Compound name
Lapatinib
Protein family
Protein Kinase
Target name
EGFR
Affinity biochemical (nM)
10.8
Affinity on-target cellular (nM)
80170
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001487a
SMILES
CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1
InChIKey
BCFGMOOMADDAQU-UHFFFAOYSA-N
NCBI gene ID
1956
UniProt ID
P00533
Synonyms
ERBB1
Mode of action
inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay (10 µM ATP)
Affinity Biochemical Source Knowledge
https://aacrjournals.org/mct/article/1/2/85/233686/The-Effects-of-the-Novel-Reversible-Epidermal
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot (phosphorylation of EGFR in BT474 cells)
Affinity on-target cellular source knowledge
https://aacrjournals.org/mct/article/1/2/85/233686/The-Effects-of-the-Novel-Reversible-Epidermal
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (literature)
Selectivity platform number of targets
317
Selectivity remarks
In-vitro potency of closest targets: Kd(EGFR) = 2.4 nM, Kd(EGFR, E746-A750del) = 8.6 nM, Kd(EGFR, G719C) = 0.92 nM, Kd(EGFR, G719S) = 2.1 nM, Kd(EGFR, L747-E749del, A750P) = 2.2 nM, Kd(EGFR, L747-T751del, Sins) = 3.5 nM, Kd(EGFR, L747-S752del, P753S) = 3.9 nM, Kd(EGFR, L858R) = 2.8 nM, Kd(EGFR, L861Q) = 1.2 nM, Kd(EGFR, S752-I759del) = 4.2 nM, Kd(ERBB2) = 7 nM, Kd(ERBB4) = 54 nM, Kd(RIPK2) = 3600 nM, Kd(STK10) = 4400 nM; In-vitro potencies of closest targets (Radiometric kinase assay (10 µM ATP)): IC50(ERBB4) = 367 nM, IC50(SRC) = 3500 nM, IC50(RAF1) >10000 nM, IC50(MAP2K1) >10000 nM, IC50(MAPK1) >10000 nM, IC50(CSF1R) >10000 nM, IC50(CDK1) >10000 nM, IC50(CDK2) >10000 nM, IC50(MAPK14) >10000 nM, IC50(TEK) >10000 nM, IC50(KDR) >10000 nM (https://aacrjournals.org/mct/article/1/2/85/233686/The-Effects-of-the-Novel-Reversible-Epidermal)
Selectivity Source Knowledge
https://www.nature.com/articles/nbt1358