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Atlas / Drug / Triazolam

Triazolam

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Also known as HalcionKentionN05CD05Triazolam civU-33,030U-33030SID50113071SID144206170

Summary

Triazolam (CHEMBL646) is an approved small-molecule sedative (ATC N05CD05) targeting GABRA1, GABRA2, and GABRA3; indicated across 6 conditions including insomnia and anxiety.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05CD05
  • Targets: 4 (GABRA1, GABRA2, GABRA3…)
  • Indications: 6 conditions
  • Clinical trials: 9
  • Chemistry: 343.2 Da · C17H12Cl2N4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL646
NameTriazolam
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID5556
ChEBICHEBI:9674
ATCN05CD05
Molecular formulaC17H12Cl2N4
Molecular weight343.2
InChIKeyJOFWLTCLBGQGBO-UHFFFAOYSA-N

SMILES: CC1=NN=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4Cl

IUPAC name: 8-chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine

Pharmacological roles (ChEBI): sedative.

Also known as: Halcion, Kention, N05CD05, Triazolam, Triazolam civ, U-33,030, U-33030, triazolam, SID50113071, TRIAZOLAM, SID144206170

Patent coverage: 5,626 distinct patent families (21,589 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 21,447 (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 subunitPositive90%P14867
GABRA2GABAA receptor α2 subunitPositive9.230%P47869
GABRA3GABAA receptor α3 subunitPositive8.840%P34903
GABRA5GABAA receptor α5 subunitPositive8.40.9%P31644

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Nuclear receptor ROR-gamma, GABA-A receptor; anion channel, Gamma-aminobutyric acid receptor subunit alpha-1, 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, 5-hydroxytryptamine receptor 2A, Alpha-1A adrenergic receptor, Kappa-type opioid receptor.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
GABRG29.23Ki0.59nMCHEMBL_ACT_599587
GABRA19.1Ki0.8nMCHEMBL_ACT_599586
O090289.1Ki0.8nMCHEMBL_ACT_684273
GABRA19Kd1nMCHEMBL_ACT_2461330
P628138.96AC501.1nMCHEMBL_ACT_25131171
GABRG28.85Ki1.43nMCHEMBL_ACT_599588
GABRG28.81Ki1.54nMCHEMBL_ACT_599589
GABRA58.4Kd4nMCHEMBL_ACT_2461351
P514506.1Potency794.3nMCHEMBL_ACT_4814933
OPRK15.76AC501716nMCHEMBL_ACT_25129971
O090285.68Ki2086nMCHEMBL_ACT_684274
HTR2A5.5AC503195nMCHEMBL_ACT_25173810

Target pathways

Aggregated over 4 target gene(s): GABRA1, GABRA2, GABRA3, GABRA5.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
GABA receptor activation4GABRA1, GABRA2, GABRA3, GABRA5
Signaling by ERBB41GABRA1

Dominant GO biological processes

GO termTargets
gamma-aminobutyric acid signaling pathway4
synaptic transmission, GABAergic4
chloride transmembrane transport4
inhibitory synapse assembly4
monoatomic ion transport4
chloride transport4
monoatomic ion transmembrane transport4
regulation of postsynaptic membrane potential4
regulation of presynaptic membrane potential2
behavioral fear response1
signal transduction1
associative learning1
inner ear receptor cell development1
innervation1
cochlea development1

Indications & clinical

Indications

6 indications (1 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
insomnia4MONDO:0013600EFO:0004698
anxiety3MONDO:0011918EFO:0005230
dementia3MONDO:0001627HP:0000726
depressive disorder3MONDO:0002050MONDO:0002050
drug dependence2MONDO:0005303EFO:0003890

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

Clinical trials

Total trials: 9.

Phase distribution

PhaseTrials
PHASE14
PHASE32
Not specified2
PHASE41

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03246724PHASE4COMPLETEDOral Versus Intravenous Sedation for Ocular Procedures
NCT01888497PHASE3COMPLETEDNext-Day Residual Effects of Gabapentin, Diphenhydramine and Triazolam on Simulated Driving Performance in Normal Volunteers
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT01017926PHASE1WITHDRAWNTriazolam Trial In Healthy Subjects To Compare Bioavailability Between Formulations Of Triazolam To Determine Their Bioequivalence In Terms Of Rate And Magnitude Of Absorption
NCT01421043PHASE1COMPLETEDA Study to Determine Whether an Oral Drops Formulation of Triazolam is Bioequivalent to a Tablet Formulation in Healthy Subjects
NCT01780259PHASE1COMPLETEDA Study to Assess the Pharmacokinetics, Safety, and Tolerability of Intranasally Administered Esketamine in Healthy Participants
NCT06837142PHASE1COMPLETEDA Drug-drug Interaction Study With TS-172 in Healthy Adult Male Subjects
NCT02822937Not specifiedCOMPLETEDSensitivity of Project: EVO Monitor Cognitive Measurements to Pharmacological Agents
NCT03360123Not specifiedCOMPLETEDComparison of Triazolam and Midazolam for Anxiolysis During Dental Treatment in the Pediatric Patient

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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 60 by shared-target count:

MoleculeSourceStatusShared targets
ALPRAZOLAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
APALUTAMIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
BREXANOLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
CHLORDIAZEPOXIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
CLONAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
DIAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
ENZALUTAMIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
FLUMAZENILChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
FLUNITRAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
GANAXOLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
LIOTHYRONINEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
PROPOFOLChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
ALFAXALONEChEMBL + PubChemPhase 2 (approved)GABRA1, GABRA2, GABRA3, GABRA5
ABECARNILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
AZD7325ChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
BAICALEINChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
BASMISANILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
BRETAZENILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
DELORAZEPAMChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
FLAVONEChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
MK-0777ChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
PROGABIDEChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
ESZOPICLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
ZOLPIDEMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
DARIGABATChEMBLPhase 2GABRA1, GABRA3, GABRA5
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
PANADIPLONChEMBLPhase 2GABRA1, GABRA3
SARIPIDEMChEMBLPhase 2GABRA1, GABRA5
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

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