Reaction Details |
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Target | Peroxisome proliferator-activated receptor alpha |
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Ligand | BDBM24566 |
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Substrate/Competitor | BDBM10852 |
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Meas. Tech. | Cell-Based Transcription Assay |
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EC50 | 1620±340 nM |
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Comments | 100 % activation. |
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Citation | Montanari, R; Saccoccia, F; Scotti, E; Crestani, M; Godio, C; Gilardi, F; Loiodice, F; Fracchiolla, G; Laghezza, A; Tortorella, P; Lavecchia, A; Novellino, E; Mazza, F; Aschi, M; Pochetti, G Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. J Med Chem51:7768-76 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Peroxisome proliferator-activated receptor alpha |
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Name: | Peroxisome proliferator-activated receptor alpha |
Synonyms: | NR1C1 | Nuclear receptor subfamily 1 group C member 1 | PPAR | PPAR alpha/gamma | PPAR-alpha | PPARA | PPARA_HUMAN | Peroxisome Proliferator-Activated Receptor alpha | Peroxisome proliferator-activated receptor | Peroxisome proliferator-activated receptor alpha (PPAR alpha) |
Type: | Enzyme |
Mol. Mass.: | 52222.08 |
Organism: | Homo sapiens (Human) |
Description: | Q07869 |
Residue: | 468 |
Sequence: | MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
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BDBM24566 |
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BDBM10852 |
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Name | BDBM24566 |
Synonyms: | 2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)acetic acid | CHEMBL295416 | JMC515449 Compound 1 | Pirinixic acid | Wyeth 14,643 |
Type | Small organic molecule |
Emp. Form. | C14H14ClN3O2S |
Mol. Mass. | 323.798 |
SMILES | Cc1cccc(Nc2cc(Cl)nc(SCC(O)=O)n2)c1C |
Structure |
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