Compound name
Lazertinib
Protein family
Protein Kinase
Target name
EGFR
Affinity biochemical (nM)
34
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002108a
SMILES
COC1=C(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)C=C(NC(C=C)=O)C(N5CCOCC5)=C1
InChIKey
RRMJMHOQSALEJJ-UHFFFAOYSA-N
NCBI gene ID
1956
UniProt ID
P00533
Synonyms
ERBB1
Mode of action
Covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
TRF KinEASE-TK assay (Cisbio using 27.71 µM ATP)
Affinity Biochemical Source Knowledge
https://www.sciencedirect.com/science/article/pii/S0223523419311183?via%3Dihub
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
304
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition, EGFR(T790M,L858R, 98%), EGFR(T790M, 101%), EGFR(L858R, 91%), EGFR(86%), EGFR(L861Q, 86%), AXL(67%), MER(71%), FER(85%), RET(86%), MLK1(97%);
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30670498/
Selectivity Number of Off-targets
0