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5-HT2A receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

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 90
Mouse 7 471 14 39.37 cM Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 20,100
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine receptor 2A 26
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
Alphafold
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 49,88
pKd 9.1 [49,88]
[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 4
pKd 9.1 [4]
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 88
pKd 8.9 [88]
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 41
pKi 9.4 [41]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 – 9.3 pKi 41,52,68
pKi 9.2 – 9.3 [41,68]
pKi 9.2 [52]
2C-B Small molecule or natural product Hs Agonist 9.2 pKi 53
pKi 9.2 (Ki 6.6x10-10 M) [53]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.1 pKi 41
pKi 9.1 [41]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.9 – 9.2 pKi 41,61
pKi 8.9 – 9.2 [41,61]
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 41
pKi 9.0 [41]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 41
pKi 9.0 [41]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 56
pKi 9.0 [56]
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 36
pKi 8.9 [36]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 52
pKi 8.7 [52]
NBOMe Small molecule or natural product Rn Agonist 8.7 pKi 22
pKi 8.7 (Ki 2.2x10-9 M) [22]
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 58
pKi 8.6 [58]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.5 pKi 62
pKi 8.5 [62]
ergometrine Small molecule or natural product Approved drug Rn Full agonist 8.5 pKi 36
pKi 8.5 [36]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.3 pKi 58
pKi 8.3 [58]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 9.2 pKi 8,61,88
pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.31x10-10 M) [8,61,88]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 58
pKi 8.2 [58]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.1 pKi 58
pKi 8.1 [58]
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 36
pKi 8.1 [36]
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 78
pKi 8.0 [78]
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 78
pKi 7.9 [78]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 28,74
pKi 7.8 [28,74]
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 44,87
pKi 7.5 – 8.1 [44,87]
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 78
pKi 7.8 [78]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 41
pKi 7.8 [41]
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 87
pKi 7.7 [87]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
pKi 7.5 [41]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
pKi 7.5 [41]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 41
pKi 7.5 [41]
N-1-isopropyl-5-MeOT Small molecule or natural product Rn Full agonist 7.4 pKi 36
pKi 7.4 [36]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 41
pKi 7.4 [41]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 74
pKi 7.3 [74]
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 2,8,36,41,52,88
pKi 6.0 – 8.4 [2,8,36,41,52,88]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 41
pKi 7.2 [41]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 7.5 pKi 41,61,88
pKi 6.8 – 7.5 [41,61,88]
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 36
pKi 7.1 [36]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 86
pKi 7.1 [86]
N-1-isopropyltryptamine Small molecule or natural product Rn Full agonist 7.1 pKi 36
pKi 7.1 [36]
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 58
pKi 7.0 [58]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.0 pKi 81
pKi 7.0 [81]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 41
pKi 6.9 [41]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 41
pKi 6.9 [41]
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 Ligand has a PDB structure Hs Full agonist 6.8 pKi 93
pKi 6.8 [93]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 pKi 35
pKi 6.7 [35]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 6.6 pKi 74
pKi 6.6 [74]
N-1-isopropyltryptamine Small molecule or natural product Hs Full agonist 6.6 pKi 36
pKi 6.6 [36]
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 8,36,41
pKi 5.5 – 7.6 [8,36,41]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.5 pKi 41
pKi 6.5 [41]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.5 pKi 46
pKi 6.5 (Ki 3.26x10-7 M) [46]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 6.4 pKi 78
pKi 6.4 [78]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 41
pKi 6.4 [41]
N-1-isopropyl-5-MeOT Small molecule or natural product Hs Full agonist 6.3 pKi 36
pKi 6.3 [36]
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 16,78,86
pKi 6.0 – 6.5 [16,78,86]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 29
pKi 6.2 (Ki 6x10-7 M) [29]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 pKi 41
pKi 6.0 [41]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.9 pKi 60
pKi 5.9 [60]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.9 pKi 86
pKi 5.9 [86]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.8 pKi 46
pKi 5.8 (Ki 1.464x10-6 M) [46]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 41
pKi 5.6 [41]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 69
pKi 5.4 [69]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 41
pKi 5.4 [41]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 41,58
pKi 5.0 – 5.5 [41,58]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.0 pKi 41
pKi 5.0 [41]
psilocin Small molecule or natural product Ligand has a PDB structure Hs Agonist 7.6 pEC50 79
pEC50 7.6 (EC50 2.4x10-8 M) [79]
Description: Determined in an [3H]inositol phosphate accumulation assay in cells stably expressing h5-HT2A.
(R)-70 [PMID: 36171289] Small molecule or natural product Hs Partial agonist 7.0 pEC50 37
pEC50 7.0 (EC50 1.1x10-7 M) [37]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pEC50 93
pEC50 6.8 [93]
mescaline Small molecule or natural product Hs Agonist 5.6 pEC50 13
pEC50 5.6 (EC50 2.6x10-6 M) [13]
Description: Potency determined in an IP3 accumulation assay
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 51
pKd 9.9 (Kd 1.3x10-10 M) [51]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Antagonist 8.6 – 9.7 pKd 41,75
pKd 8.6 – 9.7 (Kd 2.9x10-9 – 2x10-10 M) [41,75]
[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 86
pKd 9.1 [86]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Antagonist 8.8 pKd 86
pKd 8.8 [86]
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 84
pKi 10.2 (Ki 6x10-11 M) [84]
MT-1207 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 10.1 pKi 95
pKi 10.1 (Ki 7.9x10-11 M) [95]
AC-90179 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.7 pKi 94
pKi 9.7 [94]
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 42,44,81
pKi 9.3 – 10.0 [42,44,81]
pimavanserin Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inverse agonist 9.3 pKi 25,94
pKi 9.3 [25,94]
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 48,89
pKi 9.3 (Ki 5x10-10 M) [48,89]
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 42,44,81
pKi 9.2 – 9.4 [42,44,81]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.2 pKi 76,86
pKi 9.2 [76,86]
LY86057 Small molecule or natural product Hs Antagonist 9.2 pKi 36
pKi 9.2 [36]
ziprasidone 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 Antagonist 8.8 – 9.5 pKi 42,44,81,84
pKi 8.8 – 9.5 [42,44,81,84]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.0 – 9.2 pKi 16,86
pKi 9.0 – 9.2 [16,86]
[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 67
pKi 9.1 (Ki 7.9x10-10 M) [67]
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 64
pKi 9.1 (Ki 8.1x10-10 M) [64]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 81
pKi 9.0 [81]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.0 pKi 66
pKi 9.0 [66]
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 16,43
pKi 8.4 – 9.5 [16,43]
clozapine 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 16
pKi 8.9 [16]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.1 – 9.7 pKi 10,41,75
pKi 8.1 – 9.7 (Ki 7.94x10-9 – 1.99x10-10 M) [10,41,75]
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 41,76
pKi 9.4 [76]
pKi 8.3 [41]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 33
pKi 8.8 [33]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.6 – 9.0 pKi 16,86
pKi 8.6 – 9.0 [16,86]
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 42,44,81,84
pKi 8.6 – 8.9 [42,44,81,84]
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 16,66
pKi 8.4 – 9.0 [16,66]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 34
pKi 8.7 (Ki 2.03x10-9 M) [34]
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 41,43,59
pKi 7.7 – 9.6 [41,43,59]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 8
pKi 8.6 [8]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.8 – 9.4 pKi 8,41,88
pKi 7.8 – 9.4 [8,41,88]
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 81
pKi 8.6 [81]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 41
pKi 8.6 [41]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.6 pKi 36
pKi 8.6 [36]
BF-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 80
pKi 8.6 [80]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 23
pKi 8.5 (Ki 3.1x10-9 M) [23]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 41
pKi 8.5 [41]
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