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Target
Peroxisome proliferator-activated receptor delta
Ligand
BDBM28670
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
5±n/a nM
EC50
158±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 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:
BDBM28670
Synonyms:
4-bromo-2-{[3-(1,2,3,4-tetrahydroisoquinoline-2-sulfonyl)benzene]amido}benzoic acid | Anthranilic acid deriv., 8
Type:
Small organic molecule
Emp. Form.:
C23H19BrN2O5S
Mol. Mass.:
515.376
SMILES:
OC(=O)c1ccc(Br)cc1NC(=O)c1cccc(c1)S(=O)(=O)N1CCc2ccccc2C1
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: