TZD18 [Ligand Id: 2665] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL94306 |
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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 | Binding affinity for human peroxisome proliferator activated receptor alpha | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | In vitro binding affinity against human Peroxisome proliferator activated receptor alpha | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro binding affinity was tested towards human Peroxisome proliferator activated receptor alpha | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| GtoPdb | - | - | 7.6 | pIC50 | - | - | - | Endocrinology (2004) 145: 1640-8 [PMID:14701675] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | B | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | In vitro transcriptional activation in COS cells expressing human peroxisome proliferator activated receptor alpha PPAR-GAL4 chimera | F | 7.59 | pEC50 | 26 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro activity in human Peroxisome proliferator activated receptor alpha-transactivation assay | F | 7.59 | pEC50 | 26 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| 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 binding affinity was tested towards human Peroxisome proliferator activated receptor delta | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| ChEMBL | In vitro binding affinity against human Peroxisome proliferator activated receptor delta | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro activity in human Peroxisome proliferator activated receptor delta-transactivation assay | F | 5.52 | pEC50 | >3000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| 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 | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| GtoPdb | - | - | 7.24 | pIC50 | - | - | - | Endocrinology (2004) 145: 1640-8 [PMID:14701675] |
| ChEMBL | In vitro binding affinity against human peroxisome proliferator activated receptor gamma | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro binding affinity against human peroxisome proliferator activated receptor gamma | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| ChEMBL | Displacement of radio-labeled full agonist from PPARgamma receptor | F | 7.24 | pIC50 | 57 | nM | IC50 | Eur J Med Chem (2011) 46: 2513-2529 [PMID:21482446] |
| ChEMBL | In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells | F | 7.85 | pEC50 | 14 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2795-2798 [PMID:12873517] |
| ChEMBL | In vitro activity in human peroxisome proliferator activated receptor gamma-transactivation assay | F | 7.85 | pEC50 | 14 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 3541-3544 [PMID:14505666] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
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]
