L-165041 [Ligand Id: 2691] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL153057 (L-165041)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
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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 for Human PPAR alpha receptor in transcriptional activation assay F 5 pEC50 10000 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells F 6.01 pEC50 977 nM EC50 Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985]
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 PPARdelta (unknown origin) assessed as thermodynamic dissociation constant by SPR assay B 7.12 pKd 76.4 nM Kd Eur J Med Chem (2017) 127: 379-397 [PMID:28076827]
GtoPdb - - 8.2 pKi - - - J Med Chem (2000) 43: 527-50 [PMID:10691680];
J Biol Chem (1999) 274: 6718-25 [PMID:10037770]
ChEMBL Agonist activity at GAL4 DNA-binding domain fused PPARdelta receptor (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay B 7.9 pIC50 12.6 nM IC50 Eur J Med Chem (2018) 157: 791-804 [PMID:30144697]
ChEMBL Transactivation of GAL4-fused PPARbeta (delta) ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay B 6.19 pEC50 650 nM EC50 Bioorg Med Chem Lett (2012) 22: 6681-6687 [PMID:23031596]
ChEMBL Transactivation of GAL4-fused PPARbeta LBD expressed in HepG2 cells after 20 hrs by luminescence assay B 6.19 pEC50 640 nM EC50 Bioorg Med Chem Lett (2012) 22: 2527-2533 [PMID:22381047]
ChEMBL Agonist activity for Human PPAR delta receptor in transcriptional activation assay F 6.28 pEC50 530 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL Transactivation of GAL4-tagged human PPARdelta LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay B 6.68 pEC50 210 nM EC50 ACS Med Chem Lett (2019) 10: 545-551 [PMID:30996794]
ChEMBL Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells F 6.9 pEC50 125 nM EC50 Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985]
ChEMBL Agonist activity at PPARbeta (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay B 7.21 pEC50 61 nM EC50 ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410]
ChEMBL Agonist activity at PPARdelta (unknown origin) B 7.3 pEC50 50 nM EC50 Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855]
ChEMBL Transactivation of human PPARdelta expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay B 7.41 pEC50 39 nM EC50 J Med Chem (2016) 59: 61-81 [PMID:26595749]
ChEMBL Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay B 7.41 pEC50 39 nM EC50 J Med Chem (2012) 55: 10771-10775 [PMID:23130964]
ChEMBL Transactivation of human PPARdelta expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Medchemcomm (2015) 6: 1513-1517
ChEMBL Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay B 7.68 pEC50 21 nM EC50 J Med Chem (2012) 55: 37-54 [PMID:22081932]
ChEMBL Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Eur J Med Chem (2015) 89: 817-825 [PMID:25462281]
ChEMBL Agonist activity at yeast Gal4-fused human PPARdelta transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry B 7.68 pEC50 21 nM EC50 Eur J Med Chem (2022) 235: 114240-114240 [PMID:35325635]
ChEMBL Transactivation of GAL4-fused human PPARdelta LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay B 7.7 pEC50 20 nM EC50 Eur J Med Chem (2017) 127: 379-397 [PMID:28076827]
ChEMBL Agonist activity at human PPAR-delta expressed in CHO-K1 cells by PathHunter assay B 8.22 pEC50 6 nM EC50 J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Agonist activity for murine PPAR delta receptor in transcriptional activation assay F 5.42 pEC50 3800 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
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 for Human PPAR gamma receptor in transcriptional activation assay F 5.26 pEC50 5500 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]
ChEMBL Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells F 5.74 pEC50 1824 nM EC50 Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Agonist activity for murine PPAR gamma receptor in transcriptional activation assay F 5 pEC50 10000 nM EC50 J Med Chem (2000) 43: 527-550 [PMID:10691680]

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]