Bepridil

Summary

Bepridil (CHEMBL1008) is an approved small-molecule vasodilator agent (ATC C08EA02) targeting KCNT1 and KCNQ4; indicated across 1 condition including cardiovascular disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C08EA02
• Targets: 2 (KCNT1, KCNQ4)
• Indications: 1 condition
• Chemistry: 366.5 Da · C24H34N2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1008
Name	Bepridil
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2351
ChEBI	CHEBI:3061
ATC	C08EA02
Molecular formula	C24H34N2O
Molecular weight	366.5
InChIKey	UIEATEWHFDRYRU-UHFFFAOYSA-N

SMILES: CC(C)COCC(CN(CC1=CC=CC=C1)C2=CC=CC=C2)N3CCCC3

IUPAC name: N-benzyl-N-[3-(2-methylpropoxy)-2-pyrrolidin-1-ylpropyl]aniline

ChEBI definition: A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl.

Pharmacological roles (ChEBI): vasodilator agent, anti-arrhythmia drug, antihypertensive agent, calcium channel blocker.

Also known as: Bepridil, SID26755663, SID26755664, SID90341574, SID104171114, SID124879419, SID50110980, SID124879417, SID144203640, BEPRIDIL, SID170465240, bepridil

Parent form; salt/anhydrous children: CHEMBL1200382, CHEMBL1257078

Patent coverage: 2,905 distinct patent families (11,776 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
KCNT1	KNa1.1		6	1.2%	Q5JUK3
KCNQ4	Kv7.4		5	0.6%	P56696

Broader ChEMBL bioactivity targets: 47 (assay-derived). Sample: Microtubule-associated protein tau, Survival motor neuron protein, Prelamin-A/C, Inositol monophosphatase 1, 5-hydroxytryptamine receptor 2B, Cholecystokinin receptor type A, Alpha-2C adrenergic receptor, Voltage-dependent L-type calcium channel subunit alpha-1C, Alpha-2B adrenergic receptor, Sodium channel protein type 5 subunit alpha.

Bioactivity

ChEMBL activities: 38 potent at pChembl ≥ 5 of 67 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KCNH2	7.64	IC50	22.91	nM	CHEMBL_ACT_5219045
KCNH2	7.48	IC50	33	nM	CHEMBL_ACT_15257951
KCNH2	6.74	Ki	184	nM	CHEMBL_ACT_1901341
O35505	6.68	IC50	211	nM	CHEMBL_ACT_15257923
O35505	6.68	IC50	211	nM	CHEMBL_ACT_15373204
KCNH2	6.6	AC50	250.8	nM	CHEMBL_ACT_25118035
KCNH2	6.54	Ki	291	nM	CHEMBL_ACT_1901321
KCNH2	6.37	IC50	430	nM	CHEMBL_ACT_1449629
KCNH2	6.35	Ki	444	nM	CHEMBL_ACT_1794636
O35505	6.3	IC50	500	nM	CHEMBL_ACT_15373203
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_1031112
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_1427112
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_1523682
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_2358324
KCNH2	6.26	IC50	549.5	nM	CHEMBL_ACT_2645518
KCNH2	6.26	IC50	550	nM	CHEMBL_ACT_320643
SCN1A	6.08	IC50	840	nM	CHEMBL_ACT_373858
CACNA1F	6	IC50	1000	nM	CHEMBL_ACT_15373315
CACNA1C	5.85	IC50	1400	nM	CHEMBL_ACT_15373206
KCNH2	5.85	IC50	1400	nM	CHEMBL_ACT_20612224
O35505	5.81	IC50	1550	nM	CHEMBL_ACT_15777552
P97697	5.8	Potency	1585	nM	CHEMBL_ACT_4406191
SCN5A	5.68	AC50	2100	nM	CHEMBL_ACT_25158939
OPRK1	5.64	AC50	2300	nM	CHEMBL_ACT_25129533
O35505	5.58	IC50	2600	nM	CHEMBL_ACT_15373205
DRD3	5.58	AC50	2600	nM	CHEMBL_ACT_25193643
ADRA2C	5.48	AC50	3300	nM	CHEMBL_ACT_25147994
SCN5A	5.43	IC50	3700	nM	CHEMBL_ACT_15257892
ADRA1A	5.39	AC50	4045	nM	CHEMBL_ACT_25138005
KCNK2	5.39	IC50	4100	nM	CHEMBL_ACT_29291080

Target pathways

Aggregated over 2 target gene(s): KCNT1, KCNQ4.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Neuronal System	1	KCNQ4
Potassium Channels	1	KCNQ4
Voltage gated Potassium channels	1	KCNQ4
Sensory processing of sound	1	KCNQ4
Sensory processing of sound by inner hair cells of the cochlea	1	KCNQ4
Sensory processing of sound by outer hair cells of the cochlea	1	KCNQ4
Sensory Perception	1	KCNQ4

Dominant GO biological processes

GO term	Targets
potassium ion transmembrane transport	2
monoatomic ion transport	2
potassium ion transport	2
monoatomic ion transmembrane transport	2
protein homotetramerization	1
sensory perception of sound	1
inner ear morphogenesis	1
transmembrane transport	1

Indications & clinical

Indications

1 indication (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).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319

Clinical trials

Total trials: 0.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

4 molecules share ≥1 primary target. Top 4 by shared-target count:

Molecule	Source	Status	Shared targets
QUINIDINE	ChEMBL + PubChem	Phase 4 (approved)	KCNT1
EZOGABINE	ChEMBL	Phase 4 (approved)	KCNQ4
FLINDOKALNER	ChEMBL	Phase 3	KCNQ4
Loxapine	PubChem	Approved	KCNT1