Compound Detail
CHEMBL298734
LONAFARNIB 💊 Approved Drug
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💊 Approved Drug
NC(=O)N1CCC(CC(=O)N2CCC([C@H]3c4ncc(Br)cc4CCc4cc(Cl)cc(Br)c43)CC2)CC1
Basic Information
| ChEMBL ID | CHEMBL298734 |
| Name | LONAFARNIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | DHMTURDWPRKSOA-RUZDIDTESA-N |
| Therapeutic | ✓ Yes |
16
Targets
51
Activities
2
Assay Types
22
PK Parameters
20
Publications
6
Known Names
20
Indications
1
Mechanisms
Molecular Properties
638.8
MW (Da)
5.91
ALogP
3
HBA
1
HBD
79.5
PSA (Ų)
0.45
QED
2
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2020 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Protein farnesyltransferase inhibitor | INHIBITOR | Protein farnesyltransferase | ✓ | ✓ |
Indications
Laminopathies Progeria Progeria Carcinoma, Non-Small-Cell Lung Hepatitis D Leukemia, Myelomonocytic, Chronic Myelodysplastic Syndromes Neoplasm Metastasis Breast Neoplasms Leukemia, Myelogenous, Chronic, BCR-ABL Positive Liver Neoplasms Ovarian Neoplasms Urethral Neoplasms Urinary Bladder Neoplasms Astrocytoma Central Nervous System Neoplasms Colorectal Neoplasms Glioblastoma Gliosarcoma Head and Neck Neoplasms
ATC Classification
A16AX20
lonafarnib
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS
Activity Summary
IC50 38 meas. best 8.72
EC50 13 meas. best 7.92
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Protein farnesyltransferase CHEMBL2095197 | IC50 | 8.72 | 8.72 | 1.9 | 1 |
| Unchecked CHEMBL612545 | IC50 | 8.72 | 7.318 | 1.9 | 10 |
| Protein farnesyltransferase CHEMBL2094108 | IC50 | 8.72 | 8.52 | 1.9 | 11 |
| Protein farnesyltransferase CHEMBL2095178 | IC50 | 8.11 | 8.09 | 7.8 | 3 |
| Unchecked CHEMBL612545 | EC50 | 7.92 | 7.3686 | 12.0 | 7 |
| GTPase KRas CHEMBL2189121 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| NIH3T3 CHEMBL614822 | EC50 | 7.3 | 7.1167 | 50.0 | 3 |
| MCF7 CHEMBL387 | IC50 | 7.3 | 7.3 | 50.0 | 1 |
| HCT-116 CHEMBL394 | IC50 | 7.16 | 7.16 | 70.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 7.16 | 7.16 | 70.0 | 1 |
| GTPase HRas CHEMBL2167 | IC50 | 7.16 | 7.16 | 70.0 | 1 |
| NIH-H CHEMBL615000 | IC50 | 7.14 | 7.14 | 72.0 | 1 |
| HCT-116 CHEMBL394 | EC50 | 7.13 | 7.08 | 74.0 | 2 |
| COS-1 CHEMBL614563 | IC50 | 7.12 | 7.12 | 75.0 | 1 |
| Protein farnesyltransferase CHEMBL2096912 | EC50 | 7.0 | 7.0 | 100.0 | 1 |
| NIH-K CHEMBL615001 | IC50 | 6.3 | 6.3 | 500.0 | 1 |
| ATP-dependent translocase ABCB1 CHEMBL4302 | IC50 | 5.57 | 5.57 | 2700.0 | 1 |
| SARS-CoV-2 CHEMBL4303835 | IC50 | 5.3 | 5.275 | 4990.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 24100.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 31800.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 41450.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 24100.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 14700.0 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 24100.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 14700.0 | ng.hr.mL-1 | Macaca fascicularis |
| Cmax | 8840.0 | nM | Mus musculus |
| Cmax | 20000.0 | nM | Mus musculus |
| Cmax | 16600.0 | nM | Mus musculus |
| Cmax | 8.84 | ug | Mus musculus |
| Cmax | 1900.0 | nM | Macaca fascicularis |
| Cmax | 1900.0 | nM | Macaca fascicularis |
| F | 75.8 | % | Mus musculus |
| F | 76.0 | % | Mus musculus |
| F | 50.0 | % | Macaca fascicularis |
| F | 76.0 | % | Rattus norvegicus |
| F | 76.0 | % | Mus musculus |
| F | 50.0 | % | Macaca fascicularis |
| T1/2 | 1.4 | hr | Mus musculus |
| T1/2 | 1.4 | hr | Mus musculus |
| T1/2 | 3.0 | hr | Macaca fascicularis |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine