General Information of the Protein
Protein ID
PT04613
Protein Name
Free fatty acid receptor 1
Secondarily
Protein Name
G-protein coupled receptor 40
Gene Name
FFAR1
Secondarily
Gene Name
Gpr40
Sequence
MDLPPQLSFALYVSAFALGFPLNLLAIRGAVSHAKLRLTPSLVYTLHLGCSDLLLAITLPLKAVEALASGAWPLPLPFCPVFALAHFAPLYAGGGFLAALSAGRYLGAAFPFGYQAIRRPRYSWGVCVAIWALVLCHLGLALGLETSGSWLDNSTSSLGINIPVNGSPVCLEAWDPDSARPARLSFSILLFFLPLVITAFCYVGCLRALVRSGLSHKRKLRAAWVAGGALLTLLLCLGPYNASNVASFINPDLGGSWRKLGLITGAWSVVLNPLVTGYLGTGPGRGTICVTRTQRGTIQK
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Organism
Mus musculus, Mouse
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 (PubMed:23335512). 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:
Q76JU9

Secondarily ID:
A2RS88
Q8K3T5
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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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0486834
3-(4-((R)-2,3-dihydro-1H-inden-1-yloxy)phenyl)hex-4-ynoic acid
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C21H20O3
 1
1
EC50 = 47 nM
   TI
   LI
   LO
   TS
CP0377836
3-[4-(2-chloro-4-cyanophenoxy)phenyl]hex-4-ynoic acid
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C19H14ClNO3
 1
1
EC50 = 48 nM
   TI
   LI
   LO
   TS
CP0164279
3-[4-[2-(difluoromethoxy)-4-(trifluoromethyl)phenoxy]phenyl]hex-4-ynoic acid
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C20H15F5O4
 1
1
EC50 = 77 nM
   TI
   LI
   LO
   TS
CP0437999
3-[4-(2-bromo-4-cyanophenoxy)phenyl]hex-4-ynoic acid
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C19H14BrNO3
 1
1
EC50 = 88 nM
   TI
   LI
   LO
   TS
CP0438000
3-[4-(4-cyanonaphthalen-1-yl)oxyphenyl]hex-4-ynoic acid
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C23H17NO3
 1
1
EC50 = 93 nM
   TI
   LI
   LO
   TS
CP0377859
3-[4-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]oxyphenyl]hex-4-ynoic acid
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C18H13ClF3NO3
 1
1
EC50 = 95 nM
   TI
   LI
   LO
   TS
CP0483434
3-[4-[[2-(4-methylphenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-7-yl]oxy]phenyl]hex-4-ynoic acid
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C26H25NO3S
 1
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
CP0271790
3-[4-[2-(difluoromethoxy)-4-(trifluoromethyl)phenoxy]-2-fluorophenyl]hex-4-ynoic acid
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C20H14F6O4
 1
1
EC50 = 104 nM
   TI
   LI
   LO
   TS
CP0483792
3-(4-cyclopentyloxyphenyl)hex-4-ynoic acid
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C17H20O3
 1
1
EC50 = 124 nM
   TI
   LI
   LO
   TS
CP0483435
3-[4-[2-methyl-4-(trifluoromethyl)phenoxy]phenyl]hex-4-ynoic acid
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C20H17F3O3
 1
1
EC50 = 127 nM
   TI
   LI
   LO
   TS
CP0654587
cis-rac-5-(1-(4-(2-(difluoromethoxy)-4-(trifluoromethyl)phenoxy)phenyl)but-2-ynyl)oxazolidine-2,4-dione
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C21H14F5NO5
 1
1
EC50 = 136 nM
   TI
   LI
   LO
   TS
CP0438001
3-(4-isoquinolin-1-yloxyphenyl)hex-4-ynoic acid
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C21H17NO3
 1
1
EC50 = 149 nM
   TI
   LI
   LO
   TS
CP0915404
rac-5-(1-(4-(2-(difluoromethoxy)-4-(trifluoromethyl)phenoxy)phenyl)but-2-ynyl)oxazolidine-2,4-dione
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C21H14F5NO5
 1
1
EC50 = 266 nM
   TI
   LI
   LO
   TS
CP0377838
(1S,2R)-2-[4-[2-chloro-4-(trifluoromethyl)phenoxy]phenyl]-2-prop-1-ynylcyclopropane-1-carboxylic acid
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C20H14ClF3O3
 1
1
EC50 = 871 nM
   TI
   LI
   LO
   TS
CP0465447
3-[4-(3-cyanopyrazin-2-yl)oxyphenyl]hex-4-ynoic acid
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C17H13N3O3
 1
1
EC50 = 985 nM
   TI
   LI
   LO
   TS
CP0494362
3-[4-[4-(trifluoromethyl)naphthalen-1-yl]oxyphenyl]hex-4-ynoic acid
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C23H17F3O3
 1
1
EC50 = 1248 nM
   TI
   LI
   LO
   TS
CP0425833
3-[4-(5-bromopyrimidin-2-yl)oxyphenyl]hex-4-ynoic acid
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C16H13BrN2O3
 1
1
EC50 = 1484 nM
   TI
   LI
   LO
   TS
CP0917221
rac-5-(1-(4-(benzyloxy)phenyl)but-2-ynyl)oxazolidine-2,4-dione
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C20H17NO4
 1
1
EC50 = 3707 nM
   TI
   LI
   LO
   TS
CP0915705
trans-rac-5-(1-(4-(2-(difluoromethoxy)-4-(trifluoromethyl)phenoxy)phenyl)but-2-ynyl)oxazolidine-2,4-dione
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C21H14F5NO5
 1
1
EC50 = 7058 nM
   TI
   LI
   LO
   TS
CP0483433
(1R,2R)-2-[4-[2-chloro-4-(trifluoromethyl)phenoxy]phenyl]-2-prop-1-ynylcyclopropane-1-carboxylic acid
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C20H14ClF3O3
 1
1
EC50 > 40000 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02522 Free fatty acid receptor 1 Rattus norvegicus, Rat
50% Identity
Protein ID Protein Name Protein Organism
PT02793 Free fatty acid receptor 1 Homo sapiens, Human