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Atlas / Drug / Benperidol

Benperidol

drug
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Also known as AnquilBenquilMCN-JR-4584NSC-170982R-4584SID11112508SID56463215SID144204068SID170466409

Summary

Benperidol (CHEMBL297302) is an approved small molecule (ATC N05AD07) targeting DRD2 and DRD4; indicated across 5 conditions including psychotic disorder and anxiety.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05AD07
  • Targets: 2 (DRD2, DRD4)
  • Indications: 5 conditions
  • Clinical trials: 2
  • Chemistry: 381.4 Da · C22H24FN3O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL297302
NameBenperidol
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID16363
ATCN05AD07
Molecular formulaC22H24FN3O2
Molecular weight381.4
InChIKeyFEBOTPHFXYHVPL-UHFFFAOYSA-N

SMILES: C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCCC(=O)C4=CC=C(C=C4)F

IUPAC name: 3-[1-[4-(4-fluorophenyl)-4-oxobutyl]piperidin-4-yl]-1H-benzimidazol-2-one

Also known as: Anquil, Benperidol, Benquil, MCN-JR-4584, NSC-170982, R-4584, SID11112508, SID56463215, BENPERIDOL, SID144204068, SID170466409, benperidol

Patent coverage: 886 distinct patent families (3,400 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,390 (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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
DRD2D2 receptorAntagonist10.570%P14416
DRD4D4 receptorAntagonist10.180%P21917

Broader ChEMBL bioactivity targets: 31 (assay-derived). Sample: Prelamin-A/C, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, D(1A) dopamine receptor, Progesterone receptor, Beta-2 adrenergic receptor, Muscarinic acetylcholine receptor M2, Beta-1 adrenergic receptor.

Bioactivity

ChEMBL activities: 26 potent at pChembl ≥ 5 of 37 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
DRD210.57Ki0.03nMCHEMBL_ACT_16630085
DRD410.18Ki0.07nMCHEMBL_ACT_16630086
DRD39.54Ki0.29nMCHEMBL_ACT_16630087
HTR2A8.92Ki1.2nMCHEMBL_ACT_16630088
HTR2A8.46AC503.5nMCHEMBL_ACT_25173545
DRD38.28AC505.3nMCHEMBL_ACT_25193331
DRD28.11AC507.7nMCHEMBL_ACT_25140132
ADRA1A7.15AC5070.6nMCHEMBL_ACT_25217927
KCNH26.96AC50110nMCHEMBL_ACT_25117584
HTR2A6.92AC50120nMCHEMBL_ACT_25224995
HTR1A6.78AC50165.6nMCHEMBL_ACT_25215876
HRH16.14AC50730nMCHEMBL_ACT_25212310
HIF1A6.1Potency794.3nMCHEMBL_ACT_4131639
HIF1A6.1Potency794.3nMCHEMBL_ACT_4519162
ADRA2B6.07AC50850nMCHEMBL_ACT_25143506
OPRK15.94AC501149nMCHEMBL_ACT_25129248
LMNA5.8Potency1585nMCHEMBL_ACT_3648578
ADRA2C5.72AC501900nMCHEMBL_ACT_25147676
CHRM25.58AC502640nMCHEMBL_ACT_25213552
CYP2D65.2Potency6310nMCHEMBL_ACT_4973988
CYP2D65.2AC506310nMCHEMBL_ACT_6006480
HTR2B5.18AC506587nMCHEMBL_ACT_25227341
P152075.15AC507100nMCHEMBL_ACT_25232764
DRD15.12AC507500nMCHEMBL_ACT_25181241
ADRB15.07AC508500nMCHEMBL_ACT_25121584
ADRB25.07AC508600nMCHEMBL_ACT_25122721

Target pathways

Aggregated over 2 target gene(s): DRD2, DRD4.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
Dopamine receptors2DRD2, DRD4
G alpha (i) signalling events1DRD4

Dominant GO biological processes

GO termTargets
response to amphetamine2
intracellular calcium ion homeostasis2
adenylate cyclase-inhibiting dopamine receptor signaling pathway2
response to histamine2
behavioral response to cocaine2
behavioral response to ethanol2
arachidonate secretion2
negative regulation of protein secretion2
positive regulation of dopamine uptake involved in synaptic transmission2
phospholipase C-activating dopamine receptor signaling pathway2
synaptic transmission, dopaminergic2
signal transduction2
G protein-coupled receptor signaling pathway2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway2
adult behavior2

Indications & clinical

Indications

5 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).

IndicationTrial phaseMONDOEFO
psychotic disorder4MONDO:0005485EFO:0005407
anxiety3MONDO:0011918EFO:0005230
dementia3MONDO:0001627HP:0000726
depressive disorder3MONDO:0002050MONDO:0002050

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

PhaseTrials
PHASE41
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02307396PHASE4COMPLETEDEvaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients
NCT02374567PHASE3TERMINATEDPharmacovigilance 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.

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.

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

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)DRD2, DRD4
AMIODARONEChEMBLPhase 4 (approved)DRD2, DRD4
AMITRIPTYLINEChEMBLPhase 4 (approved)DRD2, DRD4
AMOXAPINEChEMBLPhase 4 (approved)DRD2, DRD4
APOMORPHINEChEMBLPhase 4 (approved)DRD2, DRD4
ARIPIPRAZOLEChEMBLPhase 4 (approved)DRD2, DRD4
ASENAPINEChEMBLPhase 4 (approved)DRD2, DRD4
ASTEMIZOLEChEMBLPhase 4 (approved)DRD2, DRD4
BREXPIPRAZOLEChEMBLPhase 4 (approved)DRD2, DRD4
BROMOCRIPTINEChEMBLPhase 4 (approved)DRD2, DRD4
CABERGOLINEChEMBLPhase 4 (approved)DRD2, DRD4
CARIPRAZINEChEMBLPhase 4 (approved)DRD2, DRD4
CARVEDILOLChEMBLPhase 4 (approved)DRD2, DRD4
CHLORPROMAZINEChEMBLPhase 4 (approved)DRD2, DRD4
CLOTRIMAZOLEChEMBLPhase 4 (approved)DRD2, DRD4
CLOZAPINEChEMBLPhase 4 (approved)DRD2, DRD4
DESLORATADINEChEMBLPhase 4 (approved)DRD2, DRD4
DISULFIRAMChEMBLPhase 4 (approved)DRD2, DRD4
DOBUTAMINEChEMBLPhase 4 (approved)DRD2, DRD4
DOPAMINEChEMBLPhase 4 (approved)DRD2, DRD4
DOXEPINChEMBLPhase 4 (approved)DRD2, DRD4
EBASTINEChEMBLPhase 4 (approved)DRD2, DRD4
ECONAZOLEChEMBLPhase 4 (approved)DRD2, DRD4
FENTANYLChEMBLPhase 4 (approved)DRD2, DRD4
FLUPHENAZINEChEMBLPhase 4 (approved)DRD2, DRD4
FROVATRIPTANChEMBLPhase 4 (approved)DRD2, DRD4
HALOPERIDOLChEMBLPhase 4 (approved)DRD2, DRD4
HALOPERIDOL DECANOATEChEMBLPhase 4 (approved)DRD2, DRD4
HYDROXYZINEChEMBLPhase 4 (approved)DRD2, DRD4
ILOPERIDONEChEMBLPhase 4 (approved)DRD2, DRD4
IMIPRAMINEChEMBLPhase 4 (approved)DRD2, DRD4
IPRINDOLEChEMBLPhase 4 (approved)DRD2, DRD4
ISOPROTERENOLChEMBLPhase 4 (approved)DRD2, DRD4
KETANSERINChEMBLPhase 4 (approved)DRD2, DRD4
LOPERAMIDEChEMBLPhase 4 (approved)DRD2, DRD4
LOXAPINEChEMBLPhase 4 (approved)DRD2, DRD4
MECLIZINEChEMBLPhase 4 (approved)DRD2, DRD4
METOCLOPRAMIDEChEMBLPhase 4 (approved)DRD2, DRD4
MIANSERINChEMBLPhase 4 (approved)DRD2, DRD4
MICONAZOLEChEMBLPhase 4 (approved)DRD2, DRD4
NEFAZODONEChEMBLPhase 4 (approved)DRD2, DRD4
OLANZAPINEChEMBLPhase 4 (approved)DRD2, DRD4
PALIPERIDONEChEMBLPhase 4 (approved)DRD2, DRD4
PERGOLIDEChEMBLPhase 4 (approved)DRD2, DRD4
PIMOZIDEChEMBLPhase 4 (approved)DRD2, DRD4
PRAMIPEXOLEChEMBLPhase 4 (approved)DRD2, DRD4
PROCHLORPERAZINEChEMBLPhase 4 (approved)DRD2, DRD4
PROMAZINEChEMBLPhase 4 (approved)DRD2, DRD4
PROMETHAZINEChEMBLPhase 4 (approved)DRD2, DRD4
QUETIAPINEChEMBLPhase 4 (approved)DRD2, DRD4
REMOXIPRIDEChEMBLPhase 4 (approved)DRD2, DRD4
RISPERIDONEChEMBLPhase 4 (approved)DRD2, DRD4
ROPINIROLEChEMBLPhase 4 (approved)DRD2, DRD4
ROTIGOTINEChEMBLPhase 4 (approved)DRD2, DRD4
SALMETEROLChEMBLPhase 4 (approved)DRD2, DRD4
SERTINDOLEChEMBLPhase 4 (approved)DRD2, DRD4
SILODOSINChEMBLPhase 4 (approved)DRD2, DRD4
SULPIRIDEChEMBLPhase 4 (approved)DRD2, DRD4
SUNITINIBChEMBLPhase 4 (approved)DRD2, DRD4
TAMOXIFENChEMBLPhase 4 (approved)DRD2, DRD4

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot