Tiapride

Summary

Tiapride (CHEMBL84158) is a phase-3 clinical-stage small molecule (ATC N05AL03); indicated across 7 conditions including anxiety and dementia.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: N05AL03
• Indications: 7 conditions
• Clinical trials: 2
• Chemistry: 328.4 Da · C15H24N2O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL84158
Name	Tiapride
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	5467
ATC	N05AL03
Molecular formula	C15H24N2O4S
Molecular weight	328.4
InChIKey	JTVPZMFULRWINT-UHFFFAOYSA-N

SMILES: CCN(CC)CCNC(=O)C1=C(C=CC(=C1)S(=O)(=O)C)OC

IUPAC name: N-[2-(diethylamino)ethyl]-2-methoxy-5-methylsulfonylbenzamide

Also known as: NSC-758225, Tiaprida, Tiapride, SID11111853, SID11111854, SID90340591, TIAPRIDE, TIAPRIDE HYDROCHLORIDE, tiapride

Parent form; salt/anhydrous children: CHEMBL1256772

Patent coverage: 1,035 distinct patent families (3,518 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,467 (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

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Prelamin-A/C, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Thyrotropin receptor, D(2) dopamine receptor, D(3) dopamine receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Muscarinic acetylcholine receptor M1, Cytochrome P450 2D6, Cytochrome P450 2C9.

Bioactivity

ChEMBL activities: 16 potent at pChembl ≥ 5 of 21 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	8.15	Potency	7.1	nM	CHEMBL_ACT_3634453
DRD2	6.52	AC50	300	nM	CHEMBL_ACT_25141015
P08482	6.45	Potency	354.8	nM	CHEMBL_ACT_4807499
DRD3	6.44	AC50	360	nM	CHEMBL_ACT_25194198
DRD3	6.41	Ki	390	nM	CHEMBL_ACT_7804281
DRD2	6.39	Ki	411	nM	CHEMBL_ACT_7804279
ADRA2A	6.11	Ki	779	nM	CHEMBL_ACT_7802178
DRD3	5.94	IC50	1149	nM	CHEMBL_ACT_7804280
DRD2	5.91	IC50	1232	nM	CHEMBL_ACT_7804278
ADRA2A	5.68	IC50	2078	nM	CHEMBL_ACT_7802177
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_3914609
TSHR	5.2	Potency	6310	nM	CHEMBL_ACT_4715090
CYP2D6	5.1	Potency	7943	nM	CHEMBL_ACT_4961576
CYP2D6	5.1	AC50	7943	nM	CHEMBL_ACT_6046011
KCNH2	5.07	AC50	8500	nM	CHEMBL_ACT_25118846
P08482	5	Potency	10000	nM	CHEMBL_ACT_4857812

Target pathways

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

Indications & clinical

Indications

7 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
anxiety	3	MONDO:0011918	EFO:0005230
dementia	3	MONDO:0001627	HP:0000726
Tourette syndrome	3	MONDO:0007661	EFO:0004895
psychotic disorder	3	MONDO:0005485	EFO:0005407
depressive disorder	3	MONDO:0002050	MONDO:0002050
tic disorder	3	MONDO:0002420	MONDO:0001074

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

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01501695	PHASE3	COMPLETED	Phase III Study of 5LGr to Treat Tic Disorder
NCT02374567	PHASE3	TERMINATED	Pharmacovigilance in Gerontopsychiatric Patients

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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