-1503 [PMID:17343371] |
| ChEMBL | Activity against murine PPAR delta receptor | B | 7.7 | pEC50 | 20 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Displacement of radiolabeled ligand from human PPARgamma by competition-binding assay | B | 5.2 | pIC50 | 6309.57 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5018-5022 [PMID:18722772] |
| ChEMBL | Displacement of [3H]GW 2433 from human PPARgamma by scintillation proximity assay | B | 5.2 | pIC50 | 6309.57 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2345-2350 [PMID:21414782] |
| ChEMBL | Agonist activity at PPARgamma | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | Bioorg Med Chem (2012) 20: 3523-3532 [PMID:22564380] |
| ChEMBL | Agonist activity at human PPARgamma by transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4625-4629 [PMID:17560785] |
| ChEMBL | Agonist activity at PPARgamma by transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4376-4380 [PMID:16750626] |
| ChEMBL | Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells | F | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| ChEMBL | Agonist activity at human PPARgamma by transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4144-4149 [PMID:17553681] |
| 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 | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 1883-1886 [PMID:19275963] |
| ChEMBL | Activity at human adipose tissue PPAR gamma 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 potency at PPARgamma in CV1 cells by cell based transient transfection assay | F | 5.05 | pEC50 | 8900 | nM | EC50 | J Med Chem (2007) 50: 685-695 [PMID:17243659] |
| ChEMBL | Effect on PPARgamma transactivation activity in HEK293 cells | B | 5.07 | pEC50 | 8600 | nM | EC50 | Bioorg Med Chem (2007) 15: 5177-5190 [PMID:17532641] |
| ChEMBL | Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 5.39 | pEC50 | 4100 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay | B | 5.39 | pEC50 | 4100 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 240-244 [PMID:21112784] |
| ChEMBL | Transactivation of human PPARgamma expressed in monkey CV-1 cells coexpressing TK-PPRE-Luc after 24 hrs by luciferase reporter gene assay | B | 5.82 | pEC50 | >1500 | nM | EC50 | Bioorg Med Chem (2018) 26: 4382-4389 [PMID:30054191] |
| ChEMBL | Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay | B | 5.92 | pEC50 | >1200 | nM | EC50 | Eur J Med Chem (2012) 53: 190-202 [PMID:22534184] |
| 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 | 6.04 | pEC50 | 912 | nM | EC50 | Bioorg Med Chem (2011) 19: 6982-6988 [PMID:22051054] |
| ChEMBL | Maximum transcriptional activation of human PPAR gamma receptor | B | 6.07 | pEC50 | 850 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Activity against murine PPAR gamma receptor | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
