General
Preferred name
mibefradil
Synonyms
MIBEFRADIL DIHYDROCHLORIDE ()
Ro 40-5967 ()
Ro 40-5967 (dihydrochloride) ()
Mibefradil (dihydrochloride) ()
Mibefradil (hydrochloride) ()
RO-40-5967/001 ()
Mibefradil hydrochloride ()
Posicor ()
RO 40-5967/001 ()
Posicor 100 ()
Posicor 50 ()
Mibefradil ()
P&D ID
PD009103
CAS
116666-63-8
116644-53-2
Tags
available
drug
Approved by
FDA
First approval
1997
Drug indication
Ovarian cancer
Glioblastoma multiforme
Drug Status
approved
withdrawn
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE
350
DESCRIPTION
Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 ??M and 18.6 ??M, respectively).
DESCRIPTION
Marketed formulations contained mibefradil dihydrochloride (PubChem CID 60662).
(GtoPdb)
DESCRIPTION
Highly selective CaV3.x blocker
(Tocris Bioactive Compound Library)
DESCRIPTION
Ca2+ channel blocker (T-type)
(Tocriscreen Plus)
DESCRIPTION
T-type Ca2+ channel blocker
(LOPAC library)
DESCRIPTION
Ca2+ channel blocker (T-type)
(Tocriscreen Total)
DESCRIPTION
Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 μM and 18.6 μM, respectively).
(TargetMol Bioactive Compound Library)
DESCRIPTION
Mibefradil, a calcium channel blocker, has modest selectivity for T-type Ca2+ channels so that could be used in the treatment of sorts of cardiovascular disease like hypertension and chronic angina pectoris. IC50: 2.7 μM (for T-type).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
2
Compound Sets
28
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugCentral
DrugCentral Approved Drugs
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NPC Screening Collection
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
Withdrawn 2.0
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
52
Molecular Weight
495.29
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
11
Ring Count
4
Aromatic Ring Count
3
cLogP
5.27
TPSA
67.45
Fraction CSP3
0.52
Chiral centers
2.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Selectivity
T-type
Target
Calcium Channel
L-type calcium channel
T-type calcium channel
ANO1, CACNA1C, CACNA1D, CACNA1F, CACNA1G, CACNA1H, CACNA1I, CACNA1S, CACNB1, CACNB2, CACNB3, CACNB4, CATSPER1, CATSPER2, CATSPER3, CATSPER4
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Metabolism
Primary Target
CaV3.x Channels (T-type)
MOA
Blocker
T-type calcium channel blocker
ATC
C08CX01
VGSC Target
Nav1.7
Nav1.2
Nav1.4
Nav1.5
Nav1.9
Solubility
10 mM in DMSO
Source data
