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Target
Peroxisome proliferator-activated receptor delta
Ligand
BDBM28774
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
50±n/a nM
Comments
76% efficacy.
Citation
Epple, R; Azimioara, M; Russo, R; Xie, Y; Wang, X; Cow, C; Wityak, J; Karanewsky, D; Bursulaya, B; Kreusch, A; Tuntland, T; Gerken, A; Iskandar, M; Saez, E; Martin Seidel, H; Tian, SS 3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2. Bioorg Med Chem Lett 16:5488-92 (2006) [PubMed] Article
More Info.:
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:
BDBM28774
Synonyms:
2-[3-(4-{[2-(2,4-dichlorophenoxy)ethyl]carbamoyl}-5-(2-methylphenyl)-1,2-oxazol-3-yl)phenyl]acetic acid | trisubstituted isoxazole, 17i
Type:
Small organic molecule
Emp. Form.:
C27H22Cl2N2O5
Mol. Mass.:
525.38
SMILES:
Cc1ccccc1-c1onc(c1C(=O)NCCOc1ccc(Cl)cc1Cl)-c1cccc(CC(O)=O)c1
Substrate