General Information of the Protein
Protein ID
PT02814
Protein Name
Gastrin-releasing peptide receptor
Secondarily
Protein Name
GRP-preferring bombesin receptor
Gene Name
GRPR
Sequence
MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSDLHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTSLKSTNPSVATFSLINGNICHERYV
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
GRP-related receptor
Function
Receptor for gastrin-releasing peptide (GRP) (PubMed:1655761). Signals via association with G proteins that activate a phosphatidylinositol-calcium second messenger system, resulting in Akt phosphorylation. Contributes to the regulation of food intake. Contributes to the perception of prurient stimuli and transmission of itch signals in the spinal cord that promote scratching behavior, but does not play a role in the perception of pain. Contributes primarily to nonhistaminergic itch sensation. In one study, shown to act in the amygdala as part of an inhibitory network which inhibits memory specifically related to learned fear (By similarity). In another study, shown to contribute to disinhibition of glutamatergic cells in the auditory cortex via signaling on vasoactive intestinal peptide-expressing cells which leads to enhanced auditory fear memories (By similarity). Contributes to the induction of sighing through signaling in the pre-Botzinger complex, a cluster of several thousand neurons in the ventrolateral medulla responsible for inspiration during respiratory activity (By similarity).
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Uniprot ID
Primary ID:
P30550

Secondarily ID:
B2R910
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HGNC ID
HGNC:4609
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
CP0384214
(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]butanediamide
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C130H204N38O31S2
 1
1
EC50 = 34 nM
   TI
   LI
   LO
   TS
CP0233482
(2S)-2-[(2-aminoacetyl)amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
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C52H73N15O12S
 1
1
EC50 = 41 nM
   TI
   LI
   LO
   TS
CP0377472
(2S)-2-[[(2S)-2-[[(2S)-2-[3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]propanoylamino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]hexanoic acid
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C58H79N11O11
 1
1
EC50 = 84 nM
   TI
   LI
   LO
   TS
CP0885728
2-[2-(4-Chloro-phenyl)-acetylamino]-pentanedioic acid 5-amide 1-{[2-(1H-indol-3-yl)-1-phenethylcarbamoyl-ethyl]-amide}
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C32H34ClN5O4
 1
1
EC50 = 12200 nM
   TI
   LI
   LO
   TS
CP0885912
2-Phenylacetylamino-pentanedioic acid 5-amide 1-{[2-(1H-indol-3-yl)-1-phenethylcarbamoyl-ethyl]-amide}
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C32H35N5O4
 1
1
EC50 = 19100 nM
   TI
   LI
   LO
   TS
CP0228324
Bombesin
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C71H110N24O18S
 1
1
Ki = 0.15 nM
   TI
   LI
   LO
   TS
CP0430110
Bombesin analogue
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C51H72N10O12
 1
1
Ki = 0.7 nM
   TI
   LI
   LO
   TS
CP0377937
(S)-3-(1H-Indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide
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C32H36N6O5
 1
1
Ki = 1 nM
   TI
   LI
   LO
   TS
CP0488194
N-(cyclohexylmethyl)-2-[[2,6-di(propan-2-yl)phenyl]carbamoyl-methylamino]-3-(1H-indol-3-yl)propanamide
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C32H44N4O2
 1
1
Ki = 1500 nM
   TI
   LI
   LO
   TS
CP0052175
(S)-2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide
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C37H47N5O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0375929
(2R)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)-2-methyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)propanamide
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C35H42N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0403347
N-(cyclohexylmethyl)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)-N-methylpropanamide
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C32H44N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0405224
N-(cyclohexylmethyl)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)-2-methylpropanamide
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C32H44N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0405291
(2S)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)-2-methyl-N-(2-phenylcyclohexyl)propanamide
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C37H46N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0429854
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-N-((R)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)-3-(1H-indol-3-yl)-2-methyl-propionamide
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C37H46N4O4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0430108
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2,N-dimethyl-propionamide
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C26H34N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0430109
N-(cyclohexylmethyl)-2-[[[2,6-di(propan-2-yl)phenyl]-methylcarbamoyl]amino]-3-(1H-indol-3-yl)propanamide
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C32H44N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0439263
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-phenyl-cyclohexylmethyl)-propionamide
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C38H48N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0439332
(R) 2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1,2,3,4-tetrahydro-naphthalen-1-yl)-propionamide
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C35H42N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0471803
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-phenethyl-propionamide
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C33H40N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0494327
N-cyclohexyl-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)-2-methylpropanamide
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C31H42N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0503475
N-(cyclohexylmethyl)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)propanamide
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C31H42N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0505439
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-N-((S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)-3-(1H-indol-3-yl)-2-methyl-propionamide
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C37H46N4O4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0510667
N-(1-cyclohexylethyl)-2-[[2,6-di(propan-2-yl)phenyl]carbamoylamino]-3-(1H-indol-3-yl)propanamide
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C32H44N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0532766
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1,2,3,4-tetrahydro-naphthalen-2-yl)-propionamide
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C35H42N4O2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0536856
2-[3-(2,6-Diisopropyl-phenyl)-ureido]-N-(2,2-dimethyl-[1,3]dioxan-5-yl)-3-(1H-indol-3-yl)-2-methyl-propionamide
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C31H42N4O4
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0228324
Bombesin
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C71H110N24O18S
 1
1 Ki = 0.15 nM
CP0341603
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]pentanediamide
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C57H76N14O10
 1
1 Ki = 0.99 nM
CP0233482
(2S)-2-[(2-aminoacetyl)amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]butanediamide
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C52H73N15O12S
 1
1 Ki = 56 nM
CP0052175
(S)-2-[3-(2,6-Diisopropyl-phenyl)-ureido]-3-(1H-indol-3-yl)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide
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C37H47N5O2
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Gastrin-releasing peptide receptor (GRPR) )
Target Type Clinical trial Target