General Information of the Protein
Protein ID
PT01365
Protein Name
Cholecystokinin receptor type A
Secondarily
Protein Name
Cholecystokinin-1 receptor
Gene Name
CCKAR
Sequence
MSHSPARQHLVESSRMDVVDSLLMNGSNITPPCELGLENETLFCLDQPQPSKEWQSALQILLYSIIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICRPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPSDAMQQSWQTFLLLILFLLPGIVMVVAYGLISLELYQGIKFDASQKKSAKEKKPSTGSSTRYEDSDGCYLQKSRPPRKLELQQLSSGSGGSRLNRIRSSSSAANLIAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTVSAEKHLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGVRGEVGEEEDGRTIRALLSRYSYSHMSTSAPPP
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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 cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
P30551
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
CP0379239
 Compound Info 
(S)-3-(3-(1-(2-(isopropyl(phenyl)amino)-2-oxoethyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)ureido)benzoic acid
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C34H31N5O6
  2
1
EC50 = 63.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 52.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0428003
 Compound Info 
2-(4-anilino-5-oxo-1-phenyl-4H-[1,2,4]triazolo[3,4-d][1,5]benzodiazepin-6-yl)-N-benzyl-N-propan-2-ylacetamide
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C34H32N6O2
  2
1
EC50 = 294 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0386006
 Compound Info 
3-(6-(2-(benzyl(isopropyl)amino)-2-oxoethyl)-5-oxo-1-phenyl-5,6-dihydro-4H-benzo[b][1,2,4]triazolo[4,3-d][1,4]diazepin-4-ylamino)benzoic acid
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C35H32N6O4
  2
1
EC50 = 428 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 17 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0373240
 Compound Info 
2-((4S)-4-((1H-indol-3-yl)methyl)-5-oxo-1-phenyl-4H-benzo[b][1,2,4]triazolo[4,3-d][1,4]diazepin-6(5H)-yl)-N-benzyl-N-isopropylacetamide
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C37H34N6O2
  2
1
EC50 = 445.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 12.2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0373242
 Compound Info 
2-(4-(1H-indazol-3-yl)-5-oxo-1-phenyl-4H-benzo[b][1,2,4]triazolo[4,3-d][1,4]diazepin-6(5H)-yl)-N-benzyl-N-isopropylacetamide
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C35H31N7O2
  2
1
EC50 = 481.2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 21 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0374787
 Compound Info 
(4S)-6-[2-[(2R)-2-[(3,5-dimethylphenyl)methyl]piperidin-1-yl]-2-oxoethyl]-4-(2H-indazol-3-ylmethyl)-1-phenyl-4H-[1,2,4]triazolo[3,4-d][1,5]benzodiazepin-5-one
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C40H39N7O2
  1
1
IC50 = 14.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00958 Cholecystokinin receptor type A Homo sapiens, Human
 Protein Info 
PT02296 Cholecystokinin receptor type A Mus musculus, Mouse
 Protein Info