Ebselen

Summary

Ebselen (CHEMBL51085) is a phase-3 clinical-stage small-molecule neuroprotective agent; indicated across 8 conditions including meniere disease and hearing loss disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 8 conditions
• Clinical trials: 11
• Chemistry: 274.19 Da · C13H9NOSe

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL51085
Name	Ebselen
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3194
ChEBI	CHEBI:77543
Molecular formula	C13H9NOSe
Molecular weight	274.19
InChIKey	DYEFUKCXAQOFHX-UHFFFAOYSA-N

SMILES: C1=CC=C(C=C1)N2C(=O)C3=CC=CC=C3[Se]2

IUPAC name: 2-phenyl-1,2-benzoselenazol-3-one

ChEBI definition: A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.

Pharmacological roles (ChEBI): neuroprotective agent, apoptosis inducer, anti-inflammatory drug, antioxidant, hepatoprotective agent, genotoxin, radical scavenger, enzyme mimic, EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP+)] inhibitor, EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor, EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor, EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor, EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor, EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, EC 3.5.4.1 (cytosine deaminase) inhibitor, EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor, ferroptosis inhibitor, antifungal agent, EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor, anticoronaviral agent, antibacterial agent, antineoplastic agent, EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor.

Also known as: DR-3305, DR3305, Ebselen, Ebselene, Ebseleno, NSC-639762, NSC-757883, SPI-1005, ebselen, SID11111148, SID11111149, SID26751591

Patent coverage: 3,444 distinct patent families (13,237 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 13,154 (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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	CoV Papain-like protease	Inhibition	5.7

Broader ChEMBL bioactivity targets: 83 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Pyruvate kinase PKM, NADPH oxidase 2, NADPH oxidase 1, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Streptokinase A, Nuclear receptor ROR-gamma, Fructose-bisphosphate aldolase, Prelamin-A/C.

Bioactivity

ChEMBL activities: 155 potent at pChembl ≥ 5 of 207 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.7	Potency	2	nM	CHEMBL_ACT_3621882
P18177	8.16	IC50	6.9	nM	CHEMBL_ACT_25452281
P0DTD1	8	IC50	10	nM	CHEMBL_ACT_25720688
GALE	7.85	IC50	14	nM	CHEMBL_ACT_1809342
IDE	7.85	IC50	14	nM	CHEMBL_ACT_19237636
P18177	7.76	IC50	17.2	nM	CHEMBL_ACT_18921892
TDP1	7.75	Potency	17.8	nM	CHEMBL_ACT_3933135
P15917	7.7	Potency	20	nM	CHEMBL_ACT_4671372
P0DTD1	7.52	IC50	30	nM	CHEMBL_ACT_19964266
P0DTD1	7.4	IC50	40	nM	CHEMBL_ACT_29250045
IDE	7.38	IC50	42	nM	CHEMBL_ACT_19237613
TDP1	7.25	Potency	56.2	nM	CHEMBL_ACT_3935691
TDP1	7.25	Potency	56.2	nM	CHEMBL_ACT_3951139
ALOX15	7.2	Potency	63.1	nM	CHEMBL_ACT_4466773
C7C422	7.14	IC50	72	nM	CHEMBL_ACT_29253132
HDAC2	7.1	Ki	80	nM	CHEMBL_ACT_25452276
CYP2C9	7.1	Potency	79.4	nM	CHEMBL_ACT_5029598
IDO1	7.03	Ki	94	nM	CHEMBL_ACT_16419289
IDO1	7.03	Ki	94	nM	CHEMBL_ACT_19051884
IDO1	7.03	Ki	94	nM	CHEMBL_ACT_24834436
P0DTD1	7.01	Ki	97	nM	CHEMBL_ACT_29297619
EPHX2	6.96	IC50	110	nM	CHEMBL_ACT_19307314
PHOSPHO1	6.96	IC50	111	nM	CHEMBL_ACT_5566652
P0DTD1	6.92	IC50	120	nM	CHEMBL_ACT_29108267
CYP2C19	6.9	Potency	125.9	nM	CHEMBL_ACT_4006175
ALDH1A1	6.9	Potency	125.9	nM	CHEMBL_ACT_4173037
ALDH1A1	6.9	Potency	125.9	nM	CHEMBL_ACT_4193958
TDP1	6.85	Potency	141.3	nM	CHEMBL_ACT_3931756
ATG4B	6.75	IC50	180	nM	CHEMBL_ACT_25872962
ATG4B	6.72	IC50	189	nM	CHEMBL_ACT_29205878

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

8 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
Meniere disease	3	MONDO:0007972	EFO:0006862
hearing loss disorder	2	MONDO:0005365	EFO:0004238
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
type 1 diabetes mellitus	2	MONDO:0005147	MONDO:0005147
type 2 diabetes mellitus	2	MONDO:0005148	MONDO:0005148
bipolar disorder	2	MONDO:0004985	MONDO:0004985
depressive disorder	1	MONDO:0002050	MONDO:0002050

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

Clinical trials

Total trials: 11.

Phase distribution

Phase	Trials
PHASE2	5
PHASE3	2
PHASE1	2
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06859788	PHASE3	RECRUITING	SPI-1005 for the Treatment of Meniere’s Disease (Open Label)
NCT00762671	PHASE2/PHASE3	COMPLETED	Signaling Mechanisms and Vascular Function in Patients With Diabetes Mellitus
NCT04677972	PHASE3	COMPLETED	SPI-1005 for the Treatment of Meniere’s Disease
NCT06340633	PHASE2	RECRUITING	SPI-1005 in Adults Receiving Cochlear Implant
NCT02603081	PHASE1/PHASE2	COMPLETED	Study to Evaluate SPI-1005 in Adults With Meniere’s Disease
NCT02779192	PHASE2	UNKNOWN	A Phase 2b Study of SPI-1005 to Prevent Acute Noise Induced Hearing Loss
NCT03013400	PHASE2	COMPLETED	Ebselen as an add-on Treatment in Hypo/Mania
NCT04483973	PHASE2	UNKNOWN	SPI-1005 Treatment in Severe COVID-19 Patients
NCT04484025	PHASE2	UNKNOWN	SPI-1005 Treatment in Moderate COVID-19 Patients
NCT01452607	PHASE1	COMPLETED	Study to Evaluate the Safety and Pharmacokinetics of SPI-1005
NCT05117710	PHASE1	UNKNOWN	IMPase in Treatment-resistant Depression

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).