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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 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 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 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 Small molecule or natural product Rn Antagonist 8.5 pKi 36