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Midazolam

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Also known as Midazolam civMidazolam in 0.8% sodium chlorideMidazolam in 0.9% sodium chlorideNayzilamUSL-261USL261SID50113067[3H]-Midazolam

Summary

Midazolam (CHEMBL655) is an approved small-molecule GABAA receptor agonist (ATC N05CD08) targeting ADRA1B and TRHR; indicated across 115 conditions including epilepsy and hypertensive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05CD08
  • Targets: 2 (ADRA1B, TRHR)
  • Indications: 115 conditions
  • Clinical trials: 943
  • Chemistry: 325.8 Da · C18H13ClFN3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL655
NameMidazolam
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID4192
ChEBICHEBI:6931
ATCN05CD08
Molecular formulaC18H13ClFN3
Molecular weight325.8
InChIKeyDDLIGBOFAVUZHB-UHFFFAOYSA-N

SMILES: CC1=NC=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4F

IUPAC name: 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine

ChEBI definition: An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.

Pharmacological roles (ChEBI): GABAA receptor agonist, anticonvulsant, anxiolytic drug, apoptosis inducer, antineoplastic agent, muscle relaxant, sedative, general anaesthetic, central nervous system depressant.

Also known as: Midazolam, Midazolam civ, Midazolam in 0.8% sodium chloride, Midazolam in 0.9% sodium chloride, Nayzilam, USL-261, USL261, midazolam, SID50113067, [3H]-Midazolam, MIDAZOLAM

Parent form; salt/anhydrous children: CHEMBL1200420, CHEMBL2106922

Patent coverage: 8,732 distinct patent families (32,889 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 32,504 (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
ADRA1Bα1B-adrenoceptorPositive3.70%P35368
TRHRTRH1 receptorAntagonist5.490%P34981

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: GABA-A receptor; anion channel, D(3) dopamine receptor, Kappa-type opioid receptor, 3’,5’-cyclic-AMP phosphodiesterase 4D, Cytochrome P450 3A4, Gamma-aminobutyric acid receptor subunit alpha-1, ATP-dependent translocase ABCB1, Translocator protein, Solute carrier family 22 member 1, Bile salt export pump.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
P162578.7Ki2nMCHEMBL_ACT_371260
O090288.7Ki2nMCHEMBL_ACT_520131
P628138.6AC502.5nMCHEMBL_ACT_25131168
CYP3A47.33IC5047nMCHEMBL_ACT_26109725
CYP3A47.21IC5061.8nMCHEMBL_ACT_24740415
CYP3A47.18IC5066.2nMCHEMBL_ACT_24822376
CYP3A47.18IC5066nMCHEMBL_ACT_25593413
CYP3A47.1IC5080nMCHEMBL_ACT_25502139
OPRK15.92AC501192nMCHEMBL_ACT_25129968
CYP3A45.61Ki2470nMCHEMBL_ACT_15152431
SLC22A15.43Ki3700nMCHEMBL_ACT_11002867
CYP3A45.09IC508100nMCHEMBL_ACT_1160708
PDE4D5AC5010000nMCHEMBL_ACT_25185923
DRD35AC5010000nMCHEMBL_ACT_25194109

Target pathways

Aggregated over 2 target gene(s): ADRA1B, TRHR.

Top Reactome pathways

10 total, by targets touching each:

PathwayTargetsGenes
G alpha (q) signalling events2ADRA1B, TRHR
Signal Transduction1ADRA1B
Signaling by GPCR1ADRA1B
Class A/1 (Rhodopsin-like receptors)1ADRA1B
Peptide ligand-binding receptors1TRHR
Amine ligand-binding receptors1ADRA1B
GPCR downstream signalling1ADRA1B
Adrenoceptors1ADRA1B
G alpha (12/13) signalling events1ADRA1B
GPCR ligand binding1ADRA1B

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway2
phospholipase C-activating G protein-coupled receptor signaling pathway2
signal transduction2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway1
positive regulation of cytosolic calcium ion concentration1
cell-cell signaling1
positive regulation of cardiac muscle hypertrophy1
regulation of vasoconstriction1
intracellular signal transduction1
positive regulation of MAPK cascade1
regulation of cardiac muscle contraction1
adenylate cyclase-activating adrenergic receptor signaling pathway1
neuron-glial cell signaling1
regulation of muscle contraction1
adrenergic receptor signaling pathway1

Indications & clinical

Indications

115 indications (2 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
hypertensive disorder3MONDO:0005044EFO:0000537
injury3MONDO:0021178EFO:0000546
cirrhosis of liver3MONDO:0005155EFO:0001422
relapsing-remitting multiple sclerosis3MONDO:0005314EFO:0003929
bone fracture3MONDO:0005315EFO:0003931
anxiety3MONDO:0011918EFO:0005230
toxic shock syndrome3MONDO:0001881EFO:0006834
dementia3MONDO:0001627HP:0000726
delirium3MONDO:0045057EFO:0009267
respiratory failure3MONDO:0021113EFO:0009686
infertility disorder3MONDO:0005047EFO:0000545
depressive disorder3MONDO:0002050MONDO:0002050
brain injury3MONDO:0043510MONDO:0043510
lung disorder3MONDO:0005275EFO:0003818
subarachnoid hemorrhage2MONDO:0005099EFO:0000713
post-traumatic stress disorder2MONDO:0005146EFO:0001358
breast neoplasm2MONDO:0021100EFO:0003869
obsessive-compulsive disorder2MONDO:0008114EFO:0004242
hypotensive disorder2MONDO:0005468EFO:0005251
visual epilepsy2MONDO:0001386HP:0001250
borderline personality disorder2MONDO:0001156HP:0012076
pulmonary tuberculosis2MONDO:0006052EFO:1000049
major depressive disorder2MONDO:0002009MONDO:0002009
cataract2MONDO:0005129MONDO:0005129
bipolar disorder2MONDO:0004985MONDO:0004985
complex regional pain syndrome2MONDO:0019369EFO:1001998
tonsillitis2MONDO:0001039MONDO:0001039
B-cell chronic lymphocytic leukemia1MONDO:0004948EFO:0000095
atopic eczema1MONDO:0004980EFO:0000274
Crohn disease1MONDO:0005011EFO:0000384
mesothelioma1MONDO:0005065EFO:0000588
neoplasm1MONDO:0005070EFO:0000616
prostate adenocarcinoma1MONDO:0005082EFO:0000673
psoriasis1MONDO:0005083EFO:0000676
rheumatoid arthritis1MONDO:0008383EFO:0000685
skin disorder1MONDO:0005093EFO:0000701
HIV infectious disease1MONDO:0005109EFO:0000764
endometriosis1MONDO:0005133EFO:0001065
plasma cell myeloma1MONDO:0009693EFO:0001378
cocaine dependence1MONDO:0005186EFO:0002610
hepatitis C virus infection1MONDO:0005231EFO:0003047
non-small cell lung carcinoma1MONDO:0005233EFO:0003060
heart failure1MONDO:0005252EFO:0003144
postmenopausal osteoporosis1MONDO:0008159EFO:0003854
drug dependence1MONDO:0005303EFO:0003890
atherosclerosis1MONDO:0005311EFO:0003914
chronic hepatitis C virus infection1MONDO:0005354EFO:0004220
chronic hepatitis B virus infection1MONDO:0005366EFO:0004239
anemia1MONDO:0002280EFO:0004272
schizoaffective disorder1MONDO:0005487EFO:0005411
infectious disease1MONDO:0005550EFO:0005741
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
aspergillosis1MONDO:0005657EFO:0007157
metabolic dysfunction-associated steatohepatitis1MONDO:0007027EFO:1001249
acute myeloid leukemia1MONDO:0018874EFO:0000222
metastatic melanoma1MONDO:0005191EFO:0002617
nicotine dependence1MONDO:0008575EFO:0003768
respiratory syncytial virus infectious disease1MONDO:0001577EFO:1001413
influenza1MONDO:0005812EFO:0007328
kidney failure1MONDO:0001106HP:0000083
cardiovascular disorder1MONDO:0004995EFO:0000319
ulcerative colitis1MONDO:0005101EFO:0000729
obesity disorder1MONDO:0011122EFO:0001073
malaria1MONDO:0005136EFO:0001068
Alzheimer disease1MONDO:0004975MONDO:0004975
amyotrophic lateral sclerosis1MONDO:0004976MONDO:0004976
type 2 diabetes mellitus1MONDO:0005148MONDO:0005148
Parkinson disease1MONDO:0005180MONDO:0005180
myositis ossificans1MONDO:0003964MONDO:0007606
sickle cell disease1MONDO:0011382MONDO:0011382
gastrointestinal stromal tumor1MONDO:0011719MONDO:0011719
tuberculosis1MONDO:0018076MONDO:0018076
inborn mitochondrial metabolism disorder1MONDO:0004069MONDO:0044970
severe acute respiratory syndrome1MONDO:0005091MONDO:0100096
melanoma1MONDO:0005105EFO:0000756
urinary tract infection1MONDO:0100338EFO:0003103
trypanosomiasis1MONDO:0000940DOID:10113
chronic obstructive pulmonary disease1MONDO:0005002EFO:0000341
anti-neutrophil antibody associated vasculitis1MONDO:0005435EFO:0004826
burn1MONDO:0043519EFO:0009516
autosomal dominant polycystic kidney disease1MONDO:0004691EFO:1001496
cystic fibrosis1MONDO:0009061MONDO:0009061
spinal muscular atrophy1MONDO:0001516MONDO:0019079
lung neoplasm1MONDO:0021117MONDO:0021117
neuralgia0MONDO:0021667EFO:0005762

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

Clinical trials

Total trials: 943.

Phase distribution

PhaseTrials
PHASE1352
PHASE4215
Not specified181
PHASE373
PHASE257
PHASE2/PHASE324
PHASE1/PHASE223
EARLY_PHASE118

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00577200PHASE4ACTIVE_NOT_RECRUITINGSafety of Driving After Minor Surgery With Monitored Anesthesia Care
NCT02078336PHASE4ACTIVE_NOT_RECRUITINGOptimization of Procedural Sedation Protocol Used for Dental Care Delivery in People With Mental Disability
NCT04119180PHASE4RECRUITINGSedation Versus Protective Stabilization for Pediatric Dental Treatment
NCT04669457PHASE4ENROLLING_BY_INVITATIONPediatric Delirium
NCT05602636PHASE4RECRUITINGAnalgesic Effect of Supraclavicular Block and Interscalene Analgesia Versus an Intercostobrachial Nerve Block Versus PCA in Forearm Surgery
NCT05934669PHASE4RECRUITINGIN Midazolam vs IN Dexmedetomidine vs IN Ketamine During Minimal Procedures in Pediatric ED
NCT05980117PHASE4RECRUITINGRemimazolam for Cataract Surgery
NCT06139692PHASE4RECRUITINGComparison of Perioperative Conscious Sedation During Endovascular Thrombectomy in Acute Ischemic Stroke
NCT06144177PHASE4RECRUITINGInduction in the Dark
NCT06614036PHASE4RECRUITINGRemimazolam Versus Midazolam for Sedation During Upper GI Endoscopy: a Randomized Controlled Trial
NCT06731088PHASE4ENROLLING_BY_INVITATIONEffect of Remazolam Besylate Combined With Remifentanil Analgesic Sedation on the Prognosis of Patients With Sepsis
NCT06736938PHASE4NOT_YET_RECRUITINGBalanced Analgosedation in Bronchoscopy: Propofol/Pethidine Versus Midazolam/Pethidine
NCT06763705PHASE4RECRUITINGComparison of Safety and Efficacy for Different Sedation Regimens During Colonoscopy
NCT06784479PHASE4ACTIVE_NOT_RECRUITINGCombination of Remimazolam and Propofol During Drug-induced Sleep Endoscopy
NCT06934811PHASE4NOT_YET_RECRUITINGCiprofol’s Impact on Oxygenator Function in Extracorporeal Membrane Oxygenation (ECMO) Patients
NCT07177235PHASE4NOT_YET_RECRUITINGKetamine for the Treatment of Refractory Status Epilepticus
NCT07190612PHASE4NOT_YET_RECRUITINGEfficacy of Propofol Combination With Either Ketamine, Dexmedetomidine or Midazolam for Sedation During Upper Gastrointestinal Endoscopic Procedures
NCT07265128PHASE4NOT_YET_RECRUITINGRemimazolam vs Midazolam to Reduce Delirium in Adults ≥65 Undergoing CPB Valve Surgery
NCT07300826PHASE4NOT_YET_RECRUITINGIntravenous Dexmedetomidine Versus Midazolam in Preventing Shivering in Trauma Patients Undergoing Lower Limb Orthopedic Surgery Under Spinal Anesthesia
NCT07425444PHASE4NOT_YET_RECRUITINGAttenuate the Stress Response in Laparoscopic Cholecystectomy
NCT07427446PHASE4RECRUITINGDexmedetomidine-Midazolam vs. Ketamine-Midazolam on Emergence Delirium
NCT07556523PHASE4RECRUITINGPatient Quality of Recovery After TAVR With Different Sedation Regimens
NCT00050180PHASE4COMPLETEDInfluence of the MDR1 Genotype on Blood Levels of Indinavir and Saquinavir in Healthy Volunteers
NCT00158873PHASE4COMPLETEDPharmaco-Economic Study Of Ultiva In Intensive Care Unit(ICU)Subjects
NCT00188227PHASE4COMPLETEDComparison of Three Different Pain and Anxiety Reducing Methods in Adult Patients Undergoing Bone Marrow Puncture
NCT00216190PHASE4COMPLETEDA Safety and Efficacy Study of Dexmedetomidine in ICU Patients Requiring Continuous Sedation
NCT00333632PHASE4WITHDRAWNEffect of Dexmedetomidine Upon Sleep Postoperatively
NCT00376831PHASE4COMPLETEDThe Efficacy of Midazolam & Ketamine Versus Midazolam & Fentanyl for Sedation in Ambulatory Colonoscopies
NCT00440960PHASE4COMPLETEDAnesthesia in Flexible Bronchoscopy for Lung Cancer Diagnostic
NCT00446420PHASE4COMPLETEDCognitive Impairment Following Sedation for Colonoscopy With Propofol, Midazolam and Fentanyl Combinations
NCT00596050PHASE4COMPLETEDKetamine Versus Etomidate for Procedural Sedation for Pediatric Orthopedic Reductions
NCT00596414PHASE4COMPLETEDSedation and Analgesia for Transjugular Liver Biopsy: A Randomized Double Blind Placebo Controlled Trial
NCT00636428PHASE4COMPLETEDClinical Trial of Oral Midazolam in Pediatric Endoscopy
NCT00667043PHASE4COMPLETEDRemifentanil and Propofol Versus Fentanyl and Midazolam for Sedation During Therapeutic Hypothermia. A Randomised, Controlled Trial
NCT00724035PHASE4COMPLETEDUltrasound-Guided Axillary or Infraclavicular Nerve Block for Upper Limb Surgery
NCT00784498PHASE4COMPLETEDProcedural Sedation Using Propofol Versus Midazolam/Ketamine in the Adult Emergency Department
NCT00789386PHASE4UNKNOWNThe Effect of Remifentanil on Established Capsaicin-Induced Hyperalgesia in Human Volunteers
NCT00808184PHASE4COMPLETEDPharmacokinetic Study of CPT-11, Raltegravir and Midazolam With Characterisation of UGT1A1 Genotype
NCT00811837PHASE4UNKNOWNThe Effect of Remifentanil on Established Sunburn-induced Hyperalgesia in Human Volunteers
NCT00839371PHASE4COMPLETEDBronchoscopy and Bispectral Index (BIS) - Guided Sedation

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 7 clinical and 30 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.

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

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRA1B
PROTIRELINChEMBL + PubChemPhase 4 (approved)TRHR
ALFUZOSINChEMBLPhase 4 (approved)ADRA1B
AMLODIPINEChEMBLPhase 4 (approved)ADRA1B
APRACLONIDINEChEMBLPhase 4 (approved)ADRA1B
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRA1B
ASENAPINEChEMBLPhase 4 (approved)ADRA1B
ATENOLOLChEMBLPhase 4 (approved)ADRA1B
AZELASTINEChEMBLPhase 4 (approved)ADRA1B
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRA1B
BRIMONIDINEChEMBLPhase 4 (approved)ADRA1B
BUSPIRONEChEMBLPhase 4 (approved)ADRA1B
CARIPRAZINEChEMBLPhase 4 (approved)ADRA1B
CINACALCETChEMBLPhase 4 (approved)ADRA1B
CISAPRIDEChEMBLPhase 4 (approved)ADRA1B
CLONIDINEChEMBLPhase 4 (approved)ADRA1B
CLOZAPINEChEMBLPhase 4 (approved)ADRA1B
DEXMEDETOMIDINEChEMBLPhase 4 (approved)ADRA1B
DOPAMINEChEMBLPhase 4 (approved)ADRA1B
DOXAZOSINChEMBLPhase 4 (approved)ADRA1B
EBASTINEChEMBLPhase 4 (approved)ADRA1B
EPINEPHRINEChEMBLPhase 4 (approved)ADRA1B
FENOLDOPAMChEMBLPhase 4 (approved)ADRA1B
FENTANYLChEMBLPhase 4 (approved)ADRA1B
HALOPERIDOLChEMBLPhase 4 (approved)ADRA1B
INDACATEROLChEMBLPhase 4 (approved)ADRA1B
INDORAMINChEMBLPhase 4 (approved)ADRA1B
ISOPROTERENOLChEMBLPhase 4 (approved)ADRA1B
LABETALOLChEMBLPhase 4 (approved)ADRA1B
LOPERAMIDEChEMBLPhase 4 (approved)ADRA1B
LUMATEPERONE TOSYLATEChEMBLPhase 4 (approved)ADRA1B
MOXISYLYTEChEMBLPhase 4 (approved)ADRA1B
NAFTOPIDILChEMBLPhase 4 (approved)ADRA1B
NEFAZODONEChEMBLPhase 4 (approved)ADRA1B
NOREPINEPHRINEChEMBLPhase 4 (approved)ADRA1B
OLANZAPINEChEMBLPhase 4 (approved)ADRA1B
OXYMETAZOLINEChEMBLPhase 4 (approved)ADRA1B
PHENTOLAMINEChEMBLPhase 4 (approved)ADRA1B
PHENYLEPHRINEChEMBLPhase 4 (approved)ADRA1B
PRAZOSINChEMBLPhase 4 (approved)ADRA1B
QUETIAPINEChEMBLPhase 4 (approved)ADRA1B
RISPERIDONEChEMBLPhase 4 (approved)ADRA1B
SERTINDOLEChEMBLPhase 4 (approved)ADRA1B
SILODOSINChEMBLPhase 4 (approved)ADRA1B
TAMSULOSINChEMBLPhase 4 (approved)ADRA1B
TEGASERODChEMBLPhase 4 (approved)ADRA1B
TERAZOSINChEMBLPhase 4 (approved)ADRA1B
TERFENADINEChEMBLPhase 4 (approved)ADRA1B
TOLAZOLINEChEMBLPhase 4 (approved)ADRA1B
VERAPAMILChEMBLPhase 4 (approved)ADRA1B
VILAZODONEChEMBLPhase 4 (approved)ADRA1B
XYLOMETAZOLINEChEMBLPhase 4 (approved)ADRA1B
ZIPRASIDONEChEMBLPhase 4 (approved)ADRA1B
BUNAZOSINChEMBLPhase 3ADRA1B
IDAZOXANChEMBLPhase 3ADRA1B
LATREPIRDINEChEMBLPhase 3ADRA1B
MEDETOMIDINEChEMBLPhase 3ADRA1B
VOLINANSERINChEMBLPhase 3ADRA1B
YOHIMBINEChEMBLPhase 3ADRA1B
ABANOQUILChEMBLPhase 2ADRA1B

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