Reaction Details
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Peroxisome proliferator-activated receptor alpha
Ligand
BDBM50030474
Substrate
n/a
Meas. Tech.
ChEMBL_1724601 (CHEMBL4139879)
EC50
10000±n/a nM
Citation
Pirat, C; Dacquet, C; Leclerc, V; Hennuyer, N; Beucher-Gaudin, M; Zanirato, G; Géant, A; Staels, B; Ktorza, A; Farce, A; Caignard, DH; Berthelot, P; Lebegue, N Anti-diabetic activity of fused PPAR?-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression. Eur J Med Chem 137:310-326 (2017) [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:
BDBM50030474
Synonyms:
Avandamet | Avandaryl | Avandia | BRL-49653 | CHEBI:50122 | Rosiglitazone | US10744117, Compound Rosiglitazone | US9562012, rosiglitazone
Type:
Small organic molecule
Emp. Form.:
C18H19N3O3S
Mol. Mass.:
357.427
SMILES:
CN(CCOc1ccc(CC2SC(=O)NC2=O)cc1)c1ccccn1
Structure:
