Molecule Details
| InChIKey | RRMJMHOQSALEJJ-UHFFFAOYSA-N |
|---|---|
| Canonical SMILES | C=CC(=O)Nc1cc(Nc2nccc(-n3cc(CN(C)C)c(-c4ccccc4)n3)n2)c(OC)cc1N1CCOCC1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 2 |
| Pfam Stratification | Homologous |
| Avg pChEMBL | 6.92 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB16216 |
|---|---|
| Drug Name | Lazertinib |
| CAS Number | 1903008-80-9 |
| Groups | approved investigational |
| ATC Codes | L01EB09 |
| Description | Lazertinib is an oral, third-generation, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).[A264299, A264304] Lazertinib was first approved in South Korea on January 18, 2021, for the treatment of _EGFR_ T790M mutation-positive non-small cell lung cancer (NSCLC) with EGFR mutat... |
Categories: Antineoplastic Agents Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Inhibitors Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Enzyme Inhibitors Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors Kinase Inhibitor OCT1 inhibitors Oxazines Protein Kinase Inhibitors UGT1A1 Inhibitors
Cross-references: BindingDB: 50555575 CHEMBL4558324 ChemSpider: 64835231 PharmGKB: PA166314341 RxCUI: 2691150 Wikipedia: Lazertinib
Target Activities (2)
DrugBank Target Actions (7)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P08684 | CYP3A4 | Cytochrome P450 3A4 | inhibitor | enzymes |
| P22309 | UGT1A1 | UDP-glucuronosyltransferase 1A1 | inhibitor | enzymes |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | substrate | enzymes |
| P09488 | P09488 | Glutathione S-transferase Mu 1 | substrate | enzymes |
| P00533 | EGFR | Epidermal growth factor receptor | inhibitor | targets |
| O15245 | SLC22A1 | Solute carrier family 22 member 1 | inhibitor | transporters |
| Q9UNQ0 | ABCG2 | Broad substrate specificity ATP-binding cassette transporter ABCG2 | inhibitor | transporters |