Compound Detail
CHEMBL354541
LOMITAPIDE 💊 Approved Drug
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💊 Approved Drug
O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1
Basic Information
| ChEMBL ID | CHEMBL354541 |
| Name | LOMITAPIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | MBBCVAKAJPKAKM-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
5
Known Names
3
Indications
Molecular Properties
693.7
MW (Da)
8.38
ALogP
3
HBA
2
HBD
61.4
PSA (Ų)
0.13
QED
2
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2012 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Cardiovascular Diseases Hyperlipoproteinemia Type II Hyperlipoproteinemia Type II
ATC Classification
C10AX12
lomitapide
Level 1: CARDIOVASCULAR SYSTEM
Level 2: LIPID MODIFYING AGENTS
Activity Summary
IC50 4 meas. best 9.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Methionine synthase CHEMBL2150844 | IC50 | 9.3 | 9.3 | 0.5 | 1 |
| Microsomal triglyceride transfer protein large subunit CHEMBL2569 | IC50 | 9.1 | 8.4333 | 0.8 | 3 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Methionine synthase | IC50 | = | 0.5 | nM | 9.3 | Inhibition of MTR (unknown origin) | 36155354 |
| Microsomal triglyceride transfer protein large subunit | IC50 | = | 0.8 | nM | 9.1 | In vitro inhibition of human microsomal triglyceride transfer protein in HepG2 c... | 11300866 |
| Microsomal triglyceride transfer protein large subunit | IC50 | = | 8.0 | nM | 8.1 | In vitro inhibition of human microsomal triglyceride transfer protein using trig... | 11300866 |
| Microsomal triglyceride transfer protein large subunit | IC50 | = | 8.0 | nM | 8.1 | In vitro inhibitory concentration against human Microsomal triglyceride transfer... | 15380200 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 11300866 | 10.1021/jm000494a | Unchecked | 4 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 11300866 | 10.1021/jm000494a | Microsomal triglyceride transfer protein large subunit | 2 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 15380200 | 10.1016/j.bmcl.2004.07.069 | Cricetinae gen. sp. | 2 |
| 11300866 | 10.1021/jm000494a | NON-PROTEIN TARGET | 2 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 1 |
| 15380200 | 10.1016/j.bmcl.2004.07.069 | HepG2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 1 |
Data from ChEMBL 36 via Core Engine