General Information of the Protein
Protein ID
PT02015
Protein Name
fMet-Leu-Phe receptor
Secondarily
Protein Name
N-formyl peptide receptor
N-formylpeptide chemoattractant receptor
Gene Name
FPR1
Sequence
METNSSLPTNISGGTPAVSAGYLFLDIITYLVFAVTFVLGVLGNGLVIWVAGFRMTHTVTTISYLNLAVADFCFTSTLPFFMVRKAMGGHWPFGWFLCKFVFTIVDINLFGSVFLIALIALDRCVCVLHPVWTQNHRTVSLAKKVIIGPWVMALLLTLPVIIRVTTVPGKTGTVACTFNFSPWTNDPKERINVAVAMLTVRGIIRFIIGFSAPMSIVAVSYGLIATKIHKQGLIKSSRPLRVLSFVAAAFFLCWSPYQVVALIATVRIRELLQGMYKEIGIAVDVTSALAFFNSCLNPMLYVFMGQDFRERLIHALPASLERALTEDSTQTSDTATNSTLPSAEVELQAK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
N-formyl methionyl peptide receptor
>
N-formyl methionyl peptide receptor
Function
High affinity receptor for N-formyl-methionyl peptides (fMLP), which are powerful neutrophil chemotactic factors (PubMed:2161213, PubMed:2176894, PubMed:10514456, PubMed:15153520). Binding of fMLP to the receptor stimulates intracellular calcium mobilization and superoxide anion release (PubMed:2161213, PubMed:1712023, PubMed:15153520, PubMed:15210802). This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system (PubMed:1712023, PubMed:10514456). Receptor for TAFA4, mediates its effects on chemoattracting macrophages, promoting phagocytosis and increasing ROS release (PubMed:25109685). Receptor for cathepsin CTSG, leading to increased phagocyte chemotaxis (PubMed:15210802).
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Uniprot ID
Primary ID:
P21462

Secondarily ID:
Q14939
Q7Z6A4
Q86U52
Q9NS48
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Ensembl ID
ENSG00000171051
HGNC ID
HGNC:3826
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0545821
 Compound Info 
1-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl]-3-phenylurea
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C18H17F2N3O3
  1
1
EC50 = 400 nM
 Bioactivity Info 
   TI
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CP0546958
 Compound Info 
(3S,4R)-3-[[5-(4-chlorophenyl)-1,2-oxazol-3-yl]amino]-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one
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C20H16ClF2N3O3
  1
1
EC50 = 470 nM
 Bioactivity Info 
   TI
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CP0569103
 Compound Info 
(3S,4R)-3-[[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]amino]-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one
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C19H15ClF2N4O3
  1
1
EC50 = 1400 nM
 Bioactivity Info 
   TI
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CP0578828
 Compound Info 
(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-3-[(5-phenyl-1,3,4-oxadiazol-2-yl)amino]pyrrolidin-2-one
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C19H16F2N4O3
  1
1
EC50 = 5500 nM
 Bioactivity Info 
   TI
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CP0399583
 Compound Info 
2-ethyl-1-[(3R)-1-[(5-ethyl-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C24H26N4O
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0424807
 Compound Info 
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-1H-1,3-benzodiazole
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C22H22N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0424809
 Compound Info 
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-(2-methylpropyl)-1H-1,3-benzodiazole
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C26H30N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0424810
 Compound Info 
2-ethyl-1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-1H-1,3-benzodiazole
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C24H26N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0424811
 Compound Info 
2-ethyl-1-[(3R)-1-{[5-(trifluoromethoxy)-1H-indol-2-yl]carbonyl}pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C23H21F3N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0440710
 Compound Info 
2-ethyl-1-[(3R)-1-[(5-fluoro-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C22H21FN4O
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0440810
 Compound Info 
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-phenyl-1H-1,3-benzodiazole
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C28H26N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0440811
 Compound Info 
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-(trifluoromethyl)-1H-1,3-benzodiazole
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C23H21F3N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0446515
 Compound Info 
2-ethyl-1-[(3S)-1-[(5-methoxy-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C23H24N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0446518
 Compound Info 
2-ethyl-1-[(3R)-1-[(5-methoxy-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C23H24N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0447652
 Compound Info 
2-ethyl-1-[(3R)-1-[(5-methoxy-1H-1,3-benzodiazol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole
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C22H23N5O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0457626
 Compound Info 
1-[(3R)-1-[(5-bromo-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-2-ethyl-1H-1,3-benzodiazole
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C22H21BrN4O
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0458640
 Compound Info 
1-[(3R)-1-[(5-chloro-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl]-2-ethyl-1H-1,3-benzodiazole
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C22H21ClN4O
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0486809
 Compound Info 
1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-methyl-1H-1,3-benzodiazole
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C23H24N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
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CP0509978
 Compound Info 
2-ethyl-1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]pyrrolidin-3-yl}-1H-1,3-benzodiazole
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C23H24N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0968206
 Compound Info 
(3S,4R)-3-((1H-benzo[d]imidazol-2-yl)amino)-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one
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C18H16F2N4O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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CP0969952
 Compound Info 
(3R,4R)-3-(1H-benzo[d]imidazol-2-yl)-4-(2,6-difluoro-4-methoxyphenyl)pyrrolidin-2-one
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C18H15F2N3O2
  1
1
EC50 > 10000 nM
 Bioactivity Info 
   TI
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Cell Line ID: CL000386 , Flp-In-CHO
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000050 , HEK293-A
 Cell Line Info 
Cell Line ID: CL000018 , HL-60
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0046087
 Compound Info 
(S)-2-[(S)-2-((S)-2-Formylamino-4-methylsulfanyl-butyrylamino)-4-methyl-pentanoylamino]-3-phenyl-propionic acid
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C21H31N3O5S
  3
1 IC50 = 20 nM
2 Kd = 3 nM
3 Ki = 42 nM
CP0701245
 Compound Info 
methyl (2R)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-cyclohexylpropanoate
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C28H33N3O4
  1
1 IC50 = 120 nM
CP0719107
 Compound Info 
methyl (2R)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
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C28H27N3O4
  1
1 IC50 = 180 nM
CP0746991
 Compound Info 
methyl (2S)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
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C28H27N3O4
  1
1 IC50 = 2400 nM
CP0838960
 Compound Info 
(2R)-Methyl 2-[(2'S)-2-cyclohexanecarboxamido-3-(1H-indol-3-yl)propanamido]-3-phenylpropanoate
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C28H33N3O4
  1
1 IC50 = 3300 nM
CP0901938
 Compound Info 
methyl (2S)-2-[[(2R)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
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C28H27N3O4
  1
1 IC50 = 10900 nM
CP0870424
 Compound Info 
(2R)-Methyl 2-[(2'S)-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanamido]-3-phenylpropanoate
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C26H31N3O5
  1
1 IC50 = 12600 nM
CP0701246
 Compound Info 
(2R)-Methyl 2-[(2'S)-2-benzamido-3-(1H-indol-3-yl)propanamido]-4-methylpentanoate
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C25H29N3O4
  1
1 IC50 = 14500 nM
CP0719108
 Compound Info 
(2R)-Methyl 2-[(2'S)-2-benzamido-3-(1H-indol-3-yl)propanamido]-3-methylbutanoate
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C24H27N3O4
  1
1 IC50 = 25300 nM
CP0946376
 Compound Info 
(2R)-Methyl 2-[(2'S)-3-(1H-indol-3-yl)-2-(3-methylbutanamido)propanamido]-3-phenylpropanoate
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C26H31N3O4
  1
1 IC50 = 27700 nM
CP0795941
 Compound Info 
methyl (2R)-2-[[(2R)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
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C28H27N3O4
  1
1 IC50 = 31300 nM
Clinical Information about the Protein
Target 1 ( N-formyl peptide receptor (FPR1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Peptic ulcer [ICD-11: DA61]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Rebamipide
 Drug Info 
Phase 3
Peptic ulcer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04925 fMet-Leu-Phe receptor Mus musculus, Mouse
 Protein Info