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Compound Detail

CHEMBL1201063

PROPAFENONE HYDROCHLORIDE
💊 Approved Drug
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💊 Approved Drug
CCCNCC(O)COc1ccccc1C(=O)CCc1ccccc1.Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1201063
Name PROPAFENONE HYDROCHLORIDE
Phase Approved
Structure Type MOL
InChI Key XWIHRGFIPXWGEF-UHFFFAOYSA-N
Therapeutic ✓ Yes
Parent Compound CHEMBL631
Active Moiety CHEMBL631

Known Names

Arythmol NSC-758640 Propafenone hcl Propafenone hydrochloride Rythmol Rythmol sr Rytmonorm
1
Targets
14
Activities
1
Assay Types
0
PK Parameters
11
Publications
7
Known Names
3
Indications
3
Mechanisms

Molecular Properties

341.4
MW (Da)
3.24
ALogP
4
HBA
2
HBD
58.6
PSA (Ų)
0.49
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1989
Availability Prescription
Chirality Racemic

Routes of Administration

Oral

Flags

Black Box Warning
USAN Stem -afenone
USAN Year 1988

Extended Properties

Molecular Formula C21H28ClNO3
MW 377.91
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.36

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Beta-1 adrenergic receptor antagonist ANTAGONIST Beta-1 adrenergic receptor ✓ ✓
Beta-2 adrenergic receptor antagonist ANTAGONIST Beta-2 adrenergic receptor ✓ ✓
Sodium channel alpha subunit blocker BLOCKER Sodium channel alpha subunit ✓ ✓

Indications

Arrhythmias, Cardiac Atrial Fibrillation Heart Failure

Drug Warnings

Black Box Warning
General Warning
Country: United States

Activity Summary

IC50 14 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
 IC50 9.64 7.6979 0.2 14

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum IC50 = 0.23 nM 9.64 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Plasmodium falciparum IC50 = 0.33 nM 9.48 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 0.35 nM 9.46 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 0.93 nM 9.03 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 0.93 nM 9.03 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1.05 nM 8.98 Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1.78 nM 8.75 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 251.19 nM 6.6 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Plasmodium falciparum IC50 = 316.23 nM 6.5 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 316.23 nM 6.5 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1000.0 nM 6.0 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1000.0 nM 6.0 Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1000.0 nM 6.0 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1584.89 nM 5.8 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910

Literature References

PubMed DOI Target Context # Activities
19734910 10.1038/nchembio.215 Plasmodium falciparum 14
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
17417631 10.1038/nchembio873 Unchecked 1
20553011 10.1021/tx1000865 Hepatotoxicity 1
20843939 10.1124/dmd.110.035113 Hepatotoxicity 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B3 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B1 1
- 10.1101/2020.04.03.023846 SARS-CoV-2 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine