lanifibranor [Ligand Id: 12737] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4091374 (Iva337, IVA-337, IVA337, Lanifibranor) |
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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]
