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 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]
