Fluspirilene

drug
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Also known as FluspirilenoImapMCN-JR-6218R 6218R-6218RedeptinSID11111163SID11112501SID11532937SID26753577SID26753578SID50106303SID85231040SID90341058SID56422781SID104171151SID50106304SID124880066SID144203693

Summary

Fluspirilene (CHEMBL46516) is an approved small molecule (ATC N05AG01) targeting HTR1A, HRH1, and HTR1D; indicated across 5 conditions including psychotic disorder and anxiety.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N05AG01
  • Targets: 5 (HTR1A, HRH1, HTR1D…)
  • Indications: 5 conditions
  • Clinical trials: 3
  • Chemistry: 475.6 Da · C29H31F2N3O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL46516
NameFluspirilene
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID3396
ATCN05AG01
Molecular formulaC29H31F2N3O
Molecular weight475.6
InChIKeyQOYHHIBFXOOADH-UHFFFAOYSA-N

SMILES: C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCC(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F

IUPAC name: 8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one

Also known as: Fluspirilene, Fluspirileno, Imap, MCN-JR-6218, R 6218, R-6218, Redeptin, SID11111163, SID11112501, SID11532937, SID26753577, SID26753578

Patent coverage: 13,156 distinct patent families (41,239 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).

GeneTargetActionpAffinityCancer dependencyUniProt
HTR1A5-HT1A receptorAntagonist7.20%P08908
HRH1H1 receptorAntagonist7.90%P35367
HTR1D5-HT1D receptorAntagonist60%P28221
HTR1E5-ht1e receptorAntagonist5.60%P28566
HTR2A5-HT2A receptorAntagonist80%P28223

Broader ChEMBL bioactivity targets: 68 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Lethal(3)malignant brain tumor-like protein 1, Microtubule-associated protein tau, Ubiquitin carboxyl-terminal hydrolase 2, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, RecQ-like DNA helicase BLM, 4’-phosphopantetheinyl transferase ffp, Thrombopoietin, NPC intracellular cholesterol transporter 1, Geminin, Endonuclease 4, Ras-related protein Rab-9A, Peripheral myelin protein 22, Protein RecA, X-box-binding protein 1, Replicative DNA helicase DnaB, Vasopressin V2 receptor, 5-hydroxytryptamine receptor 2B.

Bioactivity

ChEMBL activities: 50 potent at pChembl ≥ 5 of 115 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
KCNH27.4AC5040nMCHEMBL_ACT_25117782
DRD27.37AC5043nMCHEMBL_ACT_25140268
HTR2A7.23AC5059nMCHEMBL_ACT_25173594
DRD37AC50100nMCHEMBL_ACT_25193463
HTR2B6.82Ki151.4nMCHEMBL_ACT_3555290
SLC6A46.49AC50323nMCHEMBL_ACT_25150275
OPRL16.3Ki500nMCHEMBL_ACT_2604033
ADRA2B6.19AC50640nMCHEMBL_ACT_25143638
HRH16.07AC50850nMCHEMBL_ACT_25212447
ADRA2C6AC501000nMCHEMBL_ACT_25147813
LMNA6Potency1000nMCHEMBL_ACT_3657412
P220025.97AC501068nMCHEMBL_ACT_25119542
HTR2A5.96AC501100nMCHEMBL_ACT_25225114
HTR65.92Ki1188nMCHEMBL_ACT_12059580
GLRA15.92EC501200nMCHEMBL_ACT_15241391
OPRM15.92AC501200nMCHEMBL_ACT_25157403
OPRK15.83AC501482nMCHEMBL_ACT_25129368
CYP2D65.8Potency1585nMCHEMBL_ACT_4949899
CYP2D65.8AC501585nMCHEMBL_ACT_5987225
ADRA1A5.77AC501699nMCHEMBL_ACT_25137891
CACNA1C5.75AC501800nMCHEMBL_ACT_25159089
KCNH25.64IC502300nMCHEMBL_ACT_1449654
SLC6A35.52AC503000nMCHEMBL_ACT_25123889
ADORA35.4AC503989nMCHEMBL_ACT_25134148
HTR2B5.34AC504600nMCHEMBL_ACT_25227464
GAA5.3Potency5012nMCHEMBL_ACT_4981208
GAA5.3Potency5012nMCHEMBL_ACT_5026263
SLC6A25.22AC506000nMCHEMBL_ACT_25144939
MEN15.2Potency6310nMCHEMBL_ACT_4570626
CYP3A45.2Potency6310nMCHEMBL_ACT_4973822
CYP3A45.2Potency6310nMCHEMBL_ACT_5042848
CYP3A45.2AC506310nMCHEMBL_ACT_6057718
MC3R5.19AC506500nMCHEMBL_ACT_25183336
OPRD15.17AC506700nMCHEMBL_ACT_25154005
GHSR5.15AC507100nMCHEMBL_ACT_25172694
CYP2C195.1Potency7943nMCHEMBL_ACT_4016521
USP25.1Potency7943nMCHEMBL_ACT_4699949
NPSR15.1Potency7943nMCHEMBL_ACT_4909301
CYP2C195.1AC507943nMCHEMBL_ACT_6004299
CHRM35.09AC508100nMCHEMBL_ACT_25136627
MEN15.05Potency8912nMCHEMBL_ACT_4566864
P9WMR35.01AC509694nMCHEMBL_ACT_6543846
ADRB25AC5010100nMCHEMBL_ACT_25122819
MLNR5AC509900nMCHEMBL_ACT_25189126
NFKB15Potency10000nMCHEMBL_ACT_3672061
MAPT5Potency10000nMCHEMBL_ACT_3964071
NFKB15Potency10000nMCHEMBL_ACT_4585343
CYP2D65Potency10000nMCHEMBL_ACT_4994235
XBP15IC5010000nMCHEMBL_ACT_5514376
CYP2D65AC5010000nMCHEMBL_ACT_5988490

Target pathways

Aggregated over 5 target gene(s): HTR1A, HRH1, HTR1D, HTR1E, HTR2A.

Top Reactome pathways

10 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction4HTR1A, HTR1D, HTR1E, HTR2A
Signaling by GPCR4HTR1A, HTR1D, HTR1E, HTR2A
Class A/1 (Rhodopsin-like receptors)4HTR1A, HTR1D, HTR1E, HTR2A
Amine ligand-binding receptors4HTR1A, HTR1D, HTR1E, HTR2A
Serotonin receptors4HTR1A, HTR1D, HTR1E, HTR2A
GPCR ligand binding4HTR1A, HTR1D, HTR1E, HTR2A
GPCR downstream signalling3HTR1D, HTR1E, HTR2A
G alpha (q) signalling events2HRH1, HTR2A
G alpha (i) signalling events2HTR1D, HTR1E
Histamine receptors1HRH1

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway5
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5
chemical synaptic transmission5
signal transduction5
adenylate cyclase-inhibiting serotonin receptor signaling pathway3
adenylate cyclase-activating G protein-coupled receptor signaling pathway3
serotonin receptor signaling pathway2
positive regulation of cell population proliferation2
regulation of behavior2
G protein-coupled serotonin receptor signaling pathway2
memory2
positive regulation of vasoconstriction2
phospholipase C-activating serotonin receptor signaling pathway2
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway2
behavioral fear response1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
psychotic disorder4MONDO:0005485EFO:0005407

3 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
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: 3.

Phase distribution

PhaseTrials
PHASE41
PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02307396PHASE4COMPLETEDEvaluation of the Necessity of Long-term Pharmacological Treatment With Antipsychotics in Schizophrenic Patients
NCT02374567PHASE3TERMINATEDPharmacovigilance in Gerontopsychiatric Patients
NCT01437553Not specifiedCOMPLETEDImaging Whole Coronary Artery With Intravascular Ultrasound (Ivus) And Imap For Plaque Tissue Composition In Patients With Acute Myocardial Infarction

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.

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.

673 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR1E, HTR2A
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR1E, HTR2A
RISPERIDONEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR1E, HTR2A
RIZATRIPTANChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR1E, HTR2A
BREXPIPRAZOLEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR1E, HTR2A
LYSERGIDEChEMBLPhase 2HRH1, HTR1A, HTR1D, HTR1E, HTR2A
ASENAPINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
CLOZAPINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
CYPROHEPTADINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
ERGOTAMINEChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1D, HTR1E, HTR2A
METHYLERGONOVINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
OLANZAPINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
QUETIAPINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
SUMATRIPTANChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1D, HTR1E, HTR2A
ZIPRASIDONEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR1E, HTR2A
ZOLMITRIPTANChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1D, HTR1E, HTR2A
ARIPIPRAZOLEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
AZELASTINEChEMBLPhase 4 (approved)HRH1, HTR1D, HTR1E, HTR2A
CARIPRAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
CINACALCETChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
KETANSERINChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
MIANSERINChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
NEFAZODONEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR1D, HTR2A
SEROTONINChEMBL + PubChemPhase 3 (approved)HTR1A, HTR1D, HTR1E, HTR2A
YOHIMBINEChEMBL + PubChemPhase 3 (approved)HTR1A, HTR1D, HTR1E, HTR2A
LATREPIRDINEChEMBLPhase 3HRH1, HTR1D, HTR1E, HTR2A
MEBUFOTENINChEMBLPhase 2HTR1A, HTR1D, HTR1E, HTR2A
PENFLURIDOLChEMBLPhase 2HRH1, HTR1A, HTR1D, HTR2A
PSILOCINChEMBLPhase 2HTR1A, HTR1D, HTR1E, HTR2A
RITANSERINChEMBLPhase 2HRH1, HTR1A, HTR1E, HTR2A
SPIRAMIDEChEMBLPhase 2HRH1, HTR1A, HTR1D, HTR2A
ALMOTRIPTANChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
CANNABIDIOLChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1E, HTR2A
DESLORATADINEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
FidaxomicinChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
NARATRIPTANChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1D, HTR1E
OLODATEROLChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
PALIPERIDONEChEMBL + PubChemPhase 4 (approved)HRH1, HTR1D, HTR2A
PropoxypheneChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
REGORAFENIBChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
SORAFENIBChEMBL + PubChemPhase 4 (approved)HTR1A, HTR1E, HTR2A
TAMSULOSINChEMBL + PubChemPhase 4 (approved)HRH1, HTR1A, HTR2A
ACETOPHENAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
AMITRIPTYLINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
AMOXAPINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
APOMORPHINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
ASTEMIZOLEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
AZATADINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
BENFLUOREXChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
BENPERIDOLChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
BROMPERIDOLChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
BUSPIRONEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CABERGOLINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CHLORPROMAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CINNARIZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CISAPRIDEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CITALOPRAMChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CLEMASTINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CLOMIPRAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
CYCLOBENZAPRINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
DEXCHLORPHENIRAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
DIBENZEPINChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
DOMPERIDONEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
DOXEPINChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
DULOXETINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
EBASTINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
FLUPHENAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
FROVATRIPTANChEMBLPhase 4 (approved)HTR1A, HTR1D, HTR1E
HALOPERIDOLChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
ILOPERIDONEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
IPRINDOLEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
LORCASERINChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
LOXAPINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
LURASIDONEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
MAPROTILINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
MEFLOQUINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
METHYSERGIDEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
MIRTAZAPINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
NAFTOPIDILChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
NORTRIPTYLINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
OXYMETAZOLINEChEMBLPhase 4 (approved)HTR1A, HTR1D, HTR2A
OXYPERTINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PERGOLIDEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PERPHENAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PHENOXYBENZAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PHENTOLAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PIMOZIDEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PIPERACETAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PRENYLAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PROCHLORPERAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PROMAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PROMETHAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PROPIOMAZINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
PYRILAMINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
QUINAGOLIDEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
ROPINIROLEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
ROTIGOTINEChEMBLPhase 4 (approved)HRH1, HTR1A, HTR2A
SALMETEROLChEMBLPhase 4 (approved)HTR1A, HTR1D, HTR2A