5-HT1A
5-HT receptor subtypes.
- Measurements
- 301
- Compounds
- 76
- Binding constants
- 200
- Median pX
- 7.60
I · Identity
What this target is
Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.
5-hydroxytryptamine receptor 1A
G protein-coupled receptor for 5-hydroxytryptamine (serotonin)22957663,3138543,33762731,37935376,37935377,8138923,8393041. Also functions as a receptor for various drugs and psychoactive substances22957663,3138543,33762731,38552625,8138923,8393041. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase22957663,3138543,33762731,8138923,8393041. HTR1A is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission: signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores33762731,35610220. Beta-arrestin family members regulate signaling by mediating both receptor desensitization and resensitization processes18476671,20363322,20945968. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism18476671,20363322,20945968. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior18476671,20363322,20945968. Plays a role in the response to anxiogenic stimuli18476671,20363322,20945968
Quoted from UniProt’s FUNCTION annotation for P08908 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.
What it acts with
STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.
Where it sits in the cell
UniProt, curated Cell membrane · Cell projection, dendrite
Expression by tissue
The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.
- brain6.1 nTPM
II · Anatomy
Where the gene is transcribed
The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.
Brain
basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.
Measured but not drawn — this anatomogram has no outline for them: midbrain 0.4, spinal cord 0.3.
Body
Square-root ramp · shared scale across both plates
Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of HTR1A transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.
Brain · 7
- hippocampal formation6.1 nTPM
- cerebral cortex4.9 nTPM
- amygdala2.4 nTPM
- hypothalamus1.4 nTPM
- basal ganglia0.4 nTPM
- midbrain0.4 nTPM
- spinal cord0.3 nTPM
Peripheral and autonomic · 1
- heart muscle0.1 nTPM
Transcript is not protein. These are RNA levels for HTR1A, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.
III · Ranking
Compounds by strongest binding constant
One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.
- 01Lisuride10.10
- 02Ergotamine9.77
- 03LSD9.51
- 04LSZ8.96
- 05Methergine8.82
- 065-MeO-DET8.77
- 075-Methoxytryptamine8.60
- 08Bufotenine8.50
- 09Bromocriptine8.49
- 105-MeO-DPT8.40
- 115-MeO-AMT8.34
- 12Ergonovine8.33
- 135-MeO-DMT8.26
- 14RU-282538.24
- 15alpha-Methylserotonin7.92
- 16Methysergide7.85
- 175-Br-DMT7.77
- 185-MeO-DALT7.72
- 19meta-chlorophenylpiperazine7.64
- 205-Cl-DMT7.50
- 21DPT7.50
- 22N,N-Diethyltryptamine7.33
- 23Psilocin7.31
- 244-HO-DET7.31
- 252C-H7.15
- 26TFMPP7.09
- 274-Hydroxytryptamine7.02
- 28DALT7.00
- 295-F-DMT7.00
- 30dimemebfe7.00
- 31Tryptamine6.98
- 32DMT6.92
- 33DiPT6.92
- 34Mitragynine6.79
- 352C-I6.74
- 365-MeO-2-TMT6.70
- 37MK-2126.69
- 386-Fluoro-N,N-diethyltryptamine6.59
- 39mebfap6.35
- 40quipazine5.80
- 41Mescaline5.73
- 422,5-Dimethoxy-4-trifluoromethylamphetamine5.65
- 43DOI5.63
- 441-(2-naphthyl)piperazine5.54
- 452C-TFM5.47
- 46DOB5.42
- 47DOET5.41
- 48DOM5.14
IV · Evidence
Every measurement at this target
Each row links to the ChEMBL assay it came from.
Equilibrium binding constants 200
Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| 5-HT1A | Serotonin receptors | Ki | 0.080 | 10.10 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 0.148 | 9.83 | HUMAN | PMID 12388666 |
| 5-HT1A | Serotonin receptors | Ki | 0.170 | 9.77 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 0.170 | 9.77 | test | PMID 28792478 |
| 5-HT1A | Serotonin receptors | Ki | 0.300 | 9.52 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 0.310 | 9.51 | BOVINE | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 0.400 | 9.40 | HUMAN | PMID 7984267 |
| 5-HT1A | Serotonin receptors | Ki | 0.410 | 9.39 | HUMAN | PMID 8461029 |
| 5-HT1A | Serotonin receptors | Ki | 0.430 | 9.37 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 0.443 | 9.35 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | 0.640 | 9.19 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 0.760 | 9.12 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 1.09 | 8.96 | HUMAN | PMID 7984267 |
| 5-HT1A | Serotonin receptors | Ki | 1.10 | 8.96 | Homo sapiens | CHEMBL616134 |
| 5-HT1A | Serotonin receptors | Ki | 1.10 | 8.96 | Homo sapiens | CHEMBL615811 |
| 5-HT1A | Serotonin receptors | Ki | 1.10 | 8.96 | Homo sapiens | CHEMBL615775 |
| 5-HT1A | Serotonin receptors | Ki | 1.10 | 8.96 | HUMAN | PMID 12213075 |
| 5-HT1A | Serotonin receptors | Ki | 1.20 | 8.92 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 1.50 | 8.82 | HUMAN | PMID 28720478 |
| 5-HT1A | Serotonin receptors | Ki | 1.50 | 8.82 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 1.70 | 8.77 | Homo sapiens | CHEMBL616121 |
| 5-HT1A | Serotonin receptors | Ki | 1.98 | 8.70 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.05 | 8.69 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.50 | 8.60 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.57 | 8.59 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.57 | 8.59 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.59 | 8.59 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.68 | 8.57 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2.78 | 8.56 | HUMAN | PMID 24488404 |
| 5-HT1A | Serotonin receptors | Ki | 3.00 | 8.52 | RAT | PMID 8398139 |
| 5-HT1A | Serotonin receptors | Ki | 3.00 | 8.52 | HUMAN | PMID 26318099 |
| 5-HT1A | Serotonin receptors | Kd | 3.16 | 8.50 | Homo sapiens | CHEMBL1061237 |
| 5-HT1A | Serotonin receptors | Ki | 3.20 | 8.49 | Homo sapiens | CHEMBL615759 |
| 5-HT1A | Serotonin receptors | Ki | 3.20 | 8.49 | Rattus norvegicus | CHEMBL616081 |
| 5-HT1A | Serotonin receptors | Ki | 3.20 | 8.49 | Rattus norvegicus | CHEMBL616423 |
| 5-HT1A | Serotonin receptors | Ki | 3.22 | 8.49 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | 3.90 | 8.41 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 4.00 | 8.40 | Rattus norvegicus | CHEMBL616081 |
| 5-HT1A | Serotonin receptors | Ki | 4.00 | 8.40 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 4.10 | 8.39 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 4.60 | 8.34 | Homo sapiens | CHEMBL617484 |
| 5-HT1A | Serotonin receptors | Ki | 4.64 | 8.33 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | 4.92 | 8.31 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 5.00 | 8.30 | Rattus norvegicus | CHEMBL616691 |
| 5-HT1A | Serotonin receptors | Ki | 5.10 | 8.29 | Rattus norvegicus | CHEMBL616090 |
| 5-HT1A | Serotonin receptors | Ki | 5.10 | 8.29 | Rattus norvegicus | CHEMBL616418 |
| 5-HT1A | Serotonin receptors | Ki | 5.50 | 8.26 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 5.70 | 8.24 | Rattus norvegicus | CHEMBL616570 |
| 5-HT1A | Serotonin receptors | Ki | 6.40 | 8.19 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 6.90 | 8.16 | HUMAN | PMID 8461029 |
| 5-HT1A | Serotonin receptors | Ki | 6.91 | 8.16 | HUMAN | PMID 7984267 |
| 5-HT1A | Serotonin receptors | Ki | 7.00 | 8.15 | Rattus norvegicus | CHEMBL616691 |
| 5-HT1A | Serotonin receptors | Ki | 7.30 | 8.14 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 7.80 | 8.11 | Rattus norvegicus | CHEMBL616081 |
| 5-HT1A | Serotonin receptors | Ki | 9.00 | 8.05 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 10.00 | 8.00 | HUMAN | PMID 19925619 |
| 5-HT1A | Serotonin receptors | Ki | 10.00 | 8.00 | Rattus norvegicus | CHEMBL616423 |
| 5-HT1A | Serotonin receptors | Ki | 10.72 | 7.97 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 12.00 | 7.92 | Homo sapiens | CHEMBL617484 |
| 5-HT1A | Serotonin receptors | Ki | 12.88 | 7.89 | HUMAN | PMID 12388666 |
| 5-HT1A | Serotonin receptors | Ki | 12.90 | 7.89 | HUMAN | PMID 16051647 |
| 5-HT1A | Serotonin receptors | Ki | 14.00 | 7.85 | test | PMID 28792478 |
| 5-HT1A | Serotonin receptors | Ki | 14.00 | 7.85 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 16.90 | 7.77 | — organism not recorded | PMID 41120735 |
| 5-HT1A | Serotonin receptors | Ki | 16.98 | 7.77 | HUMAN | PMID 7984267 |
| 5-HT1A | Serotonin receptors | Ki | 19.00 | 7.72 | HUMAN | PMID 29499272 |
| 5-HT1A | Serotonin receptors | Ki | 19.00 | 7.72 | Homo sapiens | CHEMBL3756275 |
| 5-HT1A | Serotonin receptors | Ki | 19.95 | 7.70 | Homo sapiens | CHEMBL3756275 |
| 5-HT1A | Serotonin receptors | Ki | 20.00 | 7.70 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 21.20 | 7.67 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 23.00 | 7.64 | Rattus norvegicus | CHEMBL616953 |
| 5-HT1A | Serotonin receptors | Ki | 23.44 | 7.63 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 24.00 | 7.62 | Homo sapiens | CHEMBL616370 |
| 5-HT1A | Serotonin receptors | Ki | 24.00 | 7.62 | Homo sapiens | CHEMBL5527111 |
| 5-HT1A | Serotonin receptors | Ki | 24.20 | 7.62 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 25.00 | 7.60 | HUMAN | PMID 9686407 |
| 5-HT1A | Serotonin receptors | Ki | 25.00 | 7.60 | HUMAN | PMID 30768942 |
| 5-HT1A | Serotonin receptors | Ki | 25.00 | 7.60 | HUMAN | PMID 16051647 |
| 5-HT1A | Serotonin receptors | Ki | 25.00 | 7.60 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 25.12 | 7.60 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 25.70 | 7.59 | PIG | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 28.00 | 7.55 | Homo sapiens | CHEMBL993916 |
| 5-HT1A | Serotonin receptors | Ki | 31.00 | 7.51 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | 31.70 | 7.50 | — organism not recorded | PMID 41120735 |
| 5-HT1A | Serotonin receptors | Ki | 31.80 | 7.50 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 31.94 | 7.50 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 35.14 | 7.45 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 40.00 | 7.40 | BOVINE | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 42.00 | 7.38 | Rattus norvegicus | CHEMBL616089 |
| 5-HT1A | Serotonin receptors | Ki | 42.00 | 7.38 | Homo sapiens | CHEMBL5163623 |
| 5-HT1A | Serotonin receptors | Ki | 47.00 | 7.33 | Homo sapiens | CHEMBL616121 |
| 5-HT1A | Serotonin receptors | Ki | 49.00 | 7.31 | HUMAN | PMID 11101361 |
| 5-HT1A | Serotonin receptors | Ki | 49.00 | 7.31 | Homo sapiens | CHEMBL616121 |
| 5-HT1A | Serotonin receptors | Ki | 62.60 | 7.20 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 69.00 | 7.16 | Rattus norvegicus | CHEMBL616690 |
| 5-HT1A | Serotonin receptors | Ki | 70.00 | 7.15 | HUMAN | PMID 26318099 |
| 5-HT1A | Serotonin receptors | Ki | 70.79 | 7.15 | RAT | PMID 6225026 |
| 5-HT1A | Serotonin receptors | Ki | 80.60 | 7.09 | Rattus norvegicus | CHEMBL616053 |
| 5-HT1A | Serotonin receptors | Ki | 85.00 | 7.07 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 89.13 | 7.05 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 95.00 | 7.02 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 95.50 | 7.02 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 100 | 7.00 | HUMAN | PMID 29499272 |
| 5-HT1A | Serotonin receptors | Ki | 100 | 7.00 | HUMAN | PMID 15886504 |
| 5-HT1A | Serotonin receptors | Kd | 100 | 7.00 | Homo sapiens | CHEMBL1061237 |
| 5-HT1A | Serotonin receptors | Ki | 100 | 7.00 | Homo sapiens | CHEMBL3756275 |
| 5-HT1A | Serotonin receptors | Ki | 101 | 7.00 | — organism not recorded | PMID 41120735 |
| 5-HT1A | Serotonin receptors | Ki | 101 | 7.00 | Rattus norvegicus | CHEMBL616690 |
| 5-HT1A | Serotonin receptors | Ki | 105 | 6.98 | HUMAN | PMID 7984267 |
| 5-HT1A | Serotonin receptors | Ki | 120 | 6.92 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 121 | 6.92 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 128 | 6.89 | — organism not recorded | PMID 41120735 |
| 5-HT1A | Serotonin receptors | Ki | 130 | 6.89 | Rattus norvegicus | CHEMBL616108 |
| 5-HT1A | Serotonin receptors | Ki | 141 | 6.85 | BOVINE | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 145 | 6.84 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 161 | 6.79 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 170 | 6.77 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 170 | 6.77 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 174 | 6.76 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 175 | 6.76 | Rattus norvegicus | CHEMBL616108 |
| 5-HT1A | Serotonin receptors | Ki | 180 | 6.74 | HUMAN | PMID 26318099 |
| 5-HT1A | Serotonin receptors | Ki | 200 | 6.70 | Homo sapiens | CHEMBL616299 |
| 5-HT1A | Serotonin receptors | Ki | 202 | 6.69 | Rattus norvegicus | CHEMBL616953 |
| 5-HT1A | Serotonin receptors | Ki | 224 | 6.65 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 227 | 6.64 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 245 | 6.61 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 256 | 6.59 | Homo sapiens | CHEMBL616121 |
| 5-HT1A | Serotonin receptors | Ki | 259 | 6.59 | Rattus norvegicus | CHEMBL616115 |
| 5-HT1A | Serotonin receptors | Ki | 259 | 6.59 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 410 | 6.39 | Homo sapiens | CHEMBL993916 |
| 5-HT1A | Serotonin receptors | Ki | 445 | 6.35 | Rattus norvegicus | CHEMBL616690 |
| 5-HT1A | Serotonin receptors | Ki | 450 | 6.35 | HUMAN | PMID 24488404 |
| 5-HT1A | Serotonin receptors | Ki | 545 | 6.26 | RAT | PMID 8398139 |
| 5-HT1A | Serotonin receptors | Ki | 779 | 6.11 | Rattus norvegicus | CHEMBL616690 |
| 5-HT1A | Serotonin receptors | Kd | 794 | 6.10 | Homo sapiens | CHEMBL1061237 |
| 5-HT1A | Serotonin receptors | Ki | 1,585 | 5.80 | Rattus norvegicus | CHEMBL616159 |
| 5-HT1A | Serotonin receptors | Ki | 1,841 | 5.73 | HUMAN | PMID 20126400 |
| 5-HT1A | Serotonin receptors | Ki | 1,950 | 5.71 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Kd | 1,995 | 5.70 | Homo sapiens | CHEMBL1061237 |
| 5-HT1A | Serotonin receptors | Ki | 2,225 | 5.65 | Rattus norvegicus | CHEMBL616571 |
| 5-HT1A | Serotonin receptors | Ki | 2,355 | 5.63 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 2,400 | 5.62 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 2,884 | 5.54 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 3,236 | 5.49 | Rattus norvegicus | CHEMBL616344 |
| 5-HT1A | Serotonin receptors | Ki | 3,300 | 5.48 | Rattus norvegicus | CHEMBL615963 |
| 5-HT1A | Serotonin receptors | Ki | 3,422 | 5.47 | Rattus norvegicus | CHEMBL616571 |
| 5-HT1A | Serotonin receptors | Ki | 3,708 | 5.43 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 3,715 | 5.43 | RAT | PMID 6225026 |
| 5-HT1A | Serotonin receptors | Ki | 3,770 | 5.42 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 3,770 | 5.42 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 3,843 | 5.42 | HUMAN | PMID 12954071 |
| 5-HT1A | Serotonin receptors | Ki | 3,930 | 5.41 | RAT | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 4,600 | 5.34 | HUMAN | PMID 26318099 |
| 5-HT1A | Serotonin receptors | Ki | 4,677 | 5.33 | RAT | PMID 6225026 |
| 5-HT1A | Serotonin receptors | Kd | 5,012 | 5.30 | Homo sapiens | CHEMBL1061237 |
| 5-HT1A | Serotonin receptors | Ki | 6,327 | 5.20 | HUMAN | PDSP |
| 5-HT1A | Serotonin receptors | Ki | 7,267 | 5.14 | HUMAN | PMID 8382063 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615773 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5235591 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5235591 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616082 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054021 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054021 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6082494 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6082494 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615773 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5739244 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL3583837 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3756275 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3756275 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2393680 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL2393680 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054020 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6114540 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6114540 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL616228 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616681 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616588 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616428 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1006687 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1039633 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1949347 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL615962 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL615962 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL615962 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616684 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616695 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616067 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616689 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616067 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615451 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615460 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616684 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL3584692 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616109 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL615960 |
| 5-HT1A | Serotonin receptors | Ki | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL615961 |
Functional readouts 59
IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| 5-HT1A | Serotonin receptors | IC50 | 0.774 | 9.11 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | IC50 | 5.63 | 8.25 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | IC50 | 8.13 | 8.09 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | IC50 | 10.00 | 8.00 | Homo sapiens | CHEMBL615470 |
| 5-HT1A | Serotonin receptors | IC50 | 11.00 | 7.96 | Rattus norvegicus | CHEMBL884525 |
| 5-HT1A | Serotonin receptors | IC50 | 15.00 | 7.82 | Homo sapiens | CHEMBL615470 |
| 5-HT1A | Serotonin receptors | IC50 | 19.60 | 7.71 | Homo sapiens | CHEMBL616274 |
| 5-HT1A | Serotonin receptors | IC50 | 54.00 | 7.27 | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | IC50 | 86.40 | 7.06 | Homo sapiens | CHEMBL616274 |
| 5-HT1A | Serotonin receptors | IC50 | 196 | 6.71 | Homo sapiens | CHEMBL6158869 |
| 5-HT1A | Serotonin receptors | IC50 | 290 | 6.54 | Rattus norvegicus | CHEMBL615927 |
| 5-HT1A | Serotonin receptors | EC50 | 830 | 6.08 | — organism not recorded | PMID 42709856 |
| 5-HT1A | Serotonin receptors | IC50 | 1,445 | 5.84 | Homo sapiens | CHEMBL615579 |
| 5-HT1A | Serotonin receptors | IC50 | 1,445 | 5.84 | Homo sapiens | CHEMBL615580 |
| 5-HT1A | Serotonin receptors | IC50 | 2,700 | 5.57 | Rattus norvegicus | CHEMBL615926 |
| 5-HT1A | Serotonin receptors | IC50 | 4,785 | 5.32 | Homo sapiens | CHEMBL6158869 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615463 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291916 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615478 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615478 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615478 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4687644 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5529051 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6080642 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL5096612 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096613 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291896 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291896 |
| 5-HT1A | Serotonin receptors | IC50 | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291896 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291896 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291896 |
| 5-HT1A | Serotonin receptors | IC50 | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | IC50 | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL1909209 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291815 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291815 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291814 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291815 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291815 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291815 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615170 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL615170 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1614390 |
| 5-HT1A | Serotonin receptors | EC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL1614390 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
| 5-HT1A | Serotonin receptors | AC50 | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5291813 |
Other measurements 42
Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.
| Target | Class | Type | Value (nM) | pX | Organism | Assay |
|---|---|---|---|---|---|---|
| 5-HT1A | Serotonin receptors | NT | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL616019 |
| 5-HT1A | Serotonin receptors | KiAH | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616598 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054010 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054010 |
| 5-HT1A | Serotonin receptors | Emax | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5547457 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054009 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL3423625 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL3423626 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054010 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054009 |
| 5-HT1A | Serotonin receptors | Agonist | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616162 |
| 5-HT1A | Serotonin receptors | Hill coefficient | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL841450 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125277 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125277 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125266 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125267 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125268 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125269 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125271 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125272 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125273 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125274 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125275 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL6125276 |
| 5-HT1A | Serotonin receptors | Inhibition | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL4687675 |
| 5-HT1A | Serotonin receptors | Emax | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5529052 |
| 5-HT1A | Serotonin receptors | Hill coefficient | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL841450 |
| 5-HT1A | Serotonin receptors | Efficacy | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL5096616 |
| 5-HT1A | Serotonin receptors | Efficacy | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5096617 |
| 5-HT1A | Serotonin receptors | Hill coefficient | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL841450 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054010 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054009 |
| 5-HT1A | Serotonin receptors | Activity | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5054009 |
| 5-HT1A | Serotonin receptors | Binding | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL616143 |
| 5-HT1A | Serotonin receptors | k_off | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5739244 |
| 5-HT1A | Serotonin receptors | kon | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5739244 |
| 5-HT1A | Serotonin receptors | Emax | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL5547458 |
| 5-HT1A | Serotonin receptors | NT | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616322 |
| 5-HT1A | Serotonin receptors | NT | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616322 |
| 5-HT1A | Serotonin receptors | NT | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616322 |
| 5-HT1A | Serotonin receptors | NT | — no normalized value | — value does not convert to pX | Rattus norvegicus | CHEMBL616323 |
| 5-HT1A | Serotonin receptors | Binding | — no normalized value | — value does not convert to pX | Homo sapiens | CHEMBL616142 |