Diazepam

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

1963

www.ebi.ac.uk

First approval year: 1963
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Diazepam
www.ebi.ac.uk

Molecular weight: 284.75
www.ebi.ac.uk

Structure (SMILES): CN1C(=O)CN=C(c2ccccc2)c2cc(Cl)ccc21
www.ebi.ac.uk

alupram 10
Alupram 10
alupram 2
Alupram 2
alupram 5
Alupram 5
apozepam
Apozepam
atensine
Atensine
dialar
Dialar
dialar fte
Dialar fte
diastat
Diastat
diastat acudial
Diastat acudial
diazepam
Diazepam
diazepam intensol
Diazepam intensol
dizac
Dizac
e pam

And 31 more, listed on the interactive page.

10 mg diazepam
ansiolisina
Ansiolisina
centrazepam
Centrazepam
diacepin
Diacepin
diazepam
Diazepam
diazepam (or equivalence if other benzodiazepine)
Diazepam [EP MONOGRAPH]
Diazepam [GREEN BOOK]
Diazepam [HSDB]
Diazepam [IARC]
Diazepam [INN]
Diazepam [JAN]
Diazepam [MART.]
Diazepam [MI]
Diazepam [ORANGE BOOK]
Diazepam [USAN]
Diazepam [USP MONOGRAPH]
Diazepam [VANDF]
Diazepam [WHO-DD]
Diazepam 10 mg
Diazepam 10 MG

And 47 more, listed on the interactive page.

ATC classification codes

N05BA01

Sources for recorded values

www.ebi.ac.uk

CAS registry numbers

439-14-5

ChEMBL ID: CHEMBL12
www.ebi.ac.uk

InChIKey: AAOVKJBEBIDNHE-UHFFFAOYSA-N
www.ebi.ac.uk

PubChem compound IDs

3016

RxNorm IDs (RxCUI)

3322

FDA ingredient codes (UNII)

Q3JTX2Q7TU

Applicant: WAYLIS THERAP
Approval date: 15 Nov 1963
Application number: NDA013263

Patents: 8
Designations: 3
Earliest recorded loss of exclusivity: 10 Jun 2042
First in class: No
Fast track: No
Breakthrough designation: No
Orphan designation: No
Priority review: No
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only
Boxed warning: Yes

Pharmacology name: diazepam
Type: Synthetic organic
Drug name stem: -azepam
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral
Parenteral
topical

Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
O00591
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
O14764
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P14867
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P18505
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P18507
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P28472
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P31644
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P34903
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P47869
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P47870
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P48169
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
P78334
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
Q16445
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
Q8N1C3
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
Q99928
Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE_ALLOSTERIC_MODULATOR
Target
GABA-A receptor; anion channel
Protein identifier
Q9UN88
Action
Positive
Action type
POSITIVE
Target
GABAA receptor α1 subunit
Gene symbol
GABRA1
Protein identifier
P14867
Median affinity
7.79
Affinity units
pKi
Primary target
Yes
Action
Positive
Action type
POSITIVE
Target
GABAA receptor α3 subunit
Gene symbol
GABRA3
Protein identifier
P34903
Median affinity
7.77
Affinity units
pKi
Primary target
Yes
Action
Positive
Action type
POSITIVE
Target
GABAA receptor α2 subunit
Gene symbol
GABRA2
Protein identifier
P47869
Median affinity
7.77
Affinity units
pKi
Primary target
Yes

Open Targets mechanisms

Mechanism
GABA-A receptor; anion channel positive allosteric modulator
Action type
POSITIVE ALLOSTERIC MODULATOR
Target
GABA-A receptor; anion channel

Action type
ALLOSTERIC MODULATOR
Gene symbol
ADRA1A
Protein identifier
P35348
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRA1|GABRG2|GABRB3
Protein identifier
P14867|P18507|P28472
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRA1|GABRG2|GABRB2
Protein identifier
P14867|P18507|P47870
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRA1|GABRB2|GABRG3
Protein identifier
P14867|P47870|Q99928
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRG2|GABRB3|GABRA5
Protein identifier
P18507|P28472|P31644
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRG2|GABRB3|GABRA3
Protein identifier
P18507|P28472|P34903
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRG2|GABRB3|GABRA2
Protein identifier
P18507|P28472|P47869
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRG2|GABRA5|GABRB2
Protein identifier
P18507|P31644|P47870
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRG2|GABRA3|GABRB2
Protein identifier
P18507|P34903|P47870
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRB3|GABRA5|GABRG3
Protein identifier
P28472|P31644|Q99928
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRA5|GABRB2|GABRG3
Protein identifier
P31644|P47870|Q99928
Organism
Homo sapiens
Target development level
Clinical
Action type
POSITIVE ALLOSTERIC MODULATOR
Gene symbol
GABRA3|GABRB2|GABRG3
Protein identifier
P34903|P47870|Q99928
Organism
Homo sapiens
Target development level
Clinical

Condition
Epilepsy
Highest recorded phase
4
Condition identifier
EFO:0000474
Subject identifier
D004827
Condition
Wounds and Injuries
Highest recorded phase
2
Condition identifier
EFO:0000546
Subject identifier
D014947
Condition
Pain
Highest recorded phase
3
Condition identifier
EFO:0003843
Subject identifier
D010146
Condition
Anxiety
Highest recorded phase
4
Condition identifier
EFO:0005230
Subject identifier
D001007
Condition
Anxiety
Highest recorded phase
4
Condition identifier
EFO:0006788
Subject identifier
D001007
Condition
Anxiety Disorders
Highest recorded phase
4
Condition identifier
EFO:0006788
Subject identifier
D001008
Condition
Stiff-Person Syndrome
Highest recorded phase
4
Condition identifier
EFO:0007498
Subject identifier
D016750
Condition
Status Epilepticus
Highest recorded phase
3
Condition identifier
EFO:0008526
Subject identifier
D013226
Condition
Cerebral Palsy
Highest recorded phase
4
Condition identifier
EFO:1000632
Subject identifier
D002547
Condition
Epilepsy, Complex Partial
Highest recorded phase
3
Condition identifier
EFO:1000877
Subject identifier
D017029
Condition
Landau-Kleffner Syndrome
Highest recorded phase
2
Condition identifier
EFO:1001010
Subject identifier
D018887
Condition
Rotator Cuff Injuries
Highest recorded phase
2
Condition identifier
EFO:1001250
Subject identifier
D000070636
Condition
Mental Disorders
Highest recorded phase
4
Condition identifier
HP:0000713
Subject identifier
D001523
Condition
Psychomotor Agitation
Highest recorded phase
4
Condition identifier
HP:0000713
Subject identifier
D011595
Condition
Dementia
Highest recorded phase
3
Condition identifier
HP:0000726
Subject identifier
D003704
Condition
Seizures
Highest recorded phase
3
Condition identifier
HP:0001250
Subject identifier
D012640
Condition
Vertigo
Highest recorded phase
3
Condition identifier
HP:0002321
Subject identifier
D014717
Condition
Low Back Pain
Highest recorded phase
2
Condition identifier
HP:0003419
Subject identifier
D017116
Condition
Depressive Disorder
Highest recorded phase
3
Condition identifier
MONDO:0002050
Subject identifier
D003866
Condition
Schizophrenia
Highest recorded phase
3
Condition identifier
MONDO:0005090
Subject identifier
D012559

Condition identifier
EFO_0000474
Condition identifier
EFO_0000685
Condition identifier
EFO_0004263
Highest recorded phase
3
Condition identifier
EFO_0004777
Condition identifier
EFO_0006788
Condition identifier
EFO_0007498
Condition identifier
EFO_0008526
Highest recorded phase
3
Condition identifier
EFO_0009523
Condition identifier
EFO_1000632
Condition identifier
EFO_1000850
Condition identifier
EFO_1000877
Highest recorded phase
3
Condition identifier
EFO_1001250
Highest recorded phase
2
Condition identifier
EFO_1001884
Condition identifier
HP_0000360
Highest recorded phase
2
Condition identifier
HP_0000713
Condition identifier
HP_0000713
Highest recorded phase
4
Condition identifier
HP_0000739
Condition identifier
HP_0000739
Highest recorded phase
4
Condition identifier
HP_0001250
Highest recorded phase
3
Condition identifier
HP_0001259
Condition identifier
HP_0002019
Condition identifier
HP_0002027
Highest recorded phase
2
Condition identifier
HP_0002321
Highest recorded phase
3
Condition identifier
HP_0002373
Condition identifier
HP_0002384
Highest recorded phase
2

And 24 more, listed on the interactive page.

Warning
Black Box Warning
Warning
Black Box Warning
Effect
misuse

Warning
Black Box Warning
Country
United States
Warning
Black Box Warning
Effect
misuse
Country
United States

Event
aggression
Reports
320
Reporting signal score
371.226
Event
agitation
Reports
474
Reporting signal score
519.432
Event
altered state of consciousness
Reports
277
Reporting signal score
432.56
Event
bradyphrenia
Reports
143
Reporting signal score
297.219
Event
bradypnoea
Reports
198
Reporting signal score
633.29
Event
coma
Reports
1,310
Reporting signal score
3,232.54
Event
coma scale abnormal
Reports
134
Reporting signal score
327.282
Event
confusional state
Reports
547
Reporting signal score
370.758
Event
congenital nystagmus
Reports
60
Reporting signal score
248.802
Event
delirium
Reports
241
Reporting signal score
239.989
Event
depressed level of consciousness
Reports
469
Reporting signal score
693.522
Event
developmental delay
Reports
91
Reporting signal score
211.99
Event
disorientation
Reports
199
Reporting signal score
174.527
Event
disturbance in attention
Reports
210
Reporting signal score
211.344
Event
drug abuse
Reports
1,525
Reporting signal score
3,623.68
Event
drug dependence
Reports
625
Reporting signal score
1,392.6
Event
drug use disorder
Reports
116
Reporting signal score
259.847
Event
drug withdrawal convulsions
Reports
71
Reporting signal score
177.543
Event
drug withdrawal syndrome
Reports
239
Reporting signal score
228.189
Event
drug withdrawal syndrome neonatal
Reports
120
Reporting signal score
206.915
Event
dysarthria
Reports
259
Reporting signal score
267.441
Event
electrocardiogram qt prolonged
Reports
302
Reporting signal score
317.288
Event
exposure via father
Reports
189
Reporting signal score
682.752
Event
housebound
Reports
55
Reporting signal score
210.44
Event
hypotension
Reports
668
Reporting signal score
335.298

And 19 more, listed on the interactive page.

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And 10 more, listed on the interactive page.

Hydrogen bond acceptors: 2
Hydrogen bond donors: 0
Polar surface area: 32.67
Calculated partition coefficient (ALogP): 3.15
Calculated partition coefficient (XLogP): 3
Prodrug: No
Chirality: Achiral
Inorganic: No
Rule-of-five violations: 0
Rotatable bonds: 1
Heavy atoms: 20
Molecular formula: C16H13ClN2O
Monoisotopic mass: 284.0716407
Natural product: Yes

0054-3185
0054-3188
0121-0905
0140-0004
0140-0005
0172-3925
0172-3926
0172-3927
0378-0271
0378-0345
0378-0477
0404-9762
0404-9769
0404-9848
0409-1273
0409-3213
0641-6243
0641-6244
0641-6283
11534-199
11534-202
11534-203
11704-600
25021-618
43063-840

And 102 more, listed on the interactive page.

Recorded assays: 6,993
Active assays: 1,436

Confirmatory
Other
Screening
Summary

Adjuvants, Anesthesia
id.nlm.nih.gov
Anticonvulsants
id.nlm.nih.gov
Antiemetics
id.nlm.nih.gov
Hypnotics and Sedatives
id.nlm.nih.gov
Muscle Relaxants, Central
id.nlm.nih.gov
Anti-Anxiety Agents
id.nlm.nih.gov
Anesthetics, Intravenous
id.nlm.nih.gov
GABA Modulators
id.nlm.nih.gov

These details could not be displayed.

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A Multicenter Active Comparator Study of HC-ER in Adults Following Bunionectomy Surgery
A Non-inferiority Trial on Pain Relief During Oocyte Retrieval
A Pharmacokinetic Study of a Single-Dose of Diazepam Nasal Spray in Adult Epileptic Patients Experiencing a Seizure Episode
A Pharmacokinetic Study to Assess Dose Proportionality, Safety and Tolerability of Diazepam Nasal Spray in Healthy Adult Volunteers
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Approved for (6)

In development for (10)

Complex partial epilepsy Phase 3
Dementia Phase 3
Depressive disorder Phase 3
Focal epilepsy Phase 3
Injury Phase 2
Landau-Kleffner syndrome Phase 2
Peripheral vertigo Phase 3
Rotator cuff syndrome Phase 2
Schizophrenia Phase 3
Visual epilepsy Phase 3

Targets (16)

GABRA1 GABA-A receptor; anion channel positive allosteric modulator
GABRA2 GABA-A receptor; anion channel positive allosteric modulator
GABRA3 GABA-A receptor; anion channel positive allosteric modulator
GABRA4 GABA-A receptor; anion channel positive allosteric modulator
GABRA5 GABA-A receptor; anion channel positive allosteric modulator
GABRA6 GABA-A receptor; anion channel positive allosteric modulator
GABRB1 GABA-A receptor; anion channel positive allosteric modulator
GABRB2 GABA-A receptor; anion channel positive allosteric modulator
GABRB3 GABA-A receptor; anion channel positive allosteric modulator
GABRD GABA-A receptor; anion channel positive allosteric modulator
GABRE GABA-A receptor; anion channel positive allosteric modulator
GABRG1 GABA-A receptor; anion channel positive allosteric modulator
GABRG2 GABA-A receptor; anion channel positive allosteric modulator
GABRG3 GABA-A receptor; anion channel positive allosteric modulator
GABRP GABA-A receptor; anion channel positive allosteric modulator
GABRQ GABA-A receptor; anion channel positive allosteric modulator

Diazepam

Development status

Names and chemistry

Brand names (56)

Other names (72)

Identifiers

Regulatory information

United States

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action (19)

Open Targets mechanisms

DrugCentral mechanisms (12)

Investigated indications (20)

Open Targets indications (49)

Warnings (2)

Open Targets warnings (2)

Reported adverse events (44)

Trial references (35)

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Related records

Trials (271)

Approved for (6)

In development for (10)

Other linked conditions (5)

Targets (16)