OralParenteralTopicalDosed ingredientTherapeutic flag
Diazepam
CAS 439-14-5
Diazepam (CAS 439-14-5) is a Phase 4 pharmaceutical compound with 30 bioactivity targets and 6,594 adverse event associations.
SOURCE
NLM DailyMed
Label records
2
SOURCE
EMBL-EBI ChEMBL
Bioactivity
40
SOURCE
DrugCentral
Adverse signals
6,594
SOURCE
IUPHAR/BPS
PubMed IDs
6
SOURCE
EMBL-EBI ChEMBL
B25820EEF0F0
Compound Identity
Matched identifiers and naming fields for the pharmaceutical compound record.
Primary Name
Diazepam
CAS Number
439-14-5
UNII
Q3JTX2Q7TU
InChIKey
AAOVKJBEBIDNHE-UHFFFAOYSA-N
ChEMBL ID
CHEMBL12
Molecule Type
Small molecule
Source Match
EMBL-EBI ChEMBL (INCHIKEY)
Synonyms and normalized names
ValiumDiastat
black box warningdosed ingredientnatural productoralparenteraltherapeutic flagtopical
SOURCE
EMBL-EBI ChEMBL
B25820EEF0F0
Clinical Development Phase
Highest clinical development phase rendered from the matched compound identifier rows.
Phase 4 (Approved)
Approved or marketed human pharmaceutical use is represented in the source phase field.
ChEMBL CHEMBL12 | Small molecule
SOURCE
NLM DailyMed
2 label rows
Drug Label Active Ingredients
Active ingredient and active moiety rows from source drug product labels.
| Product | Ingredient | Active Moiety | Effective |
|---|---|---|---|
| Diazepam | DIAZEPAM Q3JTX2Q7TU |
DIAZEPAM | 20260505 |
| Diazepam | DIAZEPAM Q3JTX2Q7TU |
DIAZEPAM | 20260505 |
SOURCE
EMBL-EBI ChEMBL
40 bioactivity rows
Bioactivity & Target Interactions
Target-level activity records with assay counts, activity type, and measured value where present.
| Target | Activity | Value | Assays | Organism |
|---|---|---|---|---|
| - | Ki | 1539.8458461538462 nM | 127 | - |
| - | AC50 | 19613.059375 nM | 96 | - |
| - | IC50 | 8970.465395061728 nM | 79 | - |
| - | EC50 | 26492 nM | 13 | - |
| - | Kd | 6095.105 nM | 8 | - |
| - | Potency | 28580.300000000003 nM | 3 | - |
| Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel |
Kd | 7.64 | - | Homo sapiens |
| Cytochrome P450 3A4 Enzyme |
Ki | 4.42 | - | Homo sapiens |
| Alpha-1A adrenergic receptor GPCR |
Ki | 4.1 | - | Homo sapiens |
| Adenosine receptor A3 GPCR |
IC50 | 7.92 | - | Homo sapiens |
| Aldo-keto reductase family 1 member C1 Enzyme |
IC50 | 5.25 | - | Homo sapiens |
| Aldo-keto reductase family 1 member C2 Enzyme |
IC50 | 5.62 | - | Homo sapiens |
| Aldo-keto reductase family 1 member C3 Enzyme |
IC50 | 4.08 | - | Homo sapiens |
| Fatty acid-binding protein, liver Unclassified |
Ki | 6.27 | - | Rattus norvegicus |
| Acetylcholinesterase Enzyme |
Ki | 4.89 | - | Electrophorus electricus |
| Translocator protein Membrane receptor |
Kd | 6.67 | - | Rattus norvegicus |
| Thyrotropin-releasing hormone receptor GPCR |
Ki | 5.15 | - | Rattus norvegicus |
| Cholinesterase Enzyme |
Ki | 7.37 | - | Equus caballus |
| Gamma-aminobutyric acid receptor subunit alpha-1 Ion channel |
Ki | 7.96 | - | Rattus norvegicus |
| Gamma-aminobutyric acid receptor subunit alpha-2 Ion channel |
Ki | 7.82 | - | Rattus norvegicus |
| Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel |
Ki | 8.01 | - | Rattus norvegicus |
| GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel |
EC50 | 7.143 | - | Homo sapiens |
| GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel |
Ki | 7.699 | - | Homo sapiens |
| GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel |
Ki | 7.65 | - | Homo sapiens |
| GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel |
Ki | 7.959 | - | Homo sapiens |
| GABA-A receptor alpha-1/beta-2/gamma-3 Ion channel |
Ki | 6.705 | - | Homo sapiens |
| GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel |
Ki | 7.854 | - | Homo sapiens |
| GABA-A receptor; anion channel Ion channel |
Ki | 8.54 | - | Rattus norvegicus |
| GABA-A receptor; anion channel Ion channel |
Ki | 8 | - | Bos taurus |
| GABA A receptor alpha-3/beta-2/gamma-2 Ion channel |
Ki | 7.86 | - | Rattus norvegicus |
| GABA A receptor alpha-6/beta-2/gamma-2 Ion channel |
Ki | 8.68 | - | Rattus norvegicus |
| GABA-A receptor; alpha-1/beta-2/gamma-2 Ion channel |
Ki | 7.92 | - | Rattus norvegicus |
| GABA-A receptor; anion channel Ion channel |
Ki | 4.07 | - | Mus musculus |
| GABA A receptor alpha-2/beta-2/gamma-2 Ion channel |
Ki | 7.7 | - | Rattus norvegicus |
| GABA A receptor alpha-5/beta-3/gamma-2 Ion channel |
Ki | 7.96 | - | Rattus norvegicus |
| GABA A receptor alpha-3/beta-2/gamma-2 Ion channel |
Ki | 7.939 | - | Homo sapiens |
| GABA A receptor alpha-3/beta-2/gamma-3 Ion channel |
Ki | 6.665 | - | Homo sapiens |
| GABA A receptor alpha-5/beta-3/gamma-3 Ion channel |
Ki | 7.203 | - | Homo sapiens |
| GABA A receptor alpha-5/beta-2/gamma-2 Ion channel |
Ki | 8.004 | - | Homo sapiens |
| GABA A receptor alpha-5/beta-2/gamma-3 Ion channel |
Ki | 7.203 | - | Homo sapiens |
SOURCE
DrugCentral
80 associations
Adverse Event Associations
DrugCentral / FAERS disproportionality signal rows matched to this compound.
| Reaction PT | Drug AE | LLR | MedDRA |
|---|---|---|---|
| Drug abuse | 5114 | 7724.954 | 10013654 |
| Toxicity to various agents | 7397 | 7001.504 | 10070863 |
| Completed suicide | 3350 | 2786.734 | 10010144 |
| Intentional overdose | 2424 | 2751.413 | 10022523 |
| Coma | 2054 | 2149.288 | 10010071 |
| Suicide attempt | 1886 | 2036.023 | 10042464 |
| Overdose | 2739 | 2009.813 | 10033295 |
| Drug dependence | 1187 | 1551.261 | 10013663 |
| Respiratory arrest | 1262 | 1487.368 | 10038669 |
| Somnolence | 2787 | 1475.406 | 10041349 |
| Poisoning | 900 | 1458.401 | 10061355 |
| Intentional product misuse | 1377 | 1061.47 | 10074903 |
| Poisoning deliberate | 642 | 1019.48 | 10036000 |
| Respiratory depression | 744 | 949.372 | 10038678 |
| Drug withdrawal syndrome | 865 | 923.574 | 10013754 |
| Miosis | 565 | 900.832 | 10027646 |
| Intentional self-injury | 786 | 894.166 | 10022524 |
| Sopor | 720 | 855.938 | 10058709 |
| Depressed level of consciousness | 1214 | 836.167 | 10012373 |
| Agitation | 1270 | 804.346 | 10001497 |
| Cardiac arrest | 1635 | 786.081 | 10007515 |
| Suicidal ideation | 1154 | 770.605 | 10042458 |
| Cardio-respiratory arrest | 1212 | 739.063 | 10007617 |
| Aggression | 869 | 722.521 | 10001488 |
| Substance abuse | 426 | 681.301 | 10066169 |
| Drug interaction | 2761 | 669.325 | 10013710 |
| Exposure via father | 185 | 638.995 | 10071403 |
| Accidental overdose | 661 | 576.527 | 10000381 |
| Infusion related reaction | 119 | 550.704 | 10051792 |
| Pemphigus | 4 | 542.132 | 10034280 |
| Synovitis | 13 | 527.098 | 10042868 |
| Bradypnoea | 282 | 523.195 | 10006102 |
| Neuroleptic malignant syndrome | 517 | 521.911 | 10029282 |
| Rheumatoid arthritis | 113 | 507.153 | 10039073 |
| Withdrawal syndrome | 528 | 495.094 | 10048010 |
| Systemic lupus erythematosus | 45 | 475.753 | 10042945 |
| Joint swelling | 262 | 467.374 | 10023232 |
| Seizure | 1581 | 464.729 | 10039906 |
| Contraindicated product administered | 86 | 460.175 | 10078504 |
| Drug intolerance | 259 | 444.986 | 10061822 |
| Arthropathy | 115 | 433.054 | 10003285 |
| Psychotic disorder | 601 | 425.669 | 10061920 |
| Sedation | 672 | 419.375 | 10039897 |
| Glossodynia | 38 | 411.368 | 10018388 |
| Rash | 1000 | 400.225 | 10037844 |
| Arthralgia | 962 | 386.523 | 10003239 |
| Serotonin syndrome | 562 | 376.452 | 10040108 |
| Febrile neutropenia | 131 | 371.471 | 10016288 |
| Treatment failure | 135 | 370.372 | 10066901 |
| Schizophrenia | 345 | 369.35 | 10039626 |
Association rows are source-linked signal records, not incidence rates or clinical causality claims.
SOURCE
IUPHAR/BPS
4 interactions
IUPHAR Ligand-Target Data
Curated ligand-target interaction rows with action, affinity, and literature identifiers.
| Target | Action | Affinity | PubMed |
|---|---|---|---|
| GABA A receptor α1 subunit GABRA1 |
Positive | 7.789999961853027 pKi | 2551039 |
| GABA A receptor α2 subunit GABRA2 |
Positive | 7.769999980926514 pKi | 2551039 |
| GABA A receptor α3 subunit GABRA3 |
Positive | 7.769999980926514 pKi | 2551039 |
| TRH 1 receptor Trhr |
Antagonist | 5.15 pKi | 2566295 |
SOURCE
PharmGKB
6 phenotype rows
Pharmacogenomics
Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.
CYP2C9 (PA126) CYP2C9*1, CYP2C9*2
CYP2C9 *2/*2 is associated with Drug Toxicity when treated with diazepam and phenytoin in children with Epilepsy.
Evidence: -; PMID 22641027
CYP2C19 (PA124) rs28399504
Genotype AG is associated with Drug Toxicity when treated with diazepam and phenytoin in children with Epilepsy.
Evidence: -; PMID 22641027
CYP2C19 (PA124) CYP2C19 intermediate metabolizers
CYP2C19 intermediate metabolizers is not associated with dose of diazepam in people with Alcohol Withdrawal Delirium and Alcohol Withdrawal Seizures as compared to CYP2C19 normal metabolizer.
Evidence: -; PMID 27099220
CYP2C19 (PA124) CYP2C19 ultrarapid metabolizer
CYP2C19 ultrarapid metabolizer is not associated with dose of diazepam in people with Alcohol Withdrawal Delirium and Alcohol Withdrawal Seizures as compared to CYP2C19 normal metabolizer.
Evidence: -; PMID 27099220
CYP2C19 (PA124) CYP2C19*1, CYP2C19*2, CYP2C19*3
CYP2C19 *2 + *3 is associated with decreased metabolism of diazepam as compared to CYP2C19 *1.
Evidence: -; PMID 16338280
CYP2C19 CYP2C19*1, CYP2C19*2, CYP2C19*3
-
Evidence: 3; PMID 1
SOURCE
NLM RxNorm
7 name rows
Drug Names / RxNorm
Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.
| Name | RxCUI | Type | Source |
|---|---|---|---|
| Diazepam | 3322 | SU | MTHSPL |
| diazepam | 3322 | SU | MTHSPL |
| DIAZEPAM | 3322 | SU | MTHSPL |
| diazepam | 3322 | IN | RXNORM |
| diazePAM | 3322 | TMSY | RXNORM |
| Valium | 202472 | BN | RXNORM |
| Diastat | 216586 | BN | RXNORM |
SOURCE
SIDER
80 side-effect rows
Side Effects
SIDER side-effect terms mapped to the drug or same-CAS compound identity.
| Side Effect | Drug Name | MedDRA Type | Concept ID |
|---|---|---|---|
| Abdominal pain | diazepam | LLT | C0000737 |
| Abdominal pain | diazepam | PT | C0000737 |
| Abnormal behaviour | diazepam | LLT | C0233514 |
| Abnormal behaviour | diazepam | PT | C0233514 |
| Abnormal faeces | diazepam | LLT | C0162287 |
| Abnormal faeces | diazepam | PT | C0162287 |
| Abnormal vision | diazepam | LLT | C3665386 |
| Accidental injury | diazepam | LLT | C0151736 |
| Acidosis | diazepam | LLT | C0001122 |
| Acidosis | diazepam | PT | C0001122 |
| Acute coronary syndrome | diazepam | PT | C0948089 |
| Affect lability | diazepam | PT | C0233472 |
| Aggression | diazepam | LLT | C0001807 |
| Aggression | diazepam | PT | C0001807 |
| Agitation | diazepam | PT | C0085631 |
| Agitation | diazepam | PT | C0085631 |
| Agitation | diazepam | PT | C0085631 |
| Agitation | diazepam | PT | C0085631 |
| Agranulocytosis | diazepam | LLT | C0001824 |
| Agranulocytosis | diazepam | PT | C0001824 |
| Alertness decreased | diazepam | LLT | C0877609 |
| Amblyopia | diazepam | LLT | C0002418 |
| Amblyopia | diazepam | PT | C0002418 |
| Amnesia | diazepam | LLT | C0002622 |
| Amnesia | diazepam | PT | C0002622 |
| Amnesia | diazepam | PT | C0002622 |
| Anaemia | diazepam | LLT | C0002871 |
| Anaemia | diazepam | PT | C0002871 |
| Anaphylactic shock | diazepam | LLT | C0002792 |
| Anaphylactic shock | diazepam | PT | C0002792 |
| Anger | diazepam | LLT | C0002957 |
| Anger | diazepam | PT | C0002957 |
| Anger | diazepam | PT | C0002957 |
| Angiopathy | diazepam | LLT | C0042373 |
| Angiopathy | diazepam | PT | C0042373 |
| Anorectal discomfort | diazepam | PT | C2242737 |
| Anorectal discomfort | diazepam | PT | C2242737 |
| Anorectal disorder | diazepam | PT | C0687707 |
| Anorexia | diazepam | LLT | C0003123 |
| Anterograde amnesia | diazepam | LLT | C0233795 |
| Anterograde amnesia | diazepam | PT | C0233795 |
| Arrhythmia | diazepam | LLT | C0003811 |
| Arrhythmia | diazepam | PT | C0003811 |
| Arthralgia | diazepam | LLT | C0003862 |
| Arthralgia | diazepam | PT | C0003862 |
| Asthenia | diazepam | LLT | C0004093 |
| Asthenia | diazepam | PT | C0004093 |
| Asthenia | diazepam | PT | C0004093 |
| Asthma | diazepam | LLT | C0004096 |
| Asthma | diazepam | PT | C0004096 |
| Ataxia | diazepam | LLT | C0004134 |
| Ataxia | diazepam | PT | C0004134 |
| Auditory and visual hallucinations | diazepam | LLT | C0740399 |
| Back pain | diazepam | LLT | C0004604 |
| Back pain | diazepam | PT | C0004604 |
| Balance disorder | diazepam | PT | C0575090 |
| Balance disorder | diazepam | LLT | C0575090 |
| Balance disorder | diazepam | PT | C0575090 |
| Blood disorder | diazepam | LLT | C0018939 |
| Blood disorder | diazepam | PT | C0018939 |
| Blood thromboplastin decreased | diazepam | PT | C0852990 |
| Body temperature decreased | diazepam | LLT | C0020672 |
| Body temperature decreased | diazepam | PT | C0020672 |
| Bradycardia | diazepam | LLT | C0428977 |
| Bradycardia | diazepam | PT | C0428977 |
| Burning rectal | diazepam | LLT | C0541819 |
| Cardiac arrest | diazepam | LLT | C0018790 |
| Cardiac arrest | diazepam | PT | C0018790 |
| Cardiac disorder | diazepam | LLT | C0018799 |
| Cardiac disorder | diazepam | PT | C0018799 |
| Cardiac failure | diazepam | LLT | C0018801 |
| Cardiac failure | diazepam | PT | C0018801 |
| Cardiovascular insufficiency | diazepam | PT | C1392046 |
| Cerebration impaired | diazepam | LLT | C0235198 |
| Chills | diazepam | LLT | C0085593 |
| Chills | diazepam | PT | C0085593 |
| Circulatory depression | diazepam | LLT | C1610069 |
| Confusional state | diazepam | LLT | C0009676 |
| Confusional state | diazepam | PT | C0009676 |
| Conjunctivitis | diazepam | LLT | C0009763 |
SOURCE
Rendered pharma page rows
FAQPage JSON-LD
Frequently Asked Questions
Short answers generated only from the same visible source-linked rows on this page.
What is Diazepam used for in pharmaceutical contexts?
Diazepam (CAS 439-14-5) appears in DailyMed active-ingredient label rows, including Diazepam.
What are the known adverse events for Diazepam?
Diazepam has 6,594 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Drug abuse, Toxicity to various agents, Completed suicide, Intentional overdose, Coma. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.
Is Diazepam also used in cosmetics?
No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Diazepam.
What clinical phase is Diazepam in?
Diazepam is rendered with ChEMBL max phase 4 (approved).
What bioactivity targets are documented for Diazepam?
Diazepam has 40 bioactivity rows in this page query. Rendered target entries include Gamma-aminobutyric acid receptor subunit alpha-5, Cytochrome P450 3A4, Alpha-1A adrenergic receptor, Adenosine receptor A3, Aldo-keto reductase family 1 member C1.