General Information of the Protein
Protein ID
PT01206
Protein Name
Histamine H1 receptor
Gene Name
HRH1
Sequence
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Histamine receptor
Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
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Uniprot ID
Primary ID:
P35367

Secondarily ID:
A8K047
Q6P9E5
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Ensembl ID
ENSG00000196639
HGNC ID
HGNC:5182
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: CL000901 , 661W
Compound ID Compound Name Compound Formula
CP0391120
(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine
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C14H21NO
 1
1
Ki = 3162.28 nM
   TI
   LI
   LO
   TS
CP0387083
(3aS,9bS)-3a-methyl-5-phenyl-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline
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C18H20N2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0391121
(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine
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C13H19NO
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0391154
(3aS,9bS)-7,9-dimethoxy-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole
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C14H19NO3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0411059
(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine
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C18H22N2
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
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C18H19ClN4
 9
1 Activity = 1.2 nM
2 EC50 = 0.4 nM
3 Kd = 3.1 nM
4 Ki = 1 nM
5 Ki = 1.1 nM
6 Ki = 1.8 nM
7 Ki = 2.1 nM
8 Ki = 10 nM
9 Ki = 17 nM
CP0036920
2-(1H-imidazol-4-yl)ethan-1-amine
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C5H9N3
 3
1 EC50 = 13 nM
2 IC50 = 158.49 nM
3 Ki = 6000 nM
CP0062502
3H]pyrilamine
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C17H23N3O
 8
1 IC50 = 0.82 nM
2 IC50 = 1.3 nM
3 IC50 = 1.5 nM
4 IC50 = 1.8 nM
5 IC50 = 6.2 nM
6 IC50 = 12.59 nM
7 Ki = 0.95 nM
8 Ki = 2.2 nM
CP0033565
(+/-)1-(4-tert-butylphenyl)-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butan-1-ol
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C32H41NO2
 2
1 IC50 = 1 nM
2 Ki = 58 nM
CP0032319
8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
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C19H19ClN2
 2
1 IC50 = 1.84 nM
2 IC50 = 16000 nM
CP0105756
1-(17-chloro-3-oxa-2-azatetracyclo[12.4.0.02,6.07,12]octadeca-1(14),7,9,11,15,17-hexaen-4-yl)-N,N-dimethylmethanamine
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C19H21ClN2O
 1
1 IC50 = 2.344 nM
CP0264804
8-Chloro-11-[1-(5-methyl-pyridin-3-ylmethyl)-piperidin-4-ylidene]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
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C26H26ClN3
 1
1 IC50 = 3.9 nM
CP0734983
Dimethyl-(2,3,3a,8-tetrahydro-1-oxa-12b-aza-dibenzo[e,h]azulen-2-ylmethyl)-amine
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C19H22N2O
 1
1 IC50 = 6.761 nM
CP0033479
(chloropromazine) [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine
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C17H19ClN2S
 1
1 IC50 = 12 nM
CP0025032
2-(4-{1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl}phenyl)-2-methylpropanoic acid
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C32H39NO4
 2
1 IC50 = 15 nM
2 IC50 = 78 nM
CP0270497
4-[4-(3,4-dichlorophenoxy)piperidin-1-yl]-N-(4-methylphenyl)sulfonylpiperidine-1-carboxamide
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C24H29Cl2N3O4S
 2
1 IC50 = 40 nM
2 Ki = 31.62 nM
CP0297484
6-(3-(4-(3,4-dichlorophenoxy)piperidin-1-yl)propylamino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione
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C20H26Cl2N4O3
 1
1 IC50 = 58 nM
CP0068895
ethyl 4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidine-1-carboxylate
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C22H23ClN2O2
 1
1 IC50 = 290 nM
CP0204765
2-[2-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]ethanamine
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C12H12F3N3
 1
1 IC50 = 1000 nM
CP0040455
(Z)-2-butenedioate;10-(1-methyl-4-piperidinylidene)-5H-benzo[1,2]cyclohepta[3,4-b]thiophen-4-one
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C19H19NOS
 1
1 IC50 = 2300 nM
CP0056899
(2-Benzhydryloxy-ethyl)-dimethyl-amine
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C17H21NO
 1
1 IC50 = 84000 nM
CP0050128
N,N-dimethyl-1-[(2S,4R,6R)-3-oxatetracyclo[12.4.0.02,6.07,12]octadeca-1(18),7,9,11,14,16-hexaen-4-yl]methanamine
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C20H23NO
 1
1 Ki = 0.43 nM
CP0237538
2,8-Dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole
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C21H24N2
 1
1 Ki = 0.58 nM
CP0101717
(-)-Dimethyl-{2-[3-((R)-1-pyrazin-2-yl-ethyl)-1H-inden-2-yl]-ethyl}-amine
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C19H23N3
 2
1 Ki = 1.3 nM
2 Ki = 1.5 nM
CP0026495
CHEBI:51137
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C18H20N2
 1
1 Ki = 1.7 nM
CP0040184
1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine
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C28H31FN4O
 1
1 Ki = 3 nM
CP0056536
N,N-dimethyl-2-[3-(pyrazin-2-ylmethyl)-1H-inden-2-yl]ethanamine
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C18H21N3
 1
1 Ki = 4 nM
CP0044035
1-(p-chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine
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C16H19ClN2
 1
1 Ki = 7 nM
CP0180153
7-chloro-11-(4-methyl-piperazin-1-yl)-dibenzo[b,f][1,4]oxazepine
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C18H18ClN3O
 1
1 Ki = 7.762 nM
CP0150720
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
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C21H25ClN2O3
 1
1 Ki = 14 nM
CP0056747
4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(hexahydro-1H-azepin-1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1(2H)-phthalazinone
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C39H49ClN4O2
 1
1 Ki = 15.85 nM
CP0250759
1-[4-(5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-but-3-ynyl]-N-hydroxy-urea
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C27H29ClN4O3
 1
1 Ki = 150 nM
CP0046703
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
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C24H26ClFN4O
 1
1 Ki = 570 nM
CP0041262
5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole
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C14H16ClN3O
 1
1 Ki = 977.24 nM
CP0092861
2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole
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C15H20N2S
 1
1 Ki > 1000 nM
CP0044460
N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide
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C15H24N4S
 1
1 Ki > 10000 nM
CP0099745
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole
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C16H18N2O2
 1
1 Ki > 10000 nM
Clinical Information about the Protein
Target 1 ( Histamine H1 receptor (H1R) )
Target Type Successful Target
Disease 20 Target-related Diseases  20
1 Allergic rhinitis [ICD-11: CA08.0]
2 Nasal congestion [ICD-11: MD11.9]
3 Allergic conjunctivitis [ICD-11: 9A60.02]
4 Hay fever [ICD-11: CA08.00]
5 Vasomotor/allergic rhinitis [ICD-11: CA08]
6 Vertigo meniere disease [ICD-11: AB31.0]
7 Nausea [ICD-11: MD90]
8 Rhinitis [ICD-11: FA20]
9 Respiratory allergy [ICD-11: 4A80]
10 Meniere disease [ICD-11: AB31.0]
11 Depression [ICD-11: 6A70-6A7Z]
12 Morning sickness [ICD-11: SC00]
13 Parkinson disease [ICD-11: 8A00.0]
14 Anxiety disorder [ICD-11: 6B00-6B0Z]
15 Allergy [ICD-11: 4A80-4A85]
16 Headache [ICD-11: 8A80-8A84]
17 Common cold [ICD-11: CA00]
18 Ocular allergy [ICD-11: 4A81]
19 Hypersensitivity [ICD-11: 4A80-4A85]
20 Allergic skin disorder [ICD-11: 4A82]
Approved Drug(s) 45 Approved Drugs  45
1 Acrivastine Approved
Allergic rhinitis
2 Antazoline Approved
Nasal congestion
3 Azatadine Approved
Allergic rhinitis
4 Azelastine Approved
Allergic conjunctivitis
5 Bromodiphenhydramine Approved
Hay fever
6 Brompheniramine Approved
Allergic rhinitis
7 Carbinoxamine Approved
Vasomotor/allergic rhinitis
8 Cetirizine Approved
Allergic rhinitis
9 Chlorpheniramine Approved
Allergic rhinitis
10 Cinnarizine Approved
Vertigo meniere disease
11 Clemastine Approved
Allergic rhinitis
12 Cyclizine Approved
Nausea
13 Cyproheptadine Approved
Rhinitis
14 Desloratadine Approved
Allergic rhinitis
15 Dexchlorpheniramine Maleate Approved
Rhinitis
16 Dimenhydrinate Approved
Nausea
17 Dimethindene Approved
Respiratory allergy
18 Diphenhydramine Approved
Meniere disease
19 Diphenylpyraline Approved
Allergic rhinitis
20 Doxepin Approved
Depression
21 Doxylamine Approved
Morning sickness
22 Emedastine Approved
Allergic conjunctivitis
23 Epinastine Approved
Allergic conjunctivitis
24 Ergotidine Approved
Respiratory allergy
25 Ethopropazine Approved
Parkinson disease
26 Fexofenadine Approved
Allergic rhinitis
27 Hydroxyzine Approved
Anxiety disorder
28 Ketotifen Approved
Allergic conjunctivitis
29 Levocetirizine dihydrochloride Approved
Allergic rhinitis
30 Loratadine Approved
Allergy
31 Mepyramine Approved
Allergy
32 Mepyramine maleate Approved
Headache
33 Mequitazine Approved
Allergic rhinitis
34 Methdilazine Approved
Allergic rhinitis
35 Mizolastine Approved
Allergic rhinitis
36 Olopatadine Approved
Allergic conjunctivitis
37 Oxatomide Approved
Hay fever
38 Pemirolast Approved
Allergic conjunctivitis
39 Phenindamine Approved
Common cold
40 Pheniramine Approved
Hay fever
41 Promethazine Approved
Nausea
42 Tranilast Approved
Ocular allergy
43 Trimeprazine Approved
Allergic rhinitis
44 Tripelennamine Approved
Hypersensitivity
45 Triprolidine Approved
Hay fever
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Vapitadine Phase 2
Allergic skin disorder
Discontinued Drug(s) 3 Discontinued Drugs  3
1 Astemizole Withdrawn from market
Allergic rhinitis
2 Terfenadine Withdrawn from market
Allergy
3 GSK1004723 Discontinued in Phase 1
Allergic rhinitis