Compound Detail
CHEMBL4297517
MAVACAMTEN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL4297517 |
| Name | MAVACAMTEN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RLCLASQCAPXVLM-NSHDSACASA-N |
| Therapeutic | ✓ Yes |
4
Targets
5
Activities
2
Assay Types
1
PK Parameters
7
Publications
4
Known Names
3
Indications
1
Mechanisms
Molecular Properties
273.3
MW (Da)
2.29
ALogP
4
HBA
2
HBD
66.9
PSA (Ų)
0.90
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2022 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Cardiac myosin inhibitor | INHIBITOR | Cardiac myosin | ✓ | ✓ |
Indications
Cardiomyopathy, Hypertrophic Cardiovascular Diseases Heart Failure
ATC Classification
C01EB24
mavacamten
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CARDIAC THERAPY
Drug Warnings
Black Box Warning
cardiotoxicity
Activity Summary
EC50 3 meas. best 6.15
IC50 2 meas. best 6.52
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
| Rattus norvegicus CHEMBL376 | IC50 | 6.22 | 6.22 | 600.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 6.15 | 6.15 | 711.0 | 1 |
| Cytochrome P450 3A4 CHEMBL340 | EC50 | 5.66 | 5.66 | 2200.0 | 1 |
| Cytochrome P450 2B6 CHEMBL4729 | EC50 | 5.29 | 5.29 | 5100.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| T1/2 | 216.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Unchecked | IC50 | = | 300.0 | nM | 6.52 | Activation of Myosin S1 ATPase activity in bovine Cardio-myofibril | 38889609 |
| Rattus norvegicus | IC50 | = | 600.0 | nM | 6.22 | Anti-hypertrophic cardiomyopathy in po dosed Sprague-Dawley rat assessed as redu... | 34606259 |
| Unchecked | EC50 | = | 711.0 | nM | 6.15 | Activation of Myosin ATPase activity in bovine Cardio-myofibril | 39137454 |
| Cytochrome P450 3A4 | EC50 | = | 2200.0 | nM | 5.66 | Induction of CYP3A4 in human hepatocytes assessed as mRNA expression incubated f... | 34606259 |
| Cytochrome P450 2B6 | EC50 | = | 5100.0 | nM | 5.29 | Induction of CYP2B6 in human hepatocytes assessed as mRNA expression incubated f... | 34606259 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 34606259 | 10.1021/acs.jmedchem.1c01290 | Rattus norvegicus | 3 |
| 34606259 | 10.1021/acs.jmedchem.1c01290 | Unchecked | 2 |
| 34606259 | 10.1021/acs.jmedchem.1c01290 | Cytochrome P450 3A4 | 1 |
| 34606259 | 10.1021/acs.jmedchem.1c01290 | Cytochrome P450 2B6 | 1 |
| 34606259 | 10.1021/acs.jmedchem.1c01290 | ADMET | 1 |
| 38889609 | 10.1016/j.ejmech.2024.116593 | Unchecked | 1 |
| 39137454 | 10.1016/j.ejmech.2024.116759 | Unchecked | 1 |
Data from ChEMBL 36 via Core Engine