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5-HT1A receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1

Nomenclature: 5-HT1A 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 7 422 5q12.3 HTR1A 5-hydroxytryptamine receptor 1A 24,97
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
Alphafold P08908 (Hs), Q64264 (Mm), P19327 (Rn)
ChEMBL Target CHEMBL214 (Hs), CHEMBL3737 (Mm), CHEMBL273 (Rn)
DrugBank Target P08908 (Hs)
Ensembl Gene ENSG00000178394 (Hs), ENSMUSG00000021721 (Mm), ENSRNOG00000010254 (Rn)
Entrez Gene 3350 (Hs), 15550 (Mm), 24473 (Rn)
Human Protein Atlas ENSG00000178394 (Hs)
KEGG Gene hsa:3350 (Hs), mmu:15550 (Mm), rno:24473 (Rn)
OMIM 109760 (Hs)
Pharos P08908 (Hs)
RefSeq Nucleotide NM_000524 (Hs), NM_008308 (Mm), NM_012585 (Rn)
RefSeq Protein NP_000515 (Hs), NP_032334 (Mm), NP_036717 (Rn)
UniProtKB P08908 (Hs), Q64264 (Mm), P19327 (Rn)
Wikipedia HTR1A (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of SEP-363856 bound serotonin 1A (5-HT1A) receptor-Gi protein complex
PDB Id:  8W8B
Ligand:  ulotaront
Resolution:  3.0Å
Species:  Human
References:  56
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 Ligand has a PDB structure 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 9,40,70,73
⤷ pKd 6.0 – 9.4 (Kd 1x10-6 – 3.98x10-10 M) [9,40,70,73]
[3H]S-15535 Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Partial agonist 5.8 – 5.9 pKd 73
⤷ pKd 5.8 – 5.9 [73]
S-14671 Small molecule or natural product Hs Full agonist 10.2 – 10.5 pKi 71,73
⤷ pKi 10.2 – 10.5 [71,73]
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 Ligand has a PDB structure Hs Full agonist 9.4 – 10.3 pKi 69,71,73-74
⤷ pKi 9.4 – 10.3 [69,71,73-74]
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 61,61,73
⤷ pKi 9.7 – 9.8 [61,61,73]
U92016A Small molecule or natural product Hs Full agonist 9.7 pKi 58
⤷ pKi 9.7 [58]
vilazodone 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 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 71,73
⤷ pKi 9.6 – 9.7 [71,73]
roxindole Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 9.4 – 9.9 pKi 61,70
⤷ pKi 9.4 – 9.9 [61,70]
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 40,69-71,73-74
⤷ pKi 9.1 – 9.7 [40,69-71,73-74]
flesinoxan Small molecule or natural product Hs Full agonist 9.3 pKi 71
⤷ pKi 9.3 [71]
L-694,247 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.3 pKi 69
⤷ pKi 9.3 [69]
S-15535 Small molecule or natural product Hs Partial agonist 9.2 pKi 73
⤷ pKi 9.2 [73]
Lysergide Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 9.0 pKi 75
⤷ pKi 9.0 [75]
RU 24969 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 9.0 pKi 71
⤷ pKi 9.0 [71]
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 20,30,40,62,71,73,73-74
⤷ pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,30,40,62,71,73,73-74]
LY 165,163 Small molecule or natural product Hs Full agonist 8.9 pKi 71
⤷ pKi 8.9 [71]
spiroxatrine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.8 pKi 71
⤷ pKi 8.8 [71]
ipsapirone Small molecule or natural product Hs Partial agonist 8.6 – 8.8 pKi 71,73
⤷ pKi 8.6 – 8.8 [71,73]
FG-5893 Small molecule or natural product Hs Full agonist 8.7 pKi 71
⤷ pKi 8.7 [71]
pergolide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.7 pKi 61
⤷ pKi 8.7 [61]
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 71
⤷ pKi 8.6 (Ki 2.74x10-9 M) [71]
NLX-101 Small molecule or natural product Hs Full agonist 8.6 pKi 72
⤷ pKi 8.6 [72]
terguride Small molecule or natural product Approved drug Click here for species-specific activity table Hs Partial agonist 8.5 pKi 61
⤷ pKi 8.5 [61]
ziprasidone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.9 – 8.9 pKi 71,92
⤷ pKi 7.9 – 8.9 [71,92]
S 16924 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 8.4 pKi 59
⤷ pKi 8.4 [59]
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 95
⤷ pKi 8.2 [95]
tandospirone Small molecule or natural product Hs Full agonist 8.2 pKi 71
⤷ pKi 8.2 [71]
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 71,92
⤷ pKi 8.0 – 8.3 [71,92]
zalospirone Small molecule or natural product Hs Full agonist 8.1 pKi 71
⤷ pKi 8.1 [71]
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 61
⤷ pKi 7.9 [61]
buspirone Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Partial agonist 7.7 – 8.0 pKi 71,73-74
⤷ pKi 7.7 – 8.0 [71,73-74]
vortioxetine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure 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 99
⤷ pKi 7.8 [99]
BRL-15572 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Partial agonist 7.7 pKi 85
⤷ pKi 7.7 [85]
cabergoline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.7 pKi 61
⤷ pKi 7.7 [61]
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 68
⤷ pKi 7.4 [68]
naratriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 7.1 – 7.6 pKi 68-69
⤷ pKi 7.1 – 7.6 [68-69]
nafadotride Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.3 pKi 71
⤷ pKi 7.3 [71]
LP-44 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 52
⤷ pKi 7.3 (Ki 5.27x10-8 M) [52]
frovatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 7.2 pKi 103
⤷ pKi 7.2 (Ki 6x10-8 M) [103]
LP-12 Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.2 pKi 52
⤷ pKi 7.2 (Ki 6.09x10-8 M) [52]
BMY-14802 Small molecule or natural product Hs Full agonist 7.2 pKi 71
⤷ pKi 7.2 [71]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 7.2 pKi 101
⤷ pKi 7.2 [101]
avitriptan Small molecule or natural product Click here for species-specific activity table Rn Agonist 7.2 pKi 91
⤷ pKi 7.2 (Ki 7.08x10-8 M) [91]
GR 127935 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.1 – 7.2 pKi 39,85
⤷ pKi 7.1 – 7.2 [39,85]
apomorphine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 6.9 pKi 61
⤷ pKi 6.9 [61]
clozapine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 6.8 – 6.9 pKi 59,71,92
⤷ pKi 6.8 – 6.9 [59,71,92]
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 62
⤷ pKi 6.8 [62]
LP-211 Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pKi 53
⤷ pKi 6.7 (Ki 1.88x10-7 M) [53]
zolmitriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.6 pKi 68
⤷ pKi 6.6 [68]
quetiapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.5 – 6.6 pKi 71,92
⤷ pKi 6.5 – 6.6 [71,92]
piribedil Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.4 pKi 61
⤷ pKi 6.4 [61]
rizatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.4 pKi 68
⤷ pKi 6.4 [68]
LY344864 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.3 pKi 81
⤷ pKi 6.3 [81]
SB 216641 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.3 pKi 85
⤷ pKi 6.3 [85]
CP 93129 Small molecule or natural product Hs Full agonist 6.1 pKi 69
⤷ pKi 6.1 [69]
capeserod Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.0 pKi 65
⤷ pKi 6.0 [65]
sumatriptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 6.0 pKi 68
⤷ pKi 6.0 [68]
quinpirole Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.8 pKi 70
⤷ pKi 5.8 [70]
olanzapine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Full agonist 5.6 – 5.8 pKi 71,92
⤷ pKi 5.6 – 5.8 [71,92]
vilazodone 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 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 89
⤷ pIC50 7.2 [89]
ulotaront Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 51
⤷ pKi 9.7 [51]
NAN 190 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.4 pKi 71
⤷ pKi 9.4 [71]
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 100
⤷ pKi 8.6 [100]
WAY-100635 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.9 – 9.2 pKi 71,73
⤷ pKi 7.9 – 9.2 (Ki 1.26x10-8 – 6.31x10-10 M) [71,73]
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 71
⤷ pKi 8.3 [71]
(-)-tertatolol Small molecule or natural product Hs Antagonist 8.2 pKi 50,71
⤷ pKi 8.2 [50,71]
pindolol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.1 pKi 73
⤷ pKi 8.1 [73]
SB 272183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.0 pKi 102
⤷ pKi 8.0 [102]
WAY-100135 Small molecule or natural product Hs Antagonist 8.0 pKi 73
⤷ pKi 8.0 [73]
methiothepin Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 – 8.1 pKi 71,73
⤷ pKi 7.8 – 8.1 [71,73]
(S)-UH 301 Small molecule or natural product Hs Antagonist 7.9 pKi 71
⤷ pKi 7.9 (Ki 1.35x10-8 M) [71]
spiperone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.7 – 8.8 pKi 71,73-74
⤷ pKi 6.7 – 8.8 [71,73-74]
(-)-propranolol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.5 pKi 69
⤷ pKi 7.5 [69]
(S)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 88
⤷ pKi 7.5 [88]
pizotifen Small molecule or natural product Approved drug Hs Antagonist 7.4 pKi 69
⤷ pKi 7.4 [69]
GR 125,743 Small molecule or natural product Hs Antagonist 7.3 pKi 69
⤷ pKi 7.3 [69]
yohimbine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.3 pKi 62
⤷ pKi 7.3 [62]
fluspirilene Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 92
⤷ pKi 7.2 [92]
thioridazine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.1 pKi 71
⤷ pKi 7.1 [71]
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 60
⤷ pKi 6.8 [60]
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 Ligand has a PDB structure Hs Antagonist 6.8 pKi 71
⤷ pKi 6.8 [71]
(R)-flurocarazolol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 88
⤷ pKi 6.5 [88]
SB 714786 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 100
⤷ pKi 6.5 [100]
sertindole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 – 6.6 pKi 71,92
⤷ pKi 6.4 – 6.6 [71,92]
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 92
⤷ pKi 6.5 [92]
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 71,92
⤷ pKi 6.4 – 6.5 [71,92]
(+)-butaclamol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 71
⤷ pKi 6.4 [71]
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 92
⤷ pKi 6.2 [92]
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 71
⤷ pKi 6.2 [71]
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]