Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL457 (CI-719, Emfib, Gemfibrozil, Lopid, NSC-757024) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
ChEMBL | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | B | 5.14 | pKi | 7291 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692] | ||||||||
ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | B | 5.73 | pKi | 1860 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
ChEMBL | Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay | F | 4.23 | pEC50 | 59000 | nM | EC50 | Eur J Med Chem (2011) 46: 5218-5224 [PMID:21889235] |
ChEMBL | Transactivation of human PPARalpha expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay | B | 4.23 | pEC50 | 59000 | nM | EC50 | Medchemcomm (2015) 6: 1513-1517 |
GtoPdb | - | - | 4.23 | pEC50 | 59000 | nM | EC50 | Eur J Med Chem (2011) 46: 5218-24 [PMID:21889235] |
ChEMBL | Agonist activity at human PPARalpha transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 4.93 | pEC50 | 11800 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 4.16 | pEC50 | 68400 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766] | ||||||||
ChEMBL | Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2015) 58: 6507-6515 [PMID:26214366] |
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]