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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

Contents:

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
Alphafold P28223 (Hs)
ChEMBL Target CHEMBL224 (Hs), CHEMBL5377 (Mm), CHEMBL322 (Rn)
DrugBank Target P28223 (Hs)
Ensembl Gene ENSG00000102468 (Hs), ENSMUSG00000034997 (Mm), ENSRNOG00000010063 (Rn)
Entrez Gene 3356 (Hs), 15558 (Mm), 29595 (Rn)
Human Protein Atlas ENSG00000102468 (Hs)
KEGG Gene hsa:3356 (Hs), mmu:15558 (Mm), rno:29595 (Rn)
OMIM 182135 (Hs)
Pharos P28223 (Hs)
RefSeq Nucleotide NM_000621 (Hs), NM_172812 (Mm), NM_017254 (Rn)
RefSeq Protein NP_000612 (Hs), NP_766400 (Mm), NP_058950 (Rn)
UniProtKB P28223 (Hs), P35363 (Mm), P14842 (Rn)
Wikipedia HTR2A (Hs)
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 Ligand has a PDB structure 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 Ligand has a PDB structure 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