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MCF-7 Cell Growth Study from US Patent US20240043442: "SELECTIVE ESTROGEN RECEPTOR DEGRADERS AND USES THEREOF"
Assay data:50 Active, 30 Activity ≤ 1 nM, 50 Activity ≤ 1 µM, 50 Tested
SummaryRelated BioAssays by Target
Estrogen Eralpha Eurofins Panlabs panel
Assay data:1 Tested
Binding affinity towards human ESR2 in an in vitro cell free assay measured by fluorescence polarization method
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 287 Tested
Binding affinity towards human ESR1 in an in vitro cell free assay (CRO assay) measured by membrane filtration
Assay data:31 Active, 1 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 927 Tested
Binding affinity towards human ESR1 in an in vitro cell free assay (NIBR assay) measured by fluorescence polarization method
Assay data:27 Active, 1 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 1032 Tested
Antagonist activity at human ESR1 in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:8 Active, 5 Activity ≤ 1 µM, 140 Tested
Agonist activity at human ESR1 in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:2 Active, 140 Tested
Binding affinity to Estrogen receptor alpha (unknown origin) at 1 uM by displacement assay relative to control
Binding affinity to Estrogen receptor beta (unknown origin) at 1 uM by displacement assay relative to control
Induction of ER-alpha degradation in human T47D cells assessed as decrease in ER-alpha protein expression in presence of autophagy inhibitor, CQ by western blot analysis
Assay data:1 Active, 1 Tested
Induction of ER-alpha degradation in human T47D cells assessed as decrease in ER-alpha protein expression in presence of autophagy inhibitor, 3-MA of by western blot analysis
Induction of ER-alpha degradation in tamoxifen-resistant human LCC2 cells assessed as decrease in ER-alpha protein expression at 10 uM by western blot analysis
Induction of ER-alpha degradation in human T47D cells overexpressing ER-alpha assessed as decrease in MYC protein expression at 10 uM incubated for 24 hrs by western blot analysis
Induction of ER-alpha degradation in human T47D cells assessed as decrease in MYC protein expression at 1 to 5 uM incubated for 24 hrs by western blot analysis
Induction of ER-alpha degradation in human T47D cells assessed as decrease in MYC protein expression at 10 uM incubated for 24 hrs by western blot analysis
Induction of ER-alpha degradation in human T47D cells assessed as decrease in ER-alpha protein expression in presence of proteasome inhibitor, MG132 by western blot analysis
Induction of ER-alpha degradation in human T47D cells assessed as reduction in ER-alpha stability at 10 uM incubated for 3 to 9 hrs in presence of protein synthesis inhibitor, CHX by CHX chase assay based western blot analysis
Protac activity at VHL/ER alpha in human MCF7 cells assessed as degradation of ER alpha incubated for 6 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Protac activity at ER/VHL (unknown origin) degradation in human MCF7 cells assessed as maximum efficacy by immunoblotting analysis relative to control
Protac activity at ER/VHL (unknown origin) degradation in human MCF7 cells by immunoblotting analysis
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