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ChEMBL ligand: CHEMBL38508 (GW0742) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
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 | 5.6 | pEC50 | 2500 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
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 | Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay | B | 6.04 | pEC50 | 920 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
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 | 5.06 | pEC50 | 8800 | 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 human PPARdelta (unknown origin) by competitive TR-FRET assay | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (2013) 56: 1535-1543 [PMID:23286787] |
GtoPdb | - | - | 9 | pIC50 | - | - | - |
Atherosclerosis (2005) 181: 29-37 [PMID:15939051]; Bioorg Med Chem Lett (2003) 13: 1517-21 [PMID:12699745] |
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 PPARdelta LBD by cell based luciferase reporter gene assay | F | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
ChEMBL | Activation of PPARbeta-LBD (unknown origin) assessed as fluorescein-labeled coactivator C33 recruitment by TR-FRET assay | B | 7.17 | pEC50 | 67.11 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 3978-3983 [PMID:27450788] |
ChEMBL | Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 7.57 | pEC50 | 26.9 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
ChEMBL | Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 7.74 | pEC50 | 18 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
ChEMBL | Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Eur J Med Chem (2019) 164: 352-365 [PMID:30605833] |
ChEMBL | Agonist activity at human PPARdelta measured by dual luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Eur J Med Chem (2022) 229: 114061-114061 [PMID:34954593] |
ChEMBL | Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
ChEMBL | Agonist activity at pBIND tagged human PPARdelta expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay | B | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem (2022) 56: 116615-116615 [PMID:35051813] |
ChEMBL | Agonist activity at PPARdelta (unknown origin) by Alpha Screen assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Medchemcomm (2019) 10: 1412-1419 [PMID:31673308] |
ChEMBL | Agonist activity at human PPAR-delta | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
ChEMBL | Agonist activity at human PPARdelta expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay | B | 8.46 | pEC50 | 3.5 | nM | EC50 | J Med Chem (2022) 65: 1961-1978 [PMID:35089724] |
ChEMBL | Displacement of pan-PPAR fluormone from PPARdelta LBD by TR-FRET based LanthaScreen assay | B | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
ChEMBL | Agonist activity at human PPARdelta after 22 to 24 hrs by luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329] |
ChEMBL | Agonist activity at human PPARdelta expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay | B | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2020) 63: 2854-2876 [PMID:32096640] |
ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 9 | pEC50 | 1 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
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] |
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] | ||||||||
ChEMBL | Activity against murine PPAR delta receptor | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
ChEMBL | Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay | F | 8.24 | pEC50 | <=5.8 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7239-7242 [PMID:21074432] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 5.02 | pEC50 | 9530 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
ChEMBL | Maximum transcriptional activation of human PPAR gamma receptor | B | 5.7 | pEC50 | 2000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
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 | 5 | pEC50 | >10000 | 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]