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PsychedeliaDokholyan Laboratory
TargetSerotonin receptors

5-HT1D

5-HT receptor subtypes.

Measurements
136
Compounds
31
Binding constants
117
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.

Protein

5HT1D_HUMANHTR1DHomo sapiens

5-hydroxytryptamine receptor 1D

G protein-coupled receptor for 5-hydroxytryptamine (serotonin)10452531,1565658,1652050,33762731. Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances10452531,1565658,1652050,33762731. 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 cyclase10452531,1565658,1652050,33762731. HTR1D is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission by inhibiting adenylate cyclase activity33762731. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity18476671,20945968. May also play a role in regulating the release of other neurotransmitters18476671,20945968. May play a role in vasoconstriction18476671,20945968

Quoted from UniProt’s FUNCTION annotation for P28221 (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.

PartnerCombinedExperimentDatabaseText mining
GNB10.9730.9260.6500.050
GNAI10.9670.9090.6500.050
HTR1B0.9520.2920.4000.891
GNG20.9380.8310.6500.000
SLC6A40.9210.0000.0000.920
GNG70.8040.1200.6500.416
TPH10.8020.0000.0000.801
HTR3A0.7930.0000.0000.790
MAOB0.7790.0000.0000.779
GNB30.7640.2920.6500.125

Where it sits in the cell

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Enterocytes10 nCPM
  • Prostatic club cells5.2 nCPM
  • Cholangiocytes4 nCPM
  • Early spermatids2.4 nCPM
  • Respiratory deuterosomal cells2.1 nCPM
  • Brain inhibitory neurons1.9 nCPM
  • Endometrial glandular cells1.7 nCPM
  • Enteric transient amplifying cells1.6 nCPM

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.

  • intestine8 nTPM
  • brain6.2 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

cerebral cortex — 0.5 nTPM, from HTR1Dcerebellum — no resolved target expressed herehippocampal formation — 0.3 nTPM, from HTR1Damygdala — 0.5 nTPM, from HTR1Dhypothalamus — 0.7 nTPM, from HTR1Dthalamus — no resolved target expressed herebasal ganglia — 6.2 nTPM, from HTR1Dmedulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: midbrain 0.3, spinal cord 0.2, pituitary gland 0.1.

Body

heart — no resolved target expressed heresmooth muscle — no resolved target expressed herelung — 0.1 nTPM, from HTR1Dliver — no resolved target expressed herekidney — no resolved target expressed herestomach — 0.1 nTPM, from HTR1Dduodenum — 8.0 nTPM, from HTR1Dsmall intestine — 7.1 nTPM, from HTR1Dcolon — 0.2 nTPM, from HTR1Dadrenal gland — no resolved target expressed herethyroid gland — no resolved target expressed herepancreas — 0.2 nTPM, from HTR1Durinary bladder — 0.1 nTPM, from HTR1Dskeletal muscle — no resolved target expressed herespleen — no resolved target expressed heresalivary gland — no resolved target expressed here
08 nTPM

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 HTR1D 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 · 8

  • basal ganglia6.2 nTPM
  • hypothalamus0.7 nTPM
  • cerebral cortex0.5 nTPM
  • amygdala0.5 nTPM
  • hippocampal formation0.3 nTPM
  • midbrain0.3 nTPM
  • spinal cord0.2 nTPM
  • pituitary gland0.1 nTPM

Peripheral and autonomic · 7

  • duodenum8.0 nTPM
  • small intestine7.1 nTPM
  • colon0.2 nTPM
  • pancreas0.2 nTPM
  • lung0.1 nTPM
  • stomach 10.1 nTPM
  • urinary bladder0.1 nTPM

Transcript is not protein. These are RNA levels for HTR1D, 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.

  1. 01Ergotamine10.15
  2. 02Lisuride9.01
  3. 035-Methoxytryptamine8.77
  4. 04Methysergide8.44
  5. 05LSZ8.43
  6. 06LSD8.41
  7. 07Bromocriptine8.00
  8. 08Psilocin7.73
  9. 09Tryptamine7.44
  10. 10DMT7.15
  11. 115-MeO-DALT7.00
  12. 12alpha-Methylserotonin6.82
  13. 135-MeO-2-TMT6.60
  14. 14DPT6.21
  15. 15DALT6.16
  16. 16DOB6.00
  17. 17DOI5.91
  18. 18Psilocybin5.67
  19. 19Mitragynine5.59
  20. 20DiPT5.43

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 117

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
5-HT1DSerotonin receptorsKi0.07010.15RATPMID 19912901
5-HT1DSerotonin receptorsKi0.07010.15RATPMID 7984267
5-HT1DSerotonin receptorsKi0.3009.52testPMID 28792478
5-HT1DSerotonin receptorsKi0.8009.10Homo sapiensCHEMBL616927
5-HT1DSerotonin receptorsKi0.9009.05BOVINEPMID 2664084
5-HT1DSerotonin receptorsKi0.9779.01HUMANPMID 12388666
5-HT1DSerotonin receptorsKi1.009.00HUMANPDSP
5-HT1DSerotonin receptorsKi1.708.77HUMANPMID 9303569
5-HT1DSerotonin receptorsKi1.948.71DogPMID 7984267
5-HT1DSerotonin receptorsKi2.188.66HUMANPMID 7984267
5-HT1DSerotonin receptorsKi2.208.66HUMANPMID 1652050
5-HT1DSerotonin receptorsKi2.208.66Homo sapiensCHEMBL3106305
5-HT1DSerotonin receptorsKi2.398.62RATPMID 7984267
5-HT1DSerotonin receptorsKi2.408.62RATPMID 19912901
5-HT1DSerotonin receptorsKi2.508.60BOVINEPDSP
5-HT1DSerotonin receptorsKi2.638.58Homo sapiensCHEMBL3106305
5-HT1DSerotonin receptorsKi3.638.44HUMANPMID 7984267
5-HT1DSerotonin receptorsKi3.708.43Homo sapiensCHEMBL617309
5-HT1DSerotonin receptorsKi3.808.42CALFPDSP
5-HT1DSerotonin receptorsKi3.808.42CALFPDSP
5-HT1DSerotonin receptorsKi3.808.42COWPDSP
5-HT1DSerotonin receptorsKi3.908.41Homo sapiensCHEMBL617312
5-HT1DSerotonin receptorsKi3.988.40CALFPDSP
5-HT1DSerotonin receptorsKi3.988.40CALFPDSP
5-HT1DSerotonin receptorsKi3.988.40CALFPDSP
5-HT1DSerotonin receptorsKi3.988.40CALFPDSP
5-HT1DSerotonin receptorsKi3.988.40COWPDSP
5-HT1DSerotonin receptorsKi4.008.40BOVINEPMID 1565658
5-HT1DSerotonin receptorsKi4.008.40BOVINEPMID 1565658
5-HT1DSerotonin receptorsKi4.788.32HUMANPMID 7984267
5-HT1DSerotonin receptorsKi5.408.27Homo sapiensCHEMBL617303
5-HT1DSerotonin receptorsKi6.008.22HUMANPMID 21907583
5-HT1DSerotonin receptorsKi6.008.22Homo sapiensCHEMBL1831560
5-HT1DSerotonin receptorsKi6.178.21HUMANPDSP
5-HT1DSerotonin receptorsKi6.308.20DogPMID 7984267
5-HT1DSerotonin receptorsKi6.318.20CALFPDSP
5-HT1DSerotonin receptorsKi7.088.15PIGPDSP
5-HT1DSerotonin receptorsKi7.088.15COWPDSP
5-HT1DSerotonin receptorsKi7.088.15PIGPDSP
5-HT1DSerotonin receptorsKi7.088.15CALFPDSP
5-HT1DSerotonin receptorsKi7.308.14HUMANPDSP
5-HT1DSerotonin receptorsKi7.708.11RATPDSP
5-HT1DSerotonin receptorsKi7.768.11DogPMID 7984267
5-HT1DSerotonin receptorsKi8.808.06BOVINEPMID 2664084
5-HT1DSerotonin receptorsKi10.008.00HUMANPMID 19925619
5-HT1DSerotonin receptorsKi10.008.00RATPDSP
5-HT1DSerotonin receptorsKi10.727.97HUMANPMID 12388666
5-HT1DSerotonin receptorsKi12.587.90DogPMID 7984267
5-HT1DSerotonin receptorsKi14.007.85HUMANPDSP
5-HT1DSerotonin receptorsKi18.607.73HUMANPMID 20126400
5-HT1DSerotonin receptorsKi24.007.62BOVINEPDSP
5-HT1DSerotonin receptorsKi25.007.60HUMANPMID 1565658
5-HT1DSerotonin receptorsKi25.707.59PIGPDSP
5-HT1DSerotonin receptorsKi26.907.57HUMANPDSP
5-HT1DSerotonin receptorsKi28.977.54COWPDSP
5-HT1DSerotonin receptorsKi30.907.51CALFPDSP
5-HT1DSerotonin receptorsKi30.907.51DogPMID 7984267
5-HT1DSerotonin receptorsKi30.907.51COWPDSP
5-HT1DSerotonin receptorsKi30.907.51CALFPDSP
5-HT1DSerotonin receptorsKi31.607.50CALFPDSP
5-HT1DSerotonin receptorsKi34.007.47HUMANPMID 1565658
5-HT1DSerotonin receptorsKi36.007.44BOVINEPDSP
5-HT1DSerotonin receptorsKi39.807.40CALFPDSP
5-HT1DSerotonin receptorsKi40.007.40BOVINEPMID 1565658
5-HT1DSerotonin receptorsKi41.007.39RATPDSP
5-HT1DSerotonin receptorsKi41.707.38HUMANPDSP
5-HT1DSerotonin receptorsKi46.007.34HUMANPDSP
5-HT1DSerotonin receptorsKi61.007.21Homo sapiensCHEMBL617599
5-HT1DSerotonin receptorsKi69.007.16HUMANPDSP
5-HT1DSerotonin receptorsKi69.007.16testPMID 28792478
5-HT1DSerotonin receptorsKi70.007.15RATPDSP
5-HT1DSerotonin receptorsKi71.387.15COWPDSP
5-HT1DSerotonin receptorsKi72.007.14RATPDSP
5-HT1DSerotonin receptorsKi85.107.07COWPDSP
5-HT1DSerotonin receptorsKi85.107.07CALFPDSP
5-HT1DSerotonin receptorsKi85.117.07HUMANPMID 7984267
5-HT1DSerotonin receptorsKi93.007.03HUMANPDSP
5-HT1DSerotonin receptorsKi93.007.03HUMANPMID 20126400
5-HT1DSerotonin receptorsKi1007.00RATPDSP
5-HT1DSerotonin receptorsKi1007.00Homo sapiensCHEMBL3756277
5-HT1DSerotonin receptorsKi1076.97HUMANPMID 29499272
5-HT1DSerotonin receptorsKi1146.94HUMANPMID 20126400
5-HT1DSerotonin receptorsKi1206.92BOVINEPDSP
5-HT1DSerotonin receptorsKi1506.82Homo sapiensCHEMBL616732
5-HT1DSerotonin receptorsKi1506.82Homo sapiensCHEMBL3756277
5-HT1DSerotonin receptorsKi1906.72BOVINEPDSP
5-HT1DSerotonin receptorsKi2246.65PIGPDSP
5-HT1DSerotonin receptorsKi2506.60Homo sapiensCHEMBL616927
5-HT1DSerotonin receptorsKi2706.57HUMANPDSP
5-HT1DSerotonin receptorsKi2956.53CALFPDSP
5-HT1DSerotonin receptorsKi3436.46BOVINEPDSP
5-HT1DSerotonin receptorsKi3476.46DogPMID 7984267
5-HT1DSerotonin receptorsKi5216.28HUMANPMID 1565658
5-HT1DSerotonin receptorsKi6196.21HUMANPMID 20126400
5-HT1DSerotonin receptorsKi6896.16HUMANPMID 29499272
5-HT1DSerotonin receptorsKi6926.16Homo sapiensCHEMBL3756277
5-HT1DSerotonin receptorsKi1,0006.00BOVINEPMID 2664084
5-HT1DSerotonin receptorsKi1,2415.91COWPDSP
5-HT1DSerotonin receptorsKi1,4485.84COWPDSP
5-HT1DSerotonin receptorsKi1,8005.74RATPDSP
5-HT1DSerotonin receptorsKi2,1195.67HUMANPDSP
5-HT1DSerotonin receptorsKi2,5635.59HUMANPDSP
5-HT1DSerotonin receptorsKi3,4005.47RATPDSP
5-HT1DSerotonin receptorsKi3,7425.43HUMANPMID 20126400
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL616731
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235593
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235593
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL616923
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL616923
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1912147
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL616514
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739246
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756277
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756277
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL616731
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2393678
5-HT1DSerotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2393678

Functional readouts 8

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
5-HT1DSerotonin receptorsIC5024.007.62Cavia porcellusCHEMBL616649
5-HT1DSerotonin receptorsIC5049.007.31Cavia porcellusCHEMBL616649
5-HT1DSerotonin receptorsIC5049.007.31Homo sapiensCHEMBL616517
5-HT1DSerotonin receptorsEC501346.87— organism not recordedPMID 42709856
5-HT1DSerotonin receptorsIC506106.21Homo sapiensCHEMBL616519
5-HT1DSerotonin receptorsIC503,7155.43Sus scrofaCHEMBL617559
5-HT1DSerotonin receptorsIC503,7155.43Sus scrofaCHEMBL617560
5-HT1DSerotonin receptorsEC50— no normalized value— value does not convert to pXCavia porcellusCHEMBL615728

Other measurements 11

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.

TargetClassTypeValue (nM)pXOrganismAssay
5-HT1DSerotonin receptorsp[A50]— no normalized value— value does not convert to pXHomo sapiensCHEMBL617575
5-HT1DSerotonin receptorsIntrinsic activity— no normalized value— value does not convert to pXHomo sapiensCHEMBL617573
5-HT1DSerotonin receptorsIntrinsic activity— no normalized value— value does not convert to pXHomo sapiensCHEMBL617573
5-HT1DSerotonin receptorsIntrinsic activity— no normalized value— value does not convert to pXHomo sapiensCHEMBL617573
5-HT1DSerotonin receptorsSelectivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL852461
5-HT1DSerotonin receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687658
5-HT1DSerotonin receptorsk_off— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739246
5-HT1DSerotonin receptorskon— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739246
5-HT1DSerotonin receptorsSelectivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL852461
5-HT1DSerotonin receptorsp[A50]— no normalized value— value does not convert to pXHomo sapiensCHEMBL617575
5-HT1DSerotonin receptorsp[A50]— no normalized value— value does not convert to pXHomo sapiensCHEMBL617575
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