Reaction Details
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Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28718
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
465±n/a nM
Comments
82 % of maximal activation compared to reference compounds normalized to 100%.
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 Chem 50:685-95 (2007) [PubMed] Article More Info.:
Target
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:
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSCPGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFVIHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDIFLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
Inhibitor
Name:
BDBM28718
Synonyms:
2-methyl-2-phenoxypropanoic acid, 25j | 2-methyl-2-{4-[({4-methyl-2-[2-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}formamido)methyl]phenoxy}propanoic acid
Type:
Small organic molecule
Emp. Form.:
C23H21F3N2O4S
Mol. Mass.:
478.484
SMILES:
Cc1nc(sc1C(=O)NCc1ccc(OC(C)(C)C(O)=O)cc1)-c1ccccc1C(F)(F)F
Structure:
Substrate