Triflupromazine

Summary

Triflupromazine (CHEMBL570) is an approved small-molecule dopaminergic antagonist (ATC N05AA05); indicated across 1 condition including psychotic disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AA05
• Indications: 1 condition
• Chemistry: 352.4 Da · C18H19F3N2S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL570
Name	Triflupromazine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5568
ChEBI	CHEBI:9711
ATC	N05AA05
Molecular formula	C18H19F3N2S
Molecular weight	352.4
InChIKey	XSCGXQMFQXDFCW-UHFFFAOYSA-N

SMILES: CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)C(F)(F)F

IUPAC name: N,N-dimethyl-3-[2-(trifluoromethyl)phenothiazin-10-yl]propan-1-amine

ChEBI definition: A member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(dimethylamino)propyl group at the N-10 position.

Pharmacological roles (ChEBI): dopaminergic antagonist, antiemetic, first generation antipsychotic, anticoronaviral agent.

Also known as: Nivoman, Triflupromazina, Triflupromazine, Vesprin, Vetame, SID11111873, SID11111874, SID90341005, TRIFLUPROMAZINE, SID124881619, SID50100355, SID50104262

Parent form; salt/anhydrous children: CHEMBL1201102

Patent coverage: 2,141 distinct patent families (7,507 SureChEMBL compound mentions), from 1 matched compound structure(s). 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
	Maxi Cl-

Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Thrombopoietin, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, Pleiotropic ABC efflux transporter of multiple drugs, Alpha-2A adrenergic receptor, Thyrotropin receptor, D(1A) dopamine receptor, Thromboxane A2 receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 23 potent at pChembl ≥ 5 of 39 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD3	8.52	AC50	3	nM	CHEMBL_ACT_25194240
ADRA1A	8.48	AC50	3.3	nM	CHEMBL_ACT_25218601
DRD1	7.77	AC50	17.1	nM	CHEMBL_ACT_25114919
SLC6A4	7.08	AC50	82.9	nM	CHEMBL_ACT_25151036
SLC6A2	6.97	AC50	108	nM	CHEMBL_ACT_25145709
P08482	6.8	Potency	158.5	nM	CHEMBL_ACT_4807411
CHRM1	6.72	AC50	192.2	nM	CHEMBL_ACT_25209959
CYP2D6	6.4	Potency	398.1	nM	CHEMBL_ACT_4973896
CYP2D6	6.4	AC50	398.1	nM	CHEMBL_ACT_5986696
CHRM2	6.23	AC50	591	nM	CHEMBL_ACT_25195445
HTR1A	6.18	AC50	654.3	nM	CHEMBL_ACT_25164733
CYP2D6	6.1	Potency	794.3	nM	CHEMBL_ACT_4990253
CYP2D6	6.1	AC50	794.3	nM	CHEMBL_ACT_5987423
CYP1A2	6.1	AC50	794.3	nM	CHEMBL_ACT_6003401
ADRA2A	6.04	AC50	922.7	nM	CHEMBL_ACT_25156138
P08482	6	Potency	1000	nM	CHEMBL_ACT_4857742
CYP1A2	5.8	AC50	1585	nM	CHEMBL_ACT_6063804
OPRM1	5.71	AC50	1950	nM	CHEMBL_ACT_25157884
KCNH2	5.46	AC50	3500	nM	CHEMBL_ACT_25117095
SLC6A3	5.36	AC50	4385	nM	CHEMBL_ACT_25124668
P33302	5.31	IC50	4900	nM	CHEMBL_ACT_5306653
P81908	5.13	IC50	7400	nM	CHEMBL_ACT_6217880
P15917	5	Potency	10000	nM	CHEMBL_ACT_4655553

Target pathways

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

Indications & clinical

Indications

1 indication (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
psychotic disorder	4	MONDO:0005485	EFO:0005407

Clinical trials

Total trials: 0.

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).