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5-HT7 receptor

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Target id: 12

Nomenclature: 5-HT7 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 7 479 10q23.31 HTR7 5-hydroxytryptamine receptor 7 54
Mouse 7 448 19 30.3 cM Htr7 5-hydroxytryptamine (serotonin) receptor 7 45
Rat 7 448 1q53 Htr7 5-hydroxytryptamine receptor 7 37,49,51
Previous and Unofficial Names Click here for help
5-HTx | 5-HT1Y | 5-HT7 | GPRFO | serotonin receptor 7 | 5-hydroxytryptamine (serotonin) receptor 7, adenylate cyclase-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht7r_human (Hs), 5ht7r_mouse (Mm), 5ht7r_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
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]5-CT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 9.4 pKd 59
pKd 9.4 (Kd 4x10-10 M) [59]
[125I]LSD Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.9 pKd 37
pKd 8.9 [37]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.5 – 8.6 pKd 54
pKd 8.5 – 8.6 (Kd 3.16x10-9 – 2.51x10-9 M) [54]
[3H]5-HT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.1 – 9.0 pKd 5,54
pKd 8.1 – 9.0 (Kd 7.94x10-9 – 1x10-9 M) [5,54]
[3H]LSD Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Full agonist 8.2 pKd 33
pKd 8.2 [33]
LP-12 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.9 pKi 34
pKi 9.9 (Ki 1.3x10-10 M) [34]
5-CT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 9.5 – 9.9 pKi 49,51
pKi 9.5 – 9.9 [49,51]
LP-44 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.7 pKi 34
pKi 9.7 (Ki 2.2x10-10 M) [34]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 – 10.0 pKi 5,24,31,60
pKi 9.0 – 10.0 [5,24,31,60]
LP-211 Small molecule or natural product Rn Agonist 9.2 pKi 35
pKi 9.2 (Ki 5.8x10-10 M) [35]
AS-19 Small molecule or natural product Primary target of this compound Hs Agonist 9.2 pKi 29
pKi 9.2 (Ki 6x10-10 M) [29]
5-CT Small molecule or natural product Click here for species-specific activity table Mm Full agonist 9.0 pKi 45
pKi 9.0 [45]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.8 – 9.2 pKi 49,51
pKi 8.8 – 9.2 [49,51]
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 8.7 – 9.2 pKi 49,51
pKi 8.7 – 9.2 [49,51]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 8.3 – 9.5 pKi 5,24,31
pKi 8.3 – 9.5 [5,24,31]
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 8.1 – 9.6 pKi 5,18,24,31,60
pKi 8.1 – 9.6 [5,18,24,31,60]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 8.2 – 9.3 pKi 49,51
pKi 8.2 – 9.3 [49,51]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Full agonist 8.3 – 9.0 pKi 51
pKi 8.3 – 9.0 [51]
E55888 Small molecule or natural product Hs Full agonist 8.6 pKi 8
pKi 8.6 [8]
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 Mm Full agonist 8.3 pKi 45
pKi 8.3 [45]
dipropyl-5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 8.4 pKi 24
pKi 8.2 – 8.4 [24]
5-MeOT Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Full agonist 8.2 pKi 45
pKi 8.2 [45]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 49
pKi 8.0 [49]
aripiprazole 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 33
pKi 7.8 [33]
OPC 4392 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.7 pKi 33
pKi 7.7 [33]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.3 – 8.0 pKi 51
pKi 7.3 – 8.0 [51]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 – 7.8 pKi 51
pKi 7.5 – 7.8 [51]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.5 – 7.7 pKi 51
pKi 7.5 – 7.7 [51]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.4 – 7.7 pKi 51
pKi 7.4 – 7.7 [51]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.3 – 7.5 pKi 49,51
pKi 7.3 – 7.5 [49,51]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 pKi 5
pKi 7.1 [5]
bufotenine Small molecule or natural product Click here for species-specific activity table Mm Full agonist 7.0 pKi 45
pKi 7.0 [45]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 – 7.6 pKi 5,24,31,60
pKi 6.3 – 7.6 [5,24,31,60]
RU 24969 Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.9 pKi 45
pKi 6.9 [45]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 62
pKi 6.9 [62]
tryptamine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 pKi 5
pKi 6.8 [5]
2-MPP Small molecule or natural product Rn Full agonist 6.6 – 6.9 pKi 51
pKi 6.6 – 6.9 [51]
DM-1451 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.7 pKi 33
pKi 6.7 [33]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.6 pKi 45
pKi 6.6 [45]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 pKi 15
pKi 6.5 [15]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.4 – 6.6 pKi 51
pKi 6.4 – 6.6 [51]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.3 – 6.6 pKi 51
pKi 6.3 – 6.6 [51]
buspirone Small molecule or natural product Approved drug Rn Partial agonist 6.4 pKi 49
pKi 6.4 [49]
cisapride Small molecule or natural product Approved drug Click here for species-specific activity table Mm Full agonist 5.8 pKi 45
pKi 5.8 [45]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.5 pKi 39
pKi 5.5 [39]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.3 pKi 43
pKi 5.3 [43]
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
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.9 – 9.0 pKd 30,48
pKd 8.9 – 9.0 [30,48]
[3H]SB269970 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.9 pKd 59
pKd 8.9 (Kd 1.2x10-9 M) [59]
lurasidone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.3 pKi 23
pKi 9.3 (Ki 4.95x10-10 M) [23]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.3 pKi 48
pKi 9.3 [48]
methiothepin Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.0 – 9.4 pKi 51
pKi 9.0 – 9.4 [51]
tiospirone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.2 pKi 48
pKi 9.2 [48]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.4 pKi 5,24,31,60
pKi 8.4 – 9.4 [5,24,31,60]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 8.8 pKi 48
pKi 8.8 [48]
SB269970 Small molecule or natural product Hs Antagonist 8.6 – 8.9 pKi 59
pKi 8.6 – 8.9 [59]
SB656104 Small molecule or natural product Hs Antagonist 8.7 pKi 13
pKi 8.7 (Ki 1.9x10-9 M) [13]
DR-4004 Small molecule or natural product Primary target of this compound Hs Antagonist 8.7 pKi 14,27
pKi 8.7 (Ki 2x10-9 M) [14,27]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 8.9 pKi 5,24,31
pKi 8.2 – 8.9 [5,24,31]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.3 – 8.7 pKi 46,60
pKi 8.3 – 8.7 [46,60]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 8.4 pKi 46
pKi 8.4 [46]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 8.4 pKi 46
pKi 8.4 [46]
pirenperone Small molecule or natural product Hs Antagonist 8.2 – 8.5 pKi 24
pKi 8.2 – 8.5 [24]
fluperlapine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 8.3 pKi 48
pKi 8.3 [48]
methiothepin Small molecule or natural product Click here for species-specific activity table Mm Antagonist 8.2 pKi 45
pKi 8.2 [45]
JNJ-18038683 Small molecule or natural product Primary target of this compound Hs Antagonist 8.2 pKi 7
pKi 8.2 [7]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 8.1 pKi 48
pKi 8.1 [48]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 8.0 pKi 5
pKi 8.0 [5]
2-bromo-LSD Small molecule or natural product Mm Antagonist 8.0 pKi 45
pKi 8.0 [45]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.2 – 8.7 pKi 49,51
pKi 7.2 – 8.7 [49,51]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.7 – 8.2 pKi 51
pKi 7.7 – 8.2 [51]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.9 pKi 45
pKi 7.9 [45]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.9 pKi 51
pKi 7.9 [51]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.9 pKi 46
pKi 7.9 [46]
spiperone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.7 – 8.0 pKi 48-49
pKi 7.7 – 8.0 [48-49]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 8.2 pKi 5,24,31,60
pKi 7.5 – 8.2 [5,24,31,60]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.7 – 7.8 pKi 51
pKi 7.7 – 7.8 [51]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 – 8.2 pKi 30,48-49,51
pKi 7.2 – 8.2 [30,48-49,51]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.7 pKi 30
pKi 7.7 [30]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inverse agonist 7.6 pKi 46
pKi 7.6 [46]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Inverse agonist 7.6 pKi 48
pKi 7.6 [48]
mesulergine Small molecule or natural product Mm Antagonist 7.6 pKi 45
pKi 7.6 [45]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.6 pKi 48
pKi 7.6 [48]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 – 7.8 pKi 31,46,60
pKi 7.2 – 7.8 [31,46,60]
(+)-butaclamol Small molecule or natural product Mm Antagonist 7.5 pKi 45
pKi 7.5 [45]
spiperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 – 8.0 pKi 5,24,31
pKi 7.0 – 8.0 [5,24,31]
metergoline Small molecule or natural product Mm Antagonist 7.5 pKi 45
pKi 7.5 [45]
2-bromo-LSD Small molecule or natural product Hs Antagonist 7.5 pKi 5
pKi 7.5 [5]
fluperlapine Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.5 pKi 46
pKi 7.5 [46]
SB 258719 Small molecule or natural product Hs Inverse agonist 7.5 pKi 60
pKi 7.5 (Ki 3.16x10-8 M) [60]
methysergide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.1 – 7.8 pKi 5,24,31
pKi 7.1 – 7.8 [5,24,31]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 – 7.6 pKi 24
pKi 7.3 – 7.6 [24]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Mm Inverse agonist 7.4 pKi 45
pKi 7.4 [45]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.4 pKi 48
pKi 7.4 [48]
ergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.3 pKi 45
pKi 7.3 [45]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.1 – 7.5 pKi 49,51
pKi 7.1 – 7.5 [49,51]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 18
pKi 7.2 [18]
spiperone Small molecule or natural product Click here for species-specific activity table Mm Antagonist 7.2 pKi 45
pKi 7.2 [45]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 pKi 48
pKi 7.2 [48]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.0 – 7.4 pKi 49,51
pKi 7.0 – 7.4 [49,51]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 pKi 46
pKi 7.2 [46]
ritanserin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.8 – 7.4 pKi 5,31
pKi 6.8 – 7.4 [5,31]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.4 pKi 48,51
pKi 6.8 – 7.4 [48,51]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.1 pKi 46
pKi 7.1 [46]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.0 pKi 49
pKi 7.0 [49]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 25
pKi 7.0 [25]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Mm Antagonist 7.0 pKi 45
pKi 7.0 [45]
dihydroergocryptine Small molecule or natural product Mm Antagonist 7.0 pKi 45
pKi 7.0 [45]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.9 – 7.0 pKi 51
pKi 6.9 – 7.0 [51]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.0 pKi 30,48
pKi 6.8 – 7.0 [30,48]
cyproheptadine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.9 pKi 5
pKi 6.9 [5]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 15
pKi 6.8 [15]
dihydroergotamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.8 pKi 49
pKi 6.8 [49]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.6 – 6.7 pKi 51
pKi 6.6 – 6.7 [51]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.5 pKi 60
pKi 6.5 [60]
dihydroergocryptine Small molecule or natural product Rn Antagonist 6.5 pKi 49
pKi 6.5 [49]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.3 – 6.6 pKi 24
pKi 6.3 – 6.6 [24]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.3 – 6.6 pKi 30,48-49
pKi 6.3 – 6.6 [30,48-49]
buspirone Small molecule or natural product Approved drug