Etidocaine

drug
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Also known as EtidocainaW-19053 FREE BASEW-19053 [AS HYDROCHLORIDE]SID144206521

Summary

Etidocaine (CHEMBL492) is an approved small-molecule local anaesthetic (ATC N01BB57) targeting SCN2A.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N01BB57 (+1 more)
  • Targets: 1 (SCN2A)
  • Chemistry: 276.4 Da · C17H28N2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL492
NameEtidocaine
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID37497
ChEBICHEBI:4904
ATCN01BB57, N01BB07
Molecular formulaC17H28N2O
Molecular weight276.4
InChIKeyVTUSIVBDOCDNHS-UHFFFAOYSA-N

SMILES: CCCN(CC)C(CC)C(=O)NC1=C(C=CC=C1C)C

IUPAC name: N-(2,6-dimethylphenyl)-2-[ethyl(propyl)amino]butanamide

ChEBI definition: An amino acid amide in which 2-[ethyl(propyl)amino]butanoic acid and 2,6-dimethylaniline have combined to form the amide bond. Used as a local anaesthetic (amide caine), it has rapid onset and long action properties, similar to bupivacaine, and is given by injection during surgical procedures and during labour and delivery.

Pharmacological roles (ChEBI): local anaesthetic.

Also known as: Etidocaina, Etidocaine, W-19053 FREE BASE, W-19053 [AS HYDROCHLORIDE], ETIDOCAINE, SID144206521, etidocaine

Parent form; salt/anhydrous children: CHEMBL1200597

Patent coverage: 3,105 distinct patent families (11,778 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
SCN2ANav1.2Pore blocker60.1%Q99250

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Sodium channel protein type 5 subunit alpha, Sodium channel alpha subunits; brain (Types I, II, III), Potassium channel subfamily K member 3.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
SCN1A5.46IC503500nMCHEMBL_ACT_346931

Target pathways

Aggregated over 1 target gene(s): SCN2A.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Developmental Biology1SCN2A
L1CAM interactions1SCN2A
Muscle contraction1SCN2A
Axon guidance1SCN2A
Interaction between L1 and Ankyrins1SCN2A
Cardiac conduction1SCN2A
Phase 0 - rapid depolarisation1SCN2A
Nervous system development1SCN2A
Sensory Perception1SCN2A
Sensory perception of taste1SCN2A
Sensory perception of sweet, bitter, and umami (glutamate) taste1SCN2A

Dominant GO biological processes

GO termTargets
sodium ion transport1
nervous system development1
memory1
intrinsic apoptotic signaling pathway in response to osmotic stress1
neuronal action potential1
sodium ion transmembrane transport1
myelination1
neuron apoptotic process1
cellular response to hypoxia1
cardiac muscle cell action potential involved in contraction1
action potential1
regulation of heart rate1
monoatomic ion transport1
monoatomic ion transmembrane transport1
regulation of membrane potential1

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 0.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

134 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
AMIODARONEChEMBL + PubChemPhase 4 (approved)SCN2A
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)SCN2A
BROMPHENIRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
CHLORPHENIRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
COCAINEChEMBL + PubChemPhase 4 (approved)SCN2A
CYPROHEPTADINEChEMBL + PubChemPhase 4 (approved)SCN2A
DESIPRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
DIBUCAINEChEMBL + PubChemPhase 4 (approved)SCN2A
DICYCLOMINEChEMBL + PubChemPhase 4 (approved)SCN2A
DILTIAZEMChEMBL + PubChemPhase 4 (approved)SCN2A
DIPHENHYDRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
DROPERIDOLChEMBL + PubChemPhase 4 (approved)SCN2A
FELODIPINEChEMBL + PubChemPhase 4 (approved)SCN2A
FLUPHENAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
HALOPERIDOLChEMBL + PubChemPhase 4 (approved)SCN2A
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
LAMOTRIGINEChEMBL + PubChemPhase 4 (approved)SCN2A
LEVORPHANOLChEMBL + PubChemPhase 4 (approved)SCN2A
LOPERAMIDEChEMBL + PubChemPhase 4 (approved)SCN2A
MEXILETINEChEMBL + PubChemPhase 4 (approved)SCN2A
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)SCN2A
NISOLDIPINEChEMBL + PubChemPhase 4 (approved)SCN2A
PHENOXYBENZAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
PHENTOLAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
PHENYTOINChEMBL + PubChemPhase 4 (approved)SCN2A
PIMOZIDEChEMBL + PubChemPhase 4 (approved)SCN2A
PRAMOXINEChEMBL + PubChemPhase 4 (approved)SCN2A
PRAZOSINChEMBL + PubChemPhase 4 (approved)SCN2A
PRILOCAINEChEMBL + PubChemPhase 4 (approved)SCN2A
PROMETHAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
PROPARACAINEChEMBL + PubChemPhase 4 (approved)SCN2A
QUINIDINEChEMBL + PubChemPhase 4 (approved)SCN2A
QUININEChEMBL + PubChemPhase 4 (approved)SCN2A
RESERPINEChEMBL + PubChemPhase 4 (approved)SCN2A
TETRABENAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
TETRACAINEChEMBL + PubChemPhase 4 (approved)SCN2A
THIORIDAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
TRIFLUOPERAZINEChEMBL + PubChemPhase 4 (approved)SCN2A
VERAPAMILChEMBL + PubChemPhase 4 (approved)SCN2A
ARTICAINEChEMBLPhase 4 (approved)SCN2A
BENOXINATEChEMBLPhase 4 (approved)SCN2A
BEPRIDILChEMBLPhase 4 (approved)SCN2A
BUPIVACAINEChEMBLPhase 4 (approved)SCN2A
CINNARIZINEChEMBLPhase 4 (approved)SCN2A
DIPHENIDOLChEMBLPhase 4 (approved)SCN2A
HEXYLCAINEChEMBLPhase 4 (approved)SCN2A
MIANSERINChEMBLPhase 4 (approved)SCN2A
MIBEFRADILChEMBLPhase 4 (approved)SCN2A
PHENIRAMINEChEMBLPhase 4 (approved)SCN2A
PRENYLAMINEChEMBLPhase 4 (approved)SCN2A
PROMAZINEChEMBLPhase 4 (approved)SCN2A
PROPOXYCAINEChEMBLPhase 4 (approved)SCN2A
QUINACRINEChEMBLPhase 4 (approved)SCN2A
RILUZOLEChEMBLPhase 4 (approved)SCN2A
SERTINDOLEChEMBLPhase 4 (approved)SCN2A
YOHIMBINEChEMBL + PubChemPhase 3 (approved)SCN2A
AJMALINEChEMBLPhase 3SCN2A
ELECLAZINEChEMBLPhase 3SCN2A
NITRENDIPINEChEMBLPhase 3SCN2A