Reaction Details
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Peroxisome proliferator-activated receptor delta
Ligand
BDBM28731
Substrate
BDBM10852
Meas. Tech.
Cell-Based Transcription Assay
EC50
138±n/a nM
Comments
EC50s of the compound are >1 uM in PPARalpha and PPARgamma assays.
Citation
Zhang, R; Deangelis, A; Wang, A; Sieber-McMaster, E; Li, X; Russell, R; Pelton, P; Xu, J; Zhu, P; Zhou, L; Demarest, K; Murray, WV; Kuo, GH Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists. Bioorg Med Chem Lett 19:1101-4 (2009) [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:
BDBM28731
Synonyms:
2-(4-{[2-(2,4-dichlorophenoxymethyl)prop-2-en-1-yl]sulfanyl}-2-methylphenoxy)acetic acid | para-alkylthiophenoxyacetic acid, 9
Type:
Small organic molecule
Emp. Form.:
C19H18Cl2O4S
Mol. Mass.:
413.315
SMILES:
Cc1cc(SCC(=C)COc2ccc(Cl)cc2Cl)ccc1OCC(O)=O
Structure:
Substrate