General Information of the Protein
Protein ID
PT06663
Protein Name
G-protein coupled receptor 4
Gene Name
GPR4
Sequence
MDNSTGTWEGCHVDSRVDHLFPPSLYIFVIGVGLPTNCLALWAAYRQVRQRNELGVYLMNLSIADLLYICTLPLWVDYFLHHDNWIHGPGSCKLFGFIFYSNIYISIAFLCCISVDRYLAVAHPLRFARLRRVKTAVAVSSVVWATELGANSAPLFHDELFRDRYNHTFCFEKFPMERWVAWMNLYRVFVGFLFPWALMLLCYRGILRAVQSSVSTERQEKVKIKRLALSLIAIVLVCFAPYHALLLSRSAVYLGRPWDCGFEERVFSAYHSSLAFTSLNCVADPILYCLVNEGARSDVAKALHNLLRFLASNKPQEMANASLTLETPLTSKRSTTGKTSGAVWAVPPTAQGDQVPLKVLLPPAQ
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
Function
Proton-sensing G-protein coupled receptor couples to multiple intracellular signaling pathways, including GNAS/cAMP, GNAQ/phospholipase C (PLC), and GNA13/Rho pathways. Acidosis-induced GPR4 activation increases paracellular gap formation and permeability of vascular endothelial cells through the GNA12/GNA13/Rho GTPase signaling pathway. In the brain may mediate central respiratory sensitivity to CO(2)/H(+).
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Uniprot ID
Q4KLH9
Ensembl ID
ENSG00000177464
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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0456411
 Compound Info 
1-[2-[1-[4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]triazol-4-yl]ethyl]piperidin-4-ol
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C27H39N7O
  1
1
IC50 = 480 nM
 Bioactivity Info 
   TI
   LI
   LO
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CP0411513
 Compound Info 
4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-2-one
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C24H29N5O
  1
1
IC50 = 740 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0314508
 Compound Info 
US8748435, 40
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C27H37N5
  1
1
IC50 = 800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0408534
 Compound Info 
(2R)-3-[4-[(E)-3-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]prop-2-enyl]piperazin-1-yl]propane-1,2-diol
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C27H37N5O2
  1
1
IC50 = 860 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0538713
 Compound Info 
N-[4-(dimethylamino)butyl]-4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]benzamide
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C25H39N5O
  1
1
IC50 = 1260 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0476126
 Compound Info 
N-(2,2-dimethylpropyl)-2,6-dimethyl-N-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]pyrimidin-4-amine
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C28H43N5
  1
1
IC50 = 1590 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0493671
 Compound Info 
2,5,7-trimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine
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C26H35N5
  1
1
IC50 = 1840 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0392109
 Compound Info 
US8748435, 35
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C24H28N6O
  1
1
IC50 = 1840 nM
 Bioactivity Info 
   TI
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CP0493673
 Compound Info 
5-(dimethylamino)-N-[4-[[2,2-dimethylpropyl-(2,6-dimethylpyrimidin-4-yl)amino]methyl]phenyl]pentanamide
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C25H39N5O
  1
1
IC50 = 1990 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0560423
 Compound Info 
5,7-dimethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]-2-propylimidazo[4,5-b]pyridine
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C28H39N5
  1
1
IC50 = 5220 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0408465
 Compound Info 
5,7-dimethyl-2-propan-2-yl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine
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C28H39N5
  1
1
IC50 = 17240 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0493672
 Compound Info 
2-ethyl-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine
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C25H33N5
  1
1
IC50 > 20000 nM
 Bioactivity Info 
   TI
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   TS
CP0558235
 Compound Info 
5,7-dimethyl-2-(2-methylpropyl)-3-[[4-[(E)-3-(4-propan-2-ylpiperazin-1-yl)prop-1-enyl]phenyl]methyl]imidazo[4,5-b]pyridine
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C29H41N5
  1
1
IC50 > 20000 nM
 Bioactivity Info 
   TI
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   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06238 G-protein coupled receptor 4 Homo sapiens, Human
 Protein Info 
PT07048 G-protein coupled receptor 4 Mus musculus, Mouse
 Protein Info