lanifibranor [Ligand Id: 12737] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4091374 (Iva337, IVA-337, IVA337, Lanifibranor)
  • 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]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
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  • 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]
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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 Agonist activity at PPARalpha (unknown origin) B 5.51 pEC50 3060 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
GtoPdb - - 5.81 pEC50 1537 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of human GAL4-fused PPARalpha LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 5.81 pEC50 1537 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Agonist activity at human PPARalpha B 5.82 pEC50 1500 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Transactivation of mouse GAL4-fused PPARalpha LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 6.44 pEC50 366 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
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 5.53 pEC50 2962 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
GtoPdb - - 6.06 pEC50 866 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Agonist activity at human PPARdelta B 6.06 pEC50 870 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
ChEMBL Transactivation of human GAL4-fused PPARdelta LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 6.06 pEC50 866 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Transactivation of mouse GAL4-fused PPARdelta LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 5.81 pEC50 1560 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PNRC1 (302 to 327 residues) co-activator recruitment by TR-FRET assay B 5.39 pEC50 4111 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Displacement of N-terminal biotin-labeled NCOR-ID1 (2253 to 2277 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli by TR-FRET assay B 5.39 pEC50 4097 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled SRC1 (619 to 643 residues) co-activator recruitment by TR-FRET assay B 5.47 pEC50 3408 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled RIP140 (922 to 946 residues) co-activator recruitment by TR-FRET assay B 5.48 pEC50 3274 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled PGC1alpha (196 to 221 residues) co-activator recruitment by TR-FRET assay B 5.49 pEC50 3208 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (671 to 695 residues) co-activator recruitment by TR-FRET assay B 5.72 pEC50 1917 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled NCoA3 (607 to 631 residues) co-activator recruitment by TR-FRET assay B 5.83 pEC50 1484 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Displacement of N-terminal biotin-labeled SMRT-ID1 (2339 to 2363 residues) from recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli by TR-FRET assay B 5.94 pEC50 1140 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Transactivation of recombinant GST-tagged PPARgamma (unknown origin) expressed in Escherichia coli assessed as N-terminal biotin-labeled LCOR (39 to 63 residues) co-activator recruitment by TR-FRET assay B 6.14 pEC50 727 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
ChEMBL Agonist activity at PPARgamma (unknown origin) B 6.25 pEC50 558.9 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
ChEMBL Agonist activity at human PPARgamma B 6.68 pEC50 210 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
ChEMBL Transactivation of human GAL4-fused PPARgamma LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 6.69 pEC50 206 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
GtoPdb - - 6.69 pEC50 206 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Transactivation of mouse GAL4-fused PPARgamma LBD expressed in African green monkey COS7 cells co-expressing 5Gal4 pGL3 TK Luc after overnight incubation by luciferase reporter gene assay B 6.69 pEC50 202 nM EC50 J Med Chem (2018) 61: 2246-2265 [PMID:29446942]

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]