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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 87
Mouse 7 471 14 39.37 cM Htr2a 5-hydroxytryptamine (serotonin) receptor 2A 20,96
Rat 7 471 15q11 Htr2a 5-hydroxytryptamine receptor 2A 25
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), P35363 (Mm), P14842 (Rn)
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 47,85
⤷ pKd 9.1 [47,85]
[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 85
⤷ pKd 8.9 [85]
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 39
⤷ pKi 9.4 [39]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.2 – 9.3 pKi 39,50,64
⤷ pKi 9.2 – 9.3 [39,64]
pKi 9.2 [50]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.1 pKi 39
⤷ pKi 9.1 [39]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.9 – 9.2 pKi 39,58
⤷ pKi 8.9 – 9.2 [39,58]
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 39
⤷ pKi 9.0 [39]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 39
⤷ pKi 9.0 [39]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 53
⤷ pKi 9.0 [53]
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 35
⤷ pKi 8.9 [35]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.7 pKi 50
⤷ pKi 8.7 [50]
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 55
⤷ pKi 8.6 [55]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.5 pKi 59
⤷ pKi 8.5 [59]
ergometrine Small molecule or natural product Approved drug Rn Full agonist 8.5 pKi 35
⤷ pKi 8.5 [35]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.3 pKi 55
⤷ pKi 8.3 [55]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 9.2 pKi 9,58,85
⤷ pKi 7.4 – 9.2 (Ki 3.98x10-8 – 6.31x10-10 M) [9,58,85]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 55
⤷ pKi 8.2 [55]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.1 pKi 55
⤷ pKi 8.1 [55]
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 35
⤷ pKi 8.1 [35]
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 75
⤷ pKi 8.0 [75]
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 75
⤷ pKi 7.9 [75]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 27,70
⤷ pKi 7.8 [27,70]
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 42,84
⤷ pKi 7.5 – 8.1 [42,84]
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 75
⤷ pKi 7.8 [75]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 39
⤷ pKi 7.8 [39]
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 84
⤷ pKi 7.7 [84]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 39
⤷ pKi 7.5 [39]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 39
⤷ pKi 7.5 [39]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 39
⤷ pKi 7.5 [39]
N-1-isopropyl-5-MeOT Small molecule or natural product Rn Full agonist 7.4 pKi 35
⤷ pKi 7.4 [35]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 39
⤷ pKi 7.4 [39]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 70
⤷ pKi 7.3 [70]
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 2,9,35,39,50,85
⤷ pKi 6.0 – 8.4 [2,9,35,39,50,85]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 39
⤷ pKi 7.2 [39]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 7.5 pKi 39,58,85
⤷ pKi 6.8 – 7.5 [39,58,85]
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 35
⤷ pKi 7.1 [35]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 83
⤷ pKi 7.1 [83]
N-1-isopropyltryptamine Small molecule or natural product Rn Full agonist 7.1 pKi 35
⤷ pKi 7.1 [35]
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 55
⤷ pKi 7.0 [55]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.0 pKi 78
⤷ pKi 7.0 [78]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 39
⤷ pKi 6.9 [39]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 39
⤷ pKi 6.9 [39]
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 90
⤷ pKi 6.8 [90]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 pKi 34
⤷ pKi 6.7 [34]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Full agonist 6.6 pKi 70
⤷ pKi 6.6 [70]
N-1-isopropyltryptamine Small molecule or natural product Hs Full agonist 6.6 pKi 35
⤷ pKi 6.6 [35]
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 9,35,39
⤷ pKi 5.5 – 7.6 [9,35,39]
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 39
⤷ pKi 6.5 [39]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.5 pKi 44
⤷ pKi 6.5 (Ki 3.26x10-7 M) [44]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 6.4 pKi 75
⤷ pKi 6.4 [75]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.4 pKi 39
⤷ pKi 6.4 [39]
N-1-isopropyl-5-MeOT Small molecule or natural product Hs Full agonist 6.3 pKi 35
⤷ pKi 6.3 [35]
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 16,75,83
⤷ pKi 6.0 – 6.5 [16,75,83]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.2 pKi 28
⤷ pKi 6.2 (Ki 6x10-7 M) [28]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.0 pKi 39
⤷ pKi 6.0 [39]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.9 pKi 57
⤷ pKi 5.9 [57]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.9 pKi 83
⤷ pKi 5.9 [83]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.8 pKi 44
⤷ pKi 5.8 (Ki 1.464x10-6 M) [44]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 pKi 39
⤷ pKi 5.6 [39]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 65
⤷ pKi 5.4 [65]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 39
⤷ pKi 5.4 [39]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 39,55
⤷ pKi 5.0 – 5.5 [39,55]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.0 pKi 39
⤷ pKi 5.0 [39]
psilocin Small molecule or natural product Ligand has a PDB structure Hs Agonist 7.6 pEC50 76
⤷ pEC50 7.6 (EC50 2.4x10-8 M) [76]
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 Ligand has a PDB structure Hs Full agonist 6.8 pEC50 90
⤷ pEC50 6.8 [90]
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 49
⤷ pKd 9.9 (Kd 1.3x10-10 M) [49]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.6 – 9.7 pKd 39,72
⤷ pKd 8.6 – 9.7 (Kd 2.9x10-9 – 2x10-10 M) [39,72]
[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 83
⤷ pKd 9.1 [83]
[3H]ketanserin Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Antagonist 8.8 pKd 83
⤷ pKd 8.8 [83]
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 81
⤷ pKi 10.2 (Ki 6x10-11 M) [81]
AC-90179 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 9.7 pKi 91
⤷ pKi 9.7 [91]
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 40,42,78
⤷ pKi 9.3 – 10.0 [40,42,78]
pimavanserin Small molecule or natural product Approved drug Primary target of this compound Hs Inverse agonist 9.3 pKi 24,91
⤷ pKi 9.3 [24,91]
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 46,86
⤷ pKi 9.3 (Ki 5x10-10 M) [46,86]
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 40,42,78
⤷ pKi 9.2 – 9.4 [40,42,78]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.2 pKi 73,83
⤷ pKi 9.2 [73,83]
LY86057 Small molecule or natural product Hs Antagonist 9.2 pKi 35
⤷ pKi 9.2 [35]
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 40,42,78,81
⤷ pKi 8.8 – 9.5 [40,42,78,81]
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 16,83
⤷ pKi 9.0 – 9.2 [16,83]
[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 63
⤷ pKi 9.1 (Ki 7.9x10-10 M) [63]
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 61
⤷ pKi 9.1 (Ki 8.1x10-10 M) [61]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 78
⤷ pKi 9.0 [78]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.0 pKi 71
⤷ pKi 9.0 [71]
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 16,41
⤷ pKi 8.4 – 9.5 [16,41]
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 11,39,72
⤷ pKi 8.1 – 9.7 (Ki 7.94x10-9 – 1.99x10-10 M) [11,39,72]
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 39,73
⤷ pKi 9.4 [73]
pKi 8.3 [39]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 32
⤷ pKi 8.8 [32]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.6 – 9.0 pKi 16,83
⤷ pKi 8.6 – 9.0 [16,83]
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 40,42,78,81
⤷ pKi 8.6 – 8.9 [40,42,78,81]
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 16,71
⤷ pKi 8.4 – 9.0 [16,71]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 33
⤷ pKi 8.7 (Ki 2.03x10-9 M) [33]
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 39,41,56
⤷ pKi 7.7 – 9.6 [39,41,56]
(+)-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 9,39,85
⤷ pKi 7.8 – 9.4 [9,39,85]
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 78
⤷ pKi 8.6 [78]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 39
⤷ pKi 8.6 [39]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.6 pKi 35
⤷ pKi 8.6 [35]
BF-1 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 77
⤷ pKi 8.6 [77]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 22
⤷ pKi 8.5 (Ki 3.1x10-9 M) [22]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 pKi 39
⤷ pKi 8.5 [39]
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 35
⤷ pKi 8.5 [35]
LY53857 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 35
⤷ pKi 8.5 [35]
amesergide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.5 pKi 35
⤷ pKi 8.5 [35]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.5 pKi 72
⤷ pKi 8.5 [72]
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 39
⤷ pKi 8.4 [39]
LY108742 Small molecule or natural product