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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 24,96
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
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)
Natural/Endogenous Ligands Click here for help
5-hydroxytryptamine

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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 Ligand has a PDB structure 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 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 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 Ligand has a PDB structure 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 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 88
⤷ pIC50 7.2 [88]
ulotaront 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 Ligand has a PDB structure 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 Ligand has a PDB structure 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