L-796449 [Ligand Id: 2689] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL278994 (L-796449)
  • 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 In vitro binding affinity for human PPAR alpha in SPA B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Agonist activity at PPARalpha F 7.27 pIC50 53.95 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Transcriptional activation by human PPAR alpha B 7.74 pEC50 18 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Agonist activity for Human PPAR alpha receptor in transcriptional activation assay F 8.39 pEC50 4.1 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Agonist activity for murine PPAR alpha receptor in transcriptional activation assay F 5.12 pEC50 7600 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
GtoPdb - - 8.7 pKi - - - J Med Chem (2004) 47: 4118-27 [PMID:15293980];
J Biol Chem (1999) 274: 6718-25 [PMID:10037770]
ChEMBL In vitro binding affinity for human PPAR delta in SPA B 8.22 pIC50 6 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Agonist activity at PPARdelta F 8.22 pIC50 6 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Agonist activity for Human PPAR delta receptor in transcriptional activation assay F 8.1 pEC50 7.9 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
ChEMBL Binding affinity at human GST-tagged PPARdelta ligand binding domain after 1 hr by time-resolved FRET analysis B 8.1 pEC50 7.9 nM EC50 Eur. J. Med. Chem. (2012) 53: 190-202 [PMID:22534184]
ChEMBL Transcriptional activation by human PPAR delta B 8.22 pEC50 6 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
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 7.64 pEC50 23 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]
GtoPdb - - 8.7 pKi - - - J Biol Chem (1999) 274: 6718-25 [PMID:10037770]
ChEMBL In vitro binding affinity for human PPAR gamma in SPA B 7.03 pIC50 94 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Displacement of radio-labeled full agonist from PPARgamma receptor F 7.03 pIC50 94 nM IC50 Eur. J. Med. Chem. (2011) 46: 2513-2529 [PMID:21482446]
ChEMBL Agonist activity at PPARgamma F 7.03 pIC50 93.97 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Transcriptional activation by human PPAR gamma B 8.05 pEC50 9 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Agonist activity for Human PPAR gamma receptor in transcriptional activation assay F 8.28 pEC50 5.2 nM EC50 J. Med. Chem. (2000) 43: 527-550 [PMID:10691680]
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 8 pEC50 10 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]