Compound Detail

CHEMBL92870

LIDOFLAZINE

🧪 Phase II

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🧪 Phase II

Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL92870
Name	LIDOFLAZINE
Phase	Phase II
Structure Type	MOL
InChI Key	ZBIAKUMOEKILTF-UHFFFAOYSA-N
Therapeutic	✓ Yes

Known Names

Angex Clinium Lidoflazina Lidoflazine MCN-JR-7904 R 7904 R-7904

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Molecular Properties

491.6

MW (Da)

5.75

ALogP

HBA

HBD

35.6

PSA (Å²)

0.41

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

USAN Stem	-lazine
USAN Year	1966

Extended Properties

Molecular Formula	C30H35F2N3O
MW	491.63
Aromatic Rings	3
Heavy Atoms	36
NP-Likeness	-1.26

Indications

Cardiovascular Diseases

ATC Classification

C08EX01

lidoflazine

Level 1: CARDIOVASCULAR SYSTEM

Level 2: CALCIUM CHANNEL BLOCKERS

Activity Summary

IC50 6 meas. best 7.8

Ki 2 meas. best 7.11

Kd 1 meas. best 7.5

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240	IC50	7.8	7.8	15.8	2
Oryctolagus cuniculus CHEMBL374	Kd	7.5	7.5	31.6	1
Sodium channel alpha subunits; brain (Types I, II, III) CHEMBL2095171	Ki	7.11	7.11	77.0	1
Equilibrative nucleoside transporter 1 CHEMBL1997	Ki	6.55	6.55	279.9	1
Sodium channel protein type 2 subunit alpha CHEMBL3399	IC50	5.62	5.62	2400.0	1
Equilibrative nucleoside transporter 1 CHEMBL1997	IC50	5.3	5.3	4954.0	1
Unchecked CHEMBL612545	IC50	5.03	5.03	9370.0	1
SARS-CoV-2 CHEMBL4303835	IC50	4.76	4.76	17390.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Voltage-gated inwardly rectifying potassium channel KCNH2	IC50	=	15.85	nM	7.8	Inhibitory concentration against potassium channel HERG	15911273
Voltage-gated inwardly rectifying potassium channel KCNH2	IC50	=	15.85	nM	7.8	Inhibition of human ERG	21185626
Oryctolagus cuniculus	Kd	=	31.62	nM	7.5	Calcium channel-blocking activity by determined by ability to antagonize calcium...	1920352
Sodium channel alpha subunits; brain (Types I, II, III)	Ki	=	77.0	nM	7.11	Inhibition of [3H]- batrachotoxin binding to sodium channel in rat neocortical m...	8295214
Equilibrative nucleoside transporter 1	Ki	=	279.9	nM	6.55	Inhibition of ENT1 in human K562 cells by flow cytometric assay	17636949
Sodium channel protein type 2 subunit alpha	IC50	=	2400.0	nM	5.62	Inhibition of veratridine-induced Na+ influx in chinese hamster ovary cells expr...	8295214
Equilibrative nucleoside transporter 1	IC50	=	4954.0	nM	5.3	Inhibition of ENT1 in human K562 cells by flow cytometric assay	17636949
Unchecked	IC50	=	9369.99	nM	5.03	PubChem BioAssay. VEGF stimulated ADSC/ECFC co-culture nuclear area decrease (vi...	-
SARS-CoV-2	IC50	=	17390.0	nM	4.76	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity o...	-

Literature References

PubMed	DOI	Target Context	# Activities
-	10.6019/CHEMBL4651402	SARS-CoV-2	4
37468498	10.1038/s41467-023-40064-9	Nuclear receptor subfamily 1 group I member 2	3
17636949	10.1021/jm070311l	Equilibrative nucleoside transporter 1	3
37468498	10.1038/s41467-023-40064-9	Androgen receptor	2
37468498	10.1038/s41467-023-40064-9	Beta-2 adrenergic receptor	2
37468498	10.1038/s41467-023-40064-9	Beta-1 adrenergic receptor	2
37468498	10.1038/s41467-023-40064-9	Gamma-aminobutyric acid receptor subunit alpha-1	2
-	10.6019/CHEMBL4808148	Histone deacetylase 6	2
-	10.6019/CHEMBL4651402	Vero C1008	2
-	10.6019/CHEMBL4495565	SARS-CoV-2	2
37468498	10.1038/s41467-023-40064-9	Muscarinic acetylcholine receptor M2	2
37468498	10.1038/s41467-023-40064-9	Cannabinoid receptor 1	2
37468498	10.1038/s41467-023-40064-9	5-hydroxytryptamine receptor 2A	2
37468498	10.1038/s41467-023-40064-9	Alpha-1A adrenergic receptor	2
-	10.21203/rs.3.rs-23951/v1	SARS-CoV-2	2
37468498	10.1038/s41467-023-40064-9	Progesterone receptor	2
37468498	10.1038/s41467-023-40064-9	5-hydroxytryptamine receptor 2B	2
1920352	10.1021/jm00114a009	Rattus norvegicus	2
37468498	10.1038/s41467-023-40064-9	Alpha-2A adrenergic receptor	2
38318365	10.1016/j.isci.2024.108907	Deoxynucleoside triphosphate triphosphohydrolase SAMHD1	1

Data from ChEMBL 36 via Core Engine