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5-HT2A receptor

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Target id: 6

Nomenclature: 5-HT2A 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 7 471 13q14.2 HTR2A 5-hydroxytryptamine receptor 2A 86
Mouse 7 471 14 39.37 cM Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 20,95
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine receptor 2A 24
Previous and Unofficial Names Click here for help
'D' receptor | 5Ht-2 | serotonin 5HT-2 receptor | serotonin receptor 2A | 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht2a_human (Hs), 5ht2a_mouse (Mm), 5ht2a_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
tryptamine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H](+)DOB Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 9.1 pKd 46,84
pKd 9.1 [46,84]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 9.1 pKd 5
pKd 9.1 [5]
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 8.9 pKd 84
pKd 8.9 [84]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.4 pKi 2
pKi 9.4 [2]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.4 pKi 38
pKi 9.4 [38]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 – 9.3 pKi 38,49,63
pKi 9.2 – 9.3 [38,63]
pKi 9.2 [49]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.1 pKi 38
pKi 9.1 [38]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.9 – 9.2 pKi 38,57
pKi 8.9 – 9.2 [38,57]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.0 pKi 38
pKi 9.0 [38]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 38
pKi 9.0 [38]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 52
pKi 9.0 [52]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.9 pKi 34
pKi 8.9 [34]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 49
pKi 8.7 [49]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.6 pKi 54
pKi 8.6 [54]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.5 pKi 58
pKi 8.5 [58]
ergometrine Small molecule or natural product Approved drug Rn Full agonist 8.5 pKi 34
pKi 8.5 [34]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.3 pKi 54
pKi 8.3 [54]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 9.2 pKi 9,57,84
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.31x10-10 M) [9,57,84]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 54
pKi 8.2 [54]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.1 pKi 54
pKi 8.1 [54]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.1 pKi 34
pKi 8.1 [34]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.0 pKi 74
pKi 8.0 [74]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.9 pKi 74
pKi 7.9 [74]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 26,69
pKi 7.8 [26,69]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.5 – 8.1 pKi 41,83
pKi 7.5 – 8.1 [41,83]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.8 pKi 74
pKi 7.8 [74]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 38
pKi 7.8 [38]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.8 pKi 16
pKi 7.8 [16]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.7 pKi 83
pKi 7.7 [83]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 38
pKi 7.5 [38]
N-1-isopropyl-5-MeOT Small molecule or natural product Rn Full agonist 7.4 pKi 34
pKi 7.4 [34]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 38
pKi 7.4 [38]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 69
pKi 7.3 [69]
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 6.0 – 8.4 pKi 2,9,34,38,49,84
pKi 6.0 – 8.4 [2,9,34,38,49,84]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 38
pKi 7.2 [38]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 7.5 pKi 38,57,84
pKi 6.8 – 7.5 [38,57,84]
tryptamine 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 7.1 pKi 34
pKi 7.1 [34]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 82
pKi 7.1 [82]
N-1-isopropyltryptamine Small molecule or natural product Rn Full agonist 7.1 pKi 34
pKi 7.1 [34]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.0 pKi 54
pKi 7.0 [54]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.0 pKi 77
pKi 7.0 [77]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 38
pKi 6.9 [38]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 38
pKi 6.9 [38]
DOM Small molecule or natural product Rn Full agonist 6.8 pKi 16
pKi 6.8 [16]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.8 pKi 89
pKi 6.8 [89]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 pKi 33
pKi 6.7 [33]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 6.6 pKi 69
pKi 6.6 [69]
N-1-isopropyltryptamine Small molecule or natural product Hs Full agonist 6.6 pKi 34
pKi 6.6 [34]
tryptamine 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 5.5 – 7.6 pKi 9,34,38
pKi 5.5 – 7.6 [9,34,38]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 pKi 38
pKi 6.5 [38]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.5 pKi 43
pKi 6.5 (Ki 3.26x10-7 M) [43]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 6.4 pKi 74
pKi 6.4 [74]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 38
pKi 6.4 [38]
N-1-isopropyl-5-MeOT Small molecule or natural product Hs Full agonist 6.3 pKi 34
pKi 6.3 [34]
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 6.0 – 6.5 pKi 16,74,82
pKi 6.0 – 6.5 [16,74,82]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 27
pKi 6.2 (Ki 6x10-7 M) [27]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 pKi 38
pKi 6.0 [38]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.9 pKi 56
pKi 5.9 [56]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.9 pKi 82
pKi 5.9 [82]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.8 pKi 43
pKi 5.8 (Ki 1.464x10-6 M) [43]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 38
pKi 5.6 [38]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 64
pKi 5.4 [64]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 38
pKi 5.4 [38]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 38,54
pKi 5.0 – 5.5 [38,54]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.0 pKi 38
pKi 5.0 [38]
psilocin Small molecule or natural product Hs Agonist 7.6 pEC50 75
pEC50 7.6 (EC50 2.4x10-8 M) [75]
Description: Determined in an [3H]inositol phosphate accumulation assay in cells stably expressing h5-HT2A.
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.8 pEC50 89
pEC50 6.8 [89]
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
[3H]fananserin Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 9.9 pKd 48
pKd 9.9 (Kd 1.3x10-10 M) [48]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.6 – 9.7 pKd 38,71
pKd 8.6 – 9.7 (Kd 2.9x10-9 – 2x10-10 M) [38,71]
[3H]N-methylspiperone Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 9.1 pKd 82
pKd 9.1 [82]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 8.8 pKd 82
pKd 8.8 [82]
compound 3b [PMID:28943244] Small molecule or natural product Primary target of this compound Hs Antagonist 10.6 pKi 19
pKi 10.6 (Ki 2.24x10-11 M) [19]
asenapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.2 pKi 80
pKi 10.2 (Ki 6x10-11 M) [80]
AC-90179 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.7 pKi 90
pKi 9.7 [90]
risperidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 9.3 – 10.0 pKi 39,41,77
pKi 9.3 – 10.0 [39,41,77]
pimavanserin Small molecule or natural product Approved drug Primary target of this compound Hs Inverse agonist 9.3 pKi 23,90
pKi 9.3 [23,90]
Description: Ki determined in membrane radioligand binding assay.
lumateperone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.3 pKi 45,85
pKi 9.3 (Ki 5x10-10 M) [45,85]
sertindole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.2 – 9.4 pKi 39,41,77
pKi 9.2 – 9.4 [39,41,77]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.2 pKi 72,82
pKi 9.2 [72,82]
LY86057 Small molecule or natural product Hs Antagonist 9.2 pKi 34
pKi 9.2 [34]
ziprasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 – 9.5 pKi 39,41,77,80
pKi 8.8 – 9.5 [39,41,77,80]
spiperone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.0 – 9.2 pKi 16,82
pKi 9.0 – 9.2 [16,82]
[11C]GSK215083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKi 62
pKi 9.1 (Ki 7.9x10-10 M) [62]
blonanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.1 pKi 60
pKi 9.1 (Ki 8.1x10-10 M) [60]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 77
pKi 9.0 [77]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.0 pKi 70
pKi 9.0 [70]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.4 – 9.5 pKi 16,40
pKi 8.4 – 9.5 [16,40]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 8.9 pKi 16
pKi 8.9 [16]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.1 – 9.7 pKi 11,38,71
pKi 8.1 – 9.7 (Ki 7.94x10-9 – 1.99x10-10 M) [11,38,71]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.3 – 9.4 pKi 38,72
pKi 9.4 [72]
pKi 8.3 [38]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 31
pKi 8.8 [31]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.6 – 9.0 pKi 16,82
pKi 8.6 – 9.0 [16,82]
olanzapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.6 – 8.9 pKi 39,41,77,80
pKi 8.6 – 8.9 [39,41,77,80]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.7 pKi 16
pKi 8.7 [16]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.4 – 9.0 pKi 16,70
pKi 8.4 – 9.0 [16,70]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 32
pKi 8.7 (Ki 2.03x10-9 M) [32]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.7 – 9.6 pKi 38,40,55
pKi 7.7 – 9.6 [38,40,55]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 9
pKi 8.6 [9]
spiperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 9.4 pKi 9,38,84
pKi 7.8 – 9.4 [9,38,84]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.6 pKi 77
pKi 8.6 [77]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 38
pKi 8.6 [38]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.6 pKi 34
pKi 8.6 [34]
BF-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 76
pKi 8.6 [76]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 38
pKi 8.5 [38]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.5 pKi 16
pKi 8.5 [16]
LY215840 Small molecule or natural product Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
LY53857 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
amesergide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 34
pKi 8.5 [34]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.5 pKi 71
pKi 8.5 [71]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.4 pKi 38
pKi 8.4 [38]
LY108742 Small molecule or natural product Rn Antagonist 8.4 pKi 34
pKi 8.4 [34]
sergolexole Small molecule or natural product Rn Antagonist 8.4 pKi 34
pKi 8.4 [34]
clozapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 7.6 – 9.0 pKi 38,41,52,77,90
pKi 7.6 – 9.0 [38,41,52,77,90]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 77
pKi 8.3 [77]
nefazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.2 pKi 79
pKi 8.2 (Ki 5.8x10-9 M) [79]
roxindole Small molecule or natural product Click here for species-specific activity table