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 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]
