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Target
Peroxisome proliferator-activated receptor alpha
Ligand
BDBM28661
Substrate
BDBM28680
Meas. Tech.
Radioligand Binding Assay
pH
7±n/a
Temperature
295.15±n/a K
IC50
1995±n/a nM
Citation
 Shearer, BG; Patel, HS; Billin, AN; Way, JM; Winegar, DA; Lambert, MH; Xu, RX; Leesnitzer, LM; Merrihew, RV; Huet, S; Willson, TM Discovery of a novel class of PPARdelta partial agonists. Bioorg Med Chem Lett 18:5018-22 (2008) [PubMed]  Article 
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:
BDBM28661
Synonyms:
2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | CHEMBL38943 | GW 501516 | GW-501516 | GW1516 | GW501516
Type:
Small organic molecule
Emp. Form.:
C21H18F3NO3S2
Mol. Mass.:
453.498
SMILES:
Cc1nc(sc1CSc1ccc(OCC(O)=O)c(C)c1)-c1ccc(cc1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM28680
Synonyms:
2-[4-(2-{[(2,4-difluorophenyl)carbamoyl](heptyl)amino}ethyl)phenoxy]-2-methylbutanoic acid | CHEMBL195510 | GW 2331 | [3H]GW 2331
Type:
radiolabeled ligand
Emp. Form.:
C27H36F2N2O4
Mol. Mass.:
490.5825
SMILES:
CCCCCCCN(CCc1ccc(OC(C)(CC)C(O)=O)cc1)C(=O)Nc1ccc(F)cc1F
Structure:
Search PDB for entries with ligand similarity: