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ChEMBL ligand: CHEMBL3707395 (Elafibranor, Gft505, GFT-505, GFT505) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8] | ||||||||
ChEMBL | Inhibition of NLRP3 in mouse J774A.1 cells infected with FLA-ST assessed as inhibition of LPS- induced IL-1beta production by ELISA | B | 4.4 | pIC50 | 39600 | nM | IC50 | Eur J Med Chem (2021) 219: 113417-113417 [PMID:33845232] |
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 PPARalpha (unknown origin) | B | 6.09 | pEC50 | 820.3 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
ChEMBL | Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay | B | 6.12 | pEC50 | 760 | nM | EC50 | Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603] |
ChEMBL | Agonist activity at human PPARalpha transfected in human HepG2 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 6.43 | pEC50 | 375 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
ChEMBL | Agonist activity at PPARalpha (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay | B | 6.65 | pEC50 | 225 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410] |
ChEMBL | Agonist activity at PPARalpha (unknown origin) | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
GtoPdb | - | - | 8.22 | pEC50 | 6 | nM | EC50 | Expert Opin Pharmacother (2014) 15: 493-503 [PMID:24428677] |
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 6.07 | pEC50 | 842.9 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
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 | 6.14 | pEC50 | 730 | nM | EC50 | Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603] |
ChEMBL | Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 6.6 | pEC50 | 249 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
ChEMBL | Agonist activity at PPARbeta (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay | B | 6.94 | pEC50 | 115 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410] |
ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
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 human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 5.4 | pEC50 | 3962 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
ChEMBL | Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay | B | 5.55 | pEC50 | 2790 | nM | EC50 | Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603] |
ChEMBL | Agonist activity at PPARgamma (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay | B | 5.67 | pEC50 | 2116 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410] |
ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 5.73 | pEC50 | 1843.8 | nM | EC50 | J Med Chem (2022) 65: 2571-2592 [PMID:35060744] |
GtoPdb | - | - | 7.33 | pEC50 | 47 | nM | EC50 | Expert Opin Pharmacother (2014) 15: 493-503 [PMID:24428677] |
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]