General Information of the Protein
Protein ID
PT02793
Protein Name
Free fatty acid receptor 1
Secondarily
Protein Name
G-protein coupled receptor 40
Gene Name
FFAR1
Secondarily
Gene Name
GPR40
Sequence
MDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLPLKAVEALASGAWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRPCYSWGVCAAIWALVLCHLGLVFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAGPARFSLSLLLFFLPLAITAFCYVGCLRALARSGLTHRRKLRAAWVAGGALLTLLLCVGPYNASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLGRGPGLKTVCAARTQGGKSQK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
>
Free fatty acid receptor
Function
G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation (By similarity). Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.
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Uniprot ID
Primary ID:
O14842

Secondarily ID:
Q0VAS2
Q4VBL4
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HGNC ID
HGNC:4498
Subcellular Location
Cell membrane
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: CL000094 , 1321N1
Compound ID Compound Name Compound Formula
CP0058022
3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
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C19H14FNO2
 1
1
EC50 = 5.888 nM
   TI
   LI
   LO
   TS
CP0449573
3-{4-[(2',6'-Dimethylbiphenyl-3-yl)methoxy]-2-fluorophenyl}propanoic Acid
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C24H23FO3
 1
1
EC50 = 6.026 nM
   TI
   LI
   LO
   TS
CP0104146
2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid
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C29H32O7S
 2
1
EC50 = 14.13 nM
   TI
   LI
   LO
   TS
2
EC50 = 57.54 nM
   TI
   LI
   LO
   TS
CP0164260
3-(4(2'-Methylbiphenyl-3-ylmethylamino)phenyl)propanoic acid
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C23H23NO2
 4
1
EC50 = 14.79 nM
   TI
   LI
   LO
   TS
2
EC50 = 18.62 nM
   TI
   LI
   LO
   TS
3
EC50 = 34.67 nM
   TI
   LI
   LO
   TS
4
EC50 = 44.67 nM
   TI
   LI
   LO
   TS
CP0465295
3-[4-[2-(5-cyano-2-methylphenyl)ethynyl]-2-fluorophenyl]propanoic acid
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C19H14FNO2
 1
1
EC50 = 16.98 nM
   TI
   LI
   LO
   TS
CP0490943
3-[4-[2-[2-(2-cyanoethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
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C20H16FNO2
 1
1
EC50 = 18.2 nM
   TI
   LI
   LO
   TS
CP0490946
3-[4-[2-[2-(difluoromethyl)-5-fluorophenyl]ethynyl]-2-fluorophenyl]propanoic acid
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C18H12F4O2
 1
1
EC50 = 18.2 nM
   TI
   LI
   LO
   TS
CP0153669
3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]phenyl]propanoic acid
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C19H15NO2
 1
1
EC50 = 19.95 nM
   TI
   LI
   LO
   TS
CP0397768
3-[2-fluoro-4-[2-(3-methylphenyl)ethynyl]phenyl]propanoic acid
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C18H15FO2
 1
1
EC50 = 22.39 nM
   TI
   LI
   LO
   TS
CP0136178
3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid
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C22H21NO3
 3
1
EC50 = 28.84 nM
   TI
   LI
   LO
   TS
2
EC50 = 47.86 nM
   TI
   LI
   LO
   TS
3
EC50 = 87.1 nM
   TI
   LI
   LO
   TS
CP0380970
3-[2-fluoro-4-[2-(2-methylphenyl)ethynyl]phenyl]propanoic acid
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C18H15FO2
 1
1
EC50 = 33.11 nM
   TI
   LI
   LO
   TS
CP0381646
3-[2-fluoro-4-(2-phenylethynyl)phenyl]propanoic acid
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C17H13FO2
 1
1
EC50 = 35.48 nM
   TI
   LI
   LO
   TS
CP0404322
3-[2-fluoro-4-[(E)-3-methylpent-3-en-1-ynyl]phenyl]propanoic acid
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C15H15FO2
 1
1
EC50 = 37.15 nM
   TI
   LI
   LO
   TS
CP0465293
3-[4-[2-(3,5-dichlorophenyl)ethynyl]-2-fluorophenyl]propanoic acid
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C17H11Cl2FO2
 1
1
EC50 = 38.02 nM
   TI
   LI
   LO
   TS
CP0191758
3-[4-[2-(2,6-dichloropyridin-4-yl)ethynyl]phenyl]propanoic acid
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C16H11Cl2NO2
 1
1
EC50 = 40.74 nM
   TI
   LI
   LO
   TS
CP0438286
2-[4-[2-(2,6-dichloropyridin-4-yl)ethynyl]phenyl]cyclopropane-1-carboxylic acid
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C17H11Cl2NO2
 1
1
EC50 = 42.66 nM
   TI
   LI
   LO
   TS
CP0551218
3-[4-[2-(3-methylphenyl)ethynyl]phenyl]propanoic acid
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C18H16O2
 1
1
EC50 = 43.65 nM
   TI
   LI
   LO
   TS
CP0512532
3-[4-[2-(2,6-dichloro-3-methylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C17H13Cl2NO2
 1
1
EC50 = 43.65 nM
   TI
   LI
   LO
   TS
CP0085623
3-(4-(o-Tolylethynyl)phenyl)propanoic acid
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C18H16O2
 1
1
EC50 = 45.71 nM
   TI
   LI
   LO
   TS
CP0472040
3-[2-fluoro-4-[(Z)-pent-3-en-1-ynyl]phenyl]propanoic acid
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C14H13FO2
 1
1
EC50 = 47.86 nM
   TI
   LI
   LO
   TS
CP0372137
3-{4-[(2'-Methylbiphenyl-3-yl)methoxy]phenyl}propanic Acid
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C23H22O3
 4
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
2
EC50 = 81.28 nM
   TI
   LI
   LO
   TS
3
EC50 = 263.03 nM
   TI
   LI
   LO
   TS
4
EC50 = 562.34 nM
   TI
   LI
   LO
   TS
CP0406065
3-[4-[(3-phenylphenyl)methylamino]phenyl]propanoic acid
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C22H21NO2
 1
1
EC50 = 53.7 nM
   TI
   LI
   LO
   TS
CP0404981
3-{4-[(3-Phenoxybenzyl)oxy]phenyl}propanoic Acid
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C22H20O4
 1
1
EC50 = 57.54 nM
   TI
   LI
   LO
   TS
CP0466760
3-[4-[2-(3-nitrophenyl)ethynyl]phenyl]propanoic acid
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C17H13NO4
 1
1
EC50 = 58.88 nM
   TI
   LI
   LO
   TS
CP0899211
3-(4-(2'-Methoxybiphenyl-3-ylmethylamino)phenyl)propanoic acid
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C23H23NO3
 1
1
EC50 = 69.18 nM
   TI
   LI
   LO
   TS
CP0466758
3-[4-[2-(3,5-dimethylphenyl)ethynyl]phenyl]propanoic acid
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C19H18O2
 1
1
EC50 = 74.13 nM
   TI
   LI
   LO
   TS
CP0490949
3-[4-[2-[3-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
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C19H14FNO2
 1
1
EC50 = 74.13 nM
   TI
   LI
   LO
   TS
CP0484686
3-[4-[2-(3-methylthiophen-2-yl)ethynyl]phenyl]propanoic acid
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C16H14O2S
 1
1
EC50 = 75.86 nM
   TI
   LI
   LO
   TS
CP0458355
3-[4-[2-(7-chloroquinolin-4-yl)ethynyl]phenyl]propanoic acid
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C20H14ClNO2
 1
1
EC50 = 79.43 nM
   TI
   LI
   LO
   TS
CP0380317
3-[2-fluoro-4-(3-methylbut-3-en-1-ynyl)phenyl]propanoic acid
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C14H13FO2
 1
1
EC50 = 81.28 nM
   TI
   LI
   LO
   TS
CP0425922
3-[4-[[3-(trifluoromethyl)phenyl]methoxy]phenyl]propanoic acid
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C17H15F3O3
 1
1
EC50 = 83.18 nM
   TI
   LI
   LO
   TS
CP0380331
3-[4-(3,4-dimethylpent-3-en-1-ynyl)phenyl]propanoic acid
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C16H18O2
 1
1
EC50 = 83.18 nM
   TI
   LI
   LO
   TS
CP0489790
3-[4-[2-[2,3-bis[(1E)-buta-1,3-dienyl]phenyl]ethynyl]phenyl]propanoic acid
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C25H22O2
 1
1
EC50 = 85.11 nM
   TI
   LI
   LO
   TS
CP0489789
3-[4-[2-(2,3-dimethylphenyl)ethynyl]phenyl]propanoic acid
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C19H18O2
 1
1
EC50 = 87.1 nM
   TI
   LI
   LO
   TS
CP0891615
5-(4-(3-chloro-5-(trifluoromethyl)pyridin-2-yloxy)-2-methylbenzyl)thiazolidine-2,4-dione
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C17H12ClF3N2O3S
 2
1
EC50 = 87.1 nM
   TI
   LI
   LO
   TS
2
EC50 = 177.83 nM
   TI
   LI
   LO
   TS
CP0386248
3-[4-[2-[3-(trifluoromethyl)phenyl]ethynyl]phenyl]propanoic acid
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C18H13F3O2
 1
1
EC50 = 89.13 nM
   TI
   LI
   LO
   TS
CP0377499
3-[4-[(3-bromophenyl)methoxy]phenyl]propanoic acid
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C16H15BrO3
 1
1
EC50 = 89.13 nM
   TI
   LI
   LO
   TS
CP0386246
3-[4-[2-(3-cyanophenyl)ethynyl]phenyl]propanoic acid
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C18H13NO2
 1
1
EC50 = 91.2 nM
   TI
   LI
   LO
   TS
CP0179633
AMG-837
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C26H21F3O3
 2
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
2
EC50 = 169.82 nM
   TI
   LI
   LO
   TS
CP0519864
3-[4-[2-(4-methylphenyl)ethynyl]phenyl]propanoic acid
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C18H16O2
 1
1
EC50 = 107.15 nM
   TI
   LI
   LO
   TS
CP0372131
3-{4-[(2'-Methoxybiphenyl-3-yl)methoxy]phenyl}propanoic Acid
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C23H22O4
 1
1
EC50 = 120.23 nM
   TI
   LI
   LO
   TS
CP0458356
3-[4-[2-(2-fluoro-3-methylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C17H14FNO2
 1
1
EC50 = 120.23 nM
   TI
   LI
   LO
   TS
CP0896618
3-(4-(4'-Methylbiphenyl-3-ylmethylamino)phenyl)propanoic acid
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C23H23NO2
 1
1
EC50 = 125.89 nM
   TI
   LI
   LO
   TS
CP0352619
3-[4-(Biphenyl-3-ylmethoxy)phenyl]propanoic Acid
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C22H20O3
 1
1
EC50 = 134.9 nM
   TI
   LI
   LO
   TS
CP0488310
3-[4-[2-(2-chloro-3-methylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C17H14ClNO2
 1
1
EC50 = 134.9 nM
   TI
   LI
   LO
   TS
CP0381647
3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]propanoic acid
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C17H12F2O2
 1
1
EC50 = 141.25 nM
   TI
   LI
   LO
   TS
CP0375419
3-[3-fluoro-4-(2-phenylethynyl)phenyl]propanoic acid
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C17H13FO2
 1
1
EC50 = 144.54 nM
   TI
   LI
   LO
   TS
CP0439407
3-[4-[2-(3-ethynylphenyl)ethynyl]phenyl]propanoic acid
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C19H14O2
 1
1
EC50 = 154.88 nM
   TI
   LI
   LO
   TS
CP0377498
3-(4-{[(3-bromophenyl)methyl]amino}phenyl)propanoic acid
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C16H16BrNO2
 1
1
EC50 = 173.78 nM
   TI
   LI
   LO
   TS
CP0494313
3-[4-[2-(2-fluoro-5-methylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C17H14FNO2
 1
1
EC50 = 177.83 nM
   TI
   LI
   LO
   TS
CP0422154
3-(4-{[(4-phenoxyphenyl)methyl]amino}phenyl)propanoic acid
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C22H21NO3
 1
1
EC50 = 181.97 nM
   TI
   LI
   LO
   TS
CP0422117
3-[4-[[3-(trifluoromethyl)phenyl]methylamino]phenyl]propanoic acid
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C17H16F3NO2
 1
1
EC50 = 186.21 nM
   TI
   LI
   LO
   TS
CP0511567
3-[4-[2-(2-phenylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C22H17NO2
 1
1
EC50 = 186.21 nM
   TI
   LI
   LO
   TS
CP0372132
3-(4-(Phenylethynyl)phenyl)propanoic acid
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C17H14O2
 1
1
EC50 = 199.53 nM
   TI
   LI
   LO
   TS
CP0542274
3-[4-[2-(cyclohexen-1-yl)ethynyl]phenyl]propanoic acid
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C17H18O2
 1
1
EC50 = 199.53 nM
   TI
   LI
   LO
   TS
CP0404980
3-{4-[(4-Phenoxybenzyl)oxy]phenyl}propanoic Acid
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C22H20O4
 1
1
EC50 = 204.17 nM
   TI
   LI
   LO
   TS
CP0386082
3-[2-fluoro-4-[(E)-pent-3-en-1-ynyl]phenyl]propanoic acid
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C14H13FO2
 1
1
EC50 = 208.93 nM
   TI
   LI
   LO
   TS
CP0488309
3-[4-(2-thiophen-2-ylethynyl)phenyl]propanoic acid
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C15H12O2S
 1
1
EC50 = 251.19 nM
   TI
   LI
   LO
   TS
CP0511565
3-[4-[2-(2-chloropyridin-4-yl)ethynyl]phenyl]propanoic acid
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C16H12ClNO2
 1
1
EC50 = 295.12 nM
   TI
   LI
   LO
   TS
CP0394786
3-[4-[(2S)-2-methylbutoxy]phenyl]-3-phenylpropanoic acid
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C20H24O3
 1
1
EC50 = 302 nM
   TI
   LI
   LO
   TS
CP0438287
3-[4-[2-(2-chloro-3-prop-2-enylpyridin-4-yl)ethynyl]phenyl]propanoic acid
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C19H16ClNO2
 1
1
EC50 = 316.23 nM
   TI
   LI
   LO
   TS
CP0500820
3-[4-[2-(3-formylphenyl)ethynyl]phenyl]propanoic acid
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C18H14O3
 1
1
EC50 = 354.81 nM
   TI
   LI
   LO
   TS
CP0536645
3-[2-fluoro-4-[2-[3-(2-methylsulfonylethoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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C21H21FO5S
 1
1
EC50 = 363.08 nM
   TI
   LI
   LO
   TS
CP0536644
3-[2-fluoro-4-[2-[3-(3-methylsulfonylpropoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
   Show/Hide
C22H23FO5S
 1
1
EC50 = 371.54 nM
   TI
   LI
   LO
   TS
CP0380320
3-[4-(3-phenylprop-1-ynyl)phenyl]propanoic acid
   Show/Hide
C18H16O2
 1
1
EC50 = 389.05 nM
   TI
   LI
   LO
   TS
CP0404722
3-(4-{[(4-phenylphenyl)methyl]amino}phenyl)propanoic acid
   Show/Hide
C22H21NO2
 1
1
EC50 = 416.87 nM
   TI
   LI
   LO
   TS
CP0519268
3-[4-(3-methylbut-3-en-1-ynyl)phenyl]propanoic acid
   Show/Hide
C14H14O2
 1
1
EC50 = 416.87 nM
   TI
   LI
   LO
   TS
CP0380332
3-[2-fluoro-4-[(Z)-5-hydroxy-3-methylpent-3-en-1-ynyl]phenyl]propanoic acid
   Show/Hide
C15H15FO3
 1
1
EC50 = 426.58 nM
   TI
   LI
   LO
   TS
CP0416655
3-[4-[(2-bromophenyl)methoxy]phenyl]propanoic acid
   Show/Hide
C16H15BrO3
 1
1
EC50 = 446.68 nM
   TI
   LI
   LO
   TS
CP0424816
Benzyloxyphenylpropanoic acid
   Show/Hide
C16H16O3
 2
1
EC50 = 457.09 nM
   TI
   LI
   LO
   TS
2
EC50 = 831.76 nM
   TI
   LI
   LO
   TS
CP0511568
3-[4-[2-(2-phenoxypyridin-4-yl)ethynyl]phenyl]propanoic acid
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C22H17NO3
 1
1
EC50 = 478.63 nM
   TI
   LI
   LO
   TS
CP0478589
3-{4-[(4'-Methylbiphenyl-3-yl)methoxy]phenyl}propanoic Acid
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C23H22O3
 1
1
EC50 = 489.78 nM
   TI
   LI
   LO
   TS
CP0448148
3-[4-(2-cyclopentylethynyl)phenyl]propanoic acid
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C16H18O2
 1
1
EC50 = 489.78 nM
   TI
   LI
   LO
   TS
CP0527032
2-[4-[2-(3-methylphenyl)ethynyl]phenoxy]acetic acid
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C17H14O3
 1
1
EC50 = 512.86 nM
   TI
   LI
   LO
   TS
CP0484965
3-[4-[2-(2-fluoropyridin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H12FNO2
 1
1
EC50 = 512.86 nM
   TI
   LI
   LO
   TS
CP0409785
3-[4-(2-cyclohexylethynyl)phenyl]propanoic acid
   Show/Hide
C17H20O2
 1
1
EC50 = 512.86 nM
   TI
   LI
   LO
   TS
CP0422153
3-[4-[(3-cyanophenyl)methoxy]phenyl]propanoic acid
   Show/Hide
C17H15NO3
 1
1
EC50 = 524.81 nM
   TI
   LI
   LO
   TS
CP0438285
3-[4-[2-(2-methoxypyridin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H15NO3
 1
1
EC50 = 524.81 nM
   TI
   LI
   LO
   TS
CP0372138
3-[4-[(4-bromophenyl)methoxy]phenyl]propanoic acid
   Show/Hide
C16H15BrO3
 1
1
EC50 = 549.54 nM
   TI
   LI
   LO
   TS
CP0452502
3-[4-[2-(2-chloropyridin-3-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H12ClNO2
 1
1
EC50 = 602.56 nM
   TI
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CP0465294
3-[2-fluoro-4-[2-[2-(2-methylsulfonylethoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
   Show/Hide
C21H21FO5S
 1
1
EC50 = 616.6 nM
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CP0511566
3-[4-[2-(2-fluoro-5-methylpyridin-3-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H14FNO2
 1
1
EC50 = 660.69 nM
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CP0458357
3-[4-[2-(6-chloropyridin-3-yl)ethynyl]phenyl]propanoic acid
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C16H12ClNO2
 1
1
EC50 = 707.95 nM
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CP0490950
3-[2-fluoro-4-[2-[2-(3-methylsulfonylpropoxymethyl)phenyl]ethynyl]phenyl]propanoic acid
   Show/Hide
C22H23FO5S
 1
1
EC50 = 724.44 nM
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CP0406064
3-[4-(benzylamino)phenyl]propanoic acid
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C16H17NO2
 1
1
EC50 = 758.58 nM
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CP0155897
CHEBI:30805
   Show/Hide
C12H24O2
 1
1
EC50 = 758.58 nM
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CP0474329
3-[4-[2-(3-benzyl-2-chloropyridin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C23H18ClNO2
 1
1
EC50 = 794.33 nM
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CP0500819
3-[4-[2-[3-(hydroxymethyl)phenyl]ethynyl]phenyl]propanoic acid
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C18H16O3
 1
1
EC50 = 891.25 nM
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CP0378796
3-[4-(Biphenyl-4-ylmethoxy)phenyl]propanoic Acid
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C22H20O3
 1
1
EC50 = 912.01 nM
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CP0372134
3-[4-[(2-phenylphenyl)methylamino]phenyl]propanoic acid
   Show/Hide
C22H21NO2
 1
1
EC50 = 1071.52 nM
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CP0389106
3-[4-[2-[2-(2-methylphenyl)pyridin-4-yl]ethynyl]phenyl]propanoic acid
   Show/Hide
C23H19NO2
 1
1
EC50 = 1071.52 nM
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CP0439406
3-[4-[2-(3-aminophenyl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H15NO2
 1
1
EC50 = 1096.48 nM
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CP0494314
3-[4-[2-(2-methylpyridin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H15NO2
 1
1
EC50 = 1122.02 nM
   TI
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CP0439404
2-[4-(2-phenylethynyl)phenoxy]acetic acid
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C16H12O3
 1
1
EC50 = 1258.93 nM
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CP0537974
3-[2-fluoro-4-[2-[2-(methylsulfonylmethyl)phenyl]ethynyl]phenyl]propanoic acid
   Show/Hide
C19H17FO4S
 1
1
EC50 = 1445.44 nM
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CP0399330
3-(4-non-1-ynylphenyl)propanoic acid
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C18H24O2
 1
1
EC50 = 1445.44 nM
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CP0448115
3-[4-(4-phenylbut-1-ynyl)phenyl]propanoic acid
   Show/Hide
C19H18O2
 1
1
EC50 = 1819.7 nM
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CP0406070
3-[4-(Biphenyl-2-ylmethoxy)phenyl]propanoic Acid
   Show/Hide
C22H20O3
 1
1
EC50 = 1905.46 nM
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CP0489122
3-[2-fluoro-4-[2-[3-(methylsulfonylmethyl)phenyl]ethynyl]phenyl]propanoic acid
   Show/Hide
C19H17FO4S
 1
1
EC50 = 1949.84 nM
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CP0465297
3-[5-(2-phenylethynyl)pyridin-2-yl]propanoic acid
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C16H13NO2
 1
1
EC50 = 2137.96 nM
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CP0904113
3-(2-Phenylbenzofuran-5-yl)propanoic acid
   Show/Hide
C17H14O3
 1
1
EC50 = 2454.71 nM
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CP0465296
3-[6-(2-phenylethynyl)pyridin-3-yl]propanoic acid
   Show/Hide
C16H13NO2
 1
1
EC50 = 2511.89 nM
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CP0389107
3-[4-[2-(2-chloro-6-methylpyrimidin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H13ClN2O2
 1
1
EC50 = 2754.23 nM
   TI
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CP0871669
3-(4-(1-Phenylethoxy)phenyl)propanoic acid
   Show/Hide
C17H18O3
 1
1
EC50 = 3311.31 nM
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CP0915398
3-(4-phenethylphenyl)propanoic acid
   Show/Hide
C17H18O2
 1
1
EC50 = 3630.78 nM
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CP0439334
2-[4-[2-(2-methylphenyl)ethynyl]phenoxy]acetic acid
   Show/Hide
C17H14O3
 1
1
EC50 = 3715.35 nM
   TI
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CP0438288
3-[4-[2-(1,3-thiazol-5-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C14H11NO2S
 1
1
EC50 = 3890.45 nM
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CP0438290
3-[4-(2-pyridin-4-ylethynyl)phenyl]propanoic acid
   Show/Hide
C16H13NO2
 1
1
EC50 = 4073.8 nM
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CP0389108
3-[4-[2-(2-chloro-5-methylpyrimidin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H13ClN2O2
 1
1
EC50 = 4265.8 nM
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CP0399329
3-[4-(2-cyclopropylethynyl)phenyl]propanoic acid
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C14H14O2
 1
1
EC50 = 5011.87 nM
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CP0431040
2-[4-[2-(3-hydroxyphenyl)ethynyl]phenoxy]acetic acid
   Show/Hide
C16H12O4
 1
1
EC50 = 5623.41 nM
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CP0484619
3-[4-(2-pyridin-3-ylethynyl)phenyl]propanoic acid
   Show/Hide
C16H13NO2
 1
1
EC50 = 6025.6 nM
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CP0484966
3-[4-[2-(6-methylpyridin-2-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H15NO2
 1
1
EC50 = 6165.95 nM
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CP0906521
3-(4-(Phenoxymethyl)phenyl)propanoic acid
   Show/Hide
C16H16O3
 1
1
EC50 = 6309.57 nM
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CP0454906
4-fluoro-3-[(4-fluoro-1H-indol-3-yl)methyl]-1H-indole
   Show/Hide
C17H12F2N2
 1
1
EC50 = 6490 nM
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CP0393694
3-[1-(1H-indol-3-yl)butyl]-1H-indole
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C20H20N2
 1
1
EC50 = 8810 nM
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CP0404753
3-[1-(1H-indol-3-yl)-2-methylpropyl]-1H-indole
   Show/Hide
C20H20N2
 1
1
EC50 = 8890 nM
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CP0452501
3-[4-[2-(2-chloropyrimidin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C15H11ClN2O2
 1
1
EC50 = 9120.11 nM
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CP0452500
3-[4-[2-(2-methoxypyrimidin-4-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H14N2O3
 1
1
EC50 = 9549.93 nM
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CP0438289
3-[4-[2-(3-nitropyridin-2-yl)ethynyl]phenyl]propanoic acid
   Show/Hide
C16H12N2O4
 1
1
EC50 = 10964.78 nM
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CP0871670
3-(4-(Benzyloxy)-3-iodophenyl)propanoic acid
   Show/Hide
C16H15IO3
 1
1
EC50 = 12589.25 nM
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CP0452503
3-[4-(2-pyridin-2-ylethynyl)phenyl]propanoic acid
   Show/Hide
C16H13NO2
 1
1
EC50 = 13182.57 nM
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CP0878046
3-(4-(Phenylaminomethyl)phenyl)propanoic acid
   Show/Hide
C16H17NO2
 1
1
EC50 = 21379.62 nM
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CP0472042
3-(4-ethynylphenyl)propanoic acid
   Show/Hide
C11H10O2
 1
1
EC50 > 100000 nM
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CP0380330
3-[4-[2-(1-hydroxycyclohexyl)ethynyl]phenyl]propanoic acid
   Show/Hide
C17H20O3
 1
1
EC50 < 100000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0098493
CHEMBL4457303
   Show/Hide
C27H32F2O4
 1
1 EC50 = 3.7 nM
CP0179633
AMG-837
   Show/Hide
C26H21F3O3
 2
1 EC50 = 13 nM
2 EC50 = 23 nM
CP0104146
2-[(3S)-6-[[3-[2,6-dimethyl-4-(3-methylsulfonylpropoxy)phenyl]phenyl]methoxy]-2,3-dihydro-1-benzofuran-3-yl]acetic acid
   Show/Hide
C29H32O7S
 1
1 EC50 = 53 nM
CP0352619
3-[4-(Biphenyl-3-ylmethoxy)phenyl]propanoic Acid
   Show/Hide
C22H20O3
 1
1 EC50 = 75 nM
CP0013323
(3S)-3-[4-[[4-(spiro[indene-1,4'-piperidine]-1'-ylmethyl)phenyl]methoxy]phenyl]hex-4-ynoic acid
   Show/Hide
C33H33NO3
 1
1 EC50 = 233 nM
CP0136178
3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid
   Show/Hide
C22H21NO3
 1
1 EC50 = 316.23 nM
CP0384165
CHEMBL4591657
   Show/Hide
C26H31FO4
 1
1 EC50 = 1370 nM
CP0030287
(4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoic acid
   Show/Hide
C22H32O2
 1
1 EC50 = 11700 nM
CP0032783
3-[4-[[3-[4-(1,1-dioxothian-4-yl)oxy-2,6-dimethylphenyl]phenyl]methoxy]-2-fluorophenyl]propanoic acid
   Show/Hide
C29H31FO6S
 1
1 Ki = 16 nM
Clinical Information about the Protein
Target 1 ( Free fatty acid receptor 1 (GPR40) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Type-2 diabetes [ICD-11: 5A11]
2 Idiopathic pulmonary fibrosis [ICD-11: CB03.4]
3 Type 2 diabetes [ICD-11: 5A11]
4 Non-insulin dependent diabetes [ICD-11: 5A11]
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 TAK-875 Phase 3
Type-2 diabetes
2 PBI-4050 Phase 2
Idiopathic pulmonary fibrosis
3 LY-2881835 Phase 1
Type-2 diabetes
4 LY2922470 Phase 1
Type 2 diabetes
Investigative Drug(s) 1 Investigative Drug  1
1 TUG-469 Investigative
Non-insulin dependent diabetes
Preclinical Drug(s) 2 Preclinical Drugs  2
1 BMS-986118 Preclinical
Type 2 diabetes
2 DS-1558 Preclinical
Type 2 diabetes
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02522 Free fatty acid receptor 1 Rattus norvegicus, Rat
PT04613 Free fatty acid receptor 1 Mus musculus, Mouse