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PsychedeliaDokholyan Laboratory
TargetUnclassified

H1

Matched no rule. Shown as-is rather than assigned a class by guesswork. Values below are reported as measured; because this is not a molecular target, they are not treated as affinities anywhere on this site.

Measurements
47
Compounds
21
Binding constants
29
Median pX
5.85

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

HRH1_HUMANHRH1Homo sapiens

Histamine H1 receptor

G protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter33828102,8280179. Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)

Quoted from UniProt’s FUNCTION annotation for P35367 (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
GNAQ0.9990.9000.9000.977
GNB10.9030.9000.0000.070
TRPV10.8270.0000.0000.827
GNG20.8000.8000.0000.000
HDC0.7980.0000.0000.798
PLCB30.7430.0000.5000.498
GNA110.7220.0000.6500.238
GNA150.7110.0000.6500.204
GNA140.6970.0000.6500.158
IL310.6570.0000.0000.657

Where it sits in the cell

  • Plasma membrane
  • Cytosoladditional

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

  • Urothelial cells269.4 nCPM
  • Endometrial glandular cells244 nCPM
  • Fallopian tube ciliated cells227 nCPM
  • Fallopian secretory cells218.7 nCPM
  • Hofbauer cells189.5 nCPM
  • Endometrial secretory cells179.9 nCPM
  • Epididymal efferent duct ciliated cells169.1 nCPM
  • Kupffer cells163 nCPM
  • Epididymal basal cells161.2 nCPM
  • Ocular epithelial cells151.6 nCPM
  • Papillary tip epithelial cells147.9 nCPM
  • Enterocytes141.1 nCPM

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 — 6.6 nTPM, from HRH1cerebellum — no resolved target expressed herehippocampal formation — 1.7 nTPM, from HRH1amygdala — 2.8 nTPM, from HRH1hypothalamus — 1.7 nTPM, from HRH1thalamus — no resolved target expressed herebasal ganglia — 1.4 nTPM, from HRH1medulla 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: spinal cord 0.9, midbrain 0.8, pituitary gland 0.4, retina 0.2.

Body

heart — 1.4 nTPM, from HRH1smooth muscle — 5.0 nTPM, from HRH1lung — 3.7 nTPM, from HRH1liver — 0.7 nTPM, from HRH1kidney — 2.0 nTPM, from HRH1stomach — 1.6 nTPM, from HRH1duodenum — 2.5 nTPM, from HRH1small intestine — 4.1 nTPM, from HRH1colon — 7.8 nTPM, from HRH1adrenal gland — 2.8 nTPM, from HRH1thyroid gland — 1.1 nTPM, from HRH1pancreas — 0.6 nTPM, from HRH1urinary bladder — 13.3 nTPM, from HRH1skeletal muscle — 0.9 nTPM, from HRH1spleen — 0.9 nTPM, from HRH1salivary gland — 1.7 nTPM, from HRH1
013 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 HRH1 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 · 9

  • cerebral cortex6.6 nTPM
  • amygdala2.8 nTPM
  • hippocampal formation1.7 nTPM
  • hypothalamus1.7 nTPM
  • basal ganglia1.4 nTPM
  • spinal cord0.9 nTPM
  • midbrain0.8 nTPM
  • pituitary gland0.4 nTPM
  • retina0.2 nTPM

Peripheral and autonomic · 16

  • urinary bladder13.3 nTPM
  • colon7.8 nTPM
  • smooth muscle5.0 nTPM
  • small intestine4.1 nTPM
  • lung3.7 nTPM
  • adrenal gland2.8 nTPM
  • duodenum2.5 nTPM
  • kidney2.0 nTPM
  • salivary gland1.7 nTPM
  • stomach 11.6 nTPM
  • heart muscle1.4 nTPM
  • thyroid gland1.1 nTPM
  • skeletal muscle0.9 nTPM
  • spleen0.9 nTPM
  • liver0.7 nTPM
  • pancreas0.6 nTPM

Transcript is not protein. These are RNA levels for HRH1, 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. 01Lisuride7.46
  2. 02DPT6.90
  3. 03DALT6.90
  4. 04LSZ6.30
  5. 055-MeO-DALT6.30
  6. 06LSD5.96
  7. 07MDMA5.67
  8. 08Methysergide5.52
  9. 09DiPT5.45
  10. 102C-I5.21

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 29

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

TargetClassTypeValue (nM)pXOrganismAssay
H1UnclassifiedKi34.677.46GUINEA PIGPMID 12388666
H1UnclassifiedKi1256.90HUMANPMID 20126400
H1UnclassifiedKi1266.90Homo sapiensCHEMBL3756492
H1UnclassifiedKi1276.90HUMANPMID 29499272
H1UnclassifiedKi5006.30Homo sapiensCHEMBL694563
H1UnclassifiedKi5016.30Homo sapiensCHEMBL3756492
H1UnclassifiedKi5056.30HUMANPMID 29499272
H1UnclassifiedKi1,1005.96HUMANPMID 26318099
H1UnclassifiedKi1,3005.89RATPMID 282646
H1UnclassifiedKi1,5405.81RATPMID 12213075
H1UnclassifiedKi1,5405.81Homo sapiensCHEMBL694564
H1UnclassifiedKi2,1385.67HUMANPDSP
H1UnclassifiedKi2,1385.67HUMANPMID 12761331
H1UnclassifiedKi3,0005.52GUINEA PIGPDSP
H1UnclassifiedKi3,0005.52HUMANPMID 16782354
H1UnclassifiedKi3,5835.45HUMANPMID 20126400
H1UnclassifiedKi6,1005.21HUMANPMID 26318099
H1UnclassifiedKi9,0005.05HUMANPDSP
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756492
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756492
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2395820
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL2395820
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156

Functional readouts 17

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

TargetClassTypeValue (nM)pXOrganismAssay
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909156
H1UnclassifiedAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291809

Other measurements 1

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
H1UnclassifiedInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687679
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