Reaction Details |
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Target | Peroxisome proliferator-activated receptor alpha |
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Ligand | BDBM28803 |
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Substrate/Competitor | BDBM28680 |
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Meas. Tech. | PPAR alpha Fluorescence Polarization Assay (IC50) and Cell-Based Transcription Assay (EC50) |
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pH | 8±n/a |
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Temperature | 295.15±n/a K |
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IC50 | >98400±n/a nM |
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EC50 | 11600±3100 nM |
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Comments | 104 +/- 8 efficacy. |
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Citation | Mukherjee, R; Locke, KT; Miao, B; Meyers, D; Monshizadegan, H; Zhang, R; Search, D; Grimm, D; Flynn, M; O'Malley, KM; Zhang, L; Li, J; Shi, Y; Kennedy, LJ; Blanar, M; Cheng, PT; Tino, J; Srivastava, RA Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist. J Pharmacol Exp Ther327:716-26 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Peroxisome proliferator-activated receptor alpha |
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Name: | Peroxisome proliferator-activated receptor alpha |
Synonyms: | NR1C1 | Nuclear receptor subfamily 1 group C member 1 | PPAR | PPAR alpha/gamma | PPAR-alpha | PPARA | PPARA_HUMAN | Peroxisome Proliferator-Activated Receptor alpha | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor alpha (PPAR alpha) |
Type: | Enzyme |
Mol. Mass.: | 52222.08 |
Organism: | Homo sapiens (Human) |
Description: | Q07869 |
Residue: | 468 |
Sequence: | MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
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BDBM28803 |
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BDBM28680 |
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Name | BDBM28803 |
Synonyms: | 2-[4-(4-chlorophenoxy)phenoxy]propanoic acid | Clofop | Fenofibric acid | HCG 004 |
Type | Small organic molecule |
Emp. Form. | C15H13ClO4 |
Mol. Mass. | 292.714 |
SMILES | CC(Oc1ccc(Oc2ccc(Cl)cc2)cc1)C(O)=O |
Structure |
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