General Information of the Protein
Protein ID
PT04730
Protein Name
Histamine H4 receptor
Gene Name
HRH4
Sequence
MSESNSTGILPPAAQVPLAFLMSSFAFAIMVGNAVVILAFVVDRNLRHRSNYFFLNLAISDFLVGLISIPLYIPHVLFNWNFGSGICMFWLITDYLLCTASVYNIVLISYDRYQSVSNAVSYRAQHTGIMKIVAQMVAVWILAFLVNGPMILASDSWKNSTNTKDCEPGFVTEWYILTITMLLEFLLPVISVAYFNVQIYWSLWKRRALSRCPSHAGFSTTSSSASGHLHRAGVACRTSNPGLKESAASRHSESPRRKSSILVSLRTHMNSSITAFKVGSFWRSESAALRQREYAELLRGRKLARSLAILLSAFAICWAPYCLFTIVLSTYPRTERPKSVWYSIAFWLQWFNSFVNPFLYPLCHRRFQKAFWKILCVTKQPALSQNQSVSS
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Organism
Mus musculus, Mouse
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agonist) (By similarity).
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Uniprot ID
Q91ZY2
Ensembl ID
ENSG00000134489
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0041262
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole
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C14H16ClN3O
 1
1
EC50 = 2.399 nM
   TI
   LI
   LO
   TS
CP0173066
2,4-diamino-5,6-disubstituted pyrimidine, 11
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C18H23N5
 1
1
EC50 = 4.365 nM
   TI
   LI
   LO
   TS
CP0094765
14-fluoro-6-(piperazin-1-yl)-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine
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C17H20FN5
 1
1
EC50 = 4.786 nM
   TI
   LI
   LO
   TS
CP0205085
2,4-diamino-5,6-disubstituted pyrimidine, 10
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C17H21N5
 1
1
EC50 = 5.754 nM
   TI
   LI
   LO
   TS
CP0173068
2,4-diamino-5,6-disubstituted pyrimidine, 12
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C17H21N5
 1
1
EC50 = 9.12 nM
   TI
   LI
   LO
   TS
CP0173069
5-chloro-2-(piperazin-1-ylcarbonyl)-1H-indole
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C13H14ClN3O
 1
1
EC50 = 17.78 nM
   TI
   LI
   LO
   TS
CP0198951
2,4-diamino-5,6-disubstituted pyrimidine, 9
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C17H21N5
 1
1
EC50 = 18.2 nM
   TI
   LI
   LO
   TS
CP0044460
N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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C15H24N4S
 1
1
EC50 = 28.18 nM
   TI
   LI
   LO
   TS
CP0229853
2,4-diamino-5,6-disubstituted pyrimidine, 14
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C19H25N5
 1
1
EC50 = 45.71 nM
   TI
   LI
   LO
   TS
CP0388279
4-[(1E,3E)-4-[1-[4-(1H-imidazol-5-yl)butyl]-2,6-dimethylpyridin-1-ium-4-yl]buta-1,3-dienyl]-N,N-dimethylaniline;2,2,2-trifluoroacetate;2,2,2-trifluoroacetic acid
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C30H34F6N4O4
 1
1
EC50 = 50.12 nM
   TI
   LI
   LO
   TS
CP0036920
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
 1
1
EC50 = 94 nM
   TI
   LI
   LO
   TS
CP0286034
2-Aminopyrimidine analog., 25
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C15H16N6
 1
1
EC50 = 102.33 nM
   TI
   LI
   LO
   TS
CP0068173
2-Aminopyrimidine analog., 4
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C16H18N6
 1
1
EC50 = 123.03 nM
   TI
   LI
   LO
   TS
CP0382899
1-cyano-2-[[(1S,3S)-3-(1H-imidazol-5-yl)cyclopentyl]methyl]-3-(2-phenylsulfanylethyl)guanidine
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C19H24N6S
 1
1
EC50 = 166 nM
   TI
   LI
   LO
   TS
CP0377316
1-cyano-3-[[(1S,3S)-3-(1H-imidazol-5-yl)cyclopentyl]methyl]-2-methylguanidine
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C12H18N6
 1
1
EC50 = 538 nM
   TI
   LI
   LO
   TS
CP0377318
1-cyano-2-[[(1R,3R)-3-(1H-imidazol-5-yl)cyclopentyl]methyl]-3-(2-phenylsulfanylethyl)guanidine
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C19H24N6S
 1
1
EC50 = 589 nM
   TI
   LI
   LO
   TS
CP0823737
SID50106398
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C5H11Cl2N3
 1
1
EC50 = 2344.23 nM
   TI
   LI
   LO
   TS
CP0382908
1-cyano-3-[[(1R,3R)-3-(1H-imidazol-5-yl)cyclopentyl]methyl]-2-methylguanidine
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C12H18N6
 1
1
EC50 = 3631 nM
   TI
   LI
   LO
   TS
CP0224333
4-[(E)-2-(3-chlorophenyl)ethenyl]-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine
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C16H19ClN6
 1
1
Ki = 854 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0129069
4-cyclopentyl-6-piperazin-1-ylpyrimidin-2-amine
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C13H21N5
 1
1 EC50 = 7.3 nM
CP0213380
5-(3-(4-(5-fluoro-4-methyl-1H-benzo[d]imidazol-2-yl)-3-methylphenoxy)propyl)-4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine
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C24H26FN5O
 1
1 EC50 = 12 nM
CP0270460
3-[4-(5-fluoro-4-methyl-1H-benzimidazol-2-yl)-3-methylphenoxy]-N-[2-(1H-imidazol-5-yl)ethyl]propan-1-amine
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C23H26FN5O
 1
1 EC50 = 548 nM
CP0041262
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole
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C14H16ClN3O
 1
1 EC50 = 794.33 nM
CP0041493
Clobenpropit
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C14H17ClN4S
 1
1 EC50 = 851.14 nM
CP0288244
5-fluoro-4-methyl-2-(2-methyl-4-(3-((4aR,7aR)-tetrahydro-1H-pyrrolo[3,4-b]pyridin-6(2H,7H,7aH)-yl)propoxy)phenyl)-1H-benzo[d]imidazole
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C25H31FN4O
 1
1 EC50 = 1197 nM
CP0036920
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
 3
1 EC50 = 6760.83 nM
2 Kd = 42 nM
3 Ki = 42 nM
CP0058845
4-[(3R)-3-aminopyrrolidin-1-yl]-6-propan-2-ylpyrimidin-2-amine
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C11H19N5
 2
1 IC50 = 8 nM
2 Ki = 5.3 nM
CP0220828
4-N-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-1-yl]pyrimidine-2,4-diamine
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C13H22N6
 1
1 Ki = 54.95 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00122 Histamine H4 receptor Cavia porcellus, Guinea pig
PT02519 Histamine H4 receptor Rattus norvegicus, Rat