Warning: The NCBI web site requires JavaScript to function. more...
An official website of the United States government
The .gov means it's official. Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you're on a federal government site.
The site is secure. The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.
ERα TR-FRET Test from US Patent US20240217988: "ESTROGEN RECEPTOR ANTAGONIST"
Assay data:14 Active, 14 Activity ≤ 1 µM, 14 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
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
Estrogen Eralpha Eurofins Panlabs panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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
SummaryPubMed CitationRelated BioAssays by Target
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
Filters: Manage Filters
Your browsing activity is empty.
Activity recording is turned off.
Turn recording back on