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] |
| 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 | 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 | 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 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]
