General Information of the Protein
Protein ID
PT01173
Protein Name
Histamine H3 receptor
Gene Name
HRH3
Sequence
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCASSVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAGPEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAAASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSLAIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFRRAFTKLLCPQKLKVQPHGSLEQCWK
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist).
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Uniprot ID
Primary ID:
Q9QYN8

Secondarily ID:
Q9QYN6
Q9QYN7
Q9QYN9
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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: CL000026 , CHO-K1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0344770
 Compound Info 
1-{4-[2-(1H-Imidazol-4-yl)-ethylsulfanyl]-phenyl}-ethanone
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C13H14N2OS
  1
1
Ki = 0.11 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0041493
 Compound Info 
Clobenpropit
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C14H17ClN4S
  1
1
Ki = 1.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0213459
 Compound Info 
3-(1H-imidazol-4-yl)propylphenylmethyl ether
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C13H16N2O
  1
1
Ki = 2.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0227935
 Compound Info 
1-{4-[2-(1H-Imidazol-4-yl)-ethoxy]-phenyl}-ethanone
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C13H14N2O2
  1
1
Ki = 3.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0099745
 Compound Info 
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole
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C16H18N2O2
  1
1
Ki = 3.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0445198
 Compound Info 
4-(3-Phenoxy-propyl)-1H-imidazole with (0.95M)oxalic acid
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C12H14N2O
  1
1
Ki = 4.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0044460
 Compound Info 
N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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C15H24N4S
  1
1
Ki = 6.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0040043
 Compound Info 
4-[3-(4-Methoxy-phenoxy)-propyl]-1H-imidazole; compound with but-2-enedioic acid(0.25M H2O)
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C13H16N2O2
  1
1
Ki = 7.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0165491
 Compound Info 
N-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-morpholin-4-ylacetamide;dihydrochloride
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C21H33Cl2N3O3
  1
1
Ki = 9.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0358724
 Compound Info 
4-(4-Phenyl-butyl)-1H-imidazole
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C13H16N2
  1
1
Ki = 12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0041994
 Compound Info 
1-{4-[3-(1H-Imidazol-4-yl)-propoxy]-phenyl}-ethanone
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C14H16N2O2
  1
1
Ki = 29 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0347219
 Compound Info 
1-{4-[4-(1H-Imidazol-4-yl)-butoxy]-phenyl}-ethanone
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C15H18N2O2
  1
1
Ki = 36 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0184940
 Compound Info 
1-{4-[3-(1H-Imidazol-4-yl)-propylsulfanyl]-phenyl}-ethanone
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C14H16N2OS
  1
1
Ki = 44 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0214392
 Compound Info 
5-{3-[(4-iodophenyl)methoxy]propyl}-1H-imidazole
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C13H15IN2O
  1
1
Ki = 71 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000049 , C6
 Cell Line Info 
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL001008 , CHO-A3
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000074 , SK-N-MC
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0041493
 Compound Info 
Clobenpropit
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C14H17ClN4S
  1
1 Ki = 0.18 nM
CP0194592
 Compound Info 
(R)-4-(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrile
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C22H22N2O
  3
1 Ki = 0.45 nM
2 Ki = 1.23 nM
3 Ki = 1.4 nM
CP0099745
 Compound Info 
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole
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C16H18N2O2
  1
1 Ki = 0.49 nM
CP0198937
 Compound Info 
(R)-2-(1-(6-ethoxypyridazin-3-yl)-5-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C26H30N6O
  1
1 Ki = 0.49 nM
CP0193419
 Compound Info 
6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotinamide
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C21H25N3O2
  1
1 Ki = 0.631 nM
CP0090976
 Compound Info 
(R)-2-(4-methyl-2-(pyrrolidin-1-yl)pyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H31N5
  1
1 Ki = 0.72 nM
CP0044094
 Compound Info 
(R)-2-(5-methyl-1-(pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H27N5
  1
1 Ki = 0.91 nM
CP0091000
 Compound Info 
(R)-2-(2,7-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C24H27N5
  1
1 Ki = 0.93 nM
CP0056575
 Compound Info 
1-(3-(4-(piperidin-1-ylmethyl)phenoxy)propyl)piperidine
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C20H32N2O
  1
1 Ki = 1.259 nM
CP0126642
 Compound Info 
(R)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H26N4
  1
1 Ki = 1.6 nM
CP0044006
 Compound Info 
(R)-2-methyl-3-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1,8-naphthyridine
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C25H26N4
  1
1 Ki = 2 nM
CP0044460
 Compound Info 
N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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C15H24N4S
  3
1 Ki = 2.65 nM
2 Ki = 3.981 nM
3 Ki = 4 nM
CP0292222
 Compound Info 
6-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methylpyridazin-3-one
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C20H25N3O2
  1
1 Ki = 3 nM
CP0271597
 Compound Info 
6-[4-(1-cyclopentylpiperidin-4-yl)oxyphenyl]-2-methylpyridazin-3-one
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C21H27N3O2
  1
1 Ki = 6 nM
CP0282219
 Compound Info 
2-methyl-6-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyridazin-3-one
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C19H25N3O2
  1
1 Ki = 6 nM
CP0046463
 Compound Info 
3-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-1H-pyridazin-6-one
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C18H23N3O2
  1
1 Ki = 7.2 nM
CP0115802
 Compound Info 
1-((2R,4S)-2-(4-cyclobutyl-1,4-diazepane-1-carbonyl)-4-(3-fluorophenoxy)pyrrolidin-1-yl)ethanone
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C22H30FN3O3
  1
1 Ki = 27 nM
CP0066136
 Compound Info 
1-[4-[3-[(2R)-2-methylpyrrolidin-1-yl]propoxy]phenyl]-2-morpholin-4-ylethanone
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C20H30N2O3
  1
1 Ki = 50 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT03665 Histamine H3 receptor Mus musculus, Mouse
 Protein Info