| Reaction Details |
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 | Report a problem with these data |
| Target | Peroxisome proliferator-activated receptor alpha |
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| Ligand | BDBM28681 |
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| Substrate/Competitor | BDBM33283 |
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| Meas. Tech. | Scintillation Proximity Assay (IC50) and PPAR alpha Transactivation Assay (EC50) |
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| pH | 7.2±n/a |
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| Temperature | 288.15±n/a K |
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| EC50 | >12000±n/a nM |
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| Comments | 21% inhibition @ 10 uM.Efficacy=23% (The maximum efficacy of GW9578 was defined as 100%). |
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| Citation |  Casimiro-Garcia, A; Bigge, CF; Davis, JA; Padalino, T; Pulaski, J; Ohren, JF; McConnell, P; Kane, CD; Royer, LJ; Stevens, KA; Auerbach, B; Collard, W; McGregor, C; Song, K Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists. Bioorg Med Chem17:7113-25 (2009) [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 |
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| 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) |
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| Type: | Enzyme |
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| Mol. Mass.: | 52222.08 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q07869 |
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| Residue: | 468 |
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| Sequence: | MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
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| BDBM28681 |
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| BDBM33283 |
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| Name | BDBM28681 |
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| Synonyms: | 5-[(4-{2-[methyl(pyridin-2-yl)amino]ethoxy}phenyl)methyl]-1,3-thiazolidine-2,4-dione | Avandia | BRL 49653 | Brl-49653 | CHEMBL121 | ROSIGLITAZONE MALEATE | [3H]rosiglitazone | cid_5281055 | rosiglitazone |
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| Type | radiolabeled ligand |
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| Emp. Form. | C18H19N3O3S |
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| Mol. Mass. | 357.427 |
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| SMILES | CN(CCOc1ccc(Cc2sc(=O)[nH]c2O)cc1)c1ccccn1 |
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| Structure | 
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