Mesoridazine

Summary

Mesoridazine (CHEMBL1088) is an approved small-molecule dopaminergic antagonist (ATC N05AC03) targeting HTR1A, DRD1, and DRD2; indicated across 1 condition including psychotic disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N05AC03
• Targets: 6 (HTR1A, DRD1, DRD2…)
• Indications: 1 condition
• Chemistry: 386.6 Da · C21H26N2OS2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1088
Name	Mesoridazine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4078
ChEBI	CHEBI:6780
ATC	N05AC03
Molecular formula	C21H26N2OS2
Molecular weight	386.6
InChIKey	SLVMESMUVMCQIY-UHFFFAOYSA-N

SMILES: CN1CCCCC1CCN2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)C

IUPAC name: 10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfinylphenothiazine

ChEBI definition: A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group.

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

Also known as: Lidanar, Mesoridazina, Mesoridazine, NC-123, NSC-186066, TPS-23, mesoridazine, SID26756521, SID447728, MESORIDAZINE, SID144203603, SID144205571

Parent form; salt/anhydrous children: CHEMBL1201052

Patent coverage: 3,218 distinct patent families (12,814 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 12,748 (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
HTR1A	5-HT1A receptor	Antagonist	6.98	0%	P08908
DRD1	D1 receptor	Antagonist	6.99	0%	P21728
DRD2	D2 receptor	Antagonist	8.66	0%	P14416
DRD3	D3 receptor	Antagonist	7.64	0%	P35462
HTR2A	5-HT2A receptor	Antagonist	7.26	0%	P28223
HTR2C	5-HT2C receptor	Antagonist	6.39	0%	P28335

Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: Microtubule-associated protein tau, Alpha-2A adrenergic receptor, D(1A) dopamine receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 1A, Sodium-dependent noradrenaline transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor, D(3) dopamine receptor, Sodium-dependent dopamine transporter.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 18 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRA1A	7.77	AC50	17.1	nM	CHEMBL_ACT_25218727
DRD3	7.71	AC50	19.7	nM	CHEMBL_ACT_25194379
DRD1	7.15	AC50	71.2	nM	CHEMBL_ACT_25115063
CHRM2	6.82	AC50	153	nM	CHEMBL_ACT_25195589
HTR1A	6.67	AC50	214.4	nM	CHEMBL_ACT_25164877
KCNH2	6.5	IC50	320	nM	CHEMBL_ACT_2295026
KCNH2	6.5	IC50	320	nM	CHEMBL_ACT_2295137
KCNH2	6.5	IC50	316.2	nM	CHEMBL_ACT_5218929
KCNH2	6.49	IC50	323.6	nM	CHEMBL_ACT_1056883
KCNH2	6.49	IC50	323.6	nM	CHEMBL_ACT_2358296
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_1523681
ADRA2A	5.59	AC50	2587	nM	CHEMBL_ACT_25156282
OPRM1	5.52	AC50	2991	nM	CHEMBL_ACT_25158028
KCNH2	5.44	AC50	3600	nM	CHEMBL_ACT_25117376

Target pathways

Aggregated over 6 target gene(s): HTR1A, DRD1, DRD2, DRD3, HTR2A, HTR2C.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	3	HTR1A, HTR2A, HTR2C
Signaling by GPCR	3	HTR1A, HTR2A, HTR2C
Class A/1 (Rhodopsin-like receptors)	3	HTR1A, HTR2A, HTR2C
Amine ligand-binding receptors	3	HTR1A, HTR2A, HTR2C
Dopamine receptors	3	DRD1, DRD2, DRD3
Serotonin receptors	3	HTR1A, HTR2A, HTR2C
GPCR ligand binding	3	HTR1A, HTR2A, HTR2C
GPCR downstream signalling	2	HTR2A, HTR2C
G alpha (q) signalling events	2	HTR2A, HTR2C
G alpha (s) signalling events	1	DRD1
G alpha (i) signalling events	1	DRD3

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	6
signal transduction	6
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	4
response to xenobiotic stimulus	4
behavioral response to cocaine	4
locomotory behavior	4
response to cocaine	4
intracellular calcium ion homeostasis	4
behavioral fear response	3
serotonin receptor signaling pathway	3
chemical synaptic transmission	3
G protein-coupled serotonin receptor signaling pathway	3
temperature homeostasis	3
visual learning	3
dopamine metabolic process	3

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, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

820 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
DESLORATADINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
Fidaxomicin	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
Propoxyphene	ChEMBL + PubChem	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
DOXEPIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
EBASTINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ERGOTAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
FLUPHENAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
HALOPERIDOL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ILOPERIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
IMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
KETANSERIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
LOXAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
LURASIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
MAPROTILINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
METHYLERGONOVINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
METHYSERGIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
MIANSERIN	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
NEFAZODONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
OLANZAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PERGOLIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PHENOXYBENZAMINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PIMOZIDE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PROMAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
PROMETHAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
QUETIAPINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
RISPERIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
SERTINDOLE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
SUNITINIB	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
TEGASEROD	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
TERFENADINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
THIORIDAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
THIOTHIXENE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
TRAZODONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
TRIFLUOPERAZINE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
VERAPAMIL	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
ZIPRASIDONE	ChEMBL	Phase 4 (approved)	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
LISURIDE	ChEMBL	Phase 3	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C
MELITRACEN	ChEMBL	Phase 3	DRD1, DRD2, DRD3, HTR1A, HTR2A, HTR2C