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PsychedeliaDokholyan Laboratory
TargetSerotonin receptors

5-HT7

5-HT receptor subtypes.

Measurements
138
Compounds
30
Binding constants
126
Median pX
7.87

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

5HT7R_HUMANHTR7Homo sapiens

5-hydroxytryptamine receptor 7

G protein-coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen35714614,8226867. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors35714614,8226867. HTR7 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity35714614

Quoted from UniProt’s FUNCTION annotation for P34969 (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
GNAS0.9950.9260.9000.450
GNB10.9920.9260.9000.000
GNG20.9830.8310.9000.076
GNB30.9320.2920.9000.117
GNB40.9320.2920.9000.121
GNB20.9260.2920.9000.000
GNB50.9260.2920.9000.000
HTR60.9250.0000.9000.288
GNG100.9200.1200.9000.167
GNG40.9190.1900.9000.091

Where it sits in the cell

  • Nucleoplasm
  • Plasma membrane
  • Vesiclesadditional
  • Primary ciliumadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cell membrane

Expression by cell type

Single cell type RNA, the 10 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Hepatic stellate cells45.2 nCPM
  • cDC42.1 nCPM
  • Macrophages30.1 nCPM
  • Undifferentiated spermatogonia25.7 nCPM
  • Other brain neurons25 nCPM
  • Brain excitatory neurons23.4 nCPM
  • Late primary spermatocytes21.6 nCPM
  • Brain inhibitory neurons19.7 nCPM
  • monocytes16 nCPM
  • Hofbauer cells15 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.

  • parathyroid gland12.3 nTPM
  • testis8.2 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 — 1.4 nTPM, from HTR7cerebellum — no resolved target expressed herehippocampal formation — 1.0 nTPM, from HTR7amygdala — 0.4 nTPM, from HTR7hypothalamus — 2.1 nTPM, from HTR7thalamus — no resolved target expressed herebasal ganglia — 0.3 nTPM, from HTR7medulla 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 0.5, spinal cord 0.3, retina 0.1.

Body

heart — 0.1 nTPM, from HTR7smooth muscle — 0.3 nTPM, from HTR7lung — 0.2 nTPM, from HTR7liver — 0.4 nTPM, from HTR7kidney — no resolved target expressed herestomach — 0.7 nTPM, from HTR7duodenum — 0.5 nTPM, from HTR7small intestine — 1.3 nTPM, from HTR7colon — 0.6 nTPM, from HTR7adrenal gland — 0.2 nTPM, from HTR7thyroid gland — 0.1 nTPM, from HTR7pancreas — 0.1 nTPM, from HTR7urinary bladder — 2.1 nTPM, from HTR7skeletal muscle — 0.9 nTPM, from HTR7spleen — 1.0 nTPM, from HTR7salivary gland — 0.2 nTPM, from HTR7
02 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 HTR7 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

  • hypothalamus2.1 nTPM
  • cerebral cortex1.4 nTPM
  • hippocampal formation1.0 nTPM
  • midbrain0.5 nTPM
  • amygdala0.4 nTPM
  • basal ganglia0.3 nTPM
  • spinal cord0.3 nTPM
  • retina0.1 nTPM

Peripheral and autonomic · 15

  • urinary bladder2.1 nTPM
  • small intestine1.3 nTPM
  • spleen1.0 nTPM
  • skeletal muscle0.9 nTPM
  • stomach 10.7 nTPM
  • colon0.6 nTPM
  • duodenum0.5 nTPM
  • liver0.4 nTPM
  • smooth muscle0.3 nTPM
  • lung0.2 nTPM
  • adrenal gland0.2 nTPM
  • salivary gland0.2 nTPM
  • heart muscle0.1 nTPM
  • thyroid gland0.1 nTPM
  • pancreas0.1 nTPM

Transcript is not protein. These are RNA levels for HTR7, 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. 015-Methoxytryptamine9.60
  2. 02LSD9.40
  3. 03Lisuride9.30
  4. 04Bufotenine8.10
  5. 05Bromocriptine7.97
  6. 06LSZ7.92
  7. 07Methysergide7.90
  8. 08Tryptamine7.79
  9. 09Ergotamine7.77
  10. 105-MeO-DMT7.52
  11. 11Psilocin7.15
  12. 12DMT7.06
  13. 135-MeO-DALT7.05
  14. 145-MeO-2-TMT6.84
  15. 15meta-chlorophenylpiperazine6.79
  16. 16Harmalan6.55
  17. 17DPT6.55
  18. 18Psilocybin6.22
  19. 195-MeO-pyr-T6.20
  20. 20Mitragynine6.06
  21. 21quipazine5.52
  22. 22DiPT5.47
  23. 23Harmine5.26

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 126

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

TargetClassTypeValue (nM)pXOrganismAssay
5-HT7Serotonin receptorsKi0.2519.60GUINEA PIGPMID 10051134
5-HT7Serotonin receptorsKi0.3989.40GUINEA PIGPMID 10051134
5-HT7Serotonin receptorsKi0.5019.30RATPMID 9149537
5-HT7Serotonin receptorsKi0.5019.30GUINEA PIGPMID 9149537
5-HT7Serotonin receptorsKi0.5019.30HUMANPMID 9149537
5-HT7Serotonin receptorsKi0.5209.28RATPMID 7984267
5-HT7Serotonin receptorsKi0.5209.28GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi0.5209.28RATPMID 8394362
5-HT7Serotonin receptorsKi0.5709.24RATPMID 7984267
5-HT7Serotonin receptorsKi0.5709.24RATPMID 8394362
5-HT7Serotonin receptorsKi0.6319.20RATPMID 10051134
5-HT7Serotonin receptorsKi0.8909.05RATPMID 7984267
5-HT7Serotonin receptorsKi0.8909.05RATPMID 8394362
5-HT7Serotonin receptorsKi0.9309.03RATPMID 7984267
5-HT7Serotonin receptorsKi0.9339.03Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi0.9409.03MammalianPMID 7696602
5-HT7Serotonin receptorsKi0.9409.03RATPMID 8397408
5-HT7Serotonin receptorsKi1.009.00RATPMID 9149537
5-HT7Serotonin receptorsKi1.009.00GUINEA PIGPMID 7518496
5-HT7Serotonin receptorsKi1.588.80GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi1.588.80RATPMID 9149537
5-HT7Serotonin receptorsKi1.778.75RATPMID 7984267
5-HT7Serotonin receptorsKi1.788.75RATPMID 8394362
5-HT7Serotonin receptorsKi2.008.70Rattus norvegicusCHEMBL620750
5-HT7Serotonin receptorsKi2.008.70Homo sapiensCHEMBL619855
5-HT7Serotonin receptorsKi2.958.53GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi3.168.50GUINEA PIGPMID 9149537
5-HT7Serotonin receptorsKi5.008.30HUMANPMID 8226867
5-HT7Serotonin receptorsKi5.018.30HUMANPMID 7984267
5-HT7Serotonin receptorsKi5.018.30HUMANPMID 9149537
5-HT7Serotonin receptorsKi6.308.20RATPMID 7984267
5-HT7Serotonin receptorsKi6.308.20RATPMID 8397408
5-HT7Serotonin receptorsKi6.308.20MOUSEPMID 7984267
5-HT7Serotonin receptorsKi6.318.20RATPMID 9149537
5-HT7Serotonin receptorsKi6.318.20Homo sapiensCHEMBL618164
5-HT7Serotonin receptorsKi6.608.18Homo sapiensCHEMBL619865
5-HT7Serotonin receptorsKi6.608.18RATPMID 12213075
5-HT7Serotonin receptorsKi6.808.17HUMANPMID 20126400
5-HT7Serotonin receptorsKi7.948.10Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi7.948.10RATPMID 10051134
5-HT7Serotonin receptorsKi9.508.02MammalianPMID 7696602
5-HT7Serotonin receptorsKi9.508.02RATPMID 8397408
5-HT7Serotonin receptorsKi9.548.02RATPMID 7984267
5-HT7Serotonin receptorsKi9.558.02Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi10.008.00RATPMID 9149537
5-HT7Serotonin receptorsKi10.707.97RATPMID 8394362
5-HT7Serotonin receptorsKi10.717.97RATPMID 7984267
5-HT7Serotonin receptorsKi12.007.92Homo sapiensCHEMBL872928
5-HT7Serotonin receptorsKi12.507.90RATPMID 8394362
5-HT7Serotonin receptorsKi12.587.90MOUSEPMID 7984267
5-HT7Serotonin receptorsKi12.587.90RATPMID 7984267
5-HT7Serotonin receptorsKi12.597.90RATPMID 9149537
5-HT7Serotonin receptorsKi12.597.90RATPMID 10821800
5-HT7Serotonin receptorsKi12.597.90Homo sapiensCHEMBL619862
5-HT7Serotonin receptorsKi12.597.90Rattus norvegicusCHEMBL619052
5-HT7Serotonin receptorsKi13.407.87RATPMID 8394362
5-HT7Serotonin receptorsKi13.487.87RATPMID 7984267
5-HT7Serotonin receptorsKi15.487.81GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi15.857.80GUINEA PIGPMID 9149537
5-HT7Serotonin receptorsKi16.217.79RATPMID 7984267
5-HT7Serotonin receptorsKi16.407.79RATPMID 8394362
5-HT7Serotonin receptorsKi17.007.77RATPMID 8398139
5-HT7Serotonin receptorsKi17.007.77RATPMID 8398139
5-HT7Serotonin receptorsKi17.377.76RATPMID 7984267
5-HT7Serotonin receptorsKi17.377.76RATPMID 7984267
5-HT7Serotonin receptorsKi18.627.73GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi19.057.72GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi19.957.70GUINEA PIGPMID 9149537
5-HT7Serotonin receptorsKi22.387.65GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi25.127.60HUMANPMID 9149537
5-HT7Serotonin receptorsKi30.007.52HUMANPDSP
5-HT7Serotonin receptorsKi30.007.52Homo sapiensCHEMBL619855
5-HT7Serotonin receptorsKi30.907.51GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi31.627.50RATPMID 9149537
5-HT7Serotonin receptorsKi32.807.48RATPMID 8394362
5-HT7Serotonin receptorsKi33.117.48RATPMID 7984267
5-HT7Serotonin receptorsKi39.817.40GUINEA PIGPMID 7518496
5-HT7Serotonin receptorsKi39.817.40Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi48.807.31RATPMID 8394362
5-HT7Serotonin receptorsKi48.977.31RATPMID 7984267
5-HT7Serotonin receptorsKi48.977.31GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi50.117.30MOUSEPMID 7984267
5-HT7Serotonin receptorsKi64.567.19GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi71.607.15HUMANPMID 20126400
5-HT7Serotonin receptorsKi79.437.10HUMANPMID 9149537
5-HT7Serotonin receptorsKi83.007.08HUMANPMID 12825922
5-HT7Serotonin receptorsKi83.007.08HUMANPMID 8226867
5-HT7Serotonin receptorsKi83.177.08HUMANPMID 7984267
5-HT7Serotonin receptorsKi87.507.06HUMANPMID 20126400
5-HT7Serotonin receptorsKi89.137.05Homo sapiensCHEMBL3756284
5-HT7Serotonin receptorsKi90.007.05HUMANPMID 29499272
5-HT7Serotonin receptorsKi93.327.03GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi1266.90MOUSEPMID 7984267
5-HT7Serotonin receptorsKi1386.86GUINEA PIGPMID 7647964
5-HT7Serotonin receptorsKi1456.84Homo sapiensCHEMBL620829
5-HT7Serotonin receptorsKi1486.83HUMANPMID 7984267
5-HT7Serotonin receptorsKi1496.83HUMANPMID 8226867
5-HT7Serotonin receptorsKi1636.79Homo sapiensCHEMBL5163626
5-HT7Serotonin receptorsKi2006.70RATPMID 7984267
5-HT7Serotonin receptorsKi2806.55Homo sapiensCHEMBL620826
5-HT7Serotonin receptorsKi2846.55HUMANPMID 20126400
5-HT7Serotonin receptorsKi3046.52Homo sapiensCHEMBL619855
5-HT7Serotonin receptorsKi3986.40RATPMID 7984267
5-HT7Serotonin receptorsKi5986.22HUMANPDSP
5-HT7Serotonin receptorsKi6316.20Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi8656.06HUMANPDSP
5-HT7Serotonin receptorsKi1,1225.95Rattus norvegicusCHEMBL620766
5-HT7Serotonin receptorsKi1,2605.90Homo sapiensCHEMBL619855
5-HT7Serotonin receptorsKi1,2915.89testPMID 28792478
5-HT7Serotonin receptorsKi1,2915.89HUMANPDSP
5-HT7Serotonin receptorsKi3,0335.52Homo sapiensCHEMBL619855
5-HT7Serotonin receptorsKi3,4235.47HUMANPMID 20126400
5-HT7Serotonin receptorsKi5,5005.26Homo sapiensCHEMBL620826
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756284
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2396014
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2396014
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4343395
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235599
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4343395
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054018
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3584688
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXRattus norvegicusCHEMBL2166090
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5054018
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4343395
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235599
5-HT7Serotonin receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739254

Functional readouts 1

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

TargetClassTypeValue (nM)pXOrganismAssay
5-HT7Serotonin receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291827

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-HT7Serotonin receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4344373
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619053
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619053
5-HT7Serotonin receptorskon— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739254
5-HT7Serotonin receptorsk_off— no normalized value— value does not convert to pXHomo sapiensCHEMBL5739254
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619053
5-HT7Serotonin receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4429820
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619703
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619703
5-HT7Serotonin receptorsIncrease— no normalized value— value does not convert to pXRattus norvegicusCHEMBL619703
5-HT7Serotonin receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687642
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