Enoxacin

Summary

Enoxacin (CHEMBL826) is an approved small-molecule antibacterial drug (ATC J01MA04) targeting ATP6V1B2; indicated across 3 conditions including bacterial infectious disease and amyotrophic lateral sclerosis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01MA04
• Targets: 1 (ATP6V1B2)
• Indications: 3 conditions
• Clinical trials: 1
• Chemistry: 320.32 Da · C15H17FN4O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL826
Name	Enoxacin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3229
ChEBI	CHEBI:157175
ATC	J01MA04
Molecular formula	C15H17FN4O3
Molecular weight	320.32
InChIKey	IDYZIJYBMGIQMJ-UHFFFAOYSA-N

SMILES: CCN1C=C(C(=O)C2=CC(=C(N=C21)N3CCNCC3)F)C(=O)O

IUPAC name: 1-ethyl-6-fluoro-4-oxo-7-piperazin-1-yl-1,8-naphthyridine-3-carboxylic acid

ChEBI definition: A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.

Pharmacological roles (ChEBI): antibacterial drug, DNA synthesis inhibitor.

Also known as: AT-2266, CI-919, Comprecin, Enoxacin, Enoxacine, Enoxacino, Flumark, NSC-629661, NSC-758416, PD 107779, PD-107779, Penetrex

Patent coverage: 6,867 distinct patent families (25,001 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 24,889 (100%) 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
ATP6V1B2	V-type ATPase V1 motor B2 subunit	Inhibition	5	97.3% (common-essential)	P21281

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Prelamin-A/C, Thromboxane A2 receptor, DNA gyrase, RISC-loading complex subunit TARBP2, Endothelin-1 receptor, Cytochrome P450 2C9, V-type proton ATPase subunit B, brain isoform.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
TARBP2	7.03	Kd	94	nM	CHEMBL_ACT_22481908
LMNA	5.9	Potency	1259	nM	CHEMBL_ACT_3661300
TBXA2R	5.22	AC50	6060	nM	CHEMBL_ACT_25155218
ATP6V1B2	5	IC50	10000	nM	CHEMBL_ACT_2709867

Target pathways

Aggregated over 1 target gene(s): ATP6V1B2.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
ROS and RNS production in phagocytes	1	ATP6V1B2
Insulin receptor recycling	1	ATP6V1B2
Transferrin endocytosis and recycling	1	ATP6V1B2
Amino acids regulate mTORC1	1	ATP6V1B2
Ion channel transport	1	ATP6V1B2
Regulation of MITF-M-dependent genes involved in lysosome biogenesis and autophagy	1	ATP6V1B2

Dominant GO biological processes

GO term	Targets
vacuolar acidification	1
regulation of macroautophagy	1
ATP metabolic process	1
synaptic vesicle lumen acidification	1
proton transmembrane transport	1
monoatomic ion transport	1

Indications & clinical

Indications

3 indications (1 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
bacterial infectious disease	4	MONDO:0005113	EFO:0000771
amyotrophic lateral sclerosis	1	MONDO:0004976	MONDO:0004976
osteomyelitis	0	MONDO:0005246	EFO:0003102

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04840823	PHASE1/PHASE2	COMPLETED	Enoxacin for Amyotrophic Lateral Sclerosis (ALS)

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).