Lidocaine

drug
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Also known as ALGRX 3268ALGRX-3268AlphacaineDentipatchEmbolexIontocaineLidocainaLidocaine component of emlaLidocaine component of fortacinLidocaine component of lanabioticLidocaine component of oraqixLidocaine component of pliaglisLidocaine component of rocephin kitLidocaine component of syneraLidocainumLidodermLmx 4Lignocaine hclNSC-40030

Summary

Lidocaine (CHEMBL79) is an approved small-molecule local anaesthetic (ATC R02AD02) targeting SCN2A, SCN4A, and SCN5A; indicated across 121 conditions including neuralgia and disease of the tendon.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: R02AD02 (+7 more)
  • Targets: 5 (SCN2A, SCN4A, SCN5A…)
  • Indications: 121 conditions
  • Clinical trials: 1,084
  • Chemistry: 234.34 Da · C14H22N2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL79
NameLidocaine
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3676
ChEBICHEBI:6456
ATCR02AD02, D04AB01, N01BB02, S01HA07, C01BB01, N01BB52, S02DA01, C05AD01
Molecular formulaC14H22N2O
Molecular weight234.34
InChIKeyNNJVILVZKWQKPM-UHFFFAOYSA-N

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

IUPAC name: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide

ChEBI definition: The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.

Pharmacological roles (ChEBI): local anaesthetic, anti-arrhythmia drug, drug allergen.

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: ALGRX 3268, ALGRX-3268, Alphacaine, Dentipatch, Embolex, Iontocaine, Lidocaina, Lidocaine, Lidocaine component of emla, Lidocaine component of fortacin, Lidocaine component of lanabiotic, Lidocaine component of oraqix

Parent form; salt/anhydrous children: CHEMBL541521, CHEMBL1200409, CHEMBL3278065

Patent coverage: 41,033 distinct patent families (140,673 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 blocker50.1%Q99250
SCN4ANav1.4Pore blocker2.70%P35499
SCN5ANav1.5Pore blocker4.80.2%Q14524
SCN9ANav1.7Pore blocker3.30%Q15858
SCN10ANav1.8Pore blocker40.1%Q9Y5Y9

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Microtubule-associated protein tau, Prelamin-A/C, 5-hydroxytryptamine receptor 3A, Sodium channel protein type 5 subunit alpha, Beta-lactamase, Sodium channel protein type 4 subunit alpha, Sodium channel alpha subunits; brain (Types I, II, III), Melanocortin receptor 4, Muscarinic acetylcholine receptor M1, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 18 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P008116.45Potency354.8nMCHEMBL_ACT_4676386
ALDH1A16.05Potency891.3nMCHEMBL_ACT_4148909
SCN4A5.7IC502000nMCHEMBL_ACT_13905714
CYP3A45.7Potency1995nMCHEMBL_ACT_5006349
CYP3A45.7Potency1995nMCHEMBL_ACT_5074856

Target pathways

Aggregated over 5 target gene(s): SCN2A, SCN4A, SCN5A, SCN9A, SCN10A.

Top Reactome pathways

11 total, by targets touching each:

PathwayTargetsGenes
Developmental Biology5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
L1CAM interactions5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Muscle contraction5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Axon guidance5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Interaction between L1 and Ankyrins5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Cardiac conduction5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Phase 0 - rapid depolarisation5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Nervous system development5SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
Sensory Perception2SCN2A, SCN9A
Sensory perception of taste2SCN2A, SCN9A
Sensory perception of sweet, bitter, and umami (glutamate) taste2SCN2A, SCN9A

Dominant GO biological processes

GO termTargets
sodium ion transport5
sodium ion transmembrane transport5
cardiac muscle cell action potential involved in contraction5
monoatomic ion transport5
monoatomic ion transmembrane transport5
transmembrane transport5
regulation of heart rate4
monoatomic cation transmembrane transport4
action potential3
neuronal action potential2
regulation of membrane potential2
cardiac muscle cell action potential2
regulation of muscle system process2
odontogenesis of dentin-containing tooth2
regulation of atrial cardiac muscle cell membrane depolarization2

Indications & clinical

Indications

121 indications (24 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
neuralgia4MONDO:0021667EFO:0005762
disease of the tendon4MONDO:0100010EFO:1001434
frozen shoulder4MONDO:0006763EFO:1000941
arthritic joint disease4MONDO:0005578EFO:0005856
hemorrhoid4MONDO:0004872EFO:0009552
rectal disorder4MONDO:0001593EFO:0000405
urethritis4MONDO:0005297EFO:0003878
sunburn4MONDO:0005326EFO:0003958
burn4MONDO:0043519EFO:0009516
osteoarthritis4MONDO:0005178MONDO:0005178
premature ejaculation4MONDO:0001780EFO:0803321
osteoarthritis, knee3MONDO:0005416EFO:0004616
peripheral neuropathy3MONDO:0005244EFO:0003100
breast carcinoma3MONDO:0004989EFO:0000305
carpal tunnel syndrome3MONDO:0007275EFO:0004143
fibromyalgia3MONDO:0005546EFO:0005687
parathyroid gland disorder3MONDO:0001223EFO:0005754
preeclampsia3MONDO:0005081EFO:0000668
postmenopausal osteoporosis3MONDO:0008159EFO:0003854
obesity disorder3MONDO:0011122EFO:0001073
stroke disorder3MONDO:0005098EFO:0000712
nutritional disorder3MONDO:0005137EFO:0001069
overactive bladder3MONDO:0006624EFO:1000781
pulpitis3MONDO:0006937EFO:1001139
injury3MONDO:0021178EFO:0000546
morbid obesity3MONDO:0005139EFO:0001074
muscle tissue disorder3MONDO:0003939EFO:0002970
colorectal neoplasm3MONDO:0005335EFO:0004142
common cold3MONDO:0005709EFO:0007214
sinusitis3MONDO:0005961EFO:0007486
extramammary Paget disease3MONDO:0008177EFO:1000249
dysplasia of cervix3MONDO:0006736EFO:1000910
scoliosis3MONDO:0005392EFO:0004273
toxic shock syndrome3MONDO:0001881EFO:0006834
cardiac arrest3MONDO:0000745EFO:0009492
stomatitis3MONDO:0004842EFO:0009688
periarthritis3MONDO:0006898EFO:1001097
epicondylitis3MONDO:0001875EFO:1001887
pharyngitis3MONDO:0002258MONDO:0002258
breast neoplasm3MONDO:0021100MONDO:0007254
ileus3MONDO:0004567MONDO:0004567
migraine disorder3MONDO:0005277MONDO:0005277
bone fracture3MONDO:0005315EFO:0003931
pain agnosia3MONDO:0000675EFO:1001484
carcinoma2MONDO:0004993EFO:0000313
urinary tract infection2MONDO:0100338EFO:0003103
anxiety2MONDO:0011918EFO:0005230
cocaine dependence2MONDO:0005186EFO:0002610
infertility disorder2MONDO:0005047EFO:0000545
irritable bowel syndrome2MONDO:0005052EFO:0000555
heart disorder2MONDO:0005267EFO:0003777
myofascial pain syndrome2MONDO:0006862EFO:1001054
shoulder impingement syndrome2MONDO:0006968EFO:1001178
scleroderma2MONDO:0019340EFO:1001993
interstitial cystitis2MONDO:0018301EFO:0008507
diabetic neuropathy2MONDO:0006626EFO:1000783
trigeminal neuralgia2MONDO:0008599EFO:1001219
humerus fracture2MONDO:0005319EFO:0003943
leiomyoma2MONDO:0001572MONDO:0001572
neoplasm2MONDO:0005070EFO:0000616
skin disorder2MONDO:0005093EFO:0000701
temporomandibular joint disorder2MONDO:0005473EFO:0005279
anus disorder2MONDO:0002519EFO:0009660
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
spasmodic dystonia2MONDO:0000485MONDO:0000485
pulmonary arterial hypertension1MONDO:0015924EFO:0001361
squamous cell carcinoma1MONDO:0005096EFO:0000707
actinic keratosis1MONDO:0005173EFO:0002496
brain neoplasm1MONDO:0021211EFO:0003833
neuroma1MONDO:0002173EFO:0009619
lung neoplasm1MONDO:0021117MONDO:0008903
glioblastoma1MONDO:0018177EFO:0000519
cystic, mucinous, and serous neoplasm1MONDO:0006720EFO:1000889
attention deficit-hyperactivity disorder0MONDO:0007743EFO:0003888
complex regional pain syndrome0MONDO:0019369EFO:1001998
spinal fracture0MONDO:0005309EFO:0003902
skin neoplasm0MONDO:0002531EFO:0004198
parathyroid gland adenoma0MONDO:0006890EFO:1001087
radius fracture0MONDO:0005325EFO:0003957
severe cutaneous adverse reaction0MONDO:0005594EFO:0006346

41 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 1,084.

Phase distribution

PhaseTrials
Not specified419
PHASE4328
PHASE3123
PHASE281
PHASE146
PHASE2/PHASE333
EARLY_PHASE130
PHASE1/PHASE224

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03968822PHASE4ACTIVE_NOT_RECRUITINGIntralipid® 20% for Reversal of Local Anesthetics
NCT04781673PHASE4ACTIVE_NOT_RECRUITINGKetamine vs Lidocaine in Traumatic Rib Fractures
NCT05031078PHASE4ACTIVE_NOT_RECRUITINGAssessing Durable Antibody Response to HPV Vaccination
NCT05285566PHASE4RECRUITINGPain Control for Undergoing Costal Cartilage Harvesting
NCT06024733PHASE4ACTIVE_NOT_RECRUITINGIntravenous Anesthesia by Targeted Controlled Infusion Versus Inhalational Anesthesia on the Surgical Stress Response
NCT06045936PHASE4RECRUITINGA Study of Contralateral Limb Block
NCT06189781PHASE4RECRUITINGPain Injection Versus Epidural Anesthesia for Hip Surgery in Pediatric Patients With Cerebral Palsy
NCT06695585PHASE4NOT_YET_RECRUITINGOptimal Intravesical Lidocaine Volume for Pain Relief During Office Intra-detrusor Onabotulinum Toxin a Injections
NCT06710405PHASE4RECRUITINGThe Effect of Intraoperative Intravenous Lidocaine Infusion on Postoperative Pain and Recovery in Children (< 7 Years Old) Undergoing Thoracoscopic Surgery
NCT06795100PHASE4RECRUITINGPharmacokinetic Study of Intravenous Lidocaine in Young and Elderly Patients
NCT06799494PHASE4RECRUITINGHPV Vaccine Reduced Dose
NCT06918340PHASE4ACTIVE_NOT_RECRUITINGEvaluation of Analgesic Efficacy of Lidocaine and Diclofenac Spray in Radial Artery Blood Gas Sampling by Visual Analogue Scale and Perfusion Index
NCT06966102PHASE4NOT_YET_RECRUITINGLidocaine Infusion Versus Magnesium Infusion in Decreasing Fentanyl Requirements in Endoscopic Sinus Surgeries
NCT07034300PHASE4RECRUITINGLidocaine vs. Lidocaine With Dexmedetomidine for Intravenous Regional Anesthesia (IVRA) in Upper Limb Surgery
NCT07043023PHASE4NOT_YET_RECRUITINGLIDOCRIT : Effect of Continuous Intravenous LIDOcaine on Discomfort in Postoperative CRITical Care Inpatients
NCT07048769PHASE4RECRUITINGParacervical Block for Pain Reduction in Saline Infusion Sonograms
NCT07053176PHASE4ENROLLING_BY_INVITATIONImpact of Local Lidocaine Paravertebral Cervical Injection on Cervicogenic Dizziness Symptoms
NCT07073846PHASE4RECRUITINGEffect of Lidocaine-Dexmedetomidine on Pain, Inflammation, and Oxidative Stress After Bariatric Surgery.
NCT07116408PHASE4RECRUITINGIntranasal Sphenopalatine Ganglion Blockade for Headaches Following Aneurysmal Subarachnoid Hemorrhage
NCT07124650PHASE4RECRUITINGSore Throat After Open Neck Elective Surgery
NCT07154628PHASE4NOT_YET_RECRUITINGEffect of Topical Lidocaine Spraying on the Vocal Cords Before Intubation During Robotic Surgery: a Randomized Controlled Trial
NCT07169227PHASE4NOT_YET_RECRUITINGLidocaine, Paracetamol, and Dexmedetomidine for Rocuronium Injection Pain
NCT07224711PHASE4NOT_YET_RECRUITINGThe Impact of Perioperative Lidocaine Infusions on Enhanced Recovery After Non-Cardiac Surgery
NCT07231614PHASE4NOT_YET_RECRUITINGAnesthetic Effectiveness of Lidocaine Versus Articaine in Dentistry
NCT07259772PHASE4ACTIVE_NOT_RECRUITINGAnesthetic Effect of Ropivacaine on Local Infiltration Anesthesia in Arteriovenous Fistula Surgery
NCT07268924PHASE4NOT_YET_RECRUITINGThe Effect of Propofol Versus Lidocaine on Emergence Agitation in Children Undergoing Tonsillectomy.
NCT07283874PHASE4NOT_YET_RECRUITINGDoes it Matter the Volume of Injectate on the Outcome of Ultrasound-guided Perineural Injection for Carpal Tunnel Syndrome
NCT07354217PHASE4NOT_YET_RECRUITINGWorkflow Optimization During Pulse Field Ablation for Atrial Fibrillation
NCT07401745PHASE4ACTIVE_NOT_RECRUITINGOcclusal Splint Combined With Granisetron Injection for Management of Myofascial Pain Related to Temporomandibular Disorders
NCT07423650PHASE4RECRUITINGContinous Infusion of Nefopam for Patients Undergoing Pancreatoduodenectomy
NCT07429292PHASE4NOT_YET_RECRUITINGSPARK Study - Sympathetic Periarterial Radial Block in Healthy Volunteers
NCT07430085PHASE4NOT_YET_RECRUITINGPost-Operative Pain Relief: Zynrelef or Periarticular Injections in RATKA
NCT07456826PHASE4ENROLLING_BY_INVITATIONStudy Evaluating the Efficacy and Safety of Chloroprocaine HCl Ophthalmic Gel 3% vs Proparacaine Ophthalmic Solution 0.5% Plus Subconjunctival Lidocaine in Patients Undergoing Intravitreal Injections
NCT07499154PHASE4NOT_YET_RECRUITINGPerioperative Lidocaine for Lung Protection in Infants Undergoing Cardiac Surgery
NCT07546370PHASE4NOT_YET_RECRUITINGThe Effectiveness of Topical Prilocaine-Lidocaine Cream Plus Acetaminophen and Naproxen Compared to Lidocaine Injection Plus Acetaminophen and Naproxen to Manage Pain During IntraUterine Device Insertion
NCT07552766PHASE4NOT_YET_RECRUITINGA Clinical Trial on the Use of Lidocaine Infusion During Surgery for Pediatric Upper Extremity Fractures and Its Impact on Total Perioperative Opioid Requirements
NCT07601750PHASE4ENROLLING_BY_INVITATIONLocal Anesthetic Clinical Trial
NCT00209872PHASE4UNKNOWNOptimal Multimodal Analgesia in Abdominal Hysterectomy
NCT00209885PHASE4UNKNOWNOptimal Multimodal Analgesia in Laparoscopic Cholecystectomy
NCT00330941PHASE4COMPLETEDIntravenous Lidocaine and Acute Rehabilitation

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
AMIODARONEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
CHLORPROMAZINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
DILTIAZEMChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
HALOPERIDOLChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
LAMOTRIGINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
MEXILETINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
PIMOZIDEChEMBL + PubChemPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
MIBEFRADILChEMBLPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
SERTINDOLEChEMBLPhase 4 (approved)SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
AJMALINEChEMBLPhase 3SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
ELECLAZINEChEMBLPhase 3SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
NITRENDIPINEChEMBLPhase 3SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
TEDISAMILChEMBLPhase 3SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
VIXOTRIGINEChEMBLPhase 3SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
CIFENLINEChEMBLPhase 2SCN10A, SCN2A, SCN4A, SCN5A, SCN9A
CarbamazepineChEMBL + PubChemPhase 4 (approved)SCN2A, SCN4A, SCN5A, SCN9A
RILUZOLEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN4A, SCN5A, SCN9A
TETRODOTOXINChEMBLPhase 3SCN2A, SCN4A, SCN5A, SCN9A
FUNAPIDEChEMBLPhase 2SCN10A, SCN2A, SCN5A, SCN9A
PF-05089771ChEMBLPhase 2SCN2A, SCN4A, SCN5A, SCN9A
PHENYTOINChEMBL + PubChemPhase 4 (approved)SCN2A, SCN4A, SCN5A
TETRACAINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A, SCN9A
DS-1971ChEMBLPhase 2SCN2A, SCN5A, SCN9A
PF-04531083ChEMBLPhase 2SCN10A, SCN5A, SCN9A
DofetilidePubChemApprovedSCN10A, SCN2A, SCN4A
DESIPRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
DIBUCAINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
DIPHENHYDRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
DROPERIDOLChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
FELODIPINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
FLUPHENAZINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
LOPERAMIDEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
NISOLDIPINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
QUINIDINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
THIORIDAZINEChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
VERAPAMILChEMBL + PubChemPhase 4 (approved)SCN2A, SCN5A
BEPRIDILChEMBLPhase 4 (approved)SCN2A, SCN5A
ETIDOCAINEChEMBLPhase 4 (approved)SCN2A, SCN5A
PRENYLAMINEChEMBLPhase 4 (approved)SCN2A, SCN5A
MEPRYLCAINEChEMBLPhase 2SCN2A, SCN5A
BROMPHENIRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
CHLORPHENIRAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
COCAINEChEMBL + PubChemPhase 4 (approved)SCN2A
CYPROHEPTADINEChEMBL + PubChemPhase 4 (approved)SCN2A
DICYCLOMINEChEMBL + PubChemPhase 4 (approved)SCN2A
LEVORPHANOLChEMBL + PubChemPhase 4 (approved)SCN2A
PALIPERIDONEChEMBL + PubChemPhase 4 (approved)SCN5A
PHENOXYBENZAMINEChEMBL + PubChemPhase 4 (approved)SCN2A
PHENTOLAMINEChEMBL + 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
QUININEChEMBL + PubChemPhase 4 (approved)SCN2A
RESERPINEChEMBL + PubChemPhase 4 (approved)SCN2A
SAFINAMIDEChEMBL + PubChemPhase 4 (approved)SCN9A