Reaction Details
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Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28759
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
220±20 nM
Comments
100 +/- 9.5 % of maximal activation compared to Wy 14,643 normalized to 100%.
Citation
Montanari, R; Saccoccia, F; Scotti, E; Crestani, M; Godio, C; Gilardi, F; Loiodice, F; Fracchiolla, G; Laghezza, A; Tortorella, P; Lavecchia, A; Novellino, E; Mazza, F; Aschi, M; Pochetti, G Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. J Med Chem 51:7768-76 (2008) [PubMed] Article More Info.:
Target
Name:
Peroxisome proliferator-activated receptor alpha
Synonyms:
Peroxisome proliferator-activated receptor | PPAR-alpha | Nuclear receptor subfamily 1 group C member 1 | PPAR alpha/gamma | Peroxisome Proliferator-Activated Receptor alpha | Peroxisome proliferator-activated receptor alpha (PPAR alpha) | PPARA_HUMAN | PPARA | NR1C1 | PPAR
Type:
Enzyme
Mol. Mass.:
52222.08
Organism:
Human
Description:
Q07869
Residue:
468
Sequence:
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSCPGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFVIHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDIFLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
Inhibitor
Name:
BDBM28759
Synonyms:
CHEMBL191275 | (2S)-3-phenyl-2-(4-phenylphenoxy)propanoic acid | LT175 (S-1)
Type:
Small organic molecule
Emp. Form.:
C21H18O3
Mol. Mass.:
318.13
SMILES:
OC(=O)[C@H](Cc1ccccc1)Oc1ccc(cc1)-c1ccccc1 |r|
Structure:
Substrate