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ChEMBL ligand: CHEMBL24038 (Ragaglitazar) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
ChEMBL | Binding affinity for human peroxisome proliferator activated receptor alpha | B | 6.01 | pKi | 980 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
GtoPdb | - | - | 6 | pIC50 | - | - | - | J Med Chem (2003) 46: 1306-17 [PMID:12672231] |
ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand | B | 6.01 | pIC50 | 980 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
ChEMBL | Transactivation of Homo sapiens (human) PPARalpha assessed as luciferase activity by reporter gene assay | B | 5.49 | pEC50 | 3235.94 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 5.49 | pEC50 | 3235.94 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 5.49 | pEC50 | 3210 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR alpha | F | 5.49 | pEC50 | 3210 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
ChEMBL | In vitro activation of human peroxisome proliferator activated receptor alpha | B | 5.49 | pEC50 | 3210 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434] |
ChEMBL | Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell based assay | F | 5.49 | pEC50 | 3200 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275] |
ChEMBL | Agonistic activity for Peroxisome proliferator activated receptor alpha | F | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
ChEMBL | Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | B | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
ChEMBL | Agonist activity at GAL4 fused human PPARalpha LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay | B | 5.55 | pEC50 | 2800 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Binding affinity for human peroxisome proliferator activated receptor gamma | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
GtoPdb | - | - | 7.03 | pIC50 | - | - | - |
J Med Chem (2003) 46: 1306-17 [PMID:12672231]; Br J Pharmacol (2003) 140: 527-37 [PMID:12970088]; Br J Pharmacol (2005) 144: 308-16 [PMID:15655531] |
ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand | B | 7.04 | pIC50 | 92 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
ChEMBL | Agonistic activity for human Peroxisome proliferator activated receptor gamma | F | 6.22 | pEC50 | 600 | nM | EC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
ChEMBL | Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay | F | 6.22 | pEC50 | 600 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275] |
ChEMBL | Transactivation of Homo sapiens (human) PPARgamma assessed as luciferase activity by reporter gene assay | B | 6.24 | pEC50 | 575.44 | nM | EC50 | Med Chem Res (2012) 21: 2873-2884 |
ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 6.24 | pEC50 | 575.44 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
ChEMBL | In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 6.24 | pEC50 | 570 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 257-260 [PMID:12482434] |
ChEMBL | Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay | B | 6.24 | pEC50 | 570 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218] |
ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR gamma | F | 6.24 | pEC50 | 570 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
ChEMBL | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 6.24 | pEC50 | 570 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
ChEMBL | Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay | B | 6.24 | pEC50 | 570 | nM | EC50 | Med Chem Res (2013) 22: 287-302 |
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]