Compound name
Lapatinib
Protein family
Protein Kinase
Target name
ERBB2
Affinity biochemical (nM)
9.2
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
2064
UniProt ID
P04626
Synonyms
NEU, HER-2, CD340, HER2
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 ERBB2 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