Protein Information

General Information of the Protein

Protein ID	PT01357
Protein Name	Histamine H2 receptor
Secondarily Protein Name	Gastric receptor I
Gene Name	HRH2
Sequence	MAPNGTASSFCLDSTACKITITVVLAVLILITVAGNVVVCLAVGLNRRLRNLTNCFIVSLAITDLLLGLLVLPFSAIYQLSCKWSFGKVFCNIYTSLDVMLCTASILNLFMISLDRYCAVMDPLRYPVLVTPVRVAISLVLIWVISITLSFLSIHLGWNSRNETSKGNHTTSKCKVQVNEVYGLVDGLVTFYLPLLIMCITYYRIFKVARDQAKRINHISSWKAATIREHKATVTLAAVMGAFIICWFPYFTAFVYRGLRGDDAINEVLEAIVLWLGYANSALNPILYAALNRDFRTGYQQLFCCRLANRNSHKTSLRSNASQLSRTQSREPRQQEEKPLKLQVWSGTEVTAPQGATDR 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	The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) signaling pathway (By similarity). Show/Hide
Uniprot ID	Primary ID: P25021 Secondarily ID: B5BUP7 Q14464 Q7Z5R9 Show/Hide
Ensembl ID	ENSG00000113749
HGNC ID	HGNC:5183
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
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 = 1995.26 nM Bioactivity Info	TI LI LO TS
CP0391120 Compound Info	(1S,2R)-1-ethyl-7-methoxy-2-methyl-3,4-dihydro-1H-naphthalen-2-amine Show/Hide	C14H21NO	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 Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0036920 Compound Info	2-(1H-imidazol-4-yl)ethan-1-amine Show/Hide	C5H9N3	2
1	EC50 = 463 nM
2	Ki = 5000 nM
CP0035927 Compound Info	(Cimetidine) N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine,cyanide Show/Hide	C10H16N6S	6
1	IC50 = 140 nM
2	IC50 = 180 nM
3	IC50 = 270 nM
4	IC50 = 781 nM
5	Ki = 140 nM
6	Ki = 170 nM
CP0057002 Compound Info	1-[4-(1H-imidazol-5-yl)butyl]-3-methylthiourea Show/Hide	C9H16N4S	1
1	Kd = 7800 nM
CP0092861 Compound Info	2-(2-(4-tert-Butylphenylthio)ethyl)-1H-imidazole Show/Hide	C15H20N2S	1
1	Ki > 1000 nM

Clinical Information about the Protein

Target 1 ( Histamine H2 receptor (H2R) )

Target Type	Successful Target
Disease	4 Target-related Diseases				4
1	Gastric secretory disorder [ICD-11: DD90]
2	Acid-reflux disorder [ICD-11: DA22]
3	Peptic ulcer [ICD-11: DA61]
4	Duodenal ulcer [ICD-11: DA63]
Approved Drug(s)	5 Approved Drugs				5
1	Betazole	Drug Info	Approved	Gastric secretory disorder
2	Cimetidine	Drug Info	Approved	Acid-reflux disorder
3	Famotidine	Drug Info	Approved	Peptic ulcer
4	Nizatidine	Drug Info	Approved	Acid-reflux disorder
5	Ranitidine	Drug Info	Approved	Peptic ulcer
Discontinued Drug(s)	1 Discontinued Drug				1
1	KU-1257	Drug Info	Discontinued in Phase 3	Duodenal ulcer