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Atlas / Drug / Clonazepam

Clonazepam

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Also known as Clonazepam civKlonopinKlonopin rapidly disintegratingNSC-179913RavotrilRivatrilRivotrilRO-54023

Summary

Clonazepam (CHEMBL452) is an approved small-molecule anticonvulsant (ATC N03AE01) targeting GABRA1, GABRA2, and GABRA3; indicated across 15 conditions including epilepsy and panic disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N03AE01
  • Targets: 3 (GABRA1, GABRA2, GABRA3)
  • Indications: 15 conditions
  • Clinical trials: 34
  • Chemistry: 315.71 Da · C15H10ClN3O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL452
NameClonazepam
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2802
ChEBICHEBI:3756
ATCN03AE01
Molecular formulaC15H10ClN3O3
Molecular weight315.71
InChIKeyDGBIGWXXNGSACT-UHFFFAOYSA-N

SMILES: C1C(=O)NC2=C(C=C(C=C2)[N+](=O)[O-])C(=N1)C3=CC=CC=C3Cl

IUPAC name: 5-(2-chlorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one

ChEBI definition: 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.

Pharmacological roles (ChEBI): anticonvulsant, GABA modulator, anxiolytic drug.

Also known as: Clonazepam, Clonazepam civ, Klonopin, Klonopin rapidly disintegrating, NSC-179913, Ravotril, Rivatril, Rivotril, RO-54023, CLONAZEPAM, clonazepam

Patent coverage: 8,724 distinct patent families (33,297 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 33,086 (99%) of the total. 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
GABRA1GABAA receptor α1 subunitPositive8.90%P14867
GABRA2GABAA receptor α2 subunitPositive8.770%P47869
GABRA3GABAA receptor α3 subunitPositive8.70%P34903

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: GABA-A receptor; anion channel, GABA-A receptor; anion channel, GABA-A receptor; anion channel, Alpha-1A adrenergic receptor, Translocator protein, Gamma-aminobutyric acid receptor subunit alpha-1.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 9 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
GABRP9.07Ki0.85nMCHEMBL_ACT_1505241
P305359.07Ki0.85nMCHEMBL_ACT_24863111
P082199.07Ki0.85nMCHEMBL_ACT_878696
P082199.07Ki0.85nMCHEMBL_ACT_942060
P082199.07Ki0.85nMCHEMBL_ACT_960283
O090288.77IC501.7nMCHEMBL_ACT_1016962
O090288.77IC501.7nMCHEMBL_ACT_995663
P628138.6AC502.5nMCHEMBL_ACT_25131041

Target pathways

Aggregated over 3 target gene(s): GABRA1, GABRA2, GABRA3.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
GABA receptor activation3GABRA1, GABRA2, GABRA3
Signaling by ERBB41GABRA1

Dominant GO biological processes

GO termTargets
gamma-aminobutyric acid signaling pathway3
synaptic transmission, GABAergic3
chloride transmembrane transport3
inhibitory synapse assembly3
monoatomic ion transport3
chloride transport3
monoatomic ion transmembrane transport3
regulation of postsynaptic membrane potential3
regulation of presynaptic membrane potential1

Indications & clinical

Indications

3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
epilepsy4MONDO:0005027EFO:0000474
panic disorder4MONDO:0005383EFO:0004262
visual epilepsy4MONDO:0001386HP:0001250

7 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
anxiety3MONDO:0011918EFO:0005230
dementia3MONDO:0001627HP:0000726
epilepsy with generalized tonic-clonic seizures3MONDO:0005754EFO:0007262
depressive disorder3MONDO:0002050MONDO:0002050
REM sleep behavior disorder2MONDO:0005937EFO:0007462
cannabis dependence2MONDO:0005689EFO:0007191
neuralgia1MONDO:0021667EFO:0005762

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

Clinical trials

Total trials: 34.

Phase distribution

PhaseTrials
PHASE410
Not specified7
PHASE35
PHASE25
PHASE14
PHASE2/PHASE31
PHASE1/PHASE21
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06040190PHASE4RECRUITINGEffect of Treatments on Pain and Quality of Life in Individual With Burning Mouth Syndrome
NCT06133114PHASE4RECRUITINGPsychopharmacological Treatment of Emotional Distress
NCT07313371PHASE4RECRUITINGEfficacy of Clonidine in Reducing Craving in Inpatients With Cocaine and Crack Use Disorder
NCT00025740PHASE4COMPLETEDClonazepam and Paroxetine for Rapid Treatment of Post-Traumatic Stress Disorder
NCT00282828PHASE4COMPLETEDImproving Treatment Outcomes in Pharmacotherapy of Generalized Social Anxiety Disorder
NCT02690844PHASE4WITHDRAWNEffectiveness of Mucolox® and Clonazepam in Treatment of Burning Mouth Syndrome
NCT02852577PHASE4COMPLETEDLong Term Treatment of Panic Disorder With Clonazepam or Paroxetine
NCT03061136PHASE4WITHDRAWNClonazepam Effects on Brain Oscillations and Cognition in Schizophrenia
NCT04523935PHASE4COMPLETEDExcessive Crying in Children With Cerebral Palsy and Communication Deficits
NCT06357104PHASE4COMPLETEDDetoxification From the Lipid Tract
NCT00118417PHASE2/PHASE3COMPLETEDTherapies for Treatment-Resistant Panic Disorder Symptoms
NCT01011036PHASE3COMPLETEDEffects of GABA-a-Agonists on Pain Mechanisms: An Experimental Study in Healthy Volunteers
NCT01150331PHASE3COMPLETEDStudy of Antiepileptic Drug in Generalised Convulsive Status Epilepticus
NCT01870024PHASE3COMPLETEDComparison Between Lorazepam, Clonazepam and Clonazepam + Fosphenytoin for the Treatment of Out-of-hospital Generalized Status Epilepticus
NCT02134366PHASE3TERMINATEDClobazam Use in Epilepsia Partialis Continua - Pilot Study
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT00594945PHASE2COMPLETEDStudy of Intranasal Clonazepam in Adult Subjects With Epileptic Seizures
NCT01291316PHASE1/PHASE2COMPLETEDGABAergic Modulation in Pain Transmission in Human: Effect of the GABAA Agonist Clobazam on Peripheral and Central Sensitisation
NCT02312908PHASE2COMPLETEDEffect of Clonazepam on REM Sleep Behavior Disorder in Patients With Parkinsonism
NCT02789592PHASE2UNKNOWNEfficacy and Safety of Melatonin PR and Clonazepam in Patients With REM Sleep Behavior Disorder in Parkinson Disease
NCT02913924PHASE2COMPLETEDEffect of Clonazepam on Cannabis Withdrawal and Relapse in Treatment-seeking Patients
NCT04884503PHASE2COMPLETEDEvaluation of the Effectiveness of the Selected Method of Treatment of Primary Burning Mouth Syndrome
NCT00652639PHASE1COMPLETEDBioavailability Study of Clonazepam Tablets Under Fasting Conditions
NCT00652912PHASE1COMPLETEDBioavailability Study of Clonazepam ODT Under Fasting Conditions
NCT00810316PHASE1COMPLETEDEvaluate Pharmacokinetics Of Two Different Pharmaceutical Oral Formulations Of Alprazolam And A Clonazepam Tablet In Mexican Healthy Population
NCT03375034PHASE1COMPLETEDExploring the Role of the GABAergic Modulation in Pain Transmission in Human
NCT02382029EARLY_PHASE1COMPLETEDAcupuncture Versus Clonazepam in Burning Mouth Syndrome
NCT06056349Not specifiedRECRUITINGBenzodiazepine Study for the Treatment of Seizure Clusters in a Third Level Mexican Neurological Center
NCT06611202Not specifiedNOT_YET_RECRUITINGEnhancing Mobility and Mental Health in Dementia Patients
NCT07498387Not specifiedACTIVE_NOT_RECRUITINGManagement of Catatonic Features in Adolescents With Profound Autism
NCT03255642Not specifiedCOMPLETEDEfficacy and Safety of Melatonin and Clonazepam for IRBD
NCT04364321Not specifiedUNKNOWNSingle Dose of Clonazepam Versus Intermiittent Diazepam for Febrile Seizures Prevention
NCT05059418Not specifiedUNKNOWNBurning Mouth Syndrome - New Diagnostic Criteria and Treatment
NCT06217731Not specifiedCOMPLETEDInflammatory Markers in Saliva of Patients With Burning Mouth Syndrome

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 1 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.

75 molecules share ≥1 primary target. Top 75 by shared-target count:

MoleculeSourceStatusShared targets
ALPRAZOLAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
APALUTAMIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
BREXANOLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
CHLORDIAZEPOXIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
DIAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
ENZALUTAMIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
ESZOPICLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
FLUMAZENILChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
FLUNITRAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
GANAXOLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
LIOTHYRONINEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
PROPOFOLChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
TRIAZOLAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
ZOLPIDEMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
ALFAXALONEChEMBL + PubChemPhase 2 (approved)GABRA1, GABRA2, GABRA3
ABECARNILChEMBLPhase 2GABRA1, GABRA2, GABRA3
AZD7325ChEMBLPhase 2GABRA1, GABRA2, GABRA3
BAICALEINChEMBLPhase 2GABRA1, GABRA2, GABRA3
BASMISANILChEMBLPhase 2GABRA1, GABRA2, GABRA3
BRETAZENILChEMBLPhase 2GABRA1, GABRA2, GABRA3
DELORAZEPAMChEMBLPhase 2GABRA1, GABRA2, GABRA3
FLAVONEChEMBLPhase 2GABRA1, GABRA2, GABRA3
MK-0777ChEMBLPhase 2GABRA1, GABRA2, GABRA3
PROGABIDEChEMBLPhase 2GABRA1, GABRA2, GABRA3
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2
ASENAPINEChEMBLPhase 4 (approved)GABRA1, GABRA2
AZELASTINEChEMBLPhase 4 (approved)GABRA1, GABRA2
BENPERIDOLChEMBLPhase 4 (approved)GABRA1, GABRA2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)GABRA1, GABRA2
CHLORAMBUCILChEMBLPhase 4 (approved)GABRA1, GABRA2
CLOZAPINEChEMBLPhase 4 (approved)GABRA1, GABRA2
EPINASTINEChEMBLPhase 4 (approved)GABRA1, GABRA2
ETOMIDATEChEMBLPhase 4 (approved)GABRA1, GABRA2
GLAFENINEChEMBLPhase 4 (approved)GABRA1, GABRA2
SIMVASTATINChEMBLPhase 4 (approved)GABRA1, GABRA2
TIPRANAVIRChEMBLPhase 4 (approved)GABRA1, GABRA2
TROGLITAZONEChEMBLPhase 4 (approved)GABRA1, GABRA2
ZALEPLONChEMBLPhase 4 (approved)GABRA1, GABRA2
SURAMINChEMBLPhase 3GABRA1, GABRA2
TIRATRICOLChEMBLPhase 3GABRA1, GABRA2
DARIGABATChEMBLPhase 2GABRA1, GABRA3
PANADIPLONChEMBLPhase 2GABRA1, GABRA3
ZOTEPINEChEMBLPhase 2GABRA1, GABRA2
AfatinibPubChemApprovedGABRA1, GABRA2
ApixabanPubChemApprovedGABRA1, GABRA2
BinimetinibPubChemApprovedGABRA1, GABRA2
chenodiolPubChemApprovedGABRA1, GABRA2
FulvestrantPubChemApprovedGABRA1, GABRA2
gentian violetPubChemApprovedGABRA1, GABRA2
ImipenemPubChemApprovedGABRA1, GABRA2
LactulosePubChemApprovedGABRA1, GABRA2
levocarnitinePubChemApprovedGABRA1, GABRA2
podofiloxPubChemApprovedGABRA1, GABRA2
Propylene GlycolPubChemApprovedGABRA1, GABRA2
PyrazinamidePubChemApprovedGABRA1, GABRA2
PyridoxinePubChemApprovedGABRA1, GABRA2
RiociguatPubChemApprovedGABRA1, GABRA2
saxagliptinPubChemApprovedGABRA1, GABRA2
ThiaminePubChemApprovedGABRA1, GABRA2
VorapaxarPubChemApprovedGABRA1, GABRA2
LINDANEChEMBLPhase 4 (approved)GABRA1
PENTOBARBITALChEMBLPhase 4 (approved)GABRA2
STIRIPENTOLChEMBLPhase 4 (approved)GABRA1
ZURANOLONEChEMBLPhase 4 (approved)GABRA1
ALISERTIBChEMBLPhase 3GABRA1
GABOXADOLChEMBLPhase 3GABRA1
ALOGABATChEMBLPhase 2GABRA1
LORECLEZOLEChEMBLPhase 2GABRA1
PIPERINEChEMBLPhase 2GABRA1
REDAFAMDASTATChEMBLPhase 2GABRA1
SARIPIDEMChEMBLPhase 2GABRA1
ApremilastPubChemApprovedGABRA2
IdelalisibPubChemApprovedGABRA2
OlodaterolPubChemApprovedGABRA2
TavaborolePubChemApprovedGABRA2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot