L-783483 [Ligand Id: 2688] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL23296
  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
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  • 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]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
GtoPdb - - 7.9 pKd - - - Endocrinology (2002) 143: 2548-58 [PMID:12072387]
ChEMBL Displacement of [3H2]-F3-methyl AA (1) from liver X receptor-alpha in SPA assay B 7.45 pIC50 35.4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Displacement of [3H2]-F3-methyl AA (1) from liver X receptor-alpha in SPA assay B 7.45 pIC50 35.4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Inhibition of LXR alpha B 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Activity at LXR alpha as beta-lactamase transactivation in CHO cells F 5.23 pEC50 5900 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Effective concentration against liver X receptor-alpha in HEK293 cell transactivation assay B 5.75 pEC50 1790 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration against liver X receptor-alpha in HEK293 cell transactivation assay B 5.75 pEC50 1790 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration for cofactor association with recombinant liver X receptor-alpha B 7.45 pEC50 35.4 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration for cofactor association with recombinant liver X receptor-alpha B 7.45 pEC50 35.4 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Agonist activity at human recombinant LXRalpha expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRalpha ligand binding domain by HTRF assay B 7.46 pEC50 35 nM EC50 J. Nat. Prod. (2005) 68: 1247-1252 [PMID:16124770]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
GtoPdb - - 8.2 pKd - - - Endocrinology (2002) 143: 2548-58 [PMID:12072387]
ChEMBL Inhibition of LXR beta B 7.55 pIC50 28 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Displacement of [3H2]-F3-methyl AA (1) from liver X receptor-beta in SPA assay B 7.6 pIC50 24.9 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Displacement of [3H2]-F3-methyl AA (1) from liver X receptor-beta in SPA assay B 7.6 pIC50 24.9 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Activity at LXR beta as beta-lactamase transactivation in CHO cells F 5.14 pEC50 7300 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Effective concentration against liver X receptor-beta in HEK293 cell transactivation assay B 5.97 pEC50 1080 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration against liver X receptor-beta in HEK293 cell transactivation assay B 5.97 pEC50 1080 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration for cofactor association with recombinant liver X receptor-beta B 7.79 pEC50 16.1 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Effective concentration for cofactor association with recombinant liver X receptor-beta B 7.79 pEC50 16.1 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2824-2828 [PMID:15911262]
ChEMBL Agonist activity at human recombinant LXRbeta expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRbeta ligand binding domain by HTRF assay B 7.8 pEC50 16 nM EC50 J. Nat. Prod. (2005) 68: 1247-1252 [PMID:16124770]
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 6.51 pIC50 310 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Inhibition of PPAR alpha B 6.55 pIC50 280 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Agonist activity at PPARalpha F 6.55 pIC50 280 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Agonist activity at PPARalpha F 6.55 pIC50 279.9 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Transcriptional activation by human PPAR alpha B 6.9 pEC50 125 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
GtoPdb - - 9 pKd - - - J Biol Chem (1999) 274: 6718-25 [PMID:10037770]
ChEMBL In vitro binding affinity for human PPAR delta in SPA B 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Inhibition of PPAR delta B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Agonist activity at PPARdelta F 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Agonist activity at PPARdelta F 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
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 8.3 pEC50 5 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
GtoPdb - - 7.85 pKi - - - J Biol Chem (1999) 274: 6718-25 [PMID:10037770]
ChEMBL Inhibition of PPAR gamma B 6.71 pIC50 195 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 3055-3060 [PMID:16529931]
ChEMBL Agonist activity at PPARgamma F 6.71 pIC50 195 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL Agonist activity at PPARgamma F 6.71 pIC50 194.98 nM IC50 Bioorg. Med. Chem. (2012) 20: 3523-3532 [PMID:22564380]
ChEMBL In vitro binding affinity for human PPAR gamma in SPA B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]
ChEMBL Displacement of radio-labeled full agonist from PPARgamma receptor F 6.85 pIC50 140 nM IC50 Eur. J. Med. Chem. (2011) 46: 2513-2529 [PMID:21482446]
ChEMBL Transcriptional activation by human PPAR gamma B 7.64 pEC50 23 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 1277-1280 [PMID:12657263]

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]