L-783483 [Ligand Id: 2688] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL23296 |
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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 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]
