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5-HT1A receptor

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Target id: 1

Nomenclature: 5-HT1A 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 7 422 5q12.3 HTR1A 5-hydroxytryptamine receptor 1A 24,96
Mouse 7 421 13 56.92 cM Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 15
Rat 7 422 2q13 Htr1a 5-hydroxytryptamine receptor 1A 3,26
Previous and Unofficial Names Click here for help
ADRBRL1 | 5-HT1A | ADRB2RL1 | serotonin receptor 1A | Gpcr18 | 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled
Database Links Click here for help
Specialist databases
GPCRDB 5ht1a_human (Hs), 5ht1a_mouse (Mm), 5ht1a_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]NLX-112 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Full agonist 8.9 pKd 34
pKd 8.9 (Kd 1.4x10-9 M) [34]
[3H]8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 6.0 – 9.4 pKd 9,40,69,72
pKd 6.0 – 9.4 (Kd 1x10-6 – 3.98x10-10 M) [9,40,69,72]
[3H]S-15535 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist 5.8 – 5.9 pKd 72
pKd 5.8 – 5.9 [72]
S-14671 Small molecule or natural product Hs Full agonist 10.2 – 10.5 pKi 70,72
pKi 10.2 – 10.5 [70,72]
LY293284 Small molecule or natural product Hs Full agonist 10.1 pKi 9
pKi 10.1 [9]
5-CT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.4 – 10.3 pKi 68,70,72-73
pKi 9.4 – 10.3 [68,70,72-73]
lisuride Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.7 – 9.8 pKi 60,68,72
pKi 9.7 – 9.8 [60,68,72]
U92016A Small molecule or natural product Hs Full agonist 9.7 pKi 57
pKi 9.7 [57]
vilazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 9.7 pKi 19
pKi 9.7 (Ki 2x10-10 M) [19]
Description: Binding of vilazodone to human 5-HT1A receptors against [3H]8-OH-DPAT (DPAT)
S-14506 Small molecule or natural product Hs Full agonist 9.6 – 9.7 pKi 70,72
pKi 9.6 – 9.7 [70,72]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.4 – 9.9 pKi 60,60
pKi 9.4 – 9.9 [60,60]
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 9.1 – 9.7 pKi 40,68-70,72-73
pKi 9.1 – 9.7 [40,68-70,72-73]
flesinoxan Small molecule or natural product Hs Full agonist 9.3 pKi 70
pKi 9.3 [70]
L-694,247 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.3 pKi 68
pKi 9.3 [68]
S-15535 Small molecule or natural product Hs Partial agonist 9.2 pKi 72
pKi 9.2 [72]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.0 pKi 74
pKi 9.0 [74]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 70
pKi 9.0 [70]
flibanserin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Agonist 9.0 pKi 10
pKi 9.0 (Ki 1x10-9 M) [10]
8-OH-DPAT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.4 – 9.4 pKi 20,30,40,49,61,70,72-73
pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,30,40,49,61,70,72-73]
LY 165,163 Small molecule or natural product Hs Full agonist 8.9 pKi 70
pKi 8.9 [70]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.8 pKi 70
pKi 8.8 [70]
ipsapirone Small molecule or natural product Hs Partial agonist 8.6 – 8.8 pKi 70,72
pKi 8.6 – 8.8 [70,72]
FG-5893 Small molecule or natural product Hs Full agonist 8.7 pKi 70
pKi 8.7 [70]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.7 pKi 60
pKi 8.7 [60]
7-methoxy-1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.6 pKi 39
pKi 8.6 [39]
(R)-UH 301 Small molecule or natural product Hs Partial agonist 8.6 pKi 70
pKi 8.6 (Ki 2.74x10-9 M) [70]
NLX-101 Small molecule or natural product Hs Full agonist 8.6 pKi 71
pKi 8.6 [71]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.5 pKi 60
pKi 8.5 [60]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 7.9 – 8.9 pKi 70,91
pKi 7.9 – 8.9 [70,91]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 8.4 pKi 58
pKi 8.4 [58]
aripiprazole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 8.2 pKi 94
pKi 8.2 [94]
tandospirone Small molecule or natural product Hs Full agonist 8.2 pKi 70
pKi 8.2 [70]
lurasidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Partial agonist 8.2 pKi 35
pKi 8.2 (Ki 6.75x10-9 M) [35]
asenapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 8.0 – 8.3 pKi 70,91
pKi 8.0 – 8.3 [70,91]
zalospirone Small molecule or natural product Hs Full agonist 8.1 pKi 70
pKi 8.1 [70]
1-naphthylpiperazine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 39
pKi 8.0 [39]
ocaperidone Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.0 pKi 27
pKi 8.0 [27]
bromocriptine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.9 pKi 60
pKi 7.9 [60]
buspirone Small molecule or natural product Approved drug Primary target of this compound Hs Partial agonist 7.7 – 8.0 pKi 70,72-73
pKi 7.7 – 8.0 [70,72-73]
vortioxetine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.8 pKi 7
pKi 7.8 (Ki 1.5x10-8 M) [7]
LY334370 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 98
pKi 7.8 [98]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.7 pKi 84
pKi 7.7 [84]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.7 pKi 60
pKi 7.7 [60]
donitriptan Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.6 pKi 38
pKi 7.6 [38]
eletriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.4 pKi 67
pKi 7.4 [67]
naratriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.1 – 7.6 pKi 67-68
pKi 7.1 – 7.6 [67-68]
nafadotride Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 70
pKi 7.3 [70]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 51
pKi 7.3 (Ki 5.27x10-8 M) [51]
frovatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.2 pKi 102
pKi 7.2 (Ki 6x10-8 M) [102]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.2 pKi 51
pKi 7.2 (Ki 6.09x10-8 M) [51]
BMY-14802 Small molecule or natural product Hs Full agonist 7.2 pKi 70
pKi 7.2 [70]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pKi 100
pKi 7.2 [100]
avitriptan Small molecule or natural product Click here for species-specific activity table Rn Agonist 7.2 pKi 90
pKi 7.2 (Ki 7.08x10-8 M) [90]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.1 – 7.2 pKi 39,84
pKi 7.1 – 7.2 [39,84]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 6.9 pKi 60
pKi 6.9 [60]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.8 – 6.9 pKi 58,70,91
pKi 6.8 – 6.9 [58,70,91]
EMDT Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.8 pKi 29
pKi 6.8 [29]
fluparoxan Small molecule or natural product Hs Partial agonist 6.8 pKi 61
pKi 6.8 [61]
LP-211 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pKi 52
pKi 6.7 (Ki 1.88x10-7 M) [52]
zolmitriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.6 pKi 67
pKi 6.6 [67]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.5 – 6.6 pKi 70,91
pKi 6.5 – 6.6 [70,91]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.4 pKi 60
pKi 6.4 [60]
rizatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.4 pKi 67
pKi 6.4 [67]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 pKi 80
pKi 6.3 [80]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.3 pKi 84
pKi 6.3 [84]
CP 93129 Small molecule or natural product Hs Full agonist 6.1 pKi 68
pKi 6.1 [68]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.0 pKi 64
pKi 6.0 [64]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.0 pKi 67
pKi 6.0 [67]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 pKi 69
pKi 5.8 [69]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.6 – 5.8 pKi 70,91
pKi 5.6 – 5.8 [70,91]
vilazodone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Partial agonist 9.5 pIC50 32
pIC50 9.5 (IC50 3x10-10 M) [32]
BMY-7378 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.8 – 8.0 pIC50 43
pIC50 6.8 – 8.0 [43]
L-772,405 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.2 pIC50 88
pIC50 7.2 [88]
SEP-363856 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.6 pIC50 21
pIC50 5.6 (IC50 2.3x10-6 M) [21]
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]robalzotan Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.8 pKd 36
pKd 9.8 (Kd 1.58x10-10 M) [36]
[3H]WAY100635 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 9.5 pKd 43
pKd 9.5 (Kd 3x10-10 M) [43]
[3H]p-MPPF Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.4 pKd 40
pKd 8.4 [40]
Rec 15/3079 Small molecule or natural product Hs Antagonist 9.7 pKi 50
pKi 9.7 [50]
NAN 190 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKi 70
pKi 9.4 [70]
repinotan Small molecule or natural product Hs Antagonist 9.4 pKi 20
pKi 9.4 [20]
robalzotan Small molecule or natural product Hs Antagonist 9.2 pKi 37
pKi 9.2 (Ki 6.31x10-10 M) [37]
SB 649915 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKi 99
pKi 8.6 [99]
WAY-100635 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 – 9.2 pKi 70,72
pKi 7.9 – 9.2 (Ki 1.26x10-8 – 6.31x10-10 M) [70,72]
p-MPPI Small molecule or natural product Hs Antagonist 8.4 pKi 40
pKi 8.4 [40]
tiospirone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 70
pKi 8.3 [70]
(-)-tertatolol Small molecule or natural product Hs Antagonist 8.2 pKi 49,70
pKi 8.2 [49,70]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.1 pKi 72
pKi 8.1 [72]
SB 272183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 101
pKi 8.0 [101]
WAY-100135 Small molecule or natural product Hs Antagonist 8.0 pKi 72
pKi 8.0 [72]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.1 pKi 70,72
pKi 7.8 – 8.1 [70,72]
(S)-UH 301 Small molecule or natural product Hs Antagonist 7.9 pKi 70
pKi 7.9 (Ki 1.35x10-8 M) [70]
spiperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 – 8.8 pKi 70,72-73
pKi 6.7 – 8.8 [70,72-73]
(-)-propranolol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.5 pKi 68
pKi 7.5 [68]
(S)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 87
pKi 7.5 [87]
pizotifen Small molecule or natural product Approved drug Hs Antagonist 7.4 pKi 68
pKi 7.4 [68]
GR 125,743 Small molecule or natural product Hs Antagonist 7.3 pKi 68
pKi 7.3 [68]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 61
pKi 7.3 [61]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 91
pKi 7.2 [91]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.1 pKi 70
pKi 7.1 [70]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 41
pKi 7.0 [41]
mesoridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 17
pKi 7.0 (Ki 1.05x10-7 M) [17]
GR 218,231 Small molecule or natural product Hs Antagonist 6.8 pKi 59
pKi 6.8 [59]
iloperidone Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.8 pKi 44
pKi 6.8 [44]
pimozide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.8 pKi 70
pKi 6.8 [70]
(R)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 87
pKi 6.5 [87]
SB 714786 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 99
pKi 6.5 [99]
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 – 6.6 pKi 70,91
pKi 6.4 – 6.6 [70,91]
zotepine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.5 pKi 91
pKi 6.5 [91]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.4 – 6.5 pKi 70,91
pKi 6.4 – 6.5 [70,91]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 70
pKi 6.4 [70]
cyamemazine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 30
pKi 6.3 [30]
9-OH-risperidone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.2 pKi 91
pKi 6.2 [91]
chlorpromazine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.2 pKi 70
pKi 6.2 [70]
risperidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 6.2 pKi 44
pKi 6.2 [44]
MPDT Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.8 pKi 29
pKi 5.8 [29]
haloperidol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.7 – 5.8 pKi 49,58,70,91
pKi 5.7 – 5.8 [49,58,70,91]
pipamperone Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 91
pKi 5.6 [91]
raclopride Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 70
pKi 5.2 [70]
ketanserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 5.0 pKi 73
pKi 5.0 [73]
SDZ-216525 Small molecule or natural product Hs Antagonist 7.8 – 8.2 pIC50 43
pIC50 7.8 – 8.2 [43]
ritanserin Small molecule or natural product Click here for species-specific activity table