Sumanirole

Summary

Sumanirole (CHEMBL419792) is a phase-3 clinical-stage small molecule targeting DRD2; indicated across 1 condition including parkinson disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (DRD2)
• Indications: 1 condition
• Clinical trials: 3
• Chemistry: 203.24 Da · C11H13N3O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL419792
Name	Sumanirole
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9818479
Molecular formula	C11H13N3O
Molecular weight	203.24
InChIKey	RKZSNTNMEFVBDT-MRVPVSSYSA-N

SMILES: CN[C@@H]1CC2=C3C(=CC=C2)NC(=O)N3C1

IUPAC name: (10R)-10-(methylamino)-1,3-diazatricyclo[6.3.1.04,12]dodeca-4,6,8(12)-trien-2-one

Also known as: Pnu-95666, PNU-95666E, Sumanirol, Sumanirole, SID174006884, sumanirole, SUMANIROLE

Parent form; salt/anhydrous children: CHEMBL5071215

Patent coverage: 298 distinct patent families (1,016 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,008 (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
DRD2	D2 receptor	Full agonist	8.1	0%	P14416

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: 5-hydroxytryptamine receptor 1A, D(2) dopamine receptor, D(3) dopamine receptor, D(2) dopamine receptor.

Bioactivity

ChEMBL activities: 23 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DRD2	8.34	EC50	4.6	nM	CHEMBL_ACT_16566550
DRD2	8.05	Ki	9	nM	CHEMBL_ACT_123808
P61169	7.97	EC50	10.8	nM	CHEMBL_ACT_810474
DRD2	7.77	Ki	17.1	nM	CHEMBL_ACT_16565170
DRD2	7.49	EC50	32.2	nM	CHEMBL_ACT_18049331
P61169	7.46	EC50	35	nM	CHEMBL_ACT_810473
DRD2	7.33	Ki	46.3	nM	CHEMBL_ACT_18049393
DRD2	7.22	EC50	60.1	nM	CHEMBL_ACT_16566439
DRD2	7.19	EC50	64.7	nM	CHEMBL_ACT_16566495
HTR1A	7.14	Ki	73	nM	CHEMBL_ACT_123810
DRD2	7.13	EC50	74.8	nM	CHEMBL_ACT_18049526
DRD2	7.09	Ki	80.6	nM	CHEMBL_ACT_24988491
DRD2	6.78	EC50	165	nM	CHEMBL_ACT_810472
DRD3	6.73	EC50	186	nM	CHEMBL_ACT_16566467
DRD2	6.3	EC50	501.2	nM	CHEMBL_ACT_18049416
DRD3	6.26	Ki	546	nM	CHEMBL_ACT_16565154
DRD2	6.26	EC50	543.3	nM	CHEMBL_ACT_18049471
DRD3	6.24	Ki	573	nM	CHEMBL_ACT_18049372
DRD3	6.17	EC50	669	nM	CHEMBL_ACT_16566523
DRD3	6.11	Ki	784	nM	CHEMBL_ACT_24988510
DRD3	5.63	Ki	2333	nM	CHEMBL_ACT_123809
DRD3	5.2	Ki	6330	nM	CHEMBL_ACT_16566403
DRD3	5.2	Ki	6330	nM	CHEMBL_ACT_24988567

Target pathways

Aggregated over 1 target gene(s): DRD2.

Top Reactome pathways

1 total, by targets touching each:

Pathway	Targets	Genes
Dopamine receptors	1	DRD2

Dominant GO biological processes

GO term	Targets
temperature homeostasis	1
response to hypoxia	1
response to amphetamine	1
nervous system process involved in regulation of systemic arterial blood pressure	1
regulation of heart rate	1
regulation of sodium ion transport	1
G protein-coupled receptor internalization	1
positive regulation of neuroblast proliferation	1
positive regulation of receptor internalization	1
intracellular calcium ion homeostasis	1
autophagy	1
adenylate cyclase-inhibiting dopamine receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuron-neuron synaptic transmission	1
neuroblast proliferation	1

Indications & clinical

Indications

1 indication (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
Parkinson disease	3	MONDO:0005180	MONDO:0005180

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE3	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00036205	PHASE3	TERMINATED	Open Label Sumanirole Study of Safety, Tolerability, and Therapeutic Response In Patients With Parkinson’s Disease
NCT00036218	PHASE3	COMPLETED	Study Evaluating Sumanirole for the Treatment of the Signs and Symptoms of Early Parkinson’s Disease.
NCT00058838	PHASE3	COMPLETED	Study Evaluating Sumanirole for the Treatment of the Signs and Symptoms of Early Parkinson’s Disease

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

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.

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

Molecule	Source	Status	Shared targets
DIHYDROERGOTAMINE	ChEMBL + PubChem	Phase 4 (approved)	DRD2
ACETOPHENAZINE	ChEMBL	Phase 4 (approved)	DRD2
AMIODARONE	ChEMBL	Phase 4 (approved)	DRD2
AMISULPRIDE	ChEMBL	Phase 4 (approved)	DRD2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2
AMLODIPINE	ChEMBL	Phase 4 (approved)	DRD2
AMODIAQUINE	ChEMBL	Phase 4 (approved)	DRD2
AMOXAPINE	ChEMBL	Phase 4 (approved)	DRD2
AMSACRINE	ChEMBL	Phase 4 (approved)	DRD2
APOMORPHINE	ChEMBL	Phase 4 (approved)	DRD2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	DRD2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2
ARMODAFINIL	ChEMBL	Phase 4 (approved)	DRD2
ASENAPINE	ChEMBL	Phase 4 (approved)	DRD2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	DRD2
AZATADINE	ChEMBL	Phase 4 (approved)	DRD2
AZELASTINE	ChEMBL	Phase 4 (approved)	DRD2
BAZEDOXIFENE	ChEMBL	Phase 4 (approved)	DRD2
BENPERIDOL	ChEMBL	Phase 4 (approved)	DRD2
BENZQUINAMIDE	ChEMBL	Phase 4 (approved)	DRD2
BENZTROPINE	ChEMBL	Phase 4 (approved)	DRD2
BEPRIDIL	ChEMBL	Phase 4 (approved)	DRD2
BETAMETHASONE DIPROPIONATE	ChEMBL	Phase 4 (approved)	DRD2
BLONANSERIN	ChEMBL	Phase 4 (approved)	DRD2
BOSUTINIB	ChEMBL	Phase 4 (approved)	DRD2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	DRD2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	DRD2
BROMPERIDOL	ChEMBL	Phase 4 (approved)	DRD2
BUSPIRONE	ChEMBL	Phase 4 (approved)	DRD2
BUTRIPTYLINE	ChEMBL	Phase 4 (approved)	DRD2
CABERGOLINE	ChEMBL	Phase 4 (approved)	DRD2
CANNABIDIOL	ChEMBL	Phase 4 (approved)	DRD2
CARIPRAZINE	ChEMBL	Phase 4 (approved)	DRD2
CARVEDILOL	ChEMBL	Phase 4 (approved)	DRD2
CEFEPIME	ChEMBL	Phase 4 (approved)	DRD2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	DRD2
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	DRD2
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	DRD2
CINACALCET	ChEMBL	Phase 4 (approved)	DRD2
CINNARIZINE	ChEMBL	Phase 4 (approved)	DRD2
CISAPRIDE	ChEMBL	Phase 4 (approved)	DRD2
CLEMASTINE	ChEMBL	Phase 4 (approved)	DRD2
CLOFAZIMINE	ChEMBL	Phase 4 (approved)	DRD2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	DRD2
CLOZAPINE	ChEMBL	Phase 4 (approved)	DRD2
CYCLOBENZAPRINE	ChEMBL	Phase 4 (approved)	DRD2
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	DRD2
DACOMITINIB	ChEMBL	Phase 4 (approved)	DRD2
DARIFENACIN	ChEMBL	Phase 4 (approved)	DRD2
DAUNORUBICIN	ChEMBL	Phase 4 (approved)	DRD2
DESIPRAMINE	ChEMBL	Phase 4 (approved)	DRD2
DESLORATADINE	ChEMBL	Phase 4 (approved)	DRD2
DIBENZEPIN	ChEMBL	Phase 4 (approved)	DRD2
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	DRD2
DIPHENIDOL	ChEMBL	Phase 4 (approved)	DRD2
DISULFIRAM	ChEMBL	Phase 4 (approved)	DRD2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	DRD2
DOMPERIDONE	ChEMBL	Phase 4 (approved)	DRD2
DOPAMINE	ChEMBL	Phase 4 (approved)	DRD2