Zaleplon

Summary

Zaleplon (CHEMBL1521) is an approved small-molecule anticonvulsant (ATC N05CF03); indicated across 6 conditions including insomnia and anxiety.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05CF03
• Indications: 6 conditions
• Clinical trials: 9
• Chemistry: 305.33 Da · C17H15N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1521
Name	Zaleplon
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5719
ChEBI	CHEBI:10102
ATC	N05CF03
Molecular formula	C17H15N5O
Molecular weight	305.33
InChIKey	HUNXMJYCHXQEGX-UHFFFAOYSA-N

SMILES: CCN(C1=CC=CC(=C1)C2=CC=NC3=C(C=NN23)C#N)C(=O)C

IUPAC name: N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide

ChEBI definition: A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.

Pharmacological roles (ChEBI): anticonvulsant, central nervous system depressant, sedative, anxiolytic drug.

Also known as: CL 284,846, CL-284846, L-846, L846, LJC 10846, LJC-10846, LJC10846, SKP-1041, Sonata, ZAL-846, Zaleplon, Zaleplon civ

Patent coverage: 2,587 distinct patent families (9,958 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 9,946 (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

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Lysine-specific demethylase 4E, Ferritin light chain, GABA-A receptor; alpha-2/beta-3/gamma-2, GABA-A receptor; alpha-1/beta-2/gamma-2, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Aldehyde oxidase, Gamma-aminobutyric acid receptor subunit alpha-1, Mitogen-activated protein kinase 1.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
GABRA1	6.54	EC50	290	nM	CHEMBL_ACT_12662654
P62813	6.23	AC50	590	nM	CHEMBL_ACT_25130910
GABRG2	5.79	EC50	1630	nM	CHEMBL_ACT_12662653
PDE3A	5	AC50	10000	nM	CHEMBL_ACT_25191020

Target pathways

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

Indications & clinical

Indications

6 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
insomnia	4	MONDO:0013600	EFO:0004698
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
depressive disorder	3	MONDO:0002050	MONDO:0002050
sleep disorder	2	MONDO:0100081	EFO:0008568

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

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
Not specified	6
PHASE4	1
PHASE3	1
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01159652	PHASE4	COMPLETED	Hypnotic Medications and Memory: Effect of Drug Exposure During the Night
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients
NCT03489304	PHASE2	COMPLETED	Zaleplon in HIV Patients With Depression
NCT05745038	Not specified	RECRUITING	A Single Arm Pilot Trial of a Social Network Intervention
NCT07393529	Not specified	RECRUITING	A Pilot Randomized Controlled Trial of a Social Network Intervention
NCT00694187	Not specified	COMPLETED	Bioequivalency Study of Zaleplon 10 mg Capsules Under Fasting Conditions
NCT00694317	Not specified	COMPLETED	Bioequivalency Study of Zaleplon 10 mg Capsules Under Fed Conditions
NCT03118037	Not specified	TERMINATED	Transcervical Radiofrequency Ablation of Uterine Fibroids Global Registry
NCT03304652	Not specified	COMPLETED	Cerebral MRI During Sleep

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).