Reaction Details |
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Target | Peroxisome proliferator-activated receptor alpha |
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Ligand | BDBM28722 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Cell-Based Transcription Assay |
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EC50 | 1890±n/a nM |
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Comments | 171 % of maximal activation compared to reference compounds normalized to 100%. |
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Citation | Sierra, ML; Beneton, V; Boullay, AB; Boyer, T; Brewster, AG; Donche, F; Forest, MC; Fouchet, MH; Gellibert, FJ; Grillot, DA; Lambert, MH; Laroze, A; Le Grumelec, C; Linget, JM; Montana, VG; Nguyen, VL; Nicodème, E; Patel, V; Penfornis, A; Pineau, O; Pohin, D; Potvain, F; Poulain, G; Ruault, CB; Saunders, M; Toum, J; Xu, HE; Xu, RX; Pianetti, PM Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents. J Med Chem50:685-95 (2007) [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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BDBM28722 |
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BDBM10852 |
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Name | BDBM28722 |
Synonyms: | 2-methyl-2-phenoxypropanoic acid, 41 | 2-methyl-2-{4-[({5-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}formamido)methyl]phenoxy}propanoic acid |
Type | Small organic molecule |
Emp. Form. | C23H21F3N2O4S |
Mol. Mass. | 478.484 |
SMILES | Cc1sc(nc1C(=O)NCc1ccc(OC(C)(C)C(O)=O)cc1)-c1ccc(cc1)C(F)(F)F |
Structure |
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