Reaction Details Report a problem with these data
Target
Peroxisome proliferator-activated receptor delta
Ligand
BDBM29882
Substrate
BDBM28662
Meas. Tech.
Scintillation Proximity Assay (Ki) and Cell-Based Transcription Assay (EC50)
Ki
0.6±n/a nM
EC50
2000±n/a nM
Citation
Connors, RV; Wang, Z; Harrison, M; Zhang, A; Wanska, M; Hiscock, S; Fox, B; Dore, M; Labelle, M; Sudom, A; Johnstone, S; Liu, J; Walker, NP; Chai, A; Siegler, K; Li, Y; Coward, P Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma. Bioorg Med Chem Lett 19:3550-4 (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:
Human
Description:
Q03181
Residue:
441
Sequence:
MEQPQEEAPEVREEEEKEEVAEAEGAPELNGGPQHALPSSSYTDLSRSSSPPSLLDQLQMGCDGASCGSLNMECRVCGDKASGFHYGVHACEGCKGFFRRTIRMKLEYEKCERSCKIQKKNRNKCQYCRFQKCLALGMSHNAIRFGRMPEAEKRKLVAGLTANEGSQYNPQVADLKAFSKHIYNAYLKNFNMTKKKARSILTGKASHTAPFVIHDIETLWQAEKGLVWKQLVNGLPPYKEISVHVFYRCQCTTVETVRELTEFAKSIPSFSSLFLNDQVTLLKYGVHEAIFAMLASIVNKDGLLVANGSGFVTREFLRSLRKPFSDIIEPKFEFAVKFNALELDDSDLALFIAAIILCGDRPGLMNVPRVEAIQDTILRALEFHLQANHPDAQYLFPKLLQKMADLRQLVTEHAQMMQRIKKTETETSLHPLLQEIYKDMY
Inhibitor
Name:
BDBM29882
Synonyms:
alkynyl ether, 24
Type:
Small organic molecule
Emp. Form.:
C31H29F3O6S
Mol. Mass.:
586.619
SMILES:
OCCC#CCOc1cc(COc2ccc(cc2)C(F)(F)F)ccc1Sc1ccc(OCC(O)=O)c2CCCCc12
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