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5-HT2B receptor

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 7

Nomenclature: 5-HT2B 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 7 481 2q37.1 HTR2B 5-hydroxytryptamine receptor 2B 16,19,44
Mouse 7 479 1 C5 Htr2b 5-hydroxytryptamine (serotonin) receptor 2B 20
Rat 7 479 9q35 Htr2b 5-hydroxytryptamine receptor 2B 17
Previous and Unofficial Names Click here for help
5-HT2F [17,50] | 5-HT2B | serotonin receptor 2B | stomach fundus serotonin receptor | 5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht2b_human (Hs), 5ht2b_mouse (Mm), 5ht2b_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine
PDB Id:  4IB4
Ligand:  ergotamine
Resolution:  2.7Å
Species:  Human
References:  49
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
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.7 pKd 38
pKd 8.7 (Kd 2.1x10-9 M) [38]
[3H]5-HT Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.1 pKd 50
pKd 8.1 (Kd 8x10-9 M) [50]
[125I]DOI Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 7.6 – 7.7 pKd
pKd 7.6 – 7.7 (Kd 2.5x10-8 – 2x10-8 M)
methylergonovine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 9.3 pKi 14,41
pKi 9.3 [14,41]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 14
pKi 9.0 [14]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.9 pKi 27
pKi 8.9 [27]
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 Partial agonist 8.0 – 9.4 pKi 14,41,51
pKi 8.0 – 9.4 [14,41,51]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.5 – 8.9 pKi 14,41
pKi 8.5 – 8.9 [14,41]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Biased agonist 8.4 pKi 49
pKi 8.4 [49]
Description: Biased for β-arrestin sihnalling.
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.4 pKi 25
pKi 8.4 [25]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.3 pKi 33
pKi 8.3 [33]
AL-37350A Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 23
pKi 8.3 [23]
Ro 60-0175 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 14
pKi 8.3 (Ki 5.01x10-9 M) [14]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.2 pKi 27
pKi 8.2 [27]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Partial agonist 8.2 pKi 50
pKi 8.2 [50]
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 7.9 – 8.4 pKi 2,14,16,23,41
pKi 7.9 – 8.4 [2,14,16,23,41]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.9 – 8.3 pKi 2,14,16
pKi 7.9 – 8.3 [2,14,16]
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 8.0 pKi 50
pKi 8.0 [50]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.0 pKi 50
pKi 8.0 [50]
α-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 8.0 pKi 50
pKi 8.0 [50]
(+)-norfenfluramine Small molecule or natural product Hs Full agonist 8.0 pKi 41
pKi 8.0 [41]
BW723C86 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 – 8.6 pKi 2,14,42
pKi 7.3 – 8.6 (Ki 5.01x10-8 – 2.51x10-9 M) [2,14,42]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.4 – 8.5 pKi 14,32,41-42,51
pKi 7.4 – 8.5 [14,32,41-42,51]
RU 24969 Small molecule or natural product Rn Full agonist 7.8 pKi 50
pKi 7.8 [50]
DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 – 7.7 pKi 16,32,42
pKi 7.6 – 7.7 (Ki 2.51x10-8 – 1.99x10-8 M) [16,32,42]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 7.6 pKi 50
pKi 7.6 [50]
DOI Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.6 pKi 16,50
pKi 7.6 [16,50]
(+)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pKi 14
pKi 7.6 [14]
relenopride Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.5 pKi 12
pKi 7.5 (Ki 3.1x10-8 M) [12]
(R)-DOI Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 – 7.7 pKi 14,23,34
pKi 7.7 [23]
pKi 7.3 – 7.4 [14,34]
brolamfetamine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 – 7.6 pKi 14,32
pKi 7.4 – 7.6 [14,32]
VER-3323 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.5 pKi 14
pKi 7.5 [14]
dihydroergocryptine Small molecule or natural product Hs Biased agonist 7.5 pKi 49
pKi 7.5 [49]
Description: Biased for β-arrestin signalling.
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.4 pKi 37
pKi 7.4 [37]
ORG-37684 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.4 pKi 14
pKi 7.4 [14]
norfenfluramine Small molecule or natural product Hs Full agonist 7.3 pKi 41
pKi 7.3 [41]
(-)-norfenfluramine Small molecule or natural product Hs Full agonist 7.3 pKi 41
pKi 7.3 [41]
TFMPP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 14
pKi 7.2 [14]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.1 pKi 50
pKi 7.1 [50]
quipazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 pKi 14
pKi 7.1 [14]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.0 pKi 14
pKi 7.0 [14]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.0 pKi 50
pKi 7.0 [50]
Org 12962 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.0 pKi 14
pKi 7.0 [14]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 14
pKi 6.9 [14]
quipazine Small molecule or natural product Rn Full agonist 6.9 pKi 50
pKi 6.9 [50]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.7 – 6.9 pKi 14,16
pKi 6.7 – 6.9 [14,16]
5-CT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.8 pKi 16,50
pKi 6.8 [16,50]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.8 pKi 48
pKi 6.8 [48]
2-methyl-5-HT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.6 pKi 50
pKi 6.6 [50]
MK-212 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.2 – 6.8 pKi 14,42
pKi 6.2 – 6.8 [14,42]
MK-212 Small molecule or natural product Rn Full agonist 6.4 pKi 50
pKi 6.4 [50]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.2 pKi 37
pKi 6.2 [37]
CGS-12066 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 14
pKi 6.1 [14]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 pKi 35
pKi 5.8 [35]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 37
pKi 5.8 [37]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.8 pKi 28
pKi 5.8 [28]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.0 – 6.5 pKi 14,27
pKi 5.0 – 6.5 [14,27]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.7 pKi 14
pKi 5.7 [14]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 14
pKi 5.4 [14]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.4 pKi 50
pKi 5.4 [50]
lorcaserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.0 pEC50 48
pEC50 6.0 [48]
View species-specific agonist tables
Agonist Comments
Methysergide is a low intrinsic efficacy partial agonist, although in some functional assays it may behave as an antagonist.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
balovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 11.6 pKd 45
pKd 11.6 (Kd 2.7x10-12 M) [45]
[3H]rauwolscine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 8.4 pKd 51
pKd 8.4 [51]
[3H]mesulergine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Inverse agonist 7.9 pKd 14
pKd 7.9 (Kd 1.29x10-8 M) [14]
BF-1 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.1 pKi 43
pKi 10.1 [43]
RS-127445 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 – 9.5 pKi 3,14
pKi 9.0 – 9.5 (Ki 1x10-9 – 3.2x10-10 M) [3,14]
EGIS-7625 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 15
pKi 9.0 (Ki 1x10-9 M) [15]
LY53857 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 – 9.1 pKi 51
pKi 8.8 – 9.1 [51]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 – 9.2 pKi 14,51
pKi 8.7 – 9.2 [14,51]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.7 – 9.2 pKi 3,14,39,51
pKi 8.7 – 9.2 [3,14,39,51]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.9 pKi 27
pKi 8.9 [27]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 pKi 14
pKi 8.8 [14]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.0 pKi 16,51
pKi 8.4 – 9.0 [16,51]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.5 – 8.8 pKi 14-15,51
pKi 8.5 – 8.8 [14-15,51]
SB 221284 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 14
pKi 8.6 [14]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.0 – 8.8 pKi 14,25,51
pKi 8.0 – 8.8 [14,25,51]
tegaserod Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 pKi 2
pKi 8.4 [2]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.3 – 8.4 pKi 16,50
pKi 8.3 – 8.4 [16,50]
mianserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.9 – 8.8 pKi 3,14,51
pKi 7.9 – 8.8 [3,14,51]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 8.3 pKi 50
pKi 8.3 [50]
SB 215505 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 39
pKi 8.3 [39]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKi 27
pKi 8.2 [27]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.2 pKi 50
pKi 8.2 [50]
LY53857 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.2 pKi 50
pKi 8.2 [50]
rauwolscine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.4 pKi 51
pKi 7.8 – 8.4 [51]
SB 206553 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 – 8.5 pKi 2,14
pKi 7.6 – 8.5 [2,14]
SB 228357 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 – 8.1 pKi 5,39
pKi 8.0 – 8.1 [5,39]
amesergide Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.0 pKi 50
pKi 8.0 [50]
LY86057 Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.9 pKi 50
pKi 7.9 [50]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 pKi 53
pKi 7.7 [53]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 – 7.9 pKi 3,16,51
pKi 7.4 – 7.9 [3,16,51]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 27
pKi 7.5 [27]
rauwolscine Small molecule or natural product Rn Antagonist 7.4 pKi 50
pKi 7.4 [50]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.4 pKi 50
pKi 7.4 [50]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.3 pKi 27
pKi 7.3 [27]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 50
pKi 7.3 [50]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.3 pKi 50
pKi 7.3 [50]
trazodone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.1 pKi 14,41
pKi 7.1 [14,41]
SB 243213 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pKi 5
pKi 7.0 [5]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.9 pKi 27
pKi 6.9 [27]
SB 242084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 – 7.0 pKi 13-14
pKi 6.8 – 7.0 [13-14]
SB 204741 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 pKi 14
pKi 6.9 [14]
S33084 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 26
pKi 6.8 [26]
SDZ SER-082 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 14
pKi 6.7 [14]
agomelatine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 pKi 24
pKi 6.6 [24]
sarpogrelate Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.6 pKi 38
pKi 6.6 [38]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 6.8 pKi 51
pKi 6.3 – 6.8 [51]
piboserod Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 6.6 pKi 2,11
pKi 6.6 [2]
pKi 6.3 [11]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.1 – 6.7 pKi 6,14,16,38,51
pKi 6.1 – 6.7 [6,14,16,38,51]
spiperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 – 6.5 pKi 14,16,51
pKi 5.9 – 6.5 [14,16,51]
L-741,626 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 26
pKi 6.2 [26]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.8 – 6.4 pKi 51
pKi 5.8 – 6.4 [51]
RS-102221 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 – 6.1 pKi 4,14
pKi 6.0 – 6.1 [4,14]
spiramide Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 14
pKi 6.0 [14]
volinanserin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 14,39
pKi 6.0 [14,39]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 27
pKi 5.9 [27]
SB 224289 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 14
pKi 5.9 [14]
SB 277011-A Small molecule or natural product