Omeprazole

Summary

Omeprazole (CHEMBL1503) is an approved small molecule (ATC A02BC01) targeting CLCN2 and ATP4A; indicated across 74 conditions including gastroesophageal reflux disease and duodenal ulcer.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A02BC01
• Targets: 2 (CLCN2, ATP4A)
• Indications: 74 conditions
• Clinical trials: 335
• Chemistry: 345.4 Da · C17H19N3O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1503
Name	Omeprazole
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4594
ChEBI	CHEBI:77260
ATC	A02BC01
Molecular formula	C17H19N3O3S
Molecular weight	345.4
InChIKey	SUBDBMMJDZJVOS-UHFFFAOYSA-N

SMILES: CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C(N2)C=C(C=C3)OC

IUPAC name: 6-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]-1H-benzimidazole

ChEBI definition: A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.

Also known as: Antra, H 168/68, H-168/68, Losec, Losec mups, Mezzopram, Mopral, NSC-751450, NSC-759192, Omeprazol, Omeprazole, Omeprazole component of konvomep

Parent form; salt/anhydrous children: CHEMBL1567328, CHEMBL2105294

Patent coverage: 18,447 distinct patent families (52,284 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 51,090 (98%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CLCN2	ClC-2			0.1%	P51788
ATP4A	ATP4A	Inhibition		0.2%	P20648

Broader ChEMBL bioactivity targets: 35 (assay-derived). Sample: Pyruvate kinase PKM, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, Fructose-bisphosphate aldolase, 4’-phosphopantetheinyl transferase ffp, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Potassium-transporting ATPase, Sodium/potassium-transporting ATPase.

Bioactivity

ChEMBL activities: 26 potent at pChembl ≥ 5 of 73 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ATP4A	6.6	IC50	250	nM	CHEMBL_ACT_1000476
ATP4A	6.55	IC50	280	nM	CHEMBL_ACT_1000477
ATP4A	6.43	IC50	370	nM	CHEMBL_ACT_714020
ATP4A	6.3	IC50	501.2	nM	CHEMBL_ACT_545768
SMN1	5.85	Potency	1412	nM	CHEMBL_ACT_3863864
WDR5	5.77	IC50	1700	nM	CHEMBL_ACT_22463502
ATP4A	5.7	IC50	2000	nM	CHEMBL_ACT_695794
CYP2C19	5.68	IC50	2080	nM	CHEMBL_ACT_24925861
CYP2C19	5.6	Potency	2512	nM	CHEMBL_ACT_4019497
CYP2C19	5.6	AC50	2512	nM	CHEMBL_ACT_6047840
CYP2C19	5.59	IC50	2550	nM	CHEMBL_ACT_23298974
ADORA3	5.54	AC50	2877	nM	CHEMBL_ACT_25198574
MCL1	5.5	IC50	3145	nM	CHEMBL_ACT_4721957
FASN	5.47	Ki	3400	nM	CHEMBL_ACT_15194990
P18434	5.42	IC50	3800	nM	CHEMBL_ACT_1190945
ATP4A	5.42	IC50	3800	nM	CHEMBL_ACT_218932
P51450	5.35	Potency	4467	nM	CHEMBL_ACT_4991124
GSTO1	5.34	IC50	4600	nM	CHEMBL_ACT_18550646
PTGS1	5.24	AC50	5760	nM	CHEMBL_ACT_25205041
PKM	5.15	Potency	7080	nM	CHEMBL_ACT_4077934
PKM	5.15	Potency	7080	nM	CHEMBL_ACT_4824939
CYP2C19	5.06	IC50	8620	nM	CHEMBL_ACT_26153933
HPGD	5	Potency	10000	nM	CHEMBL_ACT_4768029
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_4977708
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5046736
CYP3A4	5	AC50	10000	nM	CHEMBL_ACT_6044763

Target pathways

Aggregated over 2 target gene(s): CLCN2, ATP4A.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
Stimuli-sensing channels	1	CLCN2
Transport of small molecules	1	ATP4A
Ion transport by P-type ATPases	1	ATP4A
Ion channel transport	1	ATP4A

Dominant GO biological processes

GO term	Targets
monoatomic ion transport	2
monoatomic ion transmembrane transport	2
chloride transport	1
phagocytosis, engulfment	1
stabilization of membrane potential	1
lung development	1
regulation of aldosterone biosynthetic process	1
positive regulation of oligodendrocyte differentiation	1
retina development in camera-type eye	1
regulation of resting membrane potential	1
cell differentiation involved in salivary gland development	1
cellular hypotonic response	1
acinar cell differentiation	1
regulation of membrane depolarization during action potential	1
transmembrane transport	1

Indications & clinical

Indications

74 indications (8 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
gastroesophageal reflux disease	4	MONDO:0007186	EFO:0003948
duodenal ulcer	4	MONDO:0005412	EFO:0004607
peptic ulcer disease	4	MONDO:0004247	HP:0004398
gastric ulcer	4	MONDO:0001126	EFO:0009454
esophagitis	4	MONDO:0001409	HP:0100633
Barrett esophagus	3	MONDO:0013662	EFO:0000280
injury	3	MONDO:0021178	EFO:0000546
peptic esophagitis	3	MONDO:0006896	EFO:1001095
ankylosing spondylitis	3	MONDO:0005306	EFO:0003898
relapsing-remitting multiple sclerosis	3	MONDO:0005314	EFO:0003929
cysticercosis	3	MONDO:0015484	EFO:0007231
Helicobacter pylori infectious disease	3	MONDO:0006781	EFO:1000961
dyspepsia	3	MONDO:0002268	EFO:0008533
gastric neoplasm	3	MONDO:0021085	MONDO:0001056
exocrine pancreatic insufficiency	3	MONDO:0001684	MONDO:0001684
type 1 diabetes mellitus	3	MONDO:0005147	MONDO:0005147
osteoarthritis	3	MONDO:0005178	MONDO:0005178
peripheral neuropathy	3	MONDO:0005244	EFO:0003100
idiopathic pulmonary fibrosis	2	MONDO:0800504	EFO:0000768
breast carcinoma	2	MONDO:0004989	EFO:0000305
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
MALT lymphoma	2	MONDO:0007650	EFO:0000191
lymphoma	2	MONDO:0005062	EFO:0000574
head and neck cancer	2	MONDO:0005627	EFO:0006859
Zollinger-Ellison syndrome	2	MONDO:0019610	EFO:0007549
breast neoplasm	2	MONDO:0021100	MONDO:0007254
ulcer disease	2	MONDO:0043839	MONDO:0043839
oral cavity squamous cell carcinoma	2	MONDO:0004958	EFO:0000199
pancreatic gastrin-producing neuroendocrine tumor	2	MONDO:0003525	MONDO:0003523
gastritis	2	MONDO:0004966	EFO:0000217
colorectal neoplasm	2	MONDO:0005335	MONDO:0005575
erectile dysfunction	1	MONDO:0005362	EFO:0004234
HIV infectious disease	1	MONDO:0005109	EFO:0000180
atopic eczema	1	MONDO:0004980	EFO:0000274
chronic obstructive pulmonary disease	1	MONDO:0005002	EFO:0000341
Crohn disease	1	MONDO:0005011	EFO:0000384
diabetes mellitus	1	MONDO:0005015	EFO:0000400
neoplasm	1	MONDO:0005070	EFO:0000616
psoriasis	1	MONDO:0005083	EFO:0000676
rheumatoid arthritis	1	MONDO:0008383	EFO:0000685
ulcerative colitis	1	MONDO:0005101	EFO:0000729
hepatitis C virus infection	1	MONDO:0005231	EFO:0003047
autism spectrum disorder	1	MONDO:0005258	EFO:0003756
chronic hepatitis C virus infection	1	MONDO:0005354	EFO:0004220
anemia	1	MONDO:0002280	EFO:0004272
infectious disease	1	MONDO:0005550	EFO:0005741
metastatic melanoma	1	MONDO:0005191	EFO:0002617
Clostridium infectious disease	1	MONDO:0024388	EFO:0009130
central serous chorioretinopathy	1	MONDO:0018616	EFO:0009784
congenital laryngomalacia	1	MONDO:0007878	HP:0001601
spinal muscular atrophy	1	MONDO:0001516	EFO:0008525
chronic hepatitis B virus infection	1	MONDO:0005366	EFO:0004239
Alzheimer disease	1	MONDO:0004975	MONDO:0004975
type 2 diabetes mellitus	1	MONDO:0005148	MONDO:0005148
inborn mitochondrial metabolism disorder	1	MONDO:0004069	MONDO:0044970
prostate adenocarcinoma	1	MONDO:0005082	EFO:0000673
melanoma	1	MONDO:0005105	EFO:0000756
glaucoma	1	MONDO:0005041	MONDO:0005041
sickle cell disease	1	MONDO:0011382	MONDO:0011382
exocrine pancreatic carcinoma	0	MONDO:0005192	EFO:0002618

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

Clinical trials

Total trials: 335.

Phase distribution

Phase	Trials
PHASE1	170
PHASE4	56
PHASE3	41
Not specified	31
PHASE2	22
EARLY_PHASE1	9
PHASE1/PHASE2	5
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05799105	PHASE4	RECRUITING	OPEN Versus InTact Capsule Proton Pump Inhibitors for the Treatment of Marginal Ulcers
NCT06943482	PHASE4	NOT_YET_RECRUITING	Comparing Effectiveness of Steroids and Methotrexate in Treatment of Chronic Inflammatory Breast Disease
NCT06999577	PHASE4	RECRUITING	The Mechanism Versus PPI Trial
NCT07037888	PHASE4	RECRUITING	Efficacy of Ketorolac for Postoperative Pain Management in Hip Arthroscopy: A Prospective Double-Blinded Randomized Controlled Trial
NCT07040839	PHASE4	NOT_YET_RECRUITING	Comparison of Omeprazole vs Vonoprazon in Treatment of H Pylori Infection
NCT00141102	PHASE4	COMPLETED	Study Of Celecoxib Or Diclofenac And Omeprazole For Gastrointestinal (GI) Safety In High GI Risk Patients With Arthritis
NCT00164866	PHASE4	COMPLETED	Administration of High-Dose Intravenous Proton Pump Inhibitor for Upper Gastrointestinal Bleeding Prior to Endoscopy
NCT00247130	PHASE4	WITHDRAWN	Comparison of Intravenous Omeprazole to Ranitidine on Recurrent Bleeding After Endoscopic Treatment of Bleeding Ulcer
NCT00251030	PHASE4	COMPLETED	A Study To Estimate The Effect Of Omeprazole On The Pharmacokinetics Of Nelfinavir In Healthy Subjects
NCT00272467	PHASE4	COMPLETED	Healing Effects of Rebamipide and Omeprazole in Helicobacter Pylori-positive Gastric Ulcer After Eradication Therapy
NCT00475527	PHASE4	WITHDRAWN	Helicobacter Pylori and Iron Deficiency: Prevalence of Association and Effect of Therapy
NCT00492622	PHASE4	COMPLETED	Pharmacokinetics of Immediate-Release vs. Delayed-Release Omeprazole in Gastroparesis
NCT00537732	PHASE4	TERMINATED	Omeprazole and Reflux Disease - Improvement of Clinical Outcome by Genotype-adjusted Dosing
NCT00557349	PHASE4	COMPLETED	Ulcer Prevention Study in Post Gastric Bypass Patients
NCT00582972	PHASE4	COMPLETED	Does Omeprazole Decrease Intestinal Calcium Absorption?
NCT00641264	PHASE4	COMPLETED	Quality of Life Validation in Laryngitis
NCT00693225	PHASE4	COMPLETED	Impact of Timing on the Efficacy of Zegerid 40 mg in Healing Reflux Esophagitis: A Pilot Study
NCT00808769	PHASE4	COMPLETED	Comparison of Prilosec OTC® Versus Zegerid® for Gastric Acid Suppression
NCT00838682	PHASE4	TERMINATED	Effect of High-dose Oral Rabeprazole on Recurrent Bleeding After the Endoscopic Treatment of Bleeding Peptic Ulcers
NCT00861640	PHASE4	UNKNOWN	Comparison of Oral Rabeprazole vs. iv Omeprazole in Mild to Moderate Nonvariceal Upper Gastrointestinal Bleeding
NCT01016717	PHASE4	WITHDRAWN	Clopidogrel Proton-Pump Inhibitors Study
NCT01093755	PHASE4	COMPLETED	Does Intensive Acid Suppression Reduce Esophageal Inflammation and Recurrent Barrett’s Esophagus Following Ablation?
NCT01587885	PHASE4	COMPLETED	Comparison of Two Omeprazole-Containing Products for Relief of Frequent Heartburn (MK-0764A-036)
NCT01735227	PHASE4	UNKNOWN	Omeprazole and Pantoprazole Antiplatelet Effect of Clopidogrel Clinical Trials(OPEN)
NCT01766050	PHASE4	COMPLETED	Study to Evaluate Effect of Belatacept on Pharmacokinetics of Inje Cocktail in Healthy Volunteers
NCT01777854	PHASE4	TERMINATED	Anti-reflux Control to Decrease Post Tonsillectomy Pain
NCT01795794	PHASE4	UNKNOWN	Evaluation of the Efficacy in Decreasing Iron Absorption in Patients With Congenital Dyserythropoietic Anemia Type I by Treatment With LOSEC
NCT01822600	PHASE4	COMPLETED	The Therapeutic Role of Intravenous Albumin Administration for Peptic Ulcer Bleeding Patients With Hypoalbuminemia
NCT01851863	PHASE4	COMPLETED	Compliance With Antidepressant Medication in Treatment of Functional Dyspepsia
NCT01896557	PHASE4	COMPLETED	Ranitidin Versus Omeprazole in Patients Taking Clopidogrel
NCT02013427	PHASE4	COMPLETED	Placebo In Chronic Back Pain - Double-Blind Randomized Control Trial
NCT02028234	PHASE4	UNKNOWN	Pharmacodynamic Comparison of Omeprazole Versus Pantoprazole on Platelet Reactivity in Patients With Acute Coronary Syndromes on Dual Antiplatelet Therapy With New P2Y12 Inhibitors -Trial dOPPLER-
NCT02123498	PHASE4	WITHDRAWN	The Study of Eustachian Tube Dysfunction and Laryngopharyngeal Reflux
NCT02140073	PHASE4	UNKNOWN	Research of Efficient Use of Omeprazole in Combination With Domperidone in Gastroesophageal Reflux Disease of Mild to Moderate Severity
NCT02394340	PHASE4	COMPLETED	Study Evaluating the Drug Interaction Potential of Luliconazole Cream 1% in Participants With Tinea Pedis and Tinea Cruris
NCT02500641	PHASE4	COMPLETED	Intensive Urate Lowering Therapy of Febuxostat Compared to Allopurinol on Cardiovascular Risk in Patients With Gout
NCT02505945	PHASE4	COMPLETED	The CALIBER Study Randomized Controlled Trial of LINX Versus Double-Dose Proton Pump Inhibitor Therapy for Reflux Disease
NCT02530879	PHASE4	WITHDRAWN	Comparison of Voice Therapy and Antireflex Therapy in LPR
NCT02536989	PHASE4	COMPLETED	Different Dose of Intravenous Omeprazole to Treat Bleeding Ulcer With Adherent Clot
NCT02552537	PHASE4	COMPLETED	iFAAM: The Impact of Proton-pump Inhibitors (Antacids) on Threshold Dose Distributions

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (2) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for omeprazole and CYP2C19	DPWG	CYP2C19	yes	yes
Annotation of CPIC Guideline for lansoprazole, omeprazole, pantoprazol	CPIC	CYP2C19	yes	yes

PharmGKB also curates 5 clinical and 185 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.

4 molecules share ≥1 primary target. Top 4 by shared-target count:

Molecule	Source	Status	Shared targets
CIMETIDINE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
LANSOPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
PANTOPRAZOLE	ChEMBL + PubChem	Phase 4 (approved)	ATP4A
RANITIDINE	ChEMBL	Phase 4 (approved)	ATP4A