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Safety47 Scan (DiscoverX - Eurofins)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Androgen (Testosterone) Eurofins Panlabs panel
ANDROGEN/H Eurofins SafetyScreen44 (BI)
Binding affinity towards human AR in an in vitro assay with cellular components measured by scintillation counting
Assay data:69 Active, 48 Activity ≤ 1 µM, 927 Tested
Binding affinity towards rat Ar in an in vitro cell free assay measured by fluorescence polarization method
Assay data:45 Active, 19 Activity ≤ 1 µM, 667 Tested
Antagonist activity at rat Ar in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:14 Active, 1 Activity ≤ 1 µM, 464 Tested
Agonist activity at rat Ar in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:25 Active, 11 Activity ≤ 1 µM, 615 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
In vivo protac activity at VHL/AR in human VCaP cells xenografted SCID mouse assessed as reduction in AR protein level in tumor at 50 mg/kg, ip administered as single dose measured after 3 to 48 hrs 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 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
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