Target
Peroxisome proliferator-activated receptor delta
Ligand
BDBM28676
Substrate
BDBM28662
Meas. Tech.
Radioligand Binding Assay (IC50) and Cell-Based Transcription Assay (EC50)
pH
7±n/a
Temperature
295.15±n/a K
IC50
10±n/a nM
EC50
794±n/a nM
Citation
 Shearer, BGPatel, HSBillin, ANWay, JMWinegar, DALambert, MHXu, RXLeesnitzer, LMMerrihew, RVHuet, SWillson, 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 delta
Synonyms:
NR1C2 | NUC1 | NUCI | Nuclear hormone receptor 1 | Nuclear receptor subfamily 1 group C member 2 | PPAR delta | PPAR-beta | PPARB | PPARD | PPARD_HUMAN | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor beta | Peroxisome proliferator-activated receptor delta
Type:
Enzyme
Mol. Mass.:
49910.45
Organism:
Homo sapiens (Human)
Description:
Q03181
Residue:
441
Sequence:
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQMGCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKKNRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSKHIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKEISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNKDGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGDRPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRIKKTETETSLHPLLQEIYKDMY
  
Inhibitor
Name:
BDBM28676
Synonyms:
5-chloro-2-({3-[(6-methoxy-1,2,3,4-tetrahydroisoquinoline-2-)sulfonyl]benzene}amido)benzoic acid | Anthranilic acid deriv., 15
Type:
Small organic molecule
Emp. Form.:
C24H21ClN2O6S
Mol. Mass.:
500.951
SMILES:
COc1ccc2CN(CCc2c1)S(=O)(=O)c1cccc(c1)C(=O)Nc1ccc(Cl)cc1C(O)=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM28662
Synonyms:
2-[4-(3-{[2-(2-chloro-6-fluorophenyl)ethyl][(2,3-dichlorophenyl)carbamoyl]amino}propyl)phenoxy]-2-methylpropanoic acid | CHEMBL435278 | [3H]GW 2433
Type:
radiolabeled ligand
Emp. Form.:
C28H28Cl3FN2O4
Mol. Mass.:
581.89
SMILES:
CC(C)(Oc1ccc(CCCN(CCc2c(F)cccc2Cl)C(=O)Nc2cccc(Cl)c2Cl)cc1)C(O)=O
Structure:
Search PDB for entries with ligand similarity: