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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 55
Mouse 7 448 19 30.3 cM Htr7 5-hydroxytryptamine (serotonin) receptor 7 46
Rat 7 448 1q53 Htr7 5-hydroxytryptamine receptor 7 38,50,52
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
Alphafold
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 60
pKd 9.4 (Kd 4x10-10 M) [60]
[125I]LSD Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Full agonist 8.9 pKd 38
pKd 8.9 [38]
[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 55
pKd 8.5 – 8.6 (Kd 3.16x10-9 – 2.51x10-9 M) [55]
[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 5,55
pKd 8.1 – 9.0 (Kd 7.94x10-9 – 1x10-9 M) [5,55]
[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 34
pKd 8.2 [34]
LP-12 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.9 pKi 35
pKi 9.9 (Ki 1.3x10-10 M) [35]
5-CT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 9.5 – 9.9 pKi 50,52
pKi 9.5 – 9.9 [50,52]
LP-44 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 9.7 pKi 35
pKi 9.7 (Ki 2.2x10-10 M) [35]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 – 10.0 pKi 5,25,32,61
pKi 9.0 – 10.0 [5,25,32,61]
LP-211 Small molecule or natural product Rn Agonist 9.2 pKi 36
pKi 9.2 (Ki 5.8x10-10 M) [36]
AS-19 Small molecule or natural product Primary target of this compound Hs Agonist 9.2 pKi 30
pKi 9.2 (Ki 6x10-10 M) [30]
5-CT Small molecule or natural product Click here for species-specific activity table Mm Full agonist 9.0 pKi 46
pKi 9.0 [46]
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 50,52
pKi 8.8 – 9.2 [50,52]
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 50,52
pKi 8.7 – 9.2 [50,52]
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 5,25,32
pKi 8.3 – 9.5 [5,25,32]
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 5,19,25,32,61
pKi 8.1 – 9.6 [5,19,25,32,61]
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 50,52
pKi 8.2 – 9.3 [50,52]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Rn Full agonist 8.3 – 9.0 pKi 52
pKi 8.3 – 9.0 [52]
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 46
pKi 8.3 [46]
dipropyl-5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 – 8.4 pKi 25
pKi 8.2 – 8.4 [25]
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 46
pKi 8.2 [46]
(+)-LSD Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 50
pKi 8.0 [50]
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 34
pKi 7.8 [34]
OPC 4392 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.7 pKi 34
pKi 7.7 [34]
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 52
pKi 7.3 – 8.0 [52]
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 52
pKi 7.5 – 7.8 [52]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.5 – 7.7 pKi 52
pKi 7.5 – 7.7 [52]
5-MeO-DMT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.4 – 7.7 pKi 52
pKi 7.4 – 7.7 [52]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Rn Full agonist 7.3 – 7.5 pKi 50,52
pKi 7.3 – 7.5 [50,52]
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 46
pKi 7.0 [46]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 – 7.6 pKi 5,25,32,61
pKi 6.3 – 7.6 [5,25,32,61]
RU 24969 Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.9 pKi 46
pKi 6.9 [46]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.9 pKi 63
pKi 6.9 [63]
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 52
pKi 6.6 – 6.9 [52]
DM-1451 Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.7 pKi 34
pKi 6.7 [34]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Mm Full agonist 6.6 pKi 46
pKi 6.6 [46]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.5 pKi 16
pKi 6.5 [16]
m-chlorophenylpiperazine Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.4 – 6.6 pKi 52
pKi 6.4 – 6.6 [52]
TFMPP Small molecule or natural product Click here for species-specific activity table Rn Full agonist 6.3 – 6.6 pKi 52
pKi 6.3 – 6.6 [52]
buspirone Small molecule or natural product Approved drug Rn Partial agonist 6.4 pKi 50
pKi 6.4 [50]
cisapride Small molecule or natural product Approved drug Click here for species-specific activity table Mm Full agonist 5.8 pKi 46
pKi 5.8 [46]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.5 pKi 40
pKi 5.5 [40]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.3 pKi 44
pKi 5.3 [44]
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 31,49
pKd 8.9 – 9.0 [31,49]
[3H]SB269970 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.9 pKd 60
pKd 8.9 (Kd 1.2x10-9 M) [60]
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 24
pKi 9.3 (Ki 4.95x10-10 M) [24]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 9.3 pKi 49
pKi 9.3 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.0 – 9.4 pKi 52
pKi 9.0 – 9.4 [52]
tiospirone Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.2 pKi 49
pKi 9.2 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.4 pKi 5,25,32,61
pKi 8.4 – 9.4 [5,25,32,61]
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 49
pKi 8.8 [49]
SB269970 Small molecule or natural product Hs Antagonist 8.6 – 8.9 pKi 60
pKi 8.6 – 8.9 [60]
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 15,28
pKi 8.7 (Ki 2x10-9 M) [15,28]
metergoline Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.2 – 8.9 pKi 5,25,32
pKi 8.2 – 8.9 [5,25,32]
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 47,61
pKi 8.3 – 8.7 [47,61]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 8.4 pKi 47
pKi 8.4 [47]
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 47
pKi 8.4 [47]
pirenperone Small molecule or natural product Hs Antagonist 8.2 – 8.5 pKi 25
pKi 8.2 – 8.5 [25]
fluperlapine Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 8.3 pKi 49
pKi 8.3 [49]
methiothepin Small molecule or natural product Click here for species-specific activity table Mm Antagonist 8.2 pKi 46
pKi 8.2 [46]
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 49
pKi 8.1 [49]
EGIS-11150 Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 8.1 pKi 14
pKi 8.1 (Ki 9x10-9 M) [14]
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 46
pKi 8.0 [46]
metergoline Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.2 – 8.7 pKi 50,52
pKi 7.2 – 8.7 [50,52]
mesulergine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.7 – 8.2 pKi 52
pKi 7.7 – 8.2 [52]
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 46
pKi 7.9 [46]
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 52
pKi 7.9 [52]
fluphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.9 pKi 47
pKi 7.9 [47]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 7.7 – 8.0 pKi 49-50
pKi 7.7 – 8.0 [49-50]
mesulergine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 – 8.2 pKi 5,25,32,61
pKi 7.5 – 8.2 [5,25,32,61]
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 52
pKi 7.7 – 7.8 [52]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 – 8.2 pKi 31,49-50,52
pKi 7.2 – 8.2 [31,49-50,52]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.7 pKi 31
pKi 7.7 [31]
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 47
pKi 7.6 [47]
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 49
pKi 7.6 [49]
mesulergine Small molecule or natural product Mm Antagonist 7.6 pKi 46
pKi 7.6 [46]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.6 pKi 49
pKi 7.6 [49]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 – 7.8 pKi 32,47,61
pKi 7.2 – 7.8 [32,47,61]
(+)-butaclamol Small molecule or natural product Mm Antagonist 7.5 pKi 46
pKi 7.5 [46]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.0 – 8.0 pKi 5,25,32
pKi 7.0 – 8.0 [5,25,32]
metergoline Small molecule or natural product Mm Antagonist 7.5 pKi 46
pKi 7.5 [46]
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 47
pKi 7.5 [47]
SB 258719 Small molecule or natural product Hs Inverse agonist 7.5 pKi 61
pKi 7.5 (Ki 3.16x10-8 M) [61]
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 5,25,32
pKi 7.1 – 7.8 [5,25,32]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 – 7.6 pKi 25
pKi 7.3 – 7.6 [25]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Mm Inverse agonist 7.4 pKi 46
pKi 7.4 [46]
amoxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.4 pKi 49
pKi 7.4 [49]
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 46
pKi 7.3 [46]
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 50,52
pKi 7.1 – 7.5 [50,52]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 19
pKi 7.2 [19]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Mm Antagonist 7.2 pKi 46
pKi 7.2 [46]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Inverse agonist 7.2 pKi 49
pKi 7.2 [49]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.0 – 7.4 pKi 50,52
pKi 7.0 – 7.4 [50,52]
perphenazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.2 pKi 47
pKi 7.2 [47]
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 5,32
pKi 6.8 – 7.4 [5,32]
loxapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.4 pKi 49,52
pKi 6.8 – 7.4 [49,52]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inverse agonist 7.1 pKi 47
pKi 7.1 [47]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.0 pKi 50
pKi 7.0 [50]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 26
pKi 7.0 [26]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Mm Antagonist 7.0 pKi 46
pKi 7.0 [46]
dihydroergocryptine Small molecule or natural product Mm Antagonist 7.0 pKi 46
pKi 7.0 [46]
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 52
pKi 6.9 – 7.0 [52]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 – 7.0 pKi 31,49
pKi 6.8 – 7.0 [31,49]
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 16
pKi 6.8 [16]
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 50
pKi 6.8 [50]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.6 – 6.7 pKi 52
pKi 6.6 – 6.7 [52]
olanzapine