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5-HT2C receptor

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Target id: 8

Nomenclature: 5-HT2C 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 7 458 Xq23 HTR2C 5-hydroxytryptamine receptor 2C 73
Mouse 7 459 X 68.46 cM Htr2c 5-hydroxytryptamine (serotonin) receptor 2C 24,79
Rat 7 460 Xq34 Htr2c 5-hydroxytryptamine receptor 2C 4
Previous and Unofficial Names Click here for help
5-HT1C [55] | 5-HT2C | HTR1C | 5-HTR2C | 5-hydroxytryptamine receptor 1C | serotonin 1c receptor | serotonin receptor 2C | 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRdb 5ht2c_human (Hs), 5ht2c_mouse (Mm), 5ht2c_rat (Rn)
Other databases
Alphafold P28335 (Hs), P34968 (Mm), P08909 (Rn)
ChEMBL Target CHEMBL225 (Hs), CHEMBL3006 (Mm), CHEMBL324 (Rn)
DrugBank Target P28335 (Hs)
Ensembl Gene ENSG00000147246 (Hs), ENSMUSG00000041380 (Mm), ENSRNOG00000030877 (Rn)
Entrez Gene 3358 (Hs), 15560 (Mm), 25187 (Rn)
Human Protein Atlas ENSG00000147246 (Hs)
KEGG Gene hsa:3358 (Hs), mmu:15560 (Mm), rno:25187 (Rn)
OMIM 312861 (Hs)
Pharos P28335 (Hs)
RefSeq Nucleotide NM_000868 (Hs), NM_008312 (Mm), NM_012765 (Rn)
RefSeq Protein NP_000859 (Hs), NP_032338 (Mm), NP_036897 (Rn)
UniProtKB P28335 (Hs), P34968 (Mm), P08909 (Rn)
Wikipedia HTR2C (Hs)
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

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
[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 3
⤷ pKd 9.1 [3]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 – 9.0 pKd 22
⤷ pKd 8.7 – 9.0 (Kd 2x10-9 – 1.1x10-9 M) [22]
YM348 Small molecule or natural product Hs Full agonist 9.0 pKi 37
⤷ pKi 9.0 [37]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.7 pKi 66
⤷ pKi 8.7 [66]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.7 pKi 38
⤷ pKi 8.7 [38]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 9.0 pKi 22,38
⤷ pKi 8.2 – 9.0 [22,38]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.5 pKi 44
⤷ pKi 8.5 [44]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.2 – 8.6 pKi 20
⤷ pKi 8.2 – 8.6 [20]
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.3 pKi 38
⤷ pKi 8.3 [38]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 38
⤷ pKi 8.2 [38]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.9 – 8.3 pKi 20,22,48
⤷ pKi 7.9 – 8.3 [20,22,48]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 38
⤷ pKi 8.1 [38]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 38
⤷ pKi 8.1 [38]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 8.7 pKi 22,38,44,51
⤷ pKi 8.4 [44]
pKi 7.4 – 8.7 [22,38,51]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 – 8.2 pKi 37-38
⤷ pKi 7.7 – 8.2 (Ki 1.99x10-8 – 6.31x10-9 M) [37-38]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 – 8.6 pKi 20,51,67
⤷ pKi 7.2 – 8.6 (Ki 6.31x10-8 – 2.51x10-9 M) [20,51,67]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 7.9 pKi 66
⤷ pKi 7.9 [66]
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 66
⤷ pKi 7.9 [66]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 – 8.9 pKi 20,38,51
⤷ pKi 6.8 – 8.9 [20,38,51]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 38
⤷ pKi 7.8 [38]
lorcaserin 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 Full 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 6.9 – 8.6 pKi 22,38
⤷ pKi 6.9 – 8.6 [22,38]
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 6.8 – 8.6 pKi 20,22,37-38,44
⤷ pKi 6.8 – 8.6 [20,22,37-38,44]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.7 pKi 46
⤷ pKi 7.7 [46]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.6 pKi 40
⤷ pKi 7.6 [40]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.5 – 8.5 pKi 20,22,37-38,51,67
⤷ pKi 6.5 – 8.5 [20,22,37-38,51,67]
WAY-163909 Small molecule or natural product Hs Full agonist 6.7 – 8.0 pKi 19
⤷ pKi 6.7 – 8.0 (Ki 1.99x10-7 – 1x10-8 M) [19]
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 6.7 – 7.9 pKi 32,66
⤷ pKi 6.7 – 7.9 [32,66]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.7 – 7.8 pKi 20
⤷ pKi 6.7 – 7.8 [20]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 7.2 pKi 66
⤷ pKi 7.2 [66]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 – 7.8 pKi 20,38
⤷ pKi 6.5 – 7.8 [20,38]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.0 pKi 60
⤷ pKi 7.0 [60]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 – 7.1 pKi 38,67
⤷ pKi 6.9 – 7.1 [38,67]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pKi 38
⤷ pKi 6.8 [38]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 pKi 60
⤷ pKi 6.8 [60]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.9 – 7.3 pKi 20,22,38
⤷ pKi 5.9 – 7.3 [20,22,38]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 – 7.0 pKi 22
⤷ pKi 6.2 – 7.0 [22]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 pKi 32
⤷ pKi 6.6 [32]
oxymetazoline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.3 – 6.8 pKi 22
⤷ pKi 6.3 – 6.8 [22]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 6.5 pKi 48
⤷ pKi 6.5 [48]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.6 – 7.2 pKi 20,38
⤷ pKi 5.6 – 7.2 [20,38]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 6.3 pKi 32
⤷ pKi 6.3 [32]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.6 – 7.0 pKi 20,38,67
⤷ pKi 5.6 – 7.0 [20,38,67]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 6.2 pKi 60
⤷ pKi 6.2 [60]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.2 pKi 48
⤷ pKi 6.2 [48]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.1 pKi 48
⤷ pKi 6.1 [48]
5-CT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 5.2 – 6.7 pKi 20,38
⤷ pKi 5.2 – 6.7 [20,38]
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]
CGS-12066 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 5.5 pKi 56
⤷ pKi 5.5 [56]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.3 pKi 50
⤷ pKi 5.3 [50]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 5.5 pKi 38,48
⤷ pKi 5.0 – 5.5 [38,48]
lorcaserin 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 Full agonist 8.1 pEC50 75
⤷ pEC50 8.1 [75]
lorcaserin 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 Agonist 8.2 pIC50 72
⤷ pIC50 8.2 (IC50 5.8x10-9 M) [72]
Description: IP accumulation assay.
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist - -
⤷
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]mesulergine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inverse agonist 8.7 – 9.3 pKd 22,63
⤷ pKd 8.7 – 9.3 (Kd 2.2x10-9 – 5x10-10 M) [22,63]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.3 pKi 32
⤷ pKi 9.3 [32]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 9.2 pKi 32
⤷ pKi 9.2 [32]
sertindole Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 9.0 – 9.2 pKi 34,40
⤷ pKi 9.0 – 9.2 [34,40]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.8 – 9.4 pKi 32,62
⤷ pKi 8.8 – 9.4 [32,62]
SB 228357 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.1 pKi 7,65
⤷ pKi 9.0 – 9.1 [7,65]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.7 – 9.3 pKi 30,38-39
⤷ pKi 8.7 – 9.3 [30,38-39]
FR260010 Small molecule or natural product Hs Antagonist 9.0 pKi 31
⤷ pKi 9.0 (Ki 1.1x10-9 M) [31]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.2 – 9.6 pKi 38
⤷ pKi 8.2 – 9.6 [38]
methysergide 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 8.6 – 9.1 pKi 20,38
⤷ pKi 8.6 – 9.1 [20,38]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.8 pKi 38
⤷ pKi 8.8 [38]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 8.3 – 9.2 pKi 22,38,49
⤷ pKi 8.3 – 9.2 [22,38,49]
SB 221284 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 pKi 38
⤷ pKi 8.7 [38]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 pKi 62
⤷ pKi 8.7 [62]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.6 pKi 34
⤷ pKi 8.6 [34]
SB 242084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 9.0 pKi 36,38
⤷ pKi 8.2 – 9.0 (Ki 6.31x10-9 – 1x10-9 M) [36,38]
ziprasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 7.9 – 9.0 pKi 34,40,70
⤷ pKi 7.9 – 9.0 [34,40,70]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.4 pKi 38
⤷ pKi 8.4 [38]
RS-102221 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.4 pKi 5
⤷ pKi 8.4 [5]
RS-102221 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 – 8.4 pKi 5,38
⤷ pKi 8.3 – 8.4 (Ki 5.01x10-9 – 3.98x10-9 M) [5,38]
tiospirone Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.3 pKi 34
⤷ pKi 8.3 [34]
olanzapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 8.1 – 8.4 pKi 34,40,70
⤷ pKi 8.1 – 8.4 [34,40,70]
SDZ SER-082 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 pKi 38
⤷ pKi 8.1 [38]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.1 pKi 74
⤷ pKi 8.1 (Ki 8x10-9 M) [74]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.4 – 8.7 pKi 22,34,38,40,46,76
⤷ pKi 7.4 – 8.7 [22,34,38,40,46,76]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 pKi 30
⤷ pKi 7.9 [30]
loxapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inverse agonist 7.8 – 8.0 pKi 34,40
⤷ pKi 7.8 – 8.0 [34,40]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.6 – 8.2 pKi 34,40
⤷ pKi 7.6 – 8.2 [34,40]
SB 206553 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 7.9 pKi 35,38
⤷ pKi 7.8 – 7.9 [35,38]
EGIS-7625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 39
⤷ pKi 7.7 [39]
SB 215505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 65
⤷ pKi 7.7 [65]
volinanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 7.7 pKi 38,65
⤷ pKi 7.5 – 7.7 [38,65]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.5 – 7.6 pKi 34,40
⤷ pKi 7.5 – 7.6 [34,40]
mirtazapine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.4 pKi 21
⤷ pKi 7.4 (Ki 3.9x10-8 M) [21]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.4 pKi 78
⤷ pKi 7.4 [78]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 pKi 63
⤷ pKi 7.4 [63]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 48
⤷ pKi 7.3 [48]
fluoxetine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 66
⤷ pKi 7.3 [66]
thioridazine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.2 – 7.3 pKi 34,40
⤷ pKi 7.2 – 7.3 [34,40]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.8 – 7.5 pKi 8,22,38,63
⤷ pKi 6.8 – 7.5 [8,22,38,63]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 47
⤷ pKi 7.1 [47]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 pKi 48
⤷ pKi 7.0 [48]
LY334362 Small molecule or natural product Hs Antagonist 7.0 pKi 8
⤷ pKi 7.0 [8]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 pKi 40
⤷ pKi 6.9 [40]
glemanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
⤷ pKi 6.6 [38]
trazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
⤷ pKi 6.6 [38]
idalopirdine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 pKi 41
⤷ pKi 6.6 (Ki 2.5x10-7 M) [41]
trazodone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.4 – 6.7 pKi 62,66
⤷ pKi 6.4 – 6.7 [62,66]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 48
⤷ pKi 6.5 [48]
norfluoxetine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.5 pKi 66
⤷ pKi 6.5 [66]
trifluoperazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 pKi 40
⤷ pKi 6.4 [40]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 pKi 13
⤷ pKi 6.4 (Ki 4.12x10-7 M) [13]
RS-127445 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 38
⤷ pKi 6.3 [38]
MPDT Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.2 pKi 29
⤷ pKi 6.2 [29]
agomelatine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.2 pKi 45
⤷ pKi 6.2 [45]
duloxetine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.0 pKi 11
⤷ pKi 6.0 [11]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs