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Atlas / Drug / Diazepam

Diazepam

drug
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Also known as Alupram 10Alupram 2Alupram 5AnsiolisinaAtensineApozepamCentrazepamDiacepinDialarDialar fteDiastatDiastat acudialDiazepam civDiazepam intensolDizacE-pamLA IIILA-IIILibervant

Summary

Diazepam (CHEMBL12) is an approved small-molecule anxiolytic drug (ATC N05BA01) targeting TRHR, GABRA1, and GABRA2; indicated across 18 conditions including epilepsy and anxiety.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05BA01
  • Targets: 4 (TRHR, GABRA1, GABRA2…)
  • Indications: 18 conditions
  • Clinical trials: 56
  • Chemistry: 284.74 Da · C16H13ClN2O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL12
NameDiazepam
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3016
ChEBICHEBI:49575
ATCN05BA01
Molecular formulaC16H13ClN2O
Molecular weight284.74
InChIKeyAAOVKJBEBIDNHE-UHFFFAOYSA-N

SMILES: CN1C(=O)CN=C(C2=C1C=CC(=C2)Cl)C3=CC=CC=C3

IUPAC name: 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one

ChEBI definition: A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.

Pharmacological roles (ChEBI): anxiolytic drug, anticonvulsant, sedative.

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

Also known as: Alupram 10, Alupram 2, Alupram 5, Ansiolisina, Atensine, Apozepam, Centrazepam, Diacepin, Dialar, Dialar fte, Diastat, Diastat acudial

Parent form; salt/anhydrous children: CHEMBL543191

Patent coverage: 29,956 distinct patent families (92,281 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 92,038 (100%) 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
TRHRTRH1 receptorAntagonist5.150%P34981
GABRA1GABAA receptor α1 subunitPositive7.790%P14867
GABRA2GABAA receptor α2 subunitPositive7.770%P47869
GABRA3GABAA receptor α3 subunitPositive7.770%P34903

Broader ChEMBL bioactivity targets: 43 (assay-derived). Sample: GABA-A receptor; anion channel, Gamma-aminobutyric acid receptor subunit alpha-1, GABA-A receptor; anion channel, GABA-A receptor; anion channel, GABA-A receptor; alpha-3/beta-3/gamma-2, GABA-A receptor; alpha-1/beta-3/gamma-2, GABA-A receptor; alpha-5/beta-3/gamma-2, GABA-A receptor; alpha-2/beta-3/gamma-2, GABA-A receptor; anion channel, GABA-A receptor; alpha-1/beta-2/gamma-2.

Bioactivity

ChEMBL activities: 160 potent at pChembl ≥ 5 of 170 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P305359.05Ki0.9nMCHEMBL_ACT_24863110
P185088.68Ki2.1nMCHEMBL_ACT_320295
O090288.54Ki2.9nMCHEMBL_ACT_466921
O090288.54Ki2.9nMCHEMBL_ACT_874022
O090288.4IC504nMCHEMBL_ACT_1302881
GABRP8.38IC504.2nMCHEMBL_ACT_25013383
O090288.36IC504.4nMCHEMBL_ACT_1106447
O090288.31IC504.9nMCHEMBL_ACT_1001855
O090288.31Ki4.9nMCHEMBL_ACT_1145117
O090288.31Ki4.9nMCHEMBL_ACT_1161711
O090288.31Ki4.9nMCHEMBL_ACT_351488
O090288.31Ki4.9nMCHEMBL_ACT_701710
O090288.31IC504.9nMCHEMBL_ACT_988889
O090288.3Ki5.02nMCHEMBL_ACT_139849
O090288.3Ki5nMCHEMBL_ACT_457807
O090288.3Ki5.02nMCHEMBL_ACT_501148
O090288.3IC505nMCHEMBL_ACT_507139
O090288.3Ki5nMCHEMBL_ACT_534900
P235748.3IC505nMCHEMBL_ACT_694101
O090288.3Ki5.02nMCHEMBL_ACT_927815
O090288.3IC505nMCHEMBL_ACT_930272
O090288.27IC505.4nMCHEMBL_ACT_372154
O090288.27IC505.4nMCHEMBL_ACT_422598
O090288.27IC505.4nMCHEMBL_ACT_922098
O090288.25Ki5.62nMCHEMBL_ACT_29089169
O090288.25IC505.6nMCHEMBL_ACT_992373
O090288.22Ki6nMCHEMBL_ACT_1039765
O090288.22IC506nMCHEMBL_ACT_116266
O090288.22IC506nMCHEMBL_ACT_1296375
O090288.22IC506nMCHEMBL_ACT_357786

Target pathways

Aggregated over 4 target gene(s): TRHR, GABRA1, GABRA2, GABRA3.

Top Reactome pathways

4 total, by targets touching each:

PathwayTargetsGenes
GABA receptor activation3GABRA1, GABRA2, GABRA3
Signaling by ERBB41GABRA1
Peptide ligand-binding receptors1TRHR
G alpha (q) signalling events1TRHR

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
G protein-coupled receptor signaling pathway1
phospholipase C-activating G protein-coupled receptor signaling pathway1
signal transduction1
regulation of presynaptic membrane potential1

Indications & clinical

Indications

18 indications (6 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
epilepsy4MONDO:0005027EFO:0000474
anxiety4MONDO:0011918EFO:0005230
cerebral palsy4MONDO:0006497EFO:1000632
anxiety disorder4MONDO:0005618EFO:0006788
stiff-person syndrome4MONDO:0008491EFO:0007498
visual epilepsy3MONDO:0001386HP:0001250
dementia3MONDO:0001627HP:0000726
complex partial epilepsy3MONDO:0006710EFO:1000877
depressive disorder3MONDO:0002050MONDO:0002050
Landau-Kleffner syndrome2MONDO:0009509EFO:1001010
injury2MONDO:0021178EFO:0000546
rotator cuff syndrome2MONDO:0007028EFO:1001250

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

Clinical trials

Total trials: 56.

Phase distribution

PhaseTrials
Not specified16
PHASE415
PHASE26
PHASE35
PHASE2/PHASE35
PHASE14
EARLY_PHASE14
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02078336PHASE4ACTIVE_NOT_RECRUITINGOptimization of Procedural Sedation Protocol Used for Dental Care Delivery in People With Mental Disability
NCT01221883PHASE4UNKNOWNPrevention of Posttraumatic Stress Disorder (PTSD) With Diazepam
NCT01675648PHASE4COMPLETEDLofexidine for Inpatient Opiate Detox in Singapore
NCT01939093PHASE4COMPLETEDTherapeutic Effect of Quetiapine on Methamphetamine-Induced Psychosis
NCT02177955PHASE4COMPLETEDComparative Study of Hemodynamic Changes Caused by Diazepam and Midazolam During Third Molar Surgery
NCT02494180PHASE4COMPLETEDA Non-inferiority Trial on Pain Relief During Oocyte Retrieval
NCT03293017PHASE4UNKNOWNBaclofen in Managing Acute Alcohol Withdrawal
NCT03631901PHASE4COMPLETEDComparison Between Melatonin and Diazepam for Prevention of Recurrent Simple Febrile Seizures
NCT03960671PHASE4UNKNOWNTherapeutic Drug Monitoring of Anxiolytics in Children
NCT04198233PHASE4UNKNOWNImpact of Placement of a Diazepam Suppository on Early Postoperative Pain Following Pelvic Reconstructive Surgery
NCT04216797PHASE4WITHDRAWNRectal Versus Oral Diazepam Administration in the Treatment of Levator Ani Syndrome
NCT04523935PHASE4COMPLETEDExcessive Crying in Children With Cerebral Palsy and Communication Deficits
NCT04570436PHASE4COMPLETEDEvaluating the Abuse Potential of NEURONTIN® When Taken Orally in Healthy Non-drug Dependent Participants With Sedative Drug Abuse Experience
NCT05041985PHASE4COMPLETEDClinical Efficacy of Diazepam After Whiplash
NCT05273398PHASE4COMPLETEDEffects of Diazepam on RNS Detections
NCT03825809PHASE2/PHASE3RECRUITINGNonopioid Analgesia After Labral Surgery
NCT00004297PHASE3COMPLETEDPhase III Randomized Study of Diazepam Vs Lorazepam Vs Placebo for Prehospital Treatment of Status Epilepticus
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT02646124PHASE2/PHASE3COMPLETEDDiazepam Use With Standard Management for Acute Low Back Pain
NCT02721069PHASE3COMPLETEDRepeat Dose Safety Study of NRL-1 in Epilepsy Subjects
NCT02904265PHASE2/PHASE3TERMINATEDEfficacy Study of Acetazolamide Versus Diazepam in Continuous Spike and Wave/Landau-Kleffner Syndrome
NCT02935972PHASE2/PHASE3COMPLETEDCombined Intravenous Diazepam, Local Periprostatic Nerve Block for Prostate Biopsy
NCT03818932PHASE2/PHASE3COMPLETEDNonopioid Analgesia After Anterior Cruciate Ligament Reconstruction
NCT06103188PHASE3COMPLETEDComparing the Effect of Melatonin, Diazepam, and Placebo on Decreasing the Level of Anxiety Preoperatively
NCT06293989PHASE3UNKNOWNEfficacy and Safety of Intravenous Diazepam Given at 2 Different Doses Compared to Placebo in Acute Peripheral Vertigo
NCT00326612PHASE2COMPLETEDIntranasal Midazolam Versus Rectal Diazepam for Treatment of Seizures
NCT01318369PHASE2COMPLETEDEfficacy Study of Δ9-THC to Treat Chronic Abdominal Pain
NCT01417078PHASE2COMPLETEDA Pharmacokinetic Study of a Single-Dose of Diazepam Nasal Spray in Adult Epileptic Patients Experiencing a Seizure Episode
NCT01790555PHASE2UNKNOWNPerioperative Δ9-THC for Postsurgical Pain
NCT01938092PHASE2COMPLETEDVaginal Diazepam for the Treatment of Female Pelvic Pain
NCT03818919PHASE2COMPLETEDNonopioid Analgesia After Rotator Cuff Repair
NCT05361447PHASE1/PHASE2WITHDRAWNDiazepam Trial in GAD65 Associated Epilepsy
NCT01364558PHASE1COMPLETEDA Study of Diazepam After Intranasal and Intravenous Administration to Healthy Volunteers
NCT01438749PHASE1COMPLETEDA Study of The Abuse Liability Potential of RO4917838 in Recreational Drug Users
NCT02724423PHASE1COMPLETEDRepeat-Dose Pharmacokinetics Study of NRL-1 in Epilepsy Subjects
NCT07020988PHASE1COMPLETEDA Study to Assess the Time to Onset of Action of Staccato Alprazolam Versus Midazolam and Diazepam in Healthy Participants
NCT03165500EARLY_PHASE1COMPLETEDComparative Evaluation of Three Anxiety Control Protocols in Third Molar Extraction
NCT03820193EARLY_PHASE1COMPLETEDNonopioid Analgesia After Arthroscopic Meniscus Surgery
NCT05069779EARLY_PHASE1COMPLETEDDiazepam and Blood Pressure Regulation
NCT06271096EARLY_PHASE1COMPLETEDIntramuscular Midazolam Versus Intravenous Diazepam for Acute Seizure in Children

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 17 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.

76 molecules share ≥1 primary target. Top 60 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
CLONAZEPAMChEMBLPhase 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

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
v1.1.2
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