Reaction Details
Report a problem with these data
Report a problem with these dataTarget
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28723
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
4±2 nM
Comments
98 +/- 8 % 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:
BDBM28723
Synonyms:
2-methyl-2-[4-({[4-(trifluoromethyl)-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]formamido}methyl)phenoxy]propanoic acid | 2-methyl-2-phenoxypropanoic acid, 45
Type:
Small organic molecule
Emp. Form.:
C23H18F6N2O4S
Mol. Mass.:
532.455
SMILES:
CC(C)(Oc1ccc(CNC(=O)c2sc(nc2C(F)(F)F)-c2ccc(cc2)C(F)(F)F)cc1)C(O)=O
Structure:
Substrate