MRL24 [Ligand Id: 6743] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL179330 |
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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 inhibition of human Peroxisome proliferator activated receptor alpha | B | 4.82 | pIC50 | >15000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 357-362 [PMID:15603954] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | In vitro inhibition of human Peroxisome proliferator activated receptor delta | B | 4.82 | pIC50 | >15000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 357-362 [PMID:15603954] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Inhibition of human peroxisome proliferator activated receptor gamma binding | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2437-2440 [PMID:15863293] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 357-62 [PMID:15603954] |
| ChEMBL | In vitro inhibition of human Peroxisome proliferator activated receptor gamma | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 357-362 [PMID:15603954] |
| ChEMBL | Displacement of [3H2]nTZD3 from human recombinant GST-fused PPARgamma expressed in Escherichia coli by scintillation proximity assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2009) 52: 3846-3854 [PMID:19507861] |
| ChEMBL | In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 357-362 [PMID:15603954] |
| ChEMBL | Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2009) 52: 3846-3854 [PMID:19507861] |
| ChEMBL | Activity at full length PPARgamma (unknown origin) transfected in 293T cells assessed as transactivation activity by UAS-luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2015) 58: 5381-5394 [PMID:25734377] |
| ChEMBL | Modulation of 6His-tagged PPARgamma isoform 1 LBD (203 to 477 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells assessed as increase in FITC-TRAP220 peptide recruitment after 1 to 4 hrs by TR-FRET assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Eur J Med Chem (2019) 176: 326-342 [PMID:31112893] |
| ChEMBL | Maximal intrinsic response against peroxisome proliferator activated receptor gamma transactivation | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2437-2440 [PMID:15863293] |
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]
