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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 |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]