General Information of the Protein
Protein ID
PT01919
Protein Name
Peroxisome proliferator-activated receptor alpha
Secondarily
Protein Name
Nuclear receptor subfamily 1 group C member 1
Gene Name
PPARA
Secondarily
Gene Name
Nr1c1
Ppar
Sequence
MVDTESPICPLSPLEADDLESPLSEEFLQEMGNIQEISQSIGEESSGSFGFADYQYLGSCPGSEGSVITDTLSPASSPSSVSCPVIPASTDESPGSALNIECRICGDKASGYHYGVHACEGCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSEKAKLKAEILTCEHDLKDSETADLKSLGKRIHEAYLKNFNMNKVKARVILAGKTSNNPPFVIHDMETLCMAEKTLVAKMVANGVEDKEAEVRFFHCCQCMSVETVTELTEFAKAIPGFANLDLNDQVTLLKYGVYEAIFTMLSSLMNKDGMLIAYGNGFITREFLKNLRKPFCDIMEPKFDFAMKFNALELDDSDISLFVAAIICCGDRPGLLNIGYIEKLQEGIVHVLKLHLQSNHPDDTFLFPKLLQKMVDLRQLVTEHAQLVQVIKKTESDAALHPLLQEIYRDMY
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Organism
Mus musculus, Mouse
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 1
>
Nuclear hormone receptor subfamily 1 group C
>
Nuclear hormone receptor subfamily 1 group C member 1
Function
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as a transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2.
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Uniprot ID
P23204
Ensembl ID
ENSG00000186951
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0450938
2-[4-[3-[4-[(4-methoxyphenyl)methyl]-1-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C31H35N3O5
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0538367
2-[4-[3-[1,4-bis[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
   Show/Hide
C31H35N3O4
 1
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
CP0170396
2-{[4-(2-{[(2,4-difluorophenyl)carbamoyl](heptyl)amino}ethyl)phenyl]sulfanyl}-2-methylpropanoic acid
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C26H34F2N2O3S
 1
1
EC50 = 5 nM
   TI
   LI
   LO
   TS
CP0397728
2-(4-{2-[3-(2,4-Difluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-propionic acid
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C26H34F2N2O4
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0450936
2-[4-[3-[4-[(4-chlorophenyl)methyl]-1-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C30H32ClN3O4
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0568641
2-[4-[3-[4-[(4-fluorophenyl)methyl]-1-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C30H32FN3O4
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0450935
2-[4-[3-[4-[(3-methoxyphenyl)methyl]-1-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C31H35N3O5
 1
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
CP0450937
2-[4-[3-[1-[(4-ethenylphenyl)methyl]-4-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C32H35N3O4
 1
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
CP0551890
2-[4-[3-[4-benzyl-1-[(4-methylphenyl)methyl]-5-oxo-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methylpropanoic acid
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C30H33N3O4
 1
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
CP0372746
5-[4-[2-(3,4-dimethylphenyl)-5-methyl-1,3-oxazol-4-yl]butyl]-2-methyl-1,3-dioxane-2-carboxylic acid
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C22H29NO5
 1
1
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0372747
(2s,5s)-2-methyl-5-(4-(5-methyl-2-p-tolyloxazol-4-yl)butyl)-1,3-dioxane-2-carboxylic acid
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C21H27NO5
 1
1
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0538368
2-methyl-2-[4-[3-[1-[(4-methylphenyl)methyl]-5-oxo-4-[(3,4,5-trimethoxyphenyl)methyl]-1,2,4-triazol-3-yl]propyl]phenoxy]propanoic acid
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C33H39N3O7
 1
1
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0374670
2-(4-{2-[3-(4-Fluoro-phenyl)-1-heptyl-ureido]-ethyl}-phenoxy)-2-methyl-propionic acid
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C26H35FN2O4
 1
1
EC50 = 33 nM
   TI
   LI
   LO
   TS
CP0403631
2-(4-{2-[1-(5-Cyclohexyl-pentyl)-3-(4-fluoro-phenyl)-ureido]-ethyl}-phenoxy)-2-methyl-propionic acid
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C30H41FN2O4
 1
1
EC50 = 53 nM
   TI
   LI
   LO
   TS
CP0372745
5-[4-[2-(3-fluoro-4-methylphenyl)-5-methyl-1,3-oxazol-4-yl]butyl]-2-methyl-1,3-dioxane-2-carboxylic acid
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C21H26FNO5
 1
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
CP0404578
2-(4-{2-[1-Cycloheptyl-3-(2,4-difluoro-phenyl)-ureido]-ethyl}-phenoxy)-2-methyl-propionic acid
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C26H32F2N2O4
 1
1
EC50 = 120 nM
   TI
   LI
   LO
   TS
CP0439850
2-[4-[[1-methyl-6-(1-phenylpropylcarbamoyl)-2-propylindol-3-yl]methyl]phenyl]benzoic acid
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C36H36N2O3
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0432278
2-[4-[[6-(1-phenylpropylcarbamoyl)-2-propyl-1H-indol-3-yl]methyl]phenyl]benzoic acid
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C35H34N2O3
 1
1
EC50 = 790 nM
   TI
   LI
   LO
   TS
CP0422670
2-methyl-5-[4-(5-methyl-2-phenyl-1,3-oxazol-4-yl)butyl]-1,3-dioxane-2-carboxylic acid
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C20H25NO5
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0429811
4'-((2,3-dimethyl-5-(1-phenylpropylcarbamoyl)-1H-indol-1-yl)methyl)biphenyl-2-carboxylic acid
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C34H32N2O3
 1
1
EC50 = 5510 nM
   TI
   LI
   LO
   TS
CP0083167
4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid
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C33H30N4O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0447683
4'-((6-(1-phenylpropylcarbamoyl)-2-propyl-1H-benzo[d]imidazol-1-yl)methyl)biphenyl-2-carboxylic acid
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C34H33N3O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0380009
2-[4-[[2-propyl-5-(1-propylbenzimidazol-2-yl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl]benzoic acid
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C34H32N4O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0380010
2-[4-[[5-(1-butylbenzimidazol-2-yl)-2-propylindazol-3-yl]methyl]phenyl]benzoic acid
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C35H34N4O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0421159
2-propyl-5-(1-propylbenzimidazol-2-yl)-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-a]pyridine
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C34H32N8
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0425898
N-(1-phenylpropyl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrazolo[1,5-a]pyridine-5-carboxamide
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C34H33N7O
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0430042
2-[4-[[5-(1-phenylpropylcarbamoyl)-2-propylindazol-3-yl]methyl]phenyl]benzoic acid
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C34H33N3O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0432277
5-(1-butylbenzimidazol-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]indazole
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C35H34N8
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0432279
2-[4-[[5-(1-phenylpropylcarbamoyl)-2-propylpyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl]benzoic acid
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C34H33N3O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0437799
2-[4-[[5-(1-phenylpropylcarbamoyl)-2-propyl-1H-indol-3-yl]methyl]phenyl]benzoic acid
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C35H34N2O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0439849
2-[4-[[1-methoxy-5-(1-phenylpropylcarbamoyl)-2-propylindol-3-yl]methyl]phenyl]benzoic acid
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C36H36N2O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0042877
2-(4-(4-Chlorobenzoyl)phenoxy)-2-methylpropionic acid
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C17H15ClO4
 1
1
EC50 = 18000 nM
   TI
   LI
   LO
   TS
CP0112318
2-(4-chlorophenoxy)-2-methylpropanoic acid
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C10H11ClO3
 2
1
EC50 = 50000 nM
   TI
   LI
   LO
   TS
2
EC50 = 51000 nM
   TI
   LI
   LO
   TS
CP0154373
4-[4-(4-Chloro-phenoxy)-phenyl]-4-oxo-butyric acid
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C16H13ClO4
 1
1
EC50 = 80000 nM
   TI
   LI
   LO
   TS
CP0015504
2-(4-{2-[(4-chlorophenyl)formamido]ethyl}phenoxy)-2-methylpropanoic acid
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C19H20ClNO4
 1
1
EC50 = 90000 nM
   TI
   LI
   LO
   TS
CP0378531
(S)-2-(5-(3-((2-(4-ethylphenyl)-5-methylpyrimidin-4-yl)(methyl)amino)propoxy)-2,3-dihydro-1H-inden-1-yl)acetic acid
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C28H33N3O3
 1
1
IC50 = 670 nM
   TI
   LI
   LO
   TS
CP0427747
(S)-2-(5-(3-((2-(4-isopropylphenyl)-5-methylpyrimidin-4-yl)(methyl)amino)propoxy)-2,3-dihydro-1H-inden-1-yl)acetic acid
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C29H35N3O3
 1
1
IC50 = 2530 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0257810
(2S)-3-phenyl-2-(4-phenylphenoxy)propanoic acid
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C21H18O3
 1
1 EC50 = 0.2 nM
CP0012720
2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)acetic acid
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C14H14ClN3O2S
 2
1 EC50 = 40 nM
2 Ki = 100 nM
CP0112318
2-(4-chlorophenoxy)-2-methylpropanoic acid
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C10H11ClO3
 1
1 EC50 = 42 nM
CP0150880
2-{[(3-{[2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]methoxy}phenyl)methyl](methoxycarbonyl)amino}acetic acid
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C22H21ClN2O6
 1
1 EC50 = 426 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00695 Peroxisome proliferator-activated receptor alpha Mesocricetus auratus, Golden hamster
PT03261 Peroxisome proliferator-activated receptor alpha Rattus norvegicus, Rat