Protein Information

General Information of the Protein

Protein ID	PT01513
Protein Name	5-hydroxytryptamine receptor 5A
Secondarily Protein Name	Serotonin receptor 5A
Gene Name	HTR5A
Sequence	MDLPVNLTSFSLSTPSPLETNHSLGKDDLRPSSPLLSVFGVLILTLLGFLVAATFAWNLLVLATILRVRTFHRVPHNLVASMAVSDVLVAALVMPLSLVHELSGRRWQLGRRLCQLWIACDVLCCTASIWNVTAIALDRYWSITRHMEYTLRTRKCVSNVMIALTWALSAVISLAPLLFGWGETYSEGSEECQVSREPSYAVFSTVGAFYLPLCVVLFVYWKIYKAAKFRVGSRKTNSVSPISEAVEVKDSAKQPQMVFTVRHATVTFQPEGDTWREQKEQRAALMVGILIGVFVLCWIPFFLTELISPLCSCDIPAIWKSIFLWLGYSNSFFNPLIYTAFNKNYNSAFKNFFSRQH Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Small molecule receptor (family A GPCR) > Monoamine receptor > Serotonin receptor
Function	This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins. Show/Hide
Uniprot ID	Primary ID: P47898 Secondarily ID: Q2M2D2 Show/Hide
Ensembl ID	ENSG00000157219
HGNC ID	HGNC:5300
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: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0795225 Compound Info	1-(3-Thiophen-2-yl-phenyl)-ethanone, O-(phenylaminocarbonyl)oxime Show/Hide	C19H16N2O2S	1
1	IC50 = 1 nM Bioactivity Info	TI LI LO TS
CP0395135 Compound Info	(R)-2-(4-Fluoro-phenyl)-2-{1-[3-(5-[1,2,4]triazol-4-yl-1H-indol-3-yl)-propyl]-piperidin-4-ylamino}-ethanol Show/Hide	C26H31FN6O	1
1	IC50 > 10000 nM Bioactivity Info	TI LI LO TS
CP0378052 Compound Info	(E)-N-[2-(dimethylamino)ethyl]-3-phenyl-N-[[4-[5-[(2-phenylethylamino)methyl]pyridin-2-yl]phenyl]methyl]prop-2-enamide Show/Hide	C34H38N4O	1
1	Ki = 5.012 nM Bioactivity Info	TI LI LO TS
CP0861232 Compound Info	3-Cyclopentyl-N-(2-dimethylamino-ethyl)-N-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-propionamide with di TFA Show/Hide	C38H47F6N3O5	1
1	Ki = 6.31 nM Bioactivity Info	TI LI LO TS
CP0485623 Compound Info	3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[[4-[5-[(2-phenylethylamino)methyl]pyridin-2-yl]phenyl]methyl]propanamide Show/Hide	C33H44N4O	1
1	Ki = 12.59 nM Bioactivity Info	TI LI LO TS
CP0449028 Compound Info	3-cyclopentyl-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]-N-(piperidin-2-ylmethyl)propanamide;2,2,2-trifluoroacetic acid Show/Hide	C38H48F3N3O3	1
1	Ki = 25.12 nM Bioactivity Info	TI LI LO TS
CP0526014 Compound Info	(E)-N-[2-(dimethylamino)ethyl]-3-phenyl-N-[[6-[4-[(2-phenylethylamino)methyl]phenyl]pyridin-3-yl]methyl]prop-2-enamide Show/Hide	C34H38N4O	1
1	Ki = 25.12 nM Bioactivity Info	TI LI LO TS
CP0853819 Compound Info	(E)-N-(2-Dimethylamino-ethyl)-N-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-3-phenyl-acrylamide TFA Show/Hide	C37H40F3N3O3	1
1	Ki = 25.12 nM Bioactivity Info	TI LI LO TS
CP0377983 Compound Info	3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[[6-[4-[(2-phenylethylamino)methyl]phenyl]pyridin-3-yl]methyl]propanamide Show/Hide	C33H44N4O	1
1	Ki = 31.62 nM Bioactivity Info	TI LI LO TS
CP0888292 Compound Info	3-Cyclopentyl-N-(2-dimethylamino-ethyl)-N-{4'-[(2-pyridin-2-yl-ethylamino)-methyl]-biphenyl-4-ylmethyl}-propionamide TFA Show/Hide	C35H45F3N4O3	1
1	Ki = 31.62 nM Bioactivity Info	TI LI LO TS
CP0847634 Compound Info	(E)-N-[4'-(Phenethylamino-methyl)-biphenyl-4-ylmethyl]-3-phenyl-N-pyridin-3-ylmethyl-acrylamide TFA Show/Hide	C39H36F3N3O3	1
1	Ki = 50.12 nM Bioactivity Info	TI LI LO TS
CP0497416 Compound Info	N-[2-(dimethylamino)ethyl]-2-phenyl-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]cyclopropane-1-carboxamide;2,2,2-trifluoroacetic acid Show/Hide	C38H42F3N3O3	1
1	Ki = 79.43 nM Bioactivity Info	TI LI LO TS
CP0916896 Compound Info	3-Cyclopentyl-N-(2-dimethylamino-ethyl)-N-{4'-[(2-phenoxy-ethylamino)-methyl]-biphenyl-4-ylmethyl}-propionamide TFA Show/Hide	C36H46F3N3O4	1
1	Ki = 79.43 nM Bioactivity Info	TI LI LO TS
CP0526012 Compound Info	1-benzyl-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]piperidin-4-amine Show/Hide	C34H39N3	1
1	Ki = 125.89 nM Bioactivity Info	TI LI LO TS
CP0522439 Compound Info	1-benzyl-N-[[3-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]piperidin-4-amine Show/Hide	C34H39N3	1
1	Ki = 199.53 nM Bioactivity Info	TI LI LO TS
CP0910932 Compound Info	Benzo[1,3]dioxole-5-carboxylic acid [4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-pyridin-3-ylmethyl-amide TFA Show/Hide	C38H34F3N3O5	1
1	Ki = 199.53 nM Bioactivity Info	TI LI LO TS
CP0926573 Compound Info	3-Cyclopentyl-N-(2-dimethylamino-ethyl)-N-[4'-(indan-2-ylaminomethyl)-biphenyl-4-ylmethyl]-propionamide TFA Show/Hide	C37H46F3N3O3	1
1	Ki = 251.19 nM Bioactivity Info	TI LI LO TS
CP0932580 Compound Info	(E)-2-Phenyl-ethenesulfonic acid (2-dimethylamino-ethyl)-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-amide TFA Show/Hide	C36H40F3N3O4S	1
1	Ki = 251.19 nM Bioactivity Info	TI LI LO TS
CP0911875 Compound Info	1-(2-Dimethylamino-ethyl)-1-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-3-phenyl-urea TFA Show/Hide	C35H39F3N4O3	1
1	Ki = 398.11 nM Bioactivity Info	TI LI LO TS
CP0911095 Compound Info	(E)-N-[2-(3-Methoxy-phenyl)-ethyl]-N-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-3-phenyl-acrylamide TFA Show/Hide	C42H41F3N2O4	1
1	Ki = 501.19 nM Bioactivity Info	TI LI LO TS
CP0949368 Compound Info	N-(2-Dimethylamino-ethyl)-N-[4'-(phenethylamino-methyl)-biphenyl-4-ylmethyl]-benzamide TFA Show/Hide	C35H38F3N3O3	1
1	Ki = 630.96 nM Bioactivity Info	TI LI LO TS
CP0916505 Compound Info	(E)-N-(4'-{[(Benzo[1,3]dioxol-5-ylmethyl)-amino]-methyl}-biphenyl-4-ylmethyl)-3-phenyl-N-pyridin-3-ylmethyl-acrylamide TFA Show/Hide	C39H34F3N3O5	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0926572 Compound Info	N-(4'-Aminomethyl-biphenyl-4-ylmethyl)-3-cyclopentyl-N-(2-dimethylamino-ethyl)-propionamide TFA Show/Hide	C28H38F3N3O3	1
1	Ki = 3162.28 nM Bioactivity Info	TI LI LO TS
CP0846434 Compound Info	(E)-N-{4'-[(2-Methoxy-ethylamino)-methyl]-biphenyl-4-ylmethyl}-3-phenyl-N-pyridin-3-ylmethyl-acrylamide TFA Show/Hide	C34H34F3N3O4	1
1	Ki = 6309.57 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000386 , Flp-In-CHO

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000065 , HEK293-EBNA

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0001238 Compound Info	14C-5-hydroxy tryptamine creatinine disulfate Show/Hide	C10H12N2O	10
1	IC50 = 79 nM
2	IC50 = 160 nM
3	IC50 = 180 nM
4	IC50 = 184 nM
5	IC50 = 280 nM
6	Ki = 82 nM
7	Ki = 110 nM
8	Ki = 126 nM
9	Ki = 170 nM
10	Ki = 250 nM
CP0096286 Compound Info	(R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidin-1-ylsulfonyl)phenol Show/Hide	C18H28N2O3S	2
1	Ki = 0.78 nM
2	Ki = 65 nM
CP0079728 Compound Info	5-chloro-4-methyl-1,4-dihydroquinazolin-2-amine Show/Hide	C9H10ClN3	1
1	Ki = 5.012 nM
CP0785037 Compound Info	4-methyl-3,4-dihydroquinazolin-2-amine hydroiodide Show/Hide	C9H12IN3	1
1	Ki = 38 nM
CP0002071 Compound Info	N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-N-prop-2-enylprop-2-en-1-amine Show/Hide	C17H22N2O	1
1	Ki = 3311.31 nM

Clinical Information about the Protein

Target 1 ( 5-HT 5A receptor (HTR5A) )

Target Type	Successful Target
Disease	1 Target-related Disease				1
1	Hyperprolactinaemia [ICD-11: 5A60.1]
Approved Drug(s)	1 Approved Drug				1
1	Metergolin	Drug Info	Approved	Hyperprolactinaemia

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han