Protein Information

General Information of the Protein

Protein ID	PT01492
Protein Name	5-hydroxytryptamine receptor 2A
Secondarily Protein Name	Serotonin receptor 2A
Gene Name	HTR2A
Secondarily Gene Name	Htr2
Sequence	MEILCEDNISLSSIPNSLMQLGDGPRLYHNDFNSRDANTSEASNWTIDAENRTNLSCEGYLPPTCLSILHLQEKNWSALLTTVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIADMLLGFLVMPVSMLTILYGYRWPLPSKLCAIWIYLDVLFSTASIMHLCAISLDRYVAIQNPIHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSFVAFFIPLTIMVITYFLTIKSLQKEATLCVSDLSTRAKLASFSFLPQSSLSSEKLFQRSIHREPGSYAGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNENVIGALLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENRKPLQLILVNTIPALAYKSSQLQVGQKKNSQEDAEQTVDDCSMVTLGKQQSEENCTDNIETVNEKVSCV Show/Hide
Organism	Rattus norvegicus, Rat
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Small molecule receptor (family A GPCR) > Monoamine receptor > Serotonin receptor
Function	G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction. Show/Hide
Uniprot ID	P14842
Ensembl ID	ENSG00000102468
Subcellular Location	Cell membrane Cell projection Axon Cytoplasmic vesicle Membrane Caveola Cell projection Dendrite Presynapse

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: CL000238 , A7r5

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0373324 Compound Info	(R)-2-(8-methoxymethyl-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethylamine Show/Hide	C15H17NO3	1
1	EC50 = 3.6 nM Bioactivity Info	TI LI LO TS
CP0394695 Compound Info	phenyl 2-[[8-[(2R)-2-aminopropyl]-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-4-yl]methoxy]acetate Show/Hide	C22H25NO5	1
1	EC50 = 6.2 nM Bioactivity Info	TI LI LO TS
CP0373330 Compound Info	(R)-2-(8-methoxymethyl-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethylamine Show/Hide	C15H21NO3	1
1	EC50 = 12 nM Bioactivity Info	TI LI LO TS
CP0222963 Compound Info	2-(8-bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethylamine Show/Hide	C13H16BrNO2	1
1	EC50 = 13 nM Bioactivity Info	TI LI LO TS
CP0394899 Compound Info	(R)-1-methyl-2-[8-(3-methyl-[1,2,4]oxadiazol-5-ylmethyl)-benzo[1,2-b;4,5-b']difuran-4-yl]-ethylamine Show/Hide	C17H17N3O3	1
1	EC50 = 16.9 nM Bioactivity Info	TI LI LO TS
CP0057042 Compound Info	(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine Show/Hide	C11H16INO2	1
1	EC50 = 17.8 nM Bioactivity Info	TI LI LO TS
CP0273033 Compound Info	(R)-1-(4-bromo-2,5-dimethoxyphenyl)propan-2-amine Show/Hide	C11H16BrNO2	1
1	EC50 = 20 nM Bioactivity Info	TI LI LO TS
CP0373328 Compound Info	3-[8-((R)-2-amino-propyl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl]-propionic acid methyl ester Show/Hide	C17H23NO4	1
1	EC50 = 26 nM Bioactivity Info	TI LI LO TS
CP0442976 Compound Info	(1R,2R)-2-amino-1-(8-bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-propan-1-ol Show/Hide	C13H16BrNO3	1
1	EC50 = 32.7 nM Bioactivity Info	TI LI LO TS
CP0373325 Compound Info	[8-[(2R)-2-aminopropyl]furo[2,3-f][1]benzofuran-4-yl]methanol Show/Hide	C14H15NO3	1
1	EC50 = 33 nM Bioactivity Info	TI LI LO TS
CP0394693 Compound Info	(R)-1-methyl-2-[8-(3-methyl-[1,2,4]oxadiazol-5-ylmethyl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl]-ethylamine Show/Hide	C17H21N3O3	1
1	EC50 = 49.2 nM Bioactivity Info	TI LI LO TS
CP0047728 Compound Info	(+)-2-(4-Bromo-2,5-dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H16BrNO2	1
1	EC50 = 60 nM Bioactivity Info	TI LI LO TS
CP0373329 Compound Info	(R)-2-[8-(2-methoxy-ethoxymethyl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl]-1-methyl-ethylamine Show/Hide	C17H25NO4	1
1	EC50 = 71 nM Bioactivity Info	TI LI LO TS
CP0442977 Compound Info	(1S,2R)-2-amino-1-(8-bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-propan-1-ol Show/Hide	C13H16BrNO3	1
1	EC50 = 87.8 nM Bioactivity Info	TI LI LO TS
CP0255251 Compound Info	(1R,2R)-2-Amino-1-(4-bromo-2,5-dimethoxy-phenyl)-propan-1-ol Show/Hide	C11H16BrNO3	1
1	EC50 = 100 nM Bioactivity Info	TI LI LO TS
CP0099558 Compound Info	2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-ethylamine Show/Hide	C11H16BrNO3	1
1	EC50 = 120 nM Bioactivity Info	TI LI LO TS
CP0287357 Compound Info	(1R,2R)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	EC50 = 130 nM Bioactivity Info	TI LI LO TS
CP0373332 Compound Info	[8-[(2R)-2-aminopropyl]-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-4-yl]methanol Show/Hide	C14H19NO3	1
1	EC50 = 175 nM Bioactivity Info	TI LI LO TS
CP0249508 Compound Info	(R)-2-(2,5-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	EC50 = 740 nM Bioactivity Info	TI LI LO TS
CP0126359 Compound Info	(1R,2S)-2-Amino-1-(4-bromo-2,5-dimethoxy-phenyl)-propan-1-ol Show/Hide	C11H16BrNO3	1
1	EC50 = 840 nM Bioactivity Info	TI LI LO TS
CP0435777 Compound Info	8-((R)-2-amino-propyl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-carboxylic acid methyl ester Show/Hide	C15H19NO4	1
1	EC50 = 880 nM Bioactivity Info	TI LI LO TS
CP0370559 Compound Info	(1R,2S)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	EC50 = 1330 nM Bioactivity Info	TI LI LO TS
CP0110578 Compound Info	(1S,2S)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	EC50 = 1410 nM Bioactivity Info	TI LI LO TS
CP0437883 Compound Info	2-[8-[(2R)-2-aminopropyl]-2,3,6,7-tetrahydrofuro[2,3-f][1]benzofuran-4-yl]acetic acid Show/Hide	C15H19NO4	1
1	EC50 = 4970 nM Bioactivity Info	TI LI LO TS
CP0273208 Compound Info	(1S,2R)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	EC50 = 5040 nM Bioactivity Info	TI LI LO TS
CP0393099 Compound Info	(R)-1-methyl-2-[8-(3-methyl-[1,2,4]oxadiazol-5-yl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl]-ethylamine Show/Hide	C16H19N3O3	1
1	EC50 = 8192 nM Bioactivity Info	TI LI LO TS
CP0373327 Compound Info	(R)-1-methyl-2-{8-[2-(3-methyl-[1,2,4]oxadiazol-5-yl)-ethyl]-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl}-ethylamine Show/Hide	C18H23N3O3	1
1	EC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0438963 Compound Info	3-[8-((R)-2-amino-propyl)-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl]-propionic acid Show/Hide	C16H21NO4	1
1	EC50 > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000744 , GF62

Cell Line Info

Cell Line ID: CL000035 , NIH 3T3

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0047728 Compound Info	(+)-2-(4-Bromo-2,5-dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H16BrNO2	6
1	EC50 = 72 nM
2	Ki = 0.1 nM
3	Ki = 2.2 nM
4	Ki = 22 nM
5	Ki = 32 nM
6	Ki = 41 nM
CP0075436 Compound Info	(2,3-Dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol Show/Hide	C22H28FNO3	2
1	Ki = 0.1 nM
2	Ki = 1.4 nM
CP0040626 Compound Info	1-(2,4-difluorophenethyl)-4-(phenylsulfonyl)piperidine Show/Hide	C19H21F2NO2S	1
1	Ki = 0.18 nM
CP0273033 Compound Info	(R)-1-(4-bromo-2,5-dimethoxyphenyl)propan-2-amine Show/Hide	C11H16BrNO2	1
1	Ki = 0.2 nM
CP0254846 Compound Info	((R)-4-bromo-3,6-dimethoxybenzocyclobuten-1-yl)methylamine Show/Hide	C11H14BrNO2	1
1	Ki = 0.26 nM
CP0648802 Compound Info	1-Methyl-2-(8-trifluoromethyl-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C14H13ClF3NO2	1
1	Ki = 0.29 nM
CP0287357 Compound Info	(1R,2R)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	Ki = 0.3 nM
CP0654157 Compound Info	2-(8-Bromo-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethyl-ammonium chloride Show/Hide	C13H13BrClNO2	1
1	Ki = 0.31 nM
CP0645867 Compound Info	1-Methyl-2-(8-trifluoromethyl-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C14H13ClF3NO2	1
1	Ki = 0.32 nM
CP0255251 Compound Info	(1R,2R)-2-Amino-1-(4-bromo-2,5-dimethoxy-phenyl)-propan-1-ol Show/Hide	C11H16BrNO3	1
1	Ki = 0.5 nM
CP0648823 Compound Info	2-(8-Bromo-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethyl-ammonium chloride Show/Hide	C13H13BrClNO2	1
1	Ki = 0.68 nM
CP0648800 Compound Info	1-Methyl-2-(8-trifluoromethyl-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C14H17ClF3NO2	1
1	Ki = 0.7 nM
CP0171294 Compound Info	(+/-)-(4-bromo-3,6-dimethoxybenzocyclobuten-1-yl)methylamine Show/Hide	C11H14BrNO2	1
1	Ki = 0.75 nM
CP0370559 Compound Info	(1R,2S)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	2
1	Ki = 0.8 nM
2	Ki = 17.4 nM
CP0273208 Compound Info	(1S,2R)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	2
1	Ki = 0.8 nM
2	Ki = 17.4 nM
CP0045155 Compound Info	2,5-dimethoxy-4-bromophenethylamine Show/Hide	C10H14BrNO2	1
1	Ki = 0.88 nM
CP0126359 Compound Info	(1R,2S)-2-Amino-1-(4-bromo-2,5-dimethoxy-phenyl)-propan-1-ol Show/Hide	C11H16BrNO3	1
1	Ki = 1.1 nM
CP0734420 Compound Info	2-(8-Bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethyl-ammonium chloride Show/Hide	C13H17BrClNO2	1
1	Ki = 1.2 nM
CP0686598 Compound Info	2-Benzo[1,2-b;4,5-b']difuran-4-yl-1-methyl-ethyl-ammonium chloride Show/Hide	C13H14ClNO2	1
1	Ki = 1.5 nM
CP0674016 Compound Info	1-Methyl-2-(8-trifluoromethyl-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C14H17ClF3NO2	1
1	Ki = 2 nM
CP0099558 Compound Info	2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-ethylamine Show/Hide	C11H16BrNO3	1
1	Ki = 2 nM
CP0162204 Compound Info	2-(2,5-Dimethoxy-4-trifluoromethyl-phenyl)-1-methyl-ethylamine Show/Hide	C12H16F3NO2	1
1	Ki = 2.2 nM
CP0727686 Compound Info	2-(8-Bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethyl-ammonium chloride Show/Hide	C13H17BrClNO2	1
1	Ki = 2.6 nM
CP0110578 Compound Info	(1S,2S)-2-(4-Bromo-2,5-dimethoxy-phenyl)-2-methoxy-1-methyl-ethylamine Show/Hide	C12H18BrNO3	1
1	Ki = 6 nM
CP0076323 Compound Info	2-[2-Methoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C19H25NO	1
1	Ki = 8 nM
CP0249508 Compound Info	(R)-2-(2,5-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	2
1	Ki = 9.2 nM
2	Ki = 2340 nM
CP0081321 Compound Info	1-(2,5-dimethoxy-4-(3-phenylpropyl)phenyl)propan-2-amine Show/Hide	C20H27NO2	2
1	Ki = 10 nM
2	Ki = 30 nM
CP0126146 Compound Info	6-[[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]methyl]-6,7-dihydro-5H-1-benzofuran-4-one Show/Hide	C21H21FN2O3	1
1	Ki = 10.72 nM
CP0179070 Compound Info	2-[2-Methoxy-5-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C19H25NO	2
1	Ki = 13 nM
2	Ki = 19 nM
CP0222963 Compound Info	2-(8-bromo-2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-1-methyl-ethylamine Show/Hide	C13H16BrNO2	1
1	Ki = 18 nM
CP0182842 Compound Info	2-[2-Methoxy-5-(3-phenyl-propyl)-phenyl]-ethylamine Show/Hide	C18H23NO	2
1	Ki = 20 nM
2	Ki = 30 nM
CP0157151 Compound Info	9,10-dihydroanthracene(DHA), 1a Show/Hide	C15H15N	1
1	Ki = 20 nM
CP0686394 Compound Info	2-Benzo[1,2-b;4,5-b']difuran-4-yl-1-methyl-ethyl-ammonium chloride Show/Hide	C13H14ClNO2	1
1	Ki = 37.9 nM
CP0192614 Compound Info	((S)-4-bromo-3,6-dimethoxybenzocyclobuten-1-yl)methylamine Show/Hide	C11H14BrNO2	1
1	Ki = 42 nM
CP0648799 Compound Info	1-Methyl-2-(2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C13H18ClNO2	1
1	Ki = 54.4 nM
CP0089401 Compound Info	C-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)-methylamine Show/Hide	C16H17N	1
1	Ki = 110 nM
CP0708722 Compound Info	1-Methyl-2-(2,3,6,7-tetrahydro-benzo[1,2-b;4,5-b']difuran-4-yl)-ethyl-ammonium chloride Show/Hide	C13H18ClNO2	1
1	Ki = 227 nM
CP0154007 Compound Info	2-(2,5-Dimethoxy-phenyl)-ethylamine Show/Hide	C10H15NO2	1
1	Ki = 2820 nM
CP0225516 Compound Info	(+/-)2-(2,5-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	Ki = 5200 nM

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT00825	5-hydroxytryptamine receptor 2A	Homo sapiens, Human	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han