Propofol

Summary

Propofol (CHEMBL526) is an approved small-molecule intravenous anaesthetic (ATC N01AX10) targeting PIEZO1, PIEZO2, and HCN1; indicated across 58 conditions including hypertensive disorder and subarachnoid hemorrhage.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01AX10
• Targets: 4 (PIEZO1, PIEZO2, HCN1…)
• Indications: 58 conditions
• Clinical trials: 1,127
• Chemistry: 178.27 Da · C12H18O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL526
Name	Propofol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4943
ChEBI	CHEBI:44915
ATC	N01AX10
Molecular formula	C12H18O
Molecular weight	178.27
InChIKey	OLBCVFGFOZPWHH-UHFFFAOYSA-N

SMILES: CC(C)C1=C(C(=CC=C1)C(C)C)O

IUPAC name: 2,6-di(propan-2-yl)phenol

ChEBI definition: A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.

Pharmacological roles (ChEBI): intravenous anaesthetic, sedative, radical scavenger, antiemetic, anticonvulsant.

Also known as: Diprivan, Disoprofol, Disoprivan, Fresofol, ICI 35,868, ICI-35868, ICI35,868, Lipuro, NSC-5105, Propofol, Propofol component of ketafol, Rapinovet

Parent form; salt/anhydrous children: CHEMBL154232, CHEMBL356637

Patent coverage: 9,287 distinct patent families (28,835 SureChEMBL compound mentions), from 1 matched compound structure(s). 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PIEZO1	Piezo1	Inhibition		1.2%	Q92508
PIEZO2	Piezo2	Inhibition		0%	Q9H5I5
HCN1	HCN1		5.2	0%	O60741
TRPV4	TRPV4	Inhibition	4.41	0.6%	Q9HBA0

Broader ChEMBL bioactivity targets: 26 (assay-derived). Sample: Prelamin-A/C, RecQ-like DNA helicase BLM, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], 5-hydroxytryptamine receptor 2B, GABA-A receptor; anion channel, Thyrotropin receptor, Carbonic anhydrase 2, GABA-A receptor; alpha-1/beta-3/gamma-2, GABA-A receptor; alpha-1/beta-2/gamma-2.

Bioactivity

ChEMBL activities: 21 potent at pChembl ≥ 5 of 46 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
TRPV1	8.3	IC50	5.05	nM	CHEMBL_ACT_25706555
LMNA	5.95	Potency	1122	nM	CHEMBL_ACT_3622655
GABRA1	5.7	AC50	2000	nM	CHEMBL_ACT_25233975
GABRA1	5.7	EC50	1995	nM	CHEMBL_ACT_317016
HTR2B	5.46	Ki	3499	nM	CHEMBL_ACT_7739418
PTGS1	5.42	IC50	3832	nM	CHEMBL_ACT_7737242
O09028	5.4	IC50	3950	nM	CHEMBL_ACT_1279248
GABRA1	5.39	EC50	4100	nM	CHEMBL_ACT_148916
GABRA1	5.28	EC50	5200	nM	CHEMBL_ACT_12079861
GABRA1	5.27	EC50	5400	nM	CHEMBL_ACT_22478794
HTR2B	5.26	IC50	5499	nM	CHEMBL_ACT_7739417
HTR2C	5.22	Ki	6051	nM	CHEMBL_ACT_7739420
P12530	5.12	IC50	7596	nM	CHEMBL_ACT_7739323
GABRA1	5.1	EC50	8000	nM	CHEMBL_ACT_1279252
GABRA1	5.1	IC50	8000	nM	CHEMBL_ACT_22478827
O09028	5.09	IC50	8100	nM	CHEMBL_ACT_416426
O09028	5.08	IC50	8300	nM	CHEMBL_ACT_690337
SLC6A2	5.03	IC50	9393	nM	CHEMBL_ACT_7737204
SLC6A2	5.03	Ki	9316	nM	CHEMBL_ACT_7737205
GABRA1	5	EC50	10000	nM	CHEMBL_ACT_317017
CYP1A2	5	AC50	10000	nM	CHEMBL_ACT_6038375

Target pathways

Aggregated over 4 target gene(s): PIEZO1, PIEZO2, HCN1, TRPV4.

Top Reactome pathways

5 total, by targets touching each:

Pathway	Targets	Genes
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells	2	PIEZO1, TRPV4
HCN channels	1	HCN1
TRP channels	1	TRPV4
Mechanical load activates signaling by PIEZO1 and integrins in osteocytes	1	PIEZO1
Turbulent (oscillatory, disturbed) flow shear stress activates signaling by PIEZO1 and integrins in endothelial cells	1	PIEZO1

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	4
monoatomic ion transmembrane transport	4
regulation of membrane potential	3
monoatomic cation transport	2
detection of mechanical stimulus	2
cellular response to mechanical stimulus	2
monoatomic cation transmembrane transport	2
response to mechanical stimulus	2
transmembrane transport	2
positive regulation of myotube differentiation	1
positive regulation of integrin activation	1
positive regulation of cell-cell adhesion mediated by integrin	1
detection of mechanical stimulus involved in sensory perception	1
regulation of membrane depolarization	1
neuronal action potential	1

Indications & clinical

Indications

58 indications (0 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).

Indication	Trial phase	MONDO	EFO
hypertensive disorder	3	MONDO:0005044	EFO:0000537
subarachnoid hemorrhage	3	MONDO:0005099	EFO:0000713
heart disorder	3	MONDO:0005267	EFO:0003777
neoplasm	3	MONDO:0005070	EFO:0000616
polyp	3	MONDO:0005079	EFO:0000662
stroke disorder	3	MONDO:0005098	EFO:0000712
cirrhosis of liver	3	MONDO:0005155	EFO:0001422
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
breast neoplasm	3	MONDO:0021100	EFO:0003869
toxic shock syndrome	3	MONDO:0001881	EFO:0006834
respiratory failure	3	MONDO:0021113	HP:0002093
brain aneurysm	3	MONDO:0005291	EFO:0003870
acute respiratory distress syndrome	3	MONDO:0006502	EFO:1000637
brain injury	3	MONDO:0043510	MONDO:0043510
severe acute respiratory syndrome	3	MONDO:0005091	EFO:0000694
obesity disorder	3	MONDO:0011122	EFO:0001073
ischemia reperfusion injury	3	MONDO:0005203	EFO:0002687
male reproductive organ cancer	3	MONDO:0005836	EFO:0007355
newborn respiratory distress syndrome	3	MONDO:0700081	EFO:1000644
delirium	3	MONDO:0045057	EFO:0009267
atrial fibrillation	3	MONDO:0004981	EFO:0000275
cerebral arterial disease	3	MONDO:0006693	EFO:1000859
leukemia	2	MONDO:0005059	EFO:0000565
morbid obesity	2	MONDO:0005139	EFO:0001074
hypotensive disorder	2	MONDO:0005468	EFO:0005251
injury	2	MONDO:0021178	EFO:0000546
obstructive sleep apnea syndrome	2	MONDO:0007147	EFO:0003918
intestinal polyp	2	MONDO:0005288	EFO:0003855
strabismus	2	MONDO:0003432	HP:0000486
lung neoplasm	2	MONDO:0021117	MONDO:0021117
coronary artery disorder	2	MONDO:0005010	EFO:0001645
migraine disorder	2	MONDO:0005277	MONDO:0005277
colon adenocarcinoma	2	MONDO:0002271	EFO:1001949
tonsillitis	2	MONDO:0001039	MONDO:0001039
insomnia	1	MONDO:0013600	EFO:0004698
scoliosis	1	MONDO:0005392	EFO:0004273
kidney failure	1	MONDO:0001106	EFO:1002048
major depressive disorder	1	MONDO:0002009	MONDO:0002009
chronic kidney disease	1	MONDO:0005300	EFO:0003884
tethered spinal cord syndrome	1	MONDO:0006995	EFO:1001210
colorectal neoplasm	1	MONDO:0005335	MONDO:0005575
osteonecrosis	0	MONDO:0005380	EFO:0004259
spinal stenosis	0	MONDO:0005965	EFO:0007490
depressive disorder	0	MONDO:0002050	MONDO:0002050

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

Clinical trials

Total trials: 1,127.

Phase distribution

Phase	Trials
Not specified	518
PHASE4	386
PHASE3	86
PHASE2	54
PHASE1	34
PHASE2/PHASE3	18
EARLY_PHASE1	18
PHASE1/PHASE2	13

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00577200	PHASE4	ACTIVE_NOT_RECRUITING	Safety of Driving After Minor Surgery With Monitored Anesthesia Care
NCT04475705	PHASE4	RECRUITING	Propofol vs Sevo for Paediatric Tumor Surgery
NCT04532606	PHASE4	RECRUITING	Impact of Remimazolam on Prognosis After Bladder Cancer Surgery
NCT04934683	PHASE4	ENROLLING_BY_INVITATION	The GUARDIAN Trial - Induction Agent Sub-Study
NCT05268562	PHASE4	ACTIVE_NOT_RECRUITING	Ketamine and Kidney Injury in Cardiac Surgery
NCT05305313	PHASE4	RECRUITING	Evaluation of Propofol Dosing Based on Total Body Weight Using Closes-loop Anaesthesia Delivery System
NCT05331911	PHASE4	RECRUITING	Impact of Propofol-Based Total Intravenous Anesthesia Versus Anesthesia With Sevoflurane on Long-term Outcomes With Patients Undergoing Elective Excision of Primary Liver Tumors
NCT05606692	PHASE4	RECRUITING	Influences of Propofol and Sevoflurane Anesthesia in Ovarian Cancer (Anesthetics)
NCT05663242	PHASE4	RECRUITING	The Effects of Using Different Anesthetics on the Prognosis of Primary Lung Tumors and Its Mechanism of Action
NCT05728775	PHASE4	RECRUITING	REmimazolam vs Propofol Total Intravenous Anesthesia on Outcomes After Major Noncardiac SurgEry
NCT05926336	PHASE4	RECRUITING	The Effects of Using Different Anesthetics on the Prognosis of Primary Tumors and Its Mechanism of Action
NCT05990790	PHASE4	RECRUITING	The Effect of Desflurane Versus Sevoflurane Versus Propofol on Postoperative Delirium
NCT06036095	PHASE4	RECRUITING	Total Intravenous Versus Inhalational Anesthesia- A Geriatric Anesthesia Study
NCT06068764	PHASE4	RECRUITING	Etomidate Versus Propofol in CABG Surgery
NCT06251999	PHASE4	NOT_YET_RECRUITING	Efficacy and Safety of Fospropofol for Same-day Bidirectional Endoscopy in Elderly Patients
NCT06330038	PHASE4	RECRUITING	Anesthesia and Non-small Cell Lung Cancer Recurrence
NCT06385756	PHASE4	NOT_YET_RECRUITING	Effect of Amobarbital Sodium Combined With Low-dose Propofol on Hemodynamics During Induction and Perioperative Adverse Reactions
NCT06507202	PHASE4	RECRUITING	Comparison of Remimazolam and Propofol for Recovery of Ambulatory Upper Airway Surgery
NCT06570187	PHASE4	RECRUITING	The Effect of Dexmedetomidine on the Renal Functions in Septic Critically Ill Patients
NCT06573489	PHASE4	RECRUITING	Efficacy and Safety of Fospropofol in Adult Laparoscopic Surgery: A Clinical Trial
NCT06674226	PHASE4	RECRUITING	Effects of Ciprofol on Postoperative Delirium and Outcomes in Elderly Patients Undergoing Major Thoracic Surgery
NCT06715657	PHASE4	NOT_YET_RECRUITING	Effect of Propofol Administration Time on the Incidence and Severity of Intrathecal Morphine-induced Pruritus in Parturient Undergoing Elective Cesarean Delivaries
NCT06734195	PHASE4	NOT_YET_RECRUITING	Comparing the Synergistic Effect of Caudal Dexmedetomidine and Propofol Versus Caudal Dexmedetomidine Only or Propofol Only in Prevention of Sevoflurane Related Emergence Agitation in Pediatric Patients Undergoing Congenital Inguinal Hernia Repair
NCT06736938	PHASE4	NOT_YET_RECRUITING	Balanced Analgosedation in Bronchoscopy: Propofol/Pethidine Versus Midazolam/Pethidine
NCT06763705	PHASE4	RECRUITING	Comparison of Safety and Efficacy for Different Sedation Regimens During Colonoscopy
NCT06777758	PHASE4	RECRUITING	Comparison of Remimazolam and Propofol in Endoscopic Examinations and Treatments
NCT06784479	PHASE4	ACTIVE_NOT_RECRUITING	Combination of Remimazolam and Propofol During Drug-induced Sleep Endoscopy
NCT06816173	PHASE4	NOT_YET_RECRUITING	Effect of Propofol Versus Remimazolam Intravenous Anesthesia on Respiratory Depression
NCT06951802	PHASE4	RECRUITING	Endometriosis and Pain Treatment by Intraoperative Administration of Low-dose Ketamine
NCT06952608	PHASE4	RECRUITING	Effect of Ciprofol on Intraoperative Hypotension in Elderly Patients Receiving Renin-angiotensin System Inhibitors
NCT07000526	PHASE4	RECRUITING	Inhaled Sedation in Critically Ill Patients
NCT07028593	PHASE4	RECRUITING	Effects of Ciprofol on Myocardial Injury After Non-cardiac Surgery in Video-Assisted Thoracoscopic Surgery
NCT07080528	PHASE4	ENROLLING_BY_INVITATION	Measuring of the Duration of Action of Different Doses of Rocuronium-induced Neuromuscular Block in Infants During Surgical Treatment of Craniosynostosis
NCT07094945	PHASE4	NOT_YET_RECRUITING	The Effect of Remimazolam on Postoperative Sleep Quality
NCT07118579	PHASE4	RECRUITING	Effects of Remimazolam and Ciprofol TIVA on PRAE in Pediatric Tonsillectomy and Adenoidectomy
NCT07161518	PHASE4	ENROLLING_BY_INVITATION	Characterizing Transcranial Focused Ultrasound Neuromodulation During Sedation
NCT07190612	PHASE4	NOT_YET_RECRUITING	Efficacy of Propofol Combination With Either Ketamine, Dexmedetomidine or Midazolam for Sedation During Upper Gastrointestinal Endoscopic Procedures
NCT07213544	PHASE4	RECRUITING	Remimazolam vs Propofol in Laser Burn Cases
NCT07268924	PHASE4	NOT_YET_RECRUITING	The Effect of Propofol Versus Lidocaine on Emergence Agitation in Children Undergoing Tonsillectomy.
NCT07347496	PHASE4	NOT_YET_RECRUITING	A Randomized, Controlled Clinical Trial Comparing Remimazolam Besylate Combined With Alfentanil Versus Propofol Combined With Alfentanil for Anesthesia in Thoracic Surgery

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 5 clinical and 44 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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.

6 molecules share ≥1 primary target. Top 6 by shared-target count:

Molecule	Source	Status	Shared targets
CANNABINOL	ChEMBL	Phase 3	TRPV4
CANNABIDIVARIN	ChEMBL	Phase 2	TRPV4
CANNABIGEROL	ChEMBL	Phase 2	TRPV4
GSK2798745	ChEMBL	Phase 2	TRPV4
TETRAHYDROCANNABIVARIN	ChEMBL	Phase 2	TRPV4
Ivabradine	PubChem	Approved	HCN1