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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL153057 (L-165041)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
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 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 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 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 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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]