Protein Information

General Information of the Protein

Protein ID	PT01206
Protein Name	Histamine H1 receptor
Gene Name	HRH1
Sequence	MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS Show/Hide
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. Show/Hide
Uniprot ID	Primary ID: P35367 Secondarily ID: A8K047 Q6P9E5 Show/Hide
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

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0391120 Compound Info	(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine Show/Hide	C14H21NO	1
1	Ki = 3162.28 nM Bioactivity Info	TI LI LO TS
CP0387083 Compound Info	(3aS,9bS)-3a-methyl-5-phenyl-2,3,4,9b-tetrahydro-1H-pyrrolo[2,3-c]quinoline Show/Hide	C18H20N2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0391121 Compound Info	(3S,4S)-4-ethyl-3,6-dimethyl-2,4-dihydrochromen-3-amine Show/Hide	C13H19NO	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0391154 Compound Info	(3aS,9bS)-7,9-dimethoxy-3a-methyl-2,3,4,9b-tetrahydro-1H-chromeno[3,4-b]pyrrole Show/Hide	C14H19NO3	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0411059 Compound Info	(3S,4S)-4-ethyl-3-methyl-1-phenyl-2,4-dihydroquinolin-3-amine Show/Hide	C18H22N2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000386 , Flp-In-CHO

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000065 , HEK293-EBNA

Cell Line Info

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000035 , NIH 3T3

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000074 , SK-N-MC

Cell Line Info

Cell Line ID: CL000289 , SK-N-SH

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0025667 Compound Info	2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone Show/Hide	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 Compound Info	2-(1H-imidazol-4-yl)ethan-1-amine Show/Hide	C5H9N3	3
1	EC50 = 13 nM
2	IC50 = 158.49 nM
3	Ki = 6000 nM
CP0062502 Compound Info	3H]pyrilamine Show/Hide	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 Compound Info	(+/-)1-(4-tert-butylphenyl)-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butan-1-ol Show/Hide	C32H41NO2	2
1	IC50 = 1 nM
2	Ki = 58 nM
CP0032319 Compound Info	8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine Show/Hide	C19H19ClN2	2
1	IC50 = 1.84 nM
2	IC50 = 16000 nM
CP0105756 Compound Info	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 Show/Hide	C19H21ClN2O	1
1	IC50 = 2.344 nM
CP0264804 Compound Info	8-Chloro-11-[1-(5-methyl-pyridin-3-ylmethyl)-piperidin-4-ylidene]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine Show/Hide	C26H26ClN3	1
1	IC50 = 3.9 nM
CP0734983 Compound Info	Dimethyl-(2,3,3a,8-tetrahydro-1-oxa-12b-aza-dibenzo[e,h]azulen-2-ylmethyl)-amine Show/Hide	C19H22N2O	1
1	IC50 = 6.761 nM
CP0033479 Compound Info	(chloropromazine) [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine Show/Hide	C17H19ClN2S	1
1	IC50 = 12 nM
CP0025032 Compound Info	2-(4-{1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl}phenyl)-2-methylpropanoic acid Show/Hide	C32H39NO4	2
1	IC50 = 15 nM
2	IC50 = 78 nM
CP0270497 Compound Info	4-[4-(3,4-dichlorophenoxy)piperidin-1-yl]-N-(4-methylphenyl)sulfonylpiperidine-1-carboxamide Show/Hide	C24H29Cl2N3O4S	2
1	IC50 = 40 nM
2	Ki = 31.62 nM
CP0297484 Compound Info	6-(3-(4-(3,4-dichlorophenoxy)piperidin-1-yl)propylamino)-1,3-dimethylpyrimidine-2,4(1H,3H)-dione Show/Hide	C20H26Cl2N4O3	1
1	IC50 = 58 nM
CP0068895 Compound Info	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 Show/Hide	C22H23ClN2O2	1
1	IC50 = 290 nM
CP0204765 Compound Info	2-[2-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]ethanamine Show/Hide	C12H12F3N3	1
1	IC50 = 1000 nM
CP0040455 Compound Info	(Z)-2-butenedioate;10-(1-methyl-4-piperidinylidene)-5H-benzo[1,2]cyclohepta[3,4-b]thiophen-4-one Show/Hide	C19H19NOS	1
1	IC50 = 2300 nM
CP0056899 Compound Info	(2-Benzhydryloxy-ethyl)-dimethyl-amine Show/Hide	C17H21NO	1
1	IC50 = 84000 nM
CP0050128 Compound Info	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 Show/Hide	C20H23NO	1
1	Ki = 0.43 nM
CP0237538 Compound Info	2,8-Dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H24N2	1
1	Ki = 0.58 nM
CP0101717 Compound Info	(-)-Dimethyl-{2-[3-((R)-1-pyrazin-2-yl-ethyl)-1H-inden-2-yl]-ethyl}-amine Show/Hide	C19H23N3	2
1	Ki = 1.3 nM
2	Ki = 1.5 nM
CP0026495 Compound Info	CHEBI:51137 Show/Hide	C18H20N2	1
1	Ki = 1.7 nM
CP0040184 Compound Info	1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine Show/Hide	C28H31FN4O	1
1	Ki = 3 nM
CP0056536 Compound Info	N,N-dimethyl-2-[3-(pyrazin-2-ylmethyl)-1H-inden-2-yl]ethanamine Show/Hide	C18H21N3	1
1	Ki = 4 nM
CP0044035 Compound Info	1-(p-chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine Show/Hide	C16H19ClN2	1
1	Ki = 7 nM
CP0180153 Compound Info	7-chloro-11-(4-methyl-piperazin-1-yl)-dibenzo[b,f][1,4]oxazepine Show/Hide	C18H18ClN3O	1
1	Ki = 7.762 nM
CP0150720 Compound Info	2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid Show/Hide	C21H25ClN2O3	1
1	Ki = 14 nM
CP0056747 Compound Info	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 Show/Hide	C39H49ClN4O2	1
1	Ki = 15.85 nM
CP0250759 Compound Info	1-[4-(5-{4-[(R)-(4-Chloro-phenyl)-phenyl-methyl]-piperazin-1-ylmethyl}-furan-2-yl)-but-3-ynyl]-N-hydroxy-urea Show/Hide	C27H29ClN4O3	1
1	Ki = 150 nM
CP0046703 Compound Info	1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one Show/Hide	C24H26ClFN4O	1
1	Ki = 570 nM
CP0041262 Compound Info	5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-indole Show/Hide	C14H16ClN3O	1
1	Ki = 977.24 nM
CP0092861 Compound Info	2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Show/Hide	C15H20N2S	1
1	Ki > 1000 nM
CP0044460 Compound Info	N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide Show/Hide	C15H24N4S	1
1	Ki > 10000 nM
CP0099745 Compound Info	4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole Show/Hide	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	Drug Info	Approved	Allergic rhinitis
2	Antazoline	Drug Info	Approved	Nasal congestion
3	Azatadine	Drug Info	Approved	Allergic rhinitis
4	Azelastine	Drug Info	Approved	Allergic conjunctivitis
5	Bromodiphenhydramine	Drug Info	Approved	Hay fever
6	Brompheniramine	Drug Info	Approved	Allergic rhinitis
7	Carbinoxamine	Drug Info	Approved	Vasomotor/allergic rhinitis
8	Cetirizine	Drug Info	Approved	Allergic rhinitis
9	Chlorpheniramine	Drug Info	Approved	Allergic rhinitis
10	Cinnarizine	Drug Info	Approved	Vertigo meniere disease
11	Clemastine	Drug Info	Approved	Allergic rhinitis
12	Cyclizine	Drug Info	Approved	Nausea
13	Cyproheptadine	Drug Info	Approved	Rhinitis
14	Desloratadine	Drug Info	Approved	Allergic rhinitis
15	Dexchlorpheniramine Maleate	Drug Info	Approved	Rhinitis
16	Dimenhydrinate	Drug Info	Approved	Nausea
17	Dimethindene	Drug Info	Approved	Respiratory allergy
18	Diphenhydramine	Drug Info	Approved	Meniere disease
19	Diphenylpyraline	Drug Info	Approved	Allergic rhinitis
20	Doxepin	Drug Info	Approved	Depression
21	Doxylamine	Drug Info	Approved	Morning sickness
22	Emedastine	Drug Info	Approved	Allergic conjunctivitis
23	Epinastine	Drug Info	Approved	Allergic conjunctivitis
24	Ergotidine	Drug Info	Approved	Respiratory allergy
25	Ethopropazine	Drug Info	Approved	Parkinson disease
26	Fexofenadine	Drug Info	Approved	Allergic rhinitis
27	Hydroxyzine	Drug Info	Approved	Anxiety disorder
28	Ketotifen	Drug Info	Approved	Allergic conjunctivitis
29	Levocetirizine dihydrochloride	Drug Info	Approved	Allergic rhinitis
30	Loratadine	Drug Info	Approved	Allergy
31	Mepyramine	Drug Info	Approved	Allergy
32	Mepyramine maleate	Drug Info	Approved	Headache
33	Mequitazine	Drug Info	Approved	Allergic rhinitis
34	Methdilazine	Drug Info	Approved	Allergic rhinitis
35	Mizolastine	Drug Info	Approved	Allergic rhinitis
36	Olopatadine	Drug Info	Approved	Allergic conjunctivitis
37	Oxatomide	Drug Info	Approved	Hay fever
38	Pemirolast	Drug Info	Approved	Allergic conjunctivitis
39	Phenindamine	Drug Info	Approved	Common cold
40	Pheniramine	Drug Info	Approved	Hay fever
41	Promethazine	Drug Info	Approved	Nausea
42	Tranilast	Drug Info	Approved	Ocular allergy
43	Trimeprazine	Drug Info	Approved	Allergic rhinitis
44	Tripelennamine	Drug Info	Approved	Hypersensitivity
45	Triprolidine	Drug Info	Approved	Hay fever
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Vapitadine	Drug Info	Phase 2	Allergic skin disorder
Discontinued Drug(s)	3 Discontinued Drugs				3
1	Astemizole	Drug Info	Withdrawn from market	Allergic rhinitis
2	Terfenadine	Drug Info	Withdrawn from market	Allergy
3	GSK1004723	Drug Info	Discontinued in Phase 1	Allergic rhinitis

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han