General Information of the Protein
Protein ID
PT02406
Protein Name
Histamine H2 receptor
Secondarily
Protein Name
Gastric receptor I
Gene Name
HRH2
Sequence
MAFNGTVPSFCMDFTVYKVTISVILIILILVTVAGNVVVCLAVGLNRRLRSLTNCFIVSLAVTDLLLGLLVLPFSAIYQLSCKWSFSKVFCNIYTSLDVMLCTASILNLFMISLDRYCAVTDPLRYPVLITPARVAISLVFIWVISITLSFLSIHLGWNSRNETSKDNDTIVKCKVQVNEVYGLVDGLVTFYLPLLIMCITYFRIFKIAREQARRINHIGSWKAATIREHKATVTLAAVMGAFIICWFPYFTVFVYRGLKGDDAVNEVFEDVVLWLGYANSALNPILYAALNRDFRTAYHQLFCCRLASHNSHETSLRLNNSQLNRSQCQEPRWQEDKPLNLQVWSGTEVTAPQGATNR
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Organism
Cavia porcellus, Guinea pig
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Function
The H2 subclass of histamine receptors mediates gastric acid secretion. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
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Uniprot ID
P47747
Ensembl ID
ENSG00000113749
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: CL000025 , HEK-293T
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0543300
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-benzylurea;2,2,2-trifluoroacetic acid
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C18H21F6N7O5S
  1
1
EC50 = 2.188 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0546844
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-hexylurea;2,2,2-trifluoroacetic acid
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C17H27F6N7O5S
  1
1
EC50 = 2.291 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0551746
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-pentylurea;2,2,2-trifluoroacetic acid
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C16H25F6N7O5S
  1
1
EC50 = 4.365 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0543298
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-[1-(3-fluorophenyl)ethyl]urea;dihydrochloride
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C15H22Cl2FN7OS
  1
1
EC50 = 6.918 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0546843
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-[2-methyl-3-(4-methylphenyl)propyl]urea;2,2,2-trifluoroacetic acid
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C22H29F6N7O5S
  1
1
EC50 = 14.79 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0543296
 Compound Info 
1-[(1R)-1-phenylethyl]-3-[N'-[3-(1H-1,2,4-triazol-5-yl)propyl]carbamimidoyl]urea;dihydrochloride
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C15H23Cl2N7O
  1
1
EC50 = 16.22 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0550064
 Compound Info 
1-[N'-[3-(5-amino-1,3,4-thiadiazol-2-yl)propyl]carbamimidoyl]-3-[(1R)-1-phenylethyl]urea;dihydrochloride
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C15H23Cl2N7OS
  1
1
EC50 = 25.12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0036920
 Compound Info 
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
  1
1
EC50 = 251.19 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0059545
 Compound Info 
N-[N'-[3-(1H-imidazol-5-yl)propyl]carbamimidoyl]-3-phenylbutanamide
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C17H23N5O
  1
1 EC50 = 15.85 nM
CP0036920
 Compound Info 
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
  1
1 EC50 = 1000 nM
CP0840778
 Compound Info 
N-(amino(3-(2-amino-4-methylthiazol-5-yl)propylamino)methylene)-3-phenylbutanamide
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C18H25N5OS
  1
1 Kd > 31622.78 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT03243 Histamine H2 receptor Rattus norvegicus, Rat
 Protein Info