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 | 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 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 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 activity at Gal4-fused human PPAR-alpha ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| ChEMBL | Transactivation of Gal4-fused human PPARalpha expressed in CHO cells co expressing pG5-Luc reporter | B | 5.66 | pEC50 | 2200 | nM | EC50 | Bioorg Med Chem Lett (2022) 59: 128567-128567 [PMID:35063634] |
| ChEMBL | Agonist activity at human PPARalpha (167 to 468 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 5.66 | pEC50 | 2200 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| 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 | 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 | 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 PPAR-alpha assessed as receptor transactivation by measuring maximum induction of alkaline phosphatase activity | B | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| 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 | 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 | 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 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 | 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 | Agonist activity at mouse PPARalpha (167 to 468 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 4.21 | pEC50 | 61000 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| ChEMBL | Agonist activity at Gal4-fused mouse PPAR-alpha ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 5.21 | pEC50 | 6100 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| 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 PPARdelta (unknown origin) by TR-FRET based LanthaScreen competitive binding assay | B | 7.1 | pKi | 80 | nM | Ki | ACS Med Chem Lett (2022) 13: 1131-1136 [PMID:35859875] |
| ChEMBL | Binding affinity to PPARdelta (unknown origin) assessed as inhibition constant by TR-FRET based LanthaScreen competitive binding assay | B | 8.08 | pKi | 8.3 | nM | Ki | J Med Chem (2023) 66: 4961-4978 [PMID:36967575] |
| 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) assessed as inhibition constant by Cheng-Prusoff equation analysis | B | 9 | pKi | 1 | nM | Ki | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
| 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 | Partial agonist activity at PPARdelta (unknown origin) assessed as increase in fluorescein labeled PRIP/RAP250 coactivator peptide requirement by Lanthascreen TR-FRET assay | B | 6.15 | pEC50 | 700 | nM | EC50 | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
| 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 human PPARdelta (138 to 441 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 8.02 | pEC50 | 9.5 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| ChEMBL | Agonist activity at Gal4-fused human PPAR-delta ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 8.02 | pEC50 | 9.5 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| ChEMBL | Transactivation of Gal4-fused human PPARdelta expressed in CHO cells co expressing pG5-Luc reporter | B | 8.02 | pEC50 | 9.5 | nM | EC50 | Bioorg Med Chem Lett (2022) 59: 128567-128567 [PMID:35063634] |
| 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 | 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 | 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 | 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 | 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 | 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 | 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 human PPAR-delta assessed as receptor transactivation by measuring maximum induction of alkaline phosphatase activity | B | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| ChEMBL | Agonist activity at human PPARdelta transfected in african green monkey COS7 cells assessed transactivation incubated for 16 hrs by luciferase assay | B | 9.22 | pEC50 | 0.6 | nM | EC50 | J Med Chem (2023) 66: 7331-7354 [PMID:37243609] |
| 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 PPARdelta (unknown origin) | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
| 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 Gal4-fused mouse PPARdelta expressed in CHO cells co expressing pG5-Luc reporter | B | 7.12 | pEC50 | 76 | nM | EC50 | Bioorg Med Chem Lett (2022) 59: 128567-128567 [PMID:35063634] |
| ChEMBL | Agonist activity at mouse PPARdelta (138 to 441 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 7.12 | pEC50 | 76 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| ChEMBL | Agonist activity at Gal4-fused mouse PPAR-delta ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 7.12 | pEC50 | 76 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| 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 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 | 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 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 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 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 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 (182 to 505 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 5.36 | pEC50 | 4400 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| ChEMBL | Agonist activity at Gal4-fused human PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 5.36 | pEC50 | 4400 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| ChEMBL | Transactivation of Gal4-fused human PPARgamma expressed in CHO cells co expressing pG5-Luc reporter | B | 5.36 | pEC50 | 4400 | nM | EC50 | Bioorg Med Chem Lett (2022) 59: 128567-128567 [PMID:35063634] |
| 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 PPAR-gamma assessed as receptor transactivation by measuring maximum induction of alkaline phosphatase activity | B | 6.07 | pEC50 | 850 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| 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 | Agonist activity at Gal4-fused mouse PPAR-gamma ligand binding domain expressed in CHO-K1 cells assessed as receptor transactivation incubated for 24 to 48 hrs by luciferase reporter gene assay | B | 5.46 | pEC50 | 3500 | nM | EC50 | Bioorg Med Chem (2023) 82: 117215-117215 [PMID:36840990] |
| ChEMBL | Agonist activity at mouse PPARgamma (182 to 505 residues) expressed in CHO-K1 cells co-transfected with GAL4 and pGluc reporter gene plasmid assessed as receptor transactivation incubated for 24 to 28 hrs by luciferase reporter gene assay | B | 5.46 | pEC50 | 3500 | nM | EC50 | J Med Chem (2023) 66: 11428-11446 [PMID:37552807] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
