General Information of the Protein
Protein ID
PT02587
Protein Name
Gastrin/cholecystokinin type B receptor
Secondarily
Protein Name
Cholecystokinin-2 receptor
Gene Name
CCKBR
Sequence
MELLKLNRSVQGPGPGSGSSLCRPGVSLLNSSSAGNLSCDPPRIRGTGTRELEMAIRITLYAVIFLMSVGGNVLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAISYLMGVSVSVSTLNLVAIALERYSAICRPLQARVWQTRSHAARVILATWLLSGLLMVPYPVYTMVQPVGPRVLQCMHRWPSARVQQTWSVLLLLLLFFIPGVVIAVAYGLISRELYLGLHFDGENDSETQSRARNQGGLPGGAAPGPVHQNGGCRPVTSVAGEDSDGCCVQLPRSRLEMTTLTTPTPGPVPGPRPNQAKLLAKKRVVRMLLVIVLLFFLCWLPVYSVNTWRAFDGPGAQRALSGAPISFIHLLSYVSACVNPLVYCFMHRRFRQACLDTCARCCPRPPRARPQPLPDEDPPTPSIASLSRLSYTTISTLGPG
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Cholecystokinin receptor
Function
Receptor for gastrin and cholecystokinin. The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
P30553
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: CL000383 , AR42J
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0038292
 Compound Info 
3-{2-[2-(3-tert-Butoxycarbonylamino-propionylamino)-3-(1H-indol-3-yl)-propionylamino]-4-methylsulfanyl-butyrylamino}-N-(1-carbamoyl-2-phenyl-ethyl)-succinamic acid
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C37H49N7O9S
  1
1
EC50 = 0.43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0906752
 Compound Info 
2,2',2''-(10-(2-((R)-1-((S)-1-((S)-1-((S)-2-((S)-1-(((S)-1-((S)-1-((S)-1-amino-3-(naphthalen-1-yl)-1-oxopropan-2-ylamino)-3-carboxy-1-oxopropan-2-ylamino)-1-oxohexan-2-yl)(methyl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-(4-hydroxyphenyl)-1-oxopropan-2-ylamino)-1-oxopropan-2-ylamino)-4-carboxy-1-oxobutan-2-ylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
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C73H96N14O20
  1
1
EC50 = 1.27 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0962464
 Compound Info 
2,2',2''-(10-(2-((R)-1-((S)-2-((2S,5S,8S,11S,17S)-11-((1H-indol-3-yl)methyl)-1-amino-8-butyl-5-(carboxymethyl)-18-(4-hydroxyphenyl)-9-methyl-2-(naphthalen-1-ylmethyl)-1,4,7,10,13,16-hexaoxo-3,6,9,12,15-pentaazaoctadecan-17-ylcarbamoyl)pyrrolidin-1-yl)-4-carboxy-1-oxobutan-2-ylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
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C72H94N14O20
  1
1
EC50 = 1.74 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0962465
 Compound Info 
2,2',2''-(10-(2-((R)-1-((S)-1-((S)-2-((4S,7S,10S,13S)-4-((1H-indol-3-yl)methyl)-14-amino-7-butyl-10-(carboxymethyl)-6-methyl-13-(naphthalen-1-ylmethyl)-2,5,8,11,14-pentaoxo-3,6,9,12-tetraazatetradecylcarbamoyl)pyrrolidin-1-yl)-3-(4-hydroxyphenyl)-1-oxopropan-2-ylamino)-4-carboxy-1-oxobutan-2-ylamino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid
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C72H94N14O20
  1
1
EC50 = 1.91 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0123919
 Compound Info 
(2R,4R)-1-[(R)-2-(Adamantan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propionyl]-4-(2,4-dichloro-phenoxy)-pyrrolidine-2-carboxylic acid
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C34H37Cl2N3O6
  1
1 IC50 = 37.4 nM
CP0036767
 Compound Info 
S-L-365,260
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C24H22N4O2
  1
1 IC50 = 39 nM
CP0281589
 Compound Info 
(2S,4S)-1-[(S)-2-(Adamantan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propionyl]-4-(2,4-dichloro-phenoxy)-piperidine-2-carboxylic acid
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C35H39Cl2N3O6
  1
1 IC50 = 217 nM
CP0335897
 Compound Info 
2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]-[2-(4-chlorophenyl)ethyl]amino]acetic acid
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C33H38ClN3O5
  1
1 IC50 = 217 nM
CP0149157
 Compound Info 
(2R,4R)-1-[(R)-2-(Adamantan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propionyl]-4-(2,4-difluoro-phenoxy)-pyrrolidine-2-carboxylic acid
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C34H37F2N3O6
  1
1 IC50 = 389 nM
CP0209063
 Compound Info 
(2R,4R)-1-[(R)-2-(Adamantan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methyl-propionyl]-4-(4-nitro-phenoxy)-pyrrolidine-2-carboxylic acid
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C34H38N4O8
  1
1 IC50 = 507 nM