Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4558324

LAZERTINIB
💊 Approved Drug
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
💊 Approved Drug
C=CC(=O)Nc1cc(Nc2nccc(-n3cc(CN(C)C)c(-c4ccccc4)n3)n2)c(OC)cc1N1CCOCC1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4558324
Name LAZERTINIB
Phase Approved
Structure Type MOL
InChI Key RRMJMHOQSALEJJ-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

C-18112003-G GNS-1480 GNS1480 JNJ-73841937-AAA Lazertinib YH-25448 Yh25448
5
Targets
12
Activities
3
Assay Types
0
PK Parameters
19
Publications
7
Known Names
6
Indications
3
Mechanisms

Molecular Properties

554.7
MW (Da)
4.10
ALogP
10
HBA
2
HBD
109.7
PSA (Ų)
0.28
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2024
Availability Prescription
Chirality Achiral

Routes of Administration

Oral
USAN Stem -tinib
USAN Year 2020

Extended Properties

Molecular Formula C30H34N8O3
MW 554.66
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.60

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Epidermal growth factor receptor erbB1 inhibitor INHIBITOR Epidermal growth factor receptor ✓ ✓
Epidermal growth factor receptor erbB1 inhibitor INHIBITOR Epidermal growth factor receptor ✓ ✓
Epidermal growth factor receptor erbB1 inhibitor INHIBITOR Epidermal growth factor receptor ✓ ✓

Indications

Carcinoma, Non-Small-Cell Lung Neoplasms Neoplasms Lung Neoplasms Lung Neoplasms Liver Diseases

ATC Classification

L01EB09
lazertinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

Ki 6 meas. best 8.33
IC50 4 meas. best 8.57
EC50 2 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
 IC50 8.57 8.015 2.7 2
Epidermal growth factor receptor
CHEMBL203
 Ki 8.33 7.282 4.7 5
BaF3
CHEMBL614524
 EC50 8.32 8.225 4.8 2
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
 Ki 6.36 6.36 437.0 1
A-431
CHEMBL614069
 IC50 5.44 5.44 3600.0 1
U-87 MG
CHEMBL614247
 IC50 4.48 4.48 33200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 2.7 nM 8.57 Inhibition of human EGFR cytoplasmic domain L858R/T790M mutant (669 to 1210 resi... 31869655
Epidermal growth factor receptor Ki = 4.68 nM 8.33 Binding affinity to EGFR L858R mutant (unknown origin) assessed as apparent inhi... 38134304
BaF3 EC50 = 4.8 nM 8.32 Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant ... 36518696
BaF3 EC50 = 7.4 nM 8.13 Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M m... 36518696
Epidermal growth factor receptor Ki = 34.0 nM 7.47 Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues... 36518696
Epidermal growth factor receptor Ki = 34.0 nM 7.47 Binding affinity to EGFR L858R/T790M double mutant (unknown origin) assessed as ... 38134304
Epidermal growth factor receptor IC50 = 34.6 nM 7.46 Inhibition of wild type N-terminal GST-tagged human EGFR cytoplasmic domain (669... 31869655
Epidermal growth factor receptor Ki = 271.0 nM 6.57 Inhibition of recombinant human N-terminal GST-tagged EGFR wild type (669 to 121... 36518696
Epidermal growth factor receptor Ki = 271.0 nM 6.57 Binding affinity to wild type GST-tagged EGFR (unknown origin) assessed as appar... 38134304
Receptor tyrosine-protein kinase erbB-2 Ki = 437.0 nM 6.36 Inhibition of recombinant human N-terminal GST-tagged HER2 wild type (679 to 125... 36518696
A-431 IC50 = 3600.0 nM 5.44 Antiproliferative activity against human A-431 cells harboring wild type EGFR as... 31869655
U-87 MG IC50 = 33200.0 nM 4.48 Antiproliferative activity against human U-87MG cells harboring wild type EGFR a... 31869655

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 Fibroblast 320
- 10.6019/CHEMBL5724801 U2OS 320
- 10.6019/CHEMBL5724801 HEK-293T 320
- 10.6019/CHEMBL5303304 U2OS 9
36518696 10.1021/acsmedchemlett.2c00213 Epidermal growth factor receptor 7
38134304 10.1021/acs.jmedchem.3c01502 Epidermal growth factor receptor 6
- 10.6019/CHEMBL5303304 Fibroblast 5
36518696 10.1021/acsmedchemlett.2c00213 Receptor tyrosine-protein kinase erbB-2 4
31869655 10.1016/j.ejmech.2019.111966 Epidermal growth factor receptor 4
36518696 10.1021/acsmedchemlett.2c00213 BaF3 3
36518696 10.1021/acsmedchemlett.2c00213 Unchecked 3
- 10.6019/CHEMBL5303304 HEK-293T 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
31869655 10.1016/j.ejmech.2019.111966 Unchecked 1
31869655 10.1016/j.ejmech.2019.111966 U-87 MG 1
31869655 10.1016/j.ejmech.2019.111966 NCI-H1975 1
38134304 10.1021/acs.jmedchem.3c01502 Unchecked 1
31869655 10.1016/j.ejmech.2019.111966 A-431 1

Data from ChEMBL 36 via Core Engine