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TBD from US Patent US20240034743: "TRICYCLIC COMPOUNDS AS EGFR INHIBITORS"
Assay data:135 Active, 118 Activity ≤ 1 nM, 137 Activity ≤ 1 µM, 137 Tested
SummaryRelated BioAssays by Target
Assay data:133 Active, 31 Activity ≤ 1 nM, 137 Activity ≤ 1 µM, 137 Tested
Protein Tyrosine Kinase, EGF Receptor Eurofins Panlabs panel
Assay data:1 Tested
EGFR Invitrogen Lab (UK) kinase screen (BI)
Compound was evaluated for inhibition of human EGFR in an in vitro cell free assay measured by Caliper microfluidic capillary electrophoresis, time-resolved fluorescence resonance energy transfer method
Assay data:11 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 86 Tested
Inhibition of EGFR (unknown origin) at 10 uM by biochemical hotspot kinase assay
Inhibition of human EGFR L858R mutant (669 to 1210 residues) expressed in Sf21 insect cells using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate at 10 uM incubated for 60 mins relative to control
Inhibition of human EGFR L858R mutant (669 to 1210 residues) expressed in Sf21 insect cells using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate incubated for 60 mins
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of EGFR (unknown origin) using (Glu, Tyr) 4:1 as substrate incubated for [gamma-32P]-ATP incubated for 60 mins by scintillation counter analysis
Assay data:1 Active, 1 Tested
Invivo inhibition of EGFR in BALB/c nude mouse xenografted with human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as decrease in phosphorylated-EGFR level at 15 to 30 mg/kg, po for 18 days by western blot analysis
Assay data:2 Active, 2 Tested
Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system by ELISA
Assay data:22 Active, 22 Activity ≤ 1 µM, 31 Tested
Inhibition of EGFR T790M mutant (unknown origin) expressed in baculovirus expression system by ELISA
Assay data:8 Active, 9 Activity ≤ 1 µM, 9 Tested
Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system by ELISA
Assay data:31 Active, 1 Activity ≤ 1 nM, 27 Activity ≤ 1 µM, 31 Tested
Inhibition of EGFR phosphorylation in EGF-stimulated human NCI-H1975 cells harboring EGFR L858R/T790M double mutant at 0.1 to 100 nM and measured after 2 hrs by Western blot analysis
Assay data:2 Tested
Inhibition of EGFR phosphorylation in EGF-stimulated human NCI-H1975 cells harboring EGFR L858R/T790M double mutant at 10 nM and measured after 2 hrs by Western blot analysis
Assay data:3 Active, 3 Tested
Inhibition of EGFR phosphorylation in EGF-stimulated human A-431 cells harboring wild type EGFR at 100 nM and measured after 2 hrs by Western blot analysis
Inhibition of EGFR (unknown origin)
Assay data:4 Active, 3 Activity ≤ 1 µM, 9 Tested
Inhibition of EGFR L858R/T790M mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 20 mins by HTRF assay
Potency index, ratio of osimertinib IC50 to test compound IC50 for inhibition of EGFR L858R/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 20 mins by HTRF assay
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