PC9 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.023μM |
25271963 |
NCI-H1975 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.024μM |
25271963 |
Calu3 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay, GI50=0.264μM |
25271963 |
NCI-H1975 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay, IC50=15μM |
25271963 |
PC9 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay, IC50=17μM |
25271963 |
PC9-DRH |
Function assay |
|
2 hrs |
|
Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA, IC50=0.013μM |
26756222 |
NCI-H1975 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA, IC50=0.015μM |
26756222 |
HCC827 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA, IC50=0.023μM |
26756222 |
H3255 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA, IC50=0.036μM |
26756222 |
PC9 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA, IC50=0.056μM |
26756222 |
A549 |
Function assay |
|
|
|
Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA, IC50=0.15μM |
26756222 |
H1975 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA, IC50=0.015μM |
26968253 |
PC9 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA, IC50=0.017μM |
26968253 |
LoVo |
Function assay |
|
2 hrs |
|
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA, IC50=0.48μM |
26968253 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay, IC50=0.052μM |
27131639 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay, IC50=0.893μM |
27131639 |
NCI-H1975 |
Function assay |
1 to 1000 nM |
2 hrs |
|
Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant phosphorylation in human NCI-H1975 cells at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method |
27396610 |
NCI-H1975 |
Function assay |
1 to 1000 nM |
2 hrs |
|
Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method |
27396610 |
HCC827 |
Function assay |
|
3 hrs |
|
Inhibition of EGFR E746 to A750 deletion mutant phosphorylation in human patient derived HCC827 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM |
27433829 |
H1975 |
Function assay |
|
3 hrs |
|
Inhibition of EGFR L858R/T790M mutant phosphorylation in human patient derived H1975 cells incubated for 3 hrs by ELISA method, IC50=0.0025μM |
27433829 |
H3255 |
Function assay |
|
3 hrs |
|
Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method, IC50=0.0041μM |
27433829 |
HaCaT |
Function assay |
|
3 hrs |
|
Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method, IC50=0.0737μM |
27433829 |
Sf21 |
Function assay |
|
|
|
Inhibition of N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (696-end residues) expressed in baculovirus infected Sf21 insect cells, IC50=0.012μM |
27996267 |
LoVo |
Function assay |
|
2 hrs |
|
Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA, IC50=0.48μM |
27996267 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay, IC50=0.03μM |
28033579 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay, IC50=1.604μM |
28033579 |
HCC827 |
Function assay |
|
96 hrs |
|
Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50<0.014μM |
28225269 |
NCI-H1975 |
Function assay |
|
96 hrs |
|
Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.019μM |
28225269 |
A431 |
Function assay |
|
96 hrs |
|
Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay, EC50=0.667μM |
28225269 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of full length EGFR T790M/L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50<0.0003μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of full length EGFR exon 19 deletion mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM |
28282122 |
HCC827 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.001μM |
28282122 |
PC9 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.002μM |
28282122 |
BAF3 |
Function assay |
|
4 hrs |
|
Inhibition of EGFR T790M/L858R mutant (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.002μM |
28282122 |
NCI-H1975 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.005μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.013μM |
28282122 |
H3255 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.033μM |
28282122 |
BAF3 |
Function assay |
|
4 hrs |
|
Inhibition of wild-type EGFR (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis, EC50=0.043μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.3μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of full length EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.31μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.5μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.55μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.56μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM |
28282122 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of Tel-fused EGFR L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=0.59μM |
28282122 |
BAF3 |
Growth inhibition assay |
|
72 hrs |
|
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50=1.2μM |
28282122 |
NCI-H2122 |
Function assay |
|
72 hrs |
|
Inhibition of wild-type EGFR in human NCI-H2122 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=1.2μM |
28282122 |
CHL |
Growth inhibition assay |
|
72 hrs |
|
Growth inhibition of CHL cells after 72 hrs by CellTiter-Glo assay, GI50=2.9μM |
28282122 |
H1355 |
Function assay |
|
72 hrs |
|
Inhibition of wild-type EGFR in human H1355 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3μM |
28282122 |
A549 |
Function assay |
|
72 hrs |
|
Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM |
28282122 |
H1703 |
Function assay |
|
72 hrs |
|
Inhibition of wild-type EGFR in human H1703 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay, GI50=3.5μM |
28282122 |
CHO |
Growth inhibition assay |
|
72 hrs |
|
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay, GI50=4.2μM |
28282122 |
NCI-H1975 |
Function assay |
1 uM |
4 hrs |
|
Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis |
28282122 |
NCI-H1975 |
Function assay |
1 uM |
4 hrs |
|
Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis |
28282122 |
HCC827 |
Function assay |
1 uM |
4 hrs |
|
Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis |
28282122 |
HCC827 |
Function assay |
1 uM |
4 hrs |
|
Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis |
28282122 |
NCI-H1975 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
PC9 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
HCC827 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
H3255 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
NCI-H1975 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
PC9 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
HCC827 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
H3255 |
Function assay |
1 uM |
48 hrs |
|
Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting |
28282122 |
HCC827 |
Antiproliferative assay |
|
|
|
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant, IC50=0.0616μM |
28426996 |
NCI-H1975 |
Antiproliferative assay |
|
|
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant, IC50=0.067μM |
28426996 |
HEK293 |
Function assay |
|
|
|
Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis, IC50=0.57μM |
28426996 |
A431 |
Antiproliferative assay |
|
|
|
Antiproliferative activity against human A431 cells harboring wild-type EGFR, IC50=0.6156μM |
28426996 |
Sf9 |
Function assay |
|
20 mins |
|
Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50=0.278μM |
28482151 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.006μM |
28528303 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.016μM |
28528303 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.018μM |
28528303 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.02μM |
28528303 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=0.066μM |
28528303 |
DFCI032 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs in presence of ceritinib by MTS assay, EC50=0.19μM |
28528303 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=1.748μM |
28528303 |
DFCI076 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of ceritinib, EC50=3.21μM |
28528303 |
DFCI032 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=4.73μM |
28528303 |
DFCI076 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay, EC50=7.93μM |
28528303 |
DFCI032 |
Function assay |
0.1 to 1 uM |
|
|
Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM by Western blot analysis |
28528303 |
DFCI032 |
Function assay |
0.1 to 1 uM |
|
|
Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis |
28528303 |
DFCI032 |
Function assay |
0.1 to 1 uM |
|
|
Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis |
28528303 |
NCI-H1975 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.019μM |
28603991 |
A431 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay, EC50=0.7μM |
28603991 |
PC9 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay, IC50=0.0065μM |
28716641 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay, IC50=0.0105μM |
28716641 |
NCI-H460 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay, IC50=0.4159μM |
28716641 |
BEAS2B |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay, IC50=14.9μM |
28716641 |
HCC827 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM |
28853575 |
NCI-H1975 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50<0.014μM |
28853575 |
A431 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=0.67μM |
28853575 |
A549 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay, EC50=1.83μM |
28853575 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM |
29466773 |
HCC827 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM |
29466773 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50=0.53μM |
29466773 |
NCI-H1975 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.06μM |
29486953 |
HT-29 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.65μM |
29486953 |
A549 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50=0.87μM |
29486953 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50=0.023μM |
29534926 |
NCI-H1975 |
Function assay |
|
1 hr |
|
Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA, IC50=0.041μM |
29534926 |
A431 |
Function assay |
|
1 hr |
|
Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA, IC50=0.141μM |
29534926 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.685μM |
29534926 |
HCC827 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay, IC50=0.0254μM |
29576272 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.0472μM |
29576272 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.486μM |
29576272 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay, IC50=0.041μM |
29730192 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay, IC50=1.26μM |
29730192 |
NCI-H1975 |
Antitumor assay |
10 mg/kg |
21 days |
|
Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days |
29730192 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50=0.019μM |
29853340 |
HCC827 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay, IC50=0.027μM |
29853340 |
A549 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=0.53μM |
29853340 |
NCI-H1975 |
Function assay |
1 to 100 nM |
|
|
Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method |
29906114 |
NCI-H1975 |
Function assay |
100 nM |
|
|
Inhibition of EGFR L858R/T790M double mutant in EGF-stimulated human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 100 nM by Western blot method |
29906114 |
NCI-H1975 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells preincubated for 2 hrs followed by compound washout measured up to 24 hrs by Western blot method |
29906114 |
NCI-H1975 |
Function assay |
|
2 hrs |
|
Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in ERK1/2 phosphorylation preincubated for 2 hrs followed by compound washout measured after 12 hrs by Western blot method |
29906114 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay, IC50=0.13μM |
30429956 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay, IC50=1.24μM |
30429956 |
BAF3 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=4.61μM |
30429956 |
BAF3 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay, IC50=5.15μM |
30429956 |
BAF3 |
Function assay |
1 to 3 uM |
2 hrs |
|
Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis |
30429956 |
BAF3 |
Function assay |
1 to 3 uM |
2 hrs |
|
Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis |
30429956 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, GI50=0.0028μM |
30442506 |
HCC827 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.011μM |
30442506 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, GI50=0.0401μM |
30442506 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay, IC50=0.06μM |
30442506 |
PC9 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay, IC50=0.16μM |
30442506 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.61μM |
30442506 |
Calu3 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=0.75μM |
30442506 |
Calu6 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay, IC50=5.86μM |
30442506 |
NCI-H1975 |
Function assay |
|
4 hrs |
|
Inhibition of EGFR T790M/L858R double mutant phosphorylation at Y1068 residue in human NCI-H1975 cells up to 10 uM after 4 hrs by Western blot analysis |
30442506 |
NCI-H1975 |
Function assay |
up to 10 uM |
4 hrs |
|
Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis |
30442506 |
A431 |
Function assay |
|
4 hrs |
|
Inhibition of WT EGFR phosphorylation at Y1068 residue in human A431 cells up to 10 uM after 4 hrs by Western blot analysis |
30442506 |
A431 |
Function assay |
up to 10 uM |
4 hrs |
|
Inhibition of WT EGFR in human A431 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis |
30442506 |
Sf9 |
Function assay |
|
60 mins |
|
Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.0208μM |
30471829 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay, IC50=0.096μM |
30471829 |
Sf9 |
Function assay |
|
60 mins |
|
Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay, IC50=0.5675μM |
30471829 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay, IC50=0.945μM |
30471829 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=3.242μM |
30471829 |
Aspc-1 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay, IC50=3.985μM |
30471829 |
NCI-H1975 |
Growth inhibition assay |
|
72 hrs |
|
Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.1μM |
30472599 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay, IC50=0.073μM |
30530173 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.615μM |
30530173 |
HepG2 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50=1.605μM |
30530173 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay, IC50=0.03μM |
31223440 |
A431 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay, IC50=1.44μM |
31223440 |
BAF3 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay, IC50=3.93μM |
31223440 |
BAF3 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay, IC50=5.11μM |
31223440 |
PC9 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50<0.01μM |
31446247 |
CL68 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human CL68 cells harbouring EGFR delE746-A750/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.01μM |
31446247 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.05μM |
31446247 |
CL97 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.1μM |
31446247 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=5μM |
31446247 |
A431 |
Cytotoxicity assay |
|
96 hrs |
|
Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method, CC50=0.967μM |
31560541 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.014μM |
31581004 |
PC9 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=0.016μM |
31581004 |
NCI-H292 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.084μM |
31581004 |
LO2 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=1.602μM |
31581004 |
HEK293A |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=2.418μM |
31581004 |
HK2 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=3.565μM |
31581004 |
HLF |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against human HLF cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50=8.741μM |
31581004 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.073μM |
31683104 |
A549 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.462μM |
31683104 |
HeLa |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50=0.975μM |
31683104 |
HeLa |
Function assay |
0.1 to 5 uM |
24 hrs |
|
Inhibition of EFGR protein expression in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis |
31683104 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.001μM |
31689114 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.081μM |
31689114 |
A431 |
Antiproliferative assay |
|
96 hrs |
|
Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.084μM |
31689114 |
BAF3 |
Function assay |
|
72 hrs |
|
Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=0.78μM |
31689114 |
BAF3 |
Cytotoxicity assay |
|
72 hrs |
|
Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50=1.1μM |
31689114 |
BaF3 |
Function assay |
|
4 hrs |
|
Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay, IC50=3.1μM |
31689114 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay, IC50=0.07μM |
31718182 |
NCI-H1975 |
Antiproliferative assay |
|
72 hrs |
|
Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay, IC50=3.1μM |
31718182 |
NCI-H1975 |
Cytotoxicity assay |
|
4 days |
|
Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.013μM |
ChEMBL |
A549 |
Cytotoxicity assay |
|
4 days |
|
Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay, IC50=0.31μM |
ChEMBL |
Vero |
Antiviral assay |
|
24 hrs |
|
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50=3.26μM |
ChEMBL |
Vero |
Cell viability assay |
|
72hrs |
|
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr, CC50=13.23μM |
ChEMBL |
NCI-H1975 |
Function assay |
|
16 hrs |
|
Inhibition of EGFR T790M/L858R double mutant phosphorylation in human NCI-H1975 cells up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis |
ChEMBL |
NCI-H1975 |
Function assay |
|
16 hrs |
|
Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as AKT phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis |
ChEMBL |
NCI-H1975 |
Function assay |
|
16 hrs |
|
Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as ERK1/2 phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis |
ChEMBL |