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Mibefradil

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Also known as Posicor 100Posicor 50SID11111472SID26755047SID90340964SID50110875

Summary

Mibefradil (CHEMBL45816) is an approved small molecule (ATC C08CX01) targeting CATSPER1, CATSPER2, and CATSPER3; indicated across 3 conditions including cardiovascular disorder and glioblastoma.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C08CX01
  • Targets: 11 (CATSPER1, CATSPER2, CATSPER3…)
  • Indications: 3 conditions
  • Clinical trials: 2
  • Chemistry: 495.6 Da · C29H38FN3O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL45816
NameMibefradil
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID60663
ATCC08CX01
Molecular formulaC29H38FN3O3
Molecular weight495.6
InChIKeyHBNPJJILLOYFJU-VMPREFPWSA-N

SMILES: CC(C)[C@H]1C2=C(CC[C@@]1(CCN(C)CCCC3=NC4=CC=CC=C4N3)OC(=O)COC)C=C(C=C2)F

IUPAC name: [(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methylamino]ethyl]-6-fluoro-1-propan-2-yl-3,4-dihydro-1H-naphthalen-2-yl] 2-methoxyacetate

Also known as: Mibefradil, Posicor 100, Posicor 50, mibefradil, SID11111472, SID26755047, SID90340964, SID50110875, MIBEFRADIL

Parent form; salt/anhydrous children: CHEMBL1256688, CHEMBL1421212, CHEMBL1534525

Patent coverage: 1,939 distinct patent families (7,838 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 7,697 (98%) 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
CATSPER1CatSper1Inhibition4.51.8%Q8NEC5
CATSPER2CatSper2Inhibition4.50.2%Q96P56
CATSPER3CatSper3Inhibition4.50.6%Q86XQ3
CATSPER4CatSper4Inhibition4.50.2%Q7RTX7
CACNA1CCav1.2Antagonist4.90.1%Q13936
CACNA1ACav2.1Antagonist6.50%O00555
CACNA1ECav2.3Pore blocker6.40%Q15878
CACNA1GCav3.1Antagonist6.64%O43497
CACNA1HCav3.2Pore blocker7.20.2%O95180
CACNA1ICav3.3Antagonist5.80%Q9P0X4
ANO1CaCCInhibition1.2%Q5XXA6
VRAC

Broader ChEMBL bioactivity targets: 50 (assay-derived). Sample: Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Thrombopoietin, NPC intracellular cholesterol transporter 1, Ras-related protein Rab-9A, Voltage-dependent T-type calcium channel subunit alpha-1H, Alpha-2A adrenergic receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Sodium channel protein type 5 subunit alpha, D(1A) dopamine receptor.

Bioactivity

ChEMBL activities: 101 potent at pChembl ≥ 5 of 130 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CACNA1H7.5IC5032nMCHEMBL_ACT_3519877
CYP2D67.2IC5063nMCHEMBL_ACT_12700572
CACNA1G7.19IC5064nMCHEMBL_ACT_18466523
CACNA1I6.9IC50126nMCHEMBL_ACT_2369472
CYP3A46.89IC50130nMCHEMBL_ACT_1159440
CACNA1H6.89IC50130nMCHEMBL_ACT_18466524
CACNA1I6.89IC50130nMCHEMBL_ACT_18466525
CACNA1H6.89IC50130nMCHEMBL_ACT_2097755
CACNA1F6.81IC50156nMCHEMBL_ACT_15257933
CACNA1H6.74IC50181nMCHEMBL_ACT_15687916
KCNH26.72Ki190nMCHEMBL_ACT_1901340
CACNA1C6.7IC50202nMCHEMBL_ACT_15687895
CACNA1G6.7IC50200nMCHEMBL_ACT_6324162
CACNA1C6.6IC50250nMCHEMBL_ACT_18466526
CYP3A46.55Ki280nMCHEMBL_ACT_15453751
CYP3A46.52IC50300nMCHEMBL_ACT_12163608
CYP3A46.5Potency316.2nMCHEMBL_ACT_4998089
CYP2D66.5Potency316.2nMCHEMBL_ACT_5006450
CYP3A46.5Potency316.2nMCHEMBL_ACT_5066841
CYP2D66.5AC50316.2nMCHEMBL_ACT_5987619
CYP3A46.5AC50316.2nMCHEMBL_ACT_6065864
KCNH26.45Ki353nMCHEMBL_ACT_1901320
CACNA1B6.38IC50416nMCHEMBL_ACT_3519876
CYP3A46.33IC50470nMCHEMBL_ACT_15450990
SCN5A6.3IC50500nMCHEMBL_ACT_18466530
P153906.3IC50500nMCHEMBL_ACT_18466531
P047756.3IC50500nMCHEMBL_ACT_18466532
SCN9A6.3IC50500nMCHEMBL_ACT_18466533
CACNA1F6.29IC50510nMCHEMBL_ACT_15373338
CACNA1G6.25IC50560nMCHEMBL_ACT_13849378

Target pathways

Aggregated over 11 target gene(s): CATSPER1, CATSPER2, CATSPER3, CATSPER4, CACNA1C, CACNA1A, CACNA1E, CACNA1G, CACNA1H, CACNA1I, ANO1.

Top Reactome pathways

31 total, by targets touching each:

PathwayTargetsGenes
Developmental Biology4CACNA1C, CACNA1G, CACNA1H, CACNA1I
Sperm Motility And Taxes4CATSPER1, CATSPER2, CATSPER3, CATSPER4
NCAM signaling for neurite out-growth4CACNA1C, CACNA1G, CACNA1H, CACNA1I
Muscle contraction4CACNA1C, CACNA1G, CACNA1H, CACNA1I
NCAM1 interactions4CACNA1C, CACNA1G, CACNA1H, CACNA1I
Axon guidance4CACNA1C, CACNA1G, CACNA1H, CACNA1I
Nervous system development4CACNA1C, CACNA1G, CACNA1H, CACNA1I
Metabolism3CACNA1A, CACNA1C, CACNA1E
Integration of energy metabolism3CACNA1A, CACNA1C, CACNA1E
Regulation of insulin secretion3CACNA1A, CACNA1C, CACNA1E
Smooth Muscle Contraction3CACNA1G, CACNA1H, CACNA1I
Presynaptic depolarization and calcium channel opening2CACNA1A, CACNA1E
Transmission across Chemical Synapses2CACNA1A, CACNA1E
Neuronal System2CACNA1A, CACNA1E
Disease1ANO1
Stimuli-sensing channels1ANO1
Transport of small molecules1ANO1
Adrenaline,noradrenaline inhibits insulin secretion1CACNA1C
Cardiac conduction1CACNA1C
Phase 0 - rapid depolarisation1CACNA1C
Phase 2 - plateau phase1CACNA1C
Infectious disease1ANO1
Cellular responses to stimuli1CACNA1H
SARS-CoV Infections1ANO1
SARS-CoV-2 Infection1ANO1
Induction of Cell-Cell Fusion1ANO1
Late SARS-CoV-2 Infection Events1ANO1
Viral Infection Pathways1ANO1
Ion channel transport1ANO1
Cellular responses to mechanical stimuli1CACNA1H

Dominant GO biological processes

GO termTargets
monoatomic ion transport11
monoatomic ion transmembrane transport11
calcium ion transport10
transmembrane transport10
calcium ion transmembrane transport10
calcium ion import across plasma membrane6
monoatomic cation transmembrane transport5
spermatogenesis4
cell differentiation4
flagellated sperm motility4
sperm capacitation3
regulation of membrane potential3
chemical synaptic transmission3
sodium ion transport2
establishment of localization in cell2

Indications & clinical

Indications

3 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
cardiovascular disorder4MONDO:0004995EFO:0000319
glioblastoma1MONDO:0018177EFO:0000519
central nervous system neoplasm1MONDO:0006130EFO:1000158

Clinical trials

Total trials: 2.

Phase distribution

PhaseTrials
PHASE12

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01480050PHASE1COMPLETEDMibefradil Dihydrochloride and Temozolomide in Treating Patients With Recurrent Glioma
NCT01550458PHASE1COMPLETEDSafety Study of Mibefradil When Given Four Times a Day in Healthy Volunteers

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.

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

MoleculeSourceStatusShared targets
NIMODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1A, CACNA1C, CACNA1E, CACNA1G, CACNA1H, CACNA1I
TACRINEChEMBLPhase 4 (approved)CACNA1A, CACNA1C, CACNA1E, CACNA1G, CACNA1H, CACNA1I
NIFEDIPINEChEMBL + PubChemPhase 4 (approved)CACNA1A, CACNA1C, CACNA1E, CACNA1I
PIMOZIDEChEMBL + PubChemPhase 4 (approved)CACNA1C, CACNA1G, CACNA1H, CACNA1I
APINOCALTAMIDEChEMBLPhase 2CACNA1C, CACNA1G, CACNA1H, CACNA1I
FLUNARIZINEChEMBLPhase 2CACNA1G, CACNA1H, CACNA1I
SUVECALTAMIDEChEMBLPhase 2CACNA1G, CACNA1H, CACNA1I
CILNIDIPINEChEMBLPhase 3CACNA1C, CACNA1H
Z160ChEMBLPhase 2CACNA1C, CACNA1H
AlprostadilPubChemApprovedCATSPER1, CATSPER4
dinoprostonePubChemApprovedCATSPER1, CATSPER4
ProgesteronePubChemApprovedCATSPER1, CATSPER4
CLOZAPINEChEMBL + PubChemPhase 4 (approved)CACNA1C
NITAZOXANIDEChEMBL + PubChemPhase 4 (approved)ANO1
SILDENAFILChEMBL + PubChemPhase 4 (approved)CACNA1C
SOLIFENACINChEMBL + PubChemPhase 4 (approved)CACNA1C
VARDENAFILChEMBL + PubChemPhase 4 (approved)CACNA1C
ALVIMOPANChEMBLPhase 4 (approved)CACNA1C
AMIODARONEChEMBLPhase 4 (approved)CACNA1C
AMITRIPTYLINEChEMBLPhase 4 (approved)CACNA1C
AMLODIPINEChEMBLPhase 4 (approved)CACNA1C
ASTEMIZOLEChEMBLPhase 4 (approved)CACNA1C
BEPRIDILChEMBLPhase 4 (approved)CACNA1C
CHLORPROMAZINEChEMBLPhase 4 (approved)CACNA1C
CILOSTAZOLChEMBLPhase 4 (approved)CACNA1C
CISAPRIDEChEMBLPhase 4 (approved)CACNA1C
CLEMASTINEChEMBLPhase 4 (approved)CACNA1C
CLOTRIMAZOLEChEMBLPhase 4 (approved)CACNA1C
DASATINIBChEMBLPhase 4 (approved)CACNA1C
DIAZEPAMChEMBLPhase 4 (approved)CACNA1C
DIBUCAINEChEMBLPhase 4 (approved)CACNA1C
DILTIAZEMChEMBLPhase 4 (approved)CACNA1C
DOFETILIDEChEMBLPhase 4 (approved)CACNA1C
DONEPEZILChEMBLPhase 4 (approved)CACNA1C
DORIPENEMChEMBLPhase 4 (approved)CACNA1C
DROPERIDOLChEMBLPhase 4 (approved)CACNA1C
DULOXETINEChEMBLPhase 4 (approved)CACNA1C
ESTRADIOLChEMBLPhase 4 (approved)CACNA1C
FLECAINIDEChEMBLPhase 4 (approved)CACNA1C
FLUOXETINEChEMBLPhase 4 (approved)CACNA1C
FLUSPIRILENEChEMBLPhase 4 (approved)CACNA1C
HALOFANTRINEChEMBLPhase 4 (approved)CACNA1C
HALOPERIDOLChEMBLPhase 4 (approved)CACNA1C
IBUTILIDEChEMBLPhase 4 (approved)CACNA1C
IMIPRAMINEChEMBLPhase 4 (approved)CACNA1C
ISRADIPINEChEMBLPhase 4 (approved)CACNA1C
KETAMINEChEMBLPhase 4 (approved)CACNA1C
LACOSAMIDEChEMBLPhase 4 (approved)CACNA1C
LAMIVUDINEChEMBLPhase 4 (approved)CACNA1C
LORATADINEChEMBLPhase 4 (approved)CACNA1C
METHADONEChEMBLPhase 4 (approved)CACNA1C
MEXILETINEChEMBLPhase 4 (approved)CACNA1C
MITOXANTRONEChEMBLPhase 4 (approved)CACNA1C
NEBIVOLOLChEMBLPhase 4 (approved)CACNA1C
NICARDIPINEChEMBLPhase 4 (approved)CACNA1C
NICLOSAMIDEChEMBLPhase 4 (approved)ANO1
NILOTINIBChEMBLPhase 4 (approved)CACNA1C
NISOLDIPINEChEMBLPhase 4 (approved)CACNA1C
OLICERIDINEChEMBLPhase 4 (approved)CACNA1C
PAROXETINEChEMBLPhase 4 (approved)CACNA1C

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 29

This page pulls from 29 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot