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Protein / target

Cholinesterase

Encoded byBCHEP06276Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
3
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Hydrolase activity, acting on ester bonds

Strongest disease association

Adverse effect

Via encoding gene BCHE · Genetic evidence · score 0.50

Therapeutic position

Established drug target

Small molecules

Research activity

Emerging research

3 papers · latest 2024

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

Esterase with broad substrate specificity.

View complete UniProt function annotation

Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters

Subcellular location

Secreted
Domains and Gene Ontology detail (26)

Gene Ontology

  • Cblood microparticle
  • Cendoplasmic reticulum lumen
  • Cextracellular region
  • Cextracellular space
  • Cnuclear envelope lumen
  • Cplasma membrane
  • Facetylcholinesterase activity
  • Famyloid-beta binding
  • Fcatalytic activity
  • Fcholine binding
  • Fcholinesterase activity
  • Fenzyme binding

602 aa · 68 kDa

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Synaptic signallingGOCell proliferation & survivalGOMetabolic enzyme activityGO
View supporting evidence

Synaptic signalling

  • ·negative regulation of synaptic transmission

Cell proliferation & survival

  • ·negative regulation of cell population proliferation

Metabolic enzyme activity

  • ·catalytic activity
  • ·choline metabolic process
  • ·xenobiotic metabolic process

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Approved medicines with mapped indications

1 medicine · 3 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Alzheimer's Disease1 medicine
Dementia1 medicine
Parkinson's Disease1 medicine

3 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

rivastigmine
ApprovedInhibitor

Cholinesterases; ACHE & BCHE inhibitor

Indicated for Alzheimer's Disease, Dementia, Parkinson's Disease

Acts on a complex — shared with ACHE · 1 of 2 recorded protein targets — narrow recorded profile

ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene BCHE

Gene-level evidence surfaced through the gene BCHEthat encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Alzheimer's Disease
0.78Well supported

Clinical evidence dominant · Open Targets 0.63

Parkinson's Disease
0.76Well supported

Clinical evidence dominant · Open Targets 0.61

Dementia
0.75Well supported

Clinical evidence dominant · Open Targets 0.61

Adverse effect
0.49Limited support

Genetic evidence dominant · Open Targets 0.30

Delirium
0.45Limited support

Clinical evidence dominant · Open Targets 0.35

View evidence synthesis (5)
Alzheimer's DiseaseWell supported
0.78
agreement 0.620.93
Clinical84%Literature16%

Open Targets aggregate 0.63 · 2 independent evidence families

Parkinson's DiseaseWell supported
0.76
agreement 0.600.91
Clinical85%Literature15%

Open Targets aggregate 0.61 · 2 independent evidence families

DementiaWell supported
0.75
agreement 0.600.91
Clinical87%Literature13%

Open Targets aggregate 0.61 · 2 independent evidence families

Adverse effectLimited support
0.49
agreement 0.380.61
Genetic100%

Open Targets aggregate 0.30 · 1 independent evidence family

DeliriumLimited support
0.45
agreement 0.290.60
Clinical86%Literature14%

Open Targets aggregate 0.35 · 2 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Alzheimer's Disease0.63
Parkinson's Disease0.61
Dementia0.61
Delirium0.35
Dementia, Vascular0.33
Brain Injuries0.33
Adverse effect0.30

Drug development

4 compounds recorded · 3 approved · 1 earlier-stage

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (4)
RIVASTIGMINEApproval
TACRINEApproval
PROPANIDIDUnknown
RIVASTIGMINE TARTRATEApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesEmerging

Feasibility evidence (uniprot loc high conf and go cc high conf) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (half-life data and small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (10)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · UniProt loc high confAB · GO CC high confAB · UniProt SigP or TMHMMPR · Half-life DataPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

apnea following administration of succinylcholineClinPGxapneaClinPGxpost anesthesia apneaClinPGxregulation of catalytic activityToxCast

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

SUSPENDED · via rivastigmine · NCT00102856

TERMINATED · via rivastigmine · NCT00102284

TERMINATED · via rivastigmine · NCT02374567

COMPLETED · via rivastigmine · NCT01073319

COMPLETED · via rivastigmine · NCT01030692

ClinicalTrials.gov via the drug-target graph.

What's happening now

6

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Regulatory approval2009-12-11

    Approval: Rivastigmine 1 A Pharma (EMA)

    ema · regulatory · ema · via rivastigmine

  2. Regulatory approval2009-12-11

    Approval: Rivastigmine Hexal (EMA)

    ema · regulatory · ema · via rivastigmine

  3. Regulatory approval2009-12-10

    Approval: Rivastigmine Sandoz (EMA)

    ema · regulatory · ema · via rivastigmine

  4. Regulatory approval2009-05-11

    Approval: Nimvastid (EMA)

    ema · regulatory · ema · via rivastigmine

  5. Regulatory approval1998-12-04

    Approval: Prometax (EMA)

    ema · regulatory · ema · via rivastigmine

  6. Regulatory approval1998-05-11

    Approval: Exelon (EMA)

    ema · regulatory · ema · via rivastigmine

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.

Research activity

3 papers · to 2024

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Recent

Europe PMC papers linked directly to this protein.