Protein Information

General Information of the Protein

Protein ID	PT01480
Protein Name	5-hydroxytryptamine receptor 2C
Secondarily Protein Name	5-hydroxytryptamine receptor 1C Serotonin receptor 2C
Gene Name	HTR2C
Secondarily Gene Name	5ht1c Htr1c
Sequence	MVNLGNAVRSLLMHLIGLLVWQFDISISPVAAIVTDTFNSSDGGRLFQFPDGVQNWPALSIVVIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVWPLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWAISIGVSVPIPVIGLRDESKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYFLTIYVLRRQTLMLLRGHTEEELANMSLNFLNCCCKKNGGEEENAPNPNPDQKPRRKKKEKRPRGTMQAINNEKKASKVLGIVFFVFLIMWCPFFITNILSVLCGKACNQKLMEKLLNVFVWIGYVCSGINPLVYTLFNKIYRRAFSKYLRCDYKPDKKPPVRQIPRVAATALSGRELNVNIYRHTNERVARKANDPEPGIEMQVENLELPVNPSNVVSERISSV 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 ergot alkaloid derivatives, 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 a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and feeding behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis. Show/Hide
Uniprot ID	P08909
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: CL000398 , A-9

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0423133 Compound Info	2-[2,5-Dimethoxy-4-(4-phenyl-butyl)-phenyl]-1-methyl-ethylamine Show/Hide	C21H29NO2	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0372982 Compound Info	2-{4-[3-(4-Chloro-phenyl)-propyl]-2,5-dimethoxy-phenyl}-1-methyl-ethylamine Show/Hide	C20H26ClNO2	1
1	Ki = 16 nM Bioactivity Info	TI LI LO TS
CP0437508 Compound Info	2-{2,5-Dimethoxy-4-[3-(4-methoxy-phenyl)-propyl]-phenyl}-1-methyl-ethylamine Show/Hide	C21H29NO3	1
1	Ki = 24 nM Bioactivity Info	TI LI LO TS
CP0510028 Compound Info	2-[2,5-Dimethoxy-4-(4-phenyl-butyl)-phenyl]-ethylamine Show/Hide	C20H27NO2	1
1	Ki = 25 nM Bioactivity Info	TI LI LO TS
CP0448578 Compound Info	2-[2,5-Dimethoxy-4-(3-phenyl-propyl)-phenyl]-ethylamine Show/Hide	C19H25NO2	1
1	Ki = 28 nM Bioactivity Info	TI LI LO TS
CP0436563 Compound Info	2-[2,6-Dimethoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C20H27NO2	1
1	Ki = 39 nM Bioactivity Info	TI LI LO TS
CP0397496 Compound Info	2-[3,5-Dimethoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C20H27NO2	1
1	Ki = 40 nM Bioactivity Info	TI LI LO TS
CP0081321 Compound Info	1-(2,5-dimethoxy-4-(3-phenylpropyl)phenyl)propan-2-amine Show/Hide	C20H27NO2	1
1	Ki = 50 nM Bioactivity Info	TI LI LO TS
CP0353454 Compound Info	1-(4-Fluoro-phenyl)-4-(5-methyl-1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl)-butan-1-one Show/Hide	C22H23FN2O	1
1	Ki = 60 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	Ki = 64 nM Bioactivity Info	TI LI LO TS
CP0101165 Compound Info	2-[3-(4-Fluoro-phenoxy)-propyl]-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H23FN2O	1
1	Ki = 75 nM Bioactivity Info	TI LI LO TS
CP0380282 Compound Info	2-(2,5-Dimethoxy-4-phenethyl-phenyl)-ethylamine Show/Hide	C18H23NO2	1
1	Ki = 76 nM Bioactivity Info	TI LI LO TS
CP0374767 Compound Info	2-[2,3-Dimethoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C20H27NO2	1
1	Ki = 79 nM Bioactivity Info	TI LI LO TS
CP0076323 Compound Info	2-[2-Methoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C19H25NO	1
1	Ki = 89 nM Bioactivity Info	TI LI LO TS
CP0114447 Compound Info	5-Benzyl-2-(3-phenoxy-propyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C27H28N2O	1
1	Ki = 90 nM Bioactivity Info	TI LI LO TS
CP0039881 Compound Info	1-Phenyl-4-(1,3,4,9-tetrahydro-beta-carbolin-2-yl)-butan-1-one Show/Hide	C21H22N2O	1
1	Ki = 115 nM Bioactivity Info	TI LI LO TS
CP0436882 Compound Info	2-[3-Methoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C19H25NO	1
1	Ki = 135 nM Bioactivity Info	TI LI LO TS
CP0463665 Compound Info	2-(2,5-Dimethoxy-4-phenethyl-phenyl)-1-methyl-ethylamine Show/Hide	C19H25NO2	1
1	Ki = 140 nM Bioactivity Info	TI LI LO TS
CP0039861 Compound Info	2-[3-(4-Fluoro-phenoxy)-propyl]-8-methoxy-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C22H25FN2O2	1
1	Ki = 150 nM Bioactivity Info	TI LI LO TS
CP0358145 Compound Info	2-(3-Phenoxy-propyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C20H22N2O	1
1	Ki = 160 nM Bioactivity Info	TI LI LO TS
CP0045155 Compound Info	2,5-dimethoxy-4-bromophenethylamine Show/Hide	C10H14BrNO2	1
1	Ki = 190 nM Bioactivity Info	TI LI LO TS
CP0713830 Compound Info	1-(4-Fluoro-phenyl)-4-(5-methyl-1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl)-butan-1-one oxime Show/Hide	C22H24FN3O	1
1	Ki = 190 nM Bioactivity Info	TI LI LO TS
CP0289420 Compound Info	5-Ethyl-2-(3-phenoxy-propyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C22H26N2O	1
1	Ki = 215 nM Bioactivity Info	TI LI LO TS
CP0197074 Compound Info	2-[3-(4-Fluoro-phenoxy)-propyl]-6-methoxy-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C22H25FN2O2	1
1	Ki = 225 nM Bioactivity Info	TI LI LO TS
CP0346478 Compound Info	6-Chloro-2-[3-(4-fluoro-phenoxy)-propyl]-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H22ClFN2O	1
1	Ki = 225 nM Bioactivity Info	TI LI LO TS
CP0189566 Compound Info	2-[2-(4-Fluoro-phenoxy)-ethyl]-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C20H21FN2O	1
1	Ki = 235 nM Bioactivity Info	TI LI LO TS
CP0049244 Compound Info	5-Methyl-2-(5-phenyl-pent-2-enyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C23H26N2	1
1	Ki = 245 nM Bioactivity Info	TI LI LO TS
CP0278253 Compound Info	4-Cyclohexylamino-1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-piperidine-4-carboxylic acid amide Show/Hide	C22H32FN3O2	1
1	Ki = 270 nM Bioactivity Info	TI LI LO TS
CP0148087 Compound Info	5-methyl-2-[(Z)-5-phenylpent-2-enyl]-3,4-dihydro-1H-pyrido[4,3-b]indole Show/Hide	C23H26N2	1
1	Ki = 285 nM Bioactivity Info	TI LI LO TS
CP0197840 Compound Info	5-Methyl-2-(3-phenoxy-propyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H24N2O	1
1	Ki = 285 nM Bioactivity Info	TI LI LO TS
CP0078447 Compound Info	5-Methyl-2-[3-(naphthalen-2-yloxy)-propyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C25H26N2O	1
1	Ki = 300 nM Bioactivity Info	TI LI LO TS
CP0185416 Compound Info	4-[3-(5-Methyl-1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl)-propoxy]-phenylamine Show/Hide	C21H25N3O	1
1	Ki = 300 nM Bioactivity Info	TI LI LO TS
CP0213412 Compound Info	8-Chloro-2-[3-(4-fluoro-phenoxy)-propyl]-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H22ClFN2O	1
1	Ki = 300 nM Bioactivity Info	TI LI LO TS
CP0309911 Compound Info	5-Methyl-2-[3-(4-nitro-phenoxy)-propyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C21H23N3O3	1
1	Ki = 300 nM Bioactivity Info	TI LI LO TS
CP0061220 Compound Info	2-(3-Phenoxy-propyl)-2,3,4,9-tetrahydro-1H-beta-carboline Show/Hide	C20H22N2O	1
1	Ki = 310 nM Bioactivity Info	TI LI LO TS
CP0197051 Compound Info	1-(4-Fluoro-phenyl)-4-(5-methyl-1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl)-butan-1-ol Show/Hide	C22H25FN2O	1
1	Ki = 390 nM Bioactivity Info	TI LI LO TS
CP0108357 Compound Info	5-Methyl-2-[3-(naphthalen-1-yloxy)-propyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C25H26N2O	1
1	Ki = 400 nM Bioactivity Info	TI LI LO TS
CP0189536 Compound Info	9-Methyl-2-(3-phenoxy-propyl)-2,3,4,9-tetrahydro-1H-beta-carboline Show/Hide	C21H24N2O	1
1	Ki = 400 nM Bioactivity Info	TI LI LO TS
CP0217185 Compound Info	1-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-4-isopropylamino-piperidine-4-carboxylic acid amide Show/Hide	C19H28FN3O2	1
1	Ki = 426 nM Bioactivity Info	TI LI LO TS
CP0380285 Compound Info	2-(4-(3-phenylpropyl)phenyl)ethanamine Show/Hide	C17H21N	1
1	Ki = 525 nM Bioactivity Info	TI LI LO TS
CP0460820 Compound Info	1-Methyl-2-[4-(3-phenyl-propyl)-phenyl]-ethylamine Show/Hide	C18H23N	1
1	Ki = 530 nM Bioactivity Info	TI LI LO TS
CP0097512 Compound Info	5-Methyl-2-(6-phenyl-hexyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C24H30N2	1
1	Ki = 530 nM Bioactivity Info	TI LI LO TS
CP0404231 Compound Info	2-(4-Bromo-3,5-dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H16BrNO2	1
1	Ki = 570 nM Bioactivity Info	TI LI LO TS
CP0366206 Compound Info	2-(3-Benzyloxy-propyl)-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C22H26N2O	1
1	Ki = 650 nM Bioactivity Info	TI LI LO TS
CP0201275 Compound Info	1-Cyclohexyl-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C23H32FN3O2	1
1	Ki = 677 nM Bioactivity Info	TI LI LO TS
CP0358182 Compound Info	2-[4-(4-Methoxy-phenyl)-butyl]-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C23H28N2O	1
1	Ki = 990 nM Bioactivity Info	TI LI LO TS
CP0336625 Compound Info	5-Methyl-2-(5-phenyl-pentyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole Show/Hide	C23H28N2	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0509975 Compound Info	3-Benzyl-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C25H30FN3O2	1
1	Ki = 1405 nM Bioactivity Info	TI LI LO TS
CP0040671 Compound Info	8-[4-(4-fluorophenyl)-4-keto-butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one Show/Hide	C23H26FN3O2	1
1	Ki = 1600 nM Bioactivity Info	TI LI LO TS
CP0392232 Compound Info	1-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-4-methylamino-piperidine-4-carboxylic acid amide Show/Hide	C17H24FN3O2	1
1	Ki = 4480 nM Bioactivity Info	TI LI LO TS
CP0154007 Compound Info	2-(2,5-Dimethoxy-phenyl)-ethylamine Show/Hide	C10H15NO2	1
1	Ki = 5520 nM Bioactivity Info	TI LI LO TS
CP0059946 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-1,3-dimethyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C19H26FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0063089 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C18H24FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0063768 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-1-isopropyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C20H28FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0102266 Compound Info	1-Ethyl-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C19H26FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0113075 Compound Info	3-Butyl-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C22H32FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0202170 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-1-methyl-3-propyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C21H30FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0277509 Compound Info	8-[3-(4-Fluoro-phenoxy)-propyl]-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C17H24FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0277875 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-3-isopropyl-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C21H30FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0307324 Compound Info	8-[3-(4-Fluoro-phenoxy)-propyl]-1-methyl-3-propyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C20H30FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0392231 Compound Info	3-Ethyl-8-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1-methyl-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C20H28FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0392840 Compound Info	4-Amino-1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-piperidine-4-carboxylic acid amide Show/Hide	C16H22FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0430583 Compound Info	8-[4-(4-Fluoro-phenyl)-4-oxo-butyl]-1,3,8-triaza-spiro[4.5]decan-4-one Show/Hide	C17H22FN3O2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0225516 Compound Info	(+/-)2-(2,5-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0269560 Compound Info	1-Phenylpropan-2-amin Show/Hide	C9H13N	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0392700 Compound Info	(+/-)2-(2,3-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0448481 Compound Info	(+/-)2-(2,6-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0448556 Compound Info	(+/-)2-(2-Methoxy-phenyl)-1-methyl-ethylamine Show/Hide	C10H15NO	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0507779 Compound Info	(+/-)2-(3-Methoxy-phenyl)-1-methyl-ethylamine Show/Hide	C10H15NO	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS
CP0885845 Compound Info	(+/-)2-(3,5-Dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H17NO2	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000085 , J1

Cell Line Info

Cell Line ID: CL000035 , NIH 3T3

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0001238 Compound Info	14C-5-hydroxy tryptamine creatinine disulfate Show/Hide	C10H12N2O	3
1	IC50 = 42 nM
2	IC50 = 81 nM
3	Ki = 31.62 nM
CP0071154 Compound Info	2-(5-methoxy-1H-indol-3-yl)-N,N-dimethyl-ethanamine Show/Hide	C13H18N2O	1
1	IC50 = 250 nM
CP0031743 Compound Info	1H-imidazo[4,5-c]pyridine derivative Show/Hide	C18H26N4O2S	2
1	Ki = 1.585 nM
2	Ki = 5.2 nM
CP0047728 Compound Info	(+)-2-(4-Bromo-2,5-dimethoxy-phenyl)-1-methyl-ethylamine Show/Hide	C11H16BrNO2	2
1	Ki = 2.8 nM
2	Ki = 70 nM
CP0076323 Compound Info	2-[2-Methoxy-4-(3-phenyl-propyl)-phenyl]-1-methyl-ethylamine Show/Hide	C19H25NO	1
1	Ki = 89 nM
CP0040671 Compound Info	8-[4-(4-fluorophenyl)-4-keto-butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one Show/Hide	C23H26FN3O2	1
1	Ki = 1000 nM
CP0154007 Compound Info	2-(2,5-Dimethoxy-phenyl)-ethylamine Show/Hide	C10H15NO2	1
1	Ki = 6400 nM

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT00939	5-hydroxytryptamine receptor 2C	Homo sapiens, Human	Protein Info
PT05193	5-hydroxytryptamine receptor 2C	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han