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5-HT6 receptor

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Target not currently curated in GtoImmuPdb

Target id: 11

Nomenclature: 5-HT6 receptor

Family: 5-Hydroxytryptamine receptors

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 440 1p36.13 HTR6 5-hydroxytryptamine receptor 6 21
Mouse 7 440 4 70.57 cM Htr6 5-hydroxytryptamine (serotonin) receptor 6 20
Rat 7 436 5q36 Htr6 5-hydroxytryptamine receptor 6 28,38
Previous and Unofficial Names Click here for help
5-HT6 | serotonin receptor 6 | ST-B17 | 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht6r_human (Hs), 5ht6r_mouse (Mm), 5ht6r_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 pKd 4
pKd 8.7 (Kd 2x10-9 M) [4]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 8.6 – 8.7 pKd 5,25
pKd 8.6 – 8.7 [5,25]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 7.9 pKd 5
pKd 7.9 [5]
E6801 Small molecule or natural product Hs Partial agonist 8.7 pKi 17
pKi 8.7 (Ki 1.9x10-9 M) [17]
WAY-181187 Small molecule or natural product Hs Agonist 8.7 pKi 39
pKi 8.7 [39]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.4 pKi 7
pKi 8.4 [7]
WAY-208466 Small molecule or natural product Primary target of this compound Hs Agonist 8.3 pKi 3
pKi 8.3 (Ki 4.8x10-9 M) [3]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.0 – 8.6 pKi 4,7
pKi 8.0 – 8.6 [4,7]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.8 – 8.7 pKi 5,7
pKi 7.8 – 8.7 [5,7]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.0 – 8.1 pKi 4,7
pKi 8.0 – 8.1 [4,7]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.5 – 8.3 pKi 5-7,28
pKi 7.5 – 8.3 [5-7,28]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 14
pKi 7.8 [14]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.0 – 8.6 pKi 5-7
pKi 7.0 – 8.6 [5-7]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.9 – 8.4 pKi 5-6,28
pKi 6.9 – 8.4 [5-6,28]
S 16924 Small molecule or natural product Rn Full agonist 7.6 pKi 27
pKi 7.6 [27]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.5 pKi 21
pKi 7.5 [21]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.5 pKi 6
pKi 7.5 [6]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Full agonist 7.5 pKi 28
pKi 7.5 [28]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.4 pKi 21
pKi 7.4 [21]
lergotrile Small molecule or natural product Rn Full agonist 7.4 pKi 28
pKi 7.4 [28]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.6 – 7.9 pKi 5-7,28
pKi 6.6 – 7.9 [5-7,28]
dimethyltryptamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 21
pKi 7.2 [21]
5-hydroxytryptamine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 6.8 – 7.5 pKi 4,7,21
pKi 6.8 – 7.5 [4,7,21]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.0 pKi 28
pKi 7.0 [28]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.9 pKi 6
pKi 6.9 [6]
5-benzyloxytryptamine Small molecule or natural product Rn Full agonist 6.5 – 7.2 pKi 5-6,28
pKi 6.5 – 7.2 [5-6,28]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.2 – 7.3 pKi 5
pKi 6.2 – 7.3 [5]
DM-1451 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.5 pKi 25
pKi 6.5 [25]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 21
pKi 6.4 [21]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.3 pKi 28
pKi 6.3 [28]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.8 – 6.8 pKi 5,28
pKi 5.8 – 6.8 [5,28]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 pKi 21
pKi 6.2 [21]
OPC 4392 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.2 pKi 25
pKi 6.2 [25]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 21
pKi 6.1 [21]
5-CT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.5 – 6.7 pKi 5-6,28
pKi 5.5 – 6.7 [5-6,28]
LY 165,163 Small molecule or natural product Rn Full agonist 6.1 pKi 28
pKi 6.1 [28]
CGS-12066 Small molecule or natural product Rn Full agonist 6.1 pKi 28
pKi 6.1 [28]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 5.9 pKi 34
pKi 5.9 [34]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.9 pKi 42
pKi 5.9 [42]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 34
pKi 5.8 [34]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.6 pKi 29
pKi 5.6 [29]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.6 pKi 18
pKi 5.6 [18]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.6 pKi 28
pKi 5.6 [28]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.5 pKi 6
pKi 5.5 [6]
EMD-386088 Small molecule or natural product Primary target of this compound Hs Agonist 8.1 pIC50 26
pIC50 8.1 (IC50 7.4x10-9 M) [26]
[3H]5-CT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - -
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]SB258585 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.0 pKd 16
pKd 9.0 (Kd 1x10-9 M) [16]
[3H]Ro 63-0563 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.3 pKd 7
pKd 8.3 (Kd 5x10-9 M) [7]
[11C]GSK215083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKi 31
pKi 9.8 (Ki 1.6x10-10 M) [31]
intepirdine Small molecule or natural product Primary target of this compound Hs Antagonist 9.8 pKi 23
pKi 9.8 (Ki 1.7x10-10 M) [23]
Description: HeLa cell membrane assay, displacing [3H]LSD
idalopirdine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.1 pKi 23
pKi 9.1 (Ki 8.3x10-10 M) [23]
SB399885 Small molecule or natural product Hs Antagonist 9.0 pKi 16
pKi 9.0 (Ki 1x10-9 M) [16]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.9 pKi 37
pKi 8.9 [37]
SB 271046 Small molecule or natural product Hs Antagonist 8.9 pKi 10
pKi 8.9 (Ki 1.26x10-9 M) [10]
cerlapirdine Small molecule or natural product Primary target of this compound Hs Antagonist 8.9 pKi 13
pKi 8.9 (Ki 1.3x10-9 M) [13]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.4 pKi 4,7,21
pKi 8.2 – 9.4 [4,7,21]
SB258585 Small molecule or natural product Hs Antagonist 8.5 pKi 15
pKi 8.5 [15]
SB357134 Small molecule or natural product Hs Antagonist 8.5 pKi 11
pKi 8.5 [11]
methiothepin Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.5 – 9.4 pKi 5-7,28
pKi 7.5 – 9.4 [5-7,28]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.4 pKi 37
pKi 8.4 [37]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.3 pKi 35
pKi 8.3 [35]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 8.2 pKi 37
pKi 8.2 [37]
Ro 63-0563 Small molecule or natural product Hs Antagonist 7.9 – 8.4 pKi 7,40
pKi 7.9 – 8.4 (Ki 1.26x10-8 – 3.98x10-9 M) [7,40]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.6 – 8.6 pKi 22,37
pKi 7.6 – 8.6 [22,37]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.9 – 8.3 pKi 6,28
pKi 7.9 – 8.3 [6,28]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 8.0 pKi 21,35
pKi 8.0 [21,35]
ICI 169369 Small molecule or natural product Hs Antagonist 8.0 pKi 21
pKi 8.0 [21]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.8 – 8.1 pKi 4,7,21,35
pKi 7.8 – 8.1 [4,7,21,35]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.5 – 8.4 pKi 5-7,22,27-28,37
pKi 7.5 – 8.4 [5-7,22,27-28,37]
Ro 63-0563 Small molecule or natural product Rn Antagonist 7.8 – 8.0 pKi 7,40
pKi 7.8 – 8.0 [7,40]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.5 – 8.2 pKi 28,37
pKi 7.5 – 8.2 [28,37]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
pKi 7.8 [37]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
pKi 7.8 [37]
2-bromo-LSD Small molecule or natural product Rn Antagonist 7.8 pKi 28
pKi 7.8 [28]
fluperlapine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 7.8 pKi 37
pKi 7.8 [37]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.7 – 7.8 pKi 21,35
pKi 7.7 – 7.8 [21,35]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 14
pKi 7.7 [14]
bufotenine Small molecule or natural product Rn Antagonist 7.0 – 8.4 pKi 5
pKi 7.0 – 8.4 [5]
Ro 04-6790 Small molecule or natural product Hs Antagonist 7.3 – 7.9 pKi 7,40
pKi 7.3 – 7.9 [7,40]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.4 – 7.6 pKi 21,35
pKi 7.4 – 7.6 [21,35]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 – 7.8 pKi 28,37
pKi 7.2 – 7.8 [28,37]
Ro 04-6790 Small molecule or natural product Rn Antagonist 7.4 – 7.6 pKi 7,40
pKi 7.4 – 7.6 [7,40]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.4 pKi 22
pKi 7.4 [22]
fluperlapine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.3 – 7.5 pKi 21,35
pKi 7.3 – 7.5 [21,35]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.3 – 7.4 pKi 35
pKi 7.3 – 7.4 [35]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 21
pKi 7.3 [21]
α-ergocryptine Small molecule or natural product Rn Antagonist 7.3 pKi 6
pKi 7.3 [6]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 19
pKi 7.2 [19]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.2 pKi 37
pKi 7.2 [37]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 7.4 pKi 4,7,21
pKi 7.0 – 7.4 [4,7,21]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 pKi 35
pKi 7.2 [35]
dihydroergocristine Small molecule or natural product Rn Antagonist 7.2 pKi 6
pKi 7.2 [6]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.5 – 7.8 pKi 5-7,28
pKi 6.5 – 7.8 [5-7,28]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.9 – 7.4 pKi 5,7,28
pKi 6.9 – 7.4 [5,7,28]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 – 7.3 pKi 4,7,21
pKi 6.9 – 7.3 [4,7,21]
tiospirone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.1 pKi 37
pKi 7.1 [37]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.1 pKi 35
pKi 7.1 [35]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.6 – 7.5 pKi 5-7,28
pKi 6.6 – 7.5 [5-7,28]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 – 7.2 pKi 4,7,21
pKi 6.9 – 7.2 [4,7,21]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 – 7.4 pKi 4,7,21
pKi 6.4 – 7.4 [4,7,21]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.9 pKi 28
pKi 6.9 [28]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.5 – 7.2 pKi 5,7,28
pKi 6.5 – 7.2 [5,7,28]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.8 pKi 25
pKi 6.8 [25]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 pKi 21
pKi 6.8 [21]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.5 – 6.8 pKi 4,7,21
pKi 6.5 – 6.8 [4,7,21]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.4 – 6.6 pKi 5-7,28
pKi 6.4 – 6.6 [5-7,28]
vortioxetine Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.5 pKi 1
pKi 6.5 (Ki 3.3x10-7 M) [1]
duloxetine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 pKi 12
pKi 6.4 [12]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 6.0 – 6.4 pKi 22,37
pKi 6.0 – 6.4 [22,37]
tiospirone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 21
pKi 6.0 [21]
spiperone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.8 pKi 37
pKi 5.8 [37]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 5.8 pKi 28
pKi 5.8 [28]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.6 pKi 21
pKi 5.6 [21]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.6 pKi 21
pKi 5.6 [21]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 – 5.7 pKi 4,7,21
pKi 5.4 – 5.7 [4,7,21]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.1 – 5.8 pKi 5,7,28
pKi 5.1 – 5.8 [5,7,28]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 5.2 pKi 6
pKi 5.2 [6]