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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 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
In vivo protac activity at VHL/AR in human VCaP cells xenografted SCID mouse assessed as reduction in PSA protein level in tumor at 50 mg/kg, ip administered as single dose measured after 3 to 48 hrs Western blot analysis
Assay data:1 Active, 1 Tested
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with proteasome inhibitor, MG132 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with NEDD8 activating E1 enzyme inhibitor, MLN4924 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with VHL ligand, (2S,4R)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)-N-((S)-3-(methylamino)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)pyrrolidine-2-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with proteasome inhibitor, MG132 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with NEDD8 activating E1 enzyme inhibitor, MLN4924 for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with VHL ligand, (2S,4R)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)-N-((S)-3-(methylamino)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)pyrrolidine-2-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 100 nM preincubated with N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-1-(2-hydroxyethyl)-1H-pyrazole-4-carboxamide for 2 hrs followed by compound addition and measured after 6 hrs by Western blot analysis
Protac activity at VHL/AR in human VCaP cells assessed as induction of protein degradation at 10 nM measured after 24 hrs by Western blot analysis relative to control
Protac activity at VHL/AR in human 22Rv1 cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Protac activity at VHL/AR in human VCaP cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Protac activity at VHL/AR in human LNCaP cells assessed as induction of protein degradation measured after 24 hrs by Western blot analysis
Protac activity at VHL/AR in AR-positive human VCaP cells assessed as reduction in protein level at 100 nM measured after 2 to 4 hrs by Western blot analysis
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