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PsychedeliaDokholyan Laboratory
TargetEnzymes

Acetylcholinesterase

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
75
Compounds
29
Binding constants
10
Median pX
4.70

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

ACES_HUMANACHEHomo sapiens

Acetylcholinesterase

Hydrolyzes rapidly the acetylcholine neurotransmitter released into the synaptic cleft allowing to terminate the signal transduction at the neuromuscular junction. Role in neuronal apoptosis

Quoted from UniProt’s FUNCTION annotation for P22303 (reviewed).

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
COLQ0.9890.4960.0000.980
APP0.9370.7350.0000.769
CHAT0.9330.0000.0000.933
GPCPD10.9160.0000.9000.194
CHKA0.9120.0000.9000.158
MAOB0.9100.0000.0000.902
CHKB0.9090.0000.9000.128
PHOSPHO10.9040.0000.9000.000
HSPG20.8950.1110.0000.882
DOK70.8670.0000.0000.865

Where it sits in the cell

  • Golgi apparatus
  • Vesiclesadditional

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

UniProt, curated Synapse · Secreted · Cell membrane · Nucleus

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.

  • Enterocytes122.4 nCPM
  • Colonocytes78.6 nCPM
  • Other brain neurons59.6 nCPM
  • Retinal horizontal cells50.1 nCPM
  • Retinal amacrine cells48.9 nCPM
  • Retinal ganglion cells42.5 nCPM
  • Thymic myoid cells35.4 nCPM
  • Myonuclei35.2 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.

  • skeletal muscle152.9 nTPM
  • brain103.9 nTPM
  • tongue44.9 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 — 23.4 nTPM, from ACHEcerebellum — 59.1 nTPM, from ACHEhippocampal formation — 14.5 nTPM, from ACHEamygdala — 14.7 nTPM, from ACHEhypothalamus — 103.9 nTPM, from ACHEthalamus — no resolved target expressed herebasal ganglia — 38.3 nTPM, from ACHEmedulla 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 47.7, spinal cord 14.4, pituitary gland 6.4, retina 5.3.

Body

heart — 11.4 nTPM, from ACHEsmooth muscle — 0.5 nTPM, from ACHElung — 3.3 nTPM, from ACHEliver — 3.4 nTPM, from ACHEkidney — 4.2 nTPM, from ACHEstomach — 2.0 nTPM, from ACHEduodenum — 4.6 nTPM, from ACHEsmall intestine — 7.3 nTPM, from ACHEcolon — 6.3 nTPM, from ACHEadrenal gland — 4.4 nTPM, from ACHEthyroid gland — 1.6 nTPM, from ACHEpancreas — 3.1 nTPM, from ACHEurinary bladder — 1.0 nTPM, from ACHEskeletal muscle — 152.9 nTPM, from ACHEspleen — 2.4 nTPM, from ACHEsalivary gland — 5.7 nTPM, from ACHE
0153 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 ACHE 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 · 10

  • hypothalamus103.9 nTPM
  • cerebellum59.1 nTPM
  • midbrain47.7 nTPM
  • basal ganglia38.3 nTPM
  • cerebral cortex23.4 nTPM
  • amygdala14.7 nTPM
  • hippocampal formation14.5 nTPM
  • spinal cord14.4 nTPM
  • pituitary gland6.4 nTPM
  • retina5.3 nTPM

Peripheral and autonomic · 16

  • skeletal muscle152.9 nTPM
  • heart muscle11.4 nTPM
  • small intestine7.3 nTPM
  • colon6.3 nTPM
  • salivary gland5.7 nTPM
  • duodenum4.6 nTPM
  • adrenal gland4.4 nTPM
  • kidney4.2 nTPM
  • liver3.4 nTPM
  • lung3.3 nTPM
  • pancreas3.1 nTPM
  • spleen2.4 nTPM
  • stomach 12.0 nTPM
  • thyroid gland1.6 nTPM
  • urinary bladder1.0 nTPM
  • smooth muscle0.5 nTPM

Transcript is not protein. These are RNA levels for ACHE, 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. 01Dextrorphan4.70

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 10

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

TargetClassTypeValue (nM)pXOrganismAssay
AcetylcholinesteraseEnzymesKi20,0004.70Electrophorus electricusCHEMBL1251789
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXMus musculusCHEMBL637745
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXMus musculusCHEMBL637746
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212

Functional readouts 46

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

TargetClassTypeValue (nM)pXOrganismAssay
AcetylcholinesteraseEnzymesIC504,4005.36Electrophorus electricusCHEMBL1274400
AcetylcholinesteraseEnzymesIC504,9005.31Electrophorus electricusCHEMBL2020010
AcetylcholinesteraseEnzymesIC508,6005.07Electrophorus electricusCHEMBL1274400
AcetylcholinesteraseEnzymesIC5010,1005.00Electrophorus electricusCHEMBL5157286
AcetylcholinesteraseEnzymesIC5010,1005.00Electrophorus electricusCHEMBL6128019
AcetylcholinesteraseEnzymesIC5011,2804.95Electrophorus electricusCHEMBL2020010
AcetylcholinesteraseEnzymesIC5011,3004.95Homo sapiensCHEMBL5254673
AcetylcholinesteraseEnzymesIC5011,4004.94Electrophorus electricusCHEMBL3131492
AcetylcholinesteraseEnzymesIC5012,5004.90Electrophorus electricusCHEMBL3131492
AcetylcholinesteraseEnzymesIC5014,0004.85Electrophorus electricusCHEMBL3131492
AcetylcholinesteraseEnzymesIC5017,0704.77Electrophorus electricusCHEMBL4832643
AcetylcholinesteraseEnzymesIC5020,9104.68Electrophorus electricusCHEMBL2020010
AcetylcholinesteraseEnzymesIC5022,8904.64Electrophorus electricusCHEMBL2020010
AcetylcholinesteraseEnzymesIC5023,7004.63Homo sapiensCHEMBL2020014
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020014
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020014
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020014
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235525
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5235525
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909212
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291912
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291912
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291912
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL911302
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL911302
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXRattus norvegicusCHEMBL641389
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL3879334
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL3879334
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4673487
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4023561
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5341188
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL1103849
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291723
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291723
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291723
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291723
AcetylcholinesteraseEnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291723
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020010
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020014
AcetylcholinesteraseEnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020014

Other measurements 19

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
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL4136015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2166270
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2166270
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2166270
AcetylcholinesteraseEnzymespIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL4356264
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL1105651
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXElectrophorus electricusCHEMBL2020011
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL2020015
AcetylcholinesteraseEnzymesRatio— no normalized value— value does not convert to pXMus musculusCHEMBL637748
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