Reaction Details
Report a problem with these data
Report a problem with these dataTarget
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM24566
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
1620±340 nM
Comments
100 % activation.
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:
BDBM24566
Synonyms:
JMC515449 Compound 1 | Wyeth 14,643 | 2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)acetic acid | CHEMBL295416 | Pirinixic acid
Type:
Small organic molecule
Emp. Form.:
C14H14ClN3O2S
Mol. Mass.:
323.05
SMILES:
Cc1cccc(c1C)Nc2cc(nc(n2)SCC(=O)O)Cl
Substrate
