Protein Information

General Information of the Protein

Protein ID	PT02227
Protein Name	5-hydroxytryptamine receptor 3A
Secondarily Protein Name	5-hydroxytryptamine receptor 3 Serotonin receptor 3A Serotonin-gated ion channel receptor
Gene Name	HTR3A
Secondarily Gene Name	5HT3R HTR3
Sequence	MLLWVQQALLALLLPTLLAQGEARRSRNTTRPALLRLSDYLLTNYRKGVRPVRDWRKPTTVSIDVIVYAILNVDEKNQVLTTYIWYRQYWTDEFLQWNPEDFDNITKLSIPTDSIWVPDILINEFVDVGKSPNIPYVYIRHQGEVQNYKPLQVVTACSLDIYNFPFDVQNCSLTFTSWLHTIQDINISLWRLPEKVKSDRSVFMNQGEWELLGVLPYFREFSMESSNYYAEMKFYVVIRRRPLFYVVSLLLPSIFLMVMDIVGFYLPPNSGERVSFKITLLLGYSVFLIIVSDTLPATAIGTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQQPVPAWLRHLVLERIAWLLCLREQSTSQRPPATSQATKTDDCSAMGNHCSHMGGPQDFEKSPRDRCSPPPPPREASLAVCGLLQELSSIRQFLEKRDEIREVARDWLRVGSVLDKLLFHIYLLAVLAYSITLVMLWSIWQYA Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Ion channel > Ligand-gated ion channel > 5HT3 receptor
Function	Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons. Show/Hide
Uniprot ID	Primary ID: P46098 Secondarily ID: B4DSY6 G5E986 O60854 Q7KZM7 Q99918 Q9BSZ9 Show/Hide
Ensembl ID	ENSG00000166736
HGNC ID	HGNC:5297
Subcellular Location	Postsynaptic cell membrane 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: CL000047 , 108CC15

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0051682 Compound Info	1N-amino(immino)methyl-3-chloroaniline Show/Hide	C7H8ClN3	1
1	Ki = 32 nM Bioactivity Info	TI LI LO TS
CP0635067 Compound Info	2-amino-6-chloro-3,4-dihydroquinazoline hydrochloride Show/Hide	C8H9Cl2N3	1
1	Ki = 34 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000880 , COS

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0022161 Compound Info	CAS_40796-97-2 Show/Hide	C15H17Cl2NO2	7
1	IC50 = 4.9 nM
2	IC50 = 6.7 nM
3	IC50 = 9.4 nM
4	IC50 = 10 nM
5	Ki = 3.9 nM
6	Ki = 4.7 nM
7	Ki = 6.6 nM
CP0069827 Compound Info	1-Methyl-5-[(1-propylpiperidin-4-yl)methyloxy]-pyrrolo[1,2-a]thieno[2,3-e]pyrazine Show/Hide	C19H25N3OS	1
1	IC50 = 6.918 nM
CP0022281 Compound Info	(3R)-N-pyridin-2-ylspiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amine Show/Hide	C14H18N4O	1
1	IC50 = 15 nM
CP0003085 Compound Info	(3R)-N-isoquinolin-3-ylspiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amine Show/Hide	C18H20N4O	1
1	IC50 = 480 nM
CP0031331 Compound Info	(3R)-N-(6-phenylpyrimidin-4-yl)spiro[1-azabicyclo[2.2.2]octane-3,5'-4H-1,3-oxazole]-2'-amine Show/Hide	C19H21N5O	1
1	IC50 = 9200 nM
CP0053464 Compound Info	3-amino-2-(4-(4-(quinolin-2-yl)piperazin-1-yl)butyl)-5,6,7,8-tetrahydroquinazolin-4(3H)-one Show/Hide	C25H32N6O	2
1	IC50 > 8.929 nM
2	Ki = 4.72 nM
CP0007277 Compound Info	Aloxi Show/Hide	C19H24N2O	1
1	Ki = 0.03162 nM
CP0056637 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-chloro-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one Show/Hide	C17H19ClN4O	1
1	Ki = 0.5 nM
CP0219114 Compound Info	1-(3-fluorophenyl)sulfonyl-4-piperazin-1-ylpyrrolo[3,2-c]quinoline Show/Hide	C21H19FN4O2S	1
1	Ki = 0.93 nM
CP0671236 Compound Info	(R)-2-methyl-7-(quinuclidin-3-yl)-7,8-dihydropyrazolo[3,4,5-de]isoquinolin-6(2H)-one Show/Hide	C17H20N4O	1
1	Ki = 1.7 nM
CP0285520 Compound Info	N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1H-indazole-3-carboxamide Show/Hide	C15H18N4O	1
1	Ki = 2 nM
CP0157937 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1,10-diazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one Show/Hide	C18H21N3O	1
1	Ki = 3.1 nM
CP0000082 Compound Info	CAS_68647 Show/Hide	C18H19N3O	1
1	Ki = 3.4 nM
CP0658701 Compound Info	1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]-piperazine Hydrochloride Show/Hide	C18H23ClN2S	1
1	Ki = 3.7 nM
CP0002793 Compound Info	(BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide Show/Hide	C18H24N4O	1
1	Ki = 3.981 nM
CP0688915 Compound Info	(R)-7-(quinuclidin-3-yl)-7,8-dihydropyrazolo[3,4,5-de]isoquinolin-6(2H)-one Show/Hide	C16H18N4O	1
1	Ki = 4.4 nM
CP0056638 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1,3,10-triazatricyclo[6.4.1.04,13]trideca-4,6,8(13)-triene-2,9-dione Show/Hide	C17H20N4O2	1
1	Ki = 5.7 nM
CP0056636 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-fluoro-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one Show/Hide	C17H19FN4O	1
1	Ki = 6.4 nM
CP0120282 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one Show/Hide	C17H20N4O	1
1	Ki = 8.1 nM
CP0120281 Compound Info	10-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-6-methoxy-1,2,10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one Show/Hide	C18H22N4O2	1
1	Ki = 13.5 nM

Clinical Information about the Protein

Target 1 ( 5-HT 3A receptor (HTR3A) )

Target Type	Successful Target
Disease	6 Target-related Diseases				6
1	Irritable bowel syndrome [ICD-11: DD91.0]
2	Fibromyalgia [ICD-11: MG30.01]
3	Nausea [ICD-11: MD90]
4	Anaesthesia [ICD-11: 9A78.6]
5	Gastroesophageal reflux disease [ICD-11: DA22.Z]
6	Schizophrenia [ICD-11: 6A20]
Approved Drug(s)	4 Approved Drugs				4
1	Alosetron	Drug Info	Approved	Irritable bowel syndrome
2	Levetiracetam	Drug Info	Approved	Fibromyalgia
3	Palonosetron	Drug Info	Approved	Nausea
4	Procaine	Drug Info	Approved	Anaesthesia
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Cilansetron	Drug Info	Phase 3	Irritable bowel syndrome
Discontinued Drug(s)	2 Discontinued Drugs				2
1	Norcisapride	Drug Info	Discontinued in Phase 2	Gastroesophageal reflux disease
2	BP4.879a	Drug Info	Terminated	Schizophrenia
Preclinical Drug(s)	1 Preclinical Drug				1
1	ATI-17000	Drug Info	Preclinical	Irritable bowel syndrome

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han