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Binding affinity to GST tagged AR LBD (unknown orign) by radioligand binding assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of androgen receptor in human 22Rv1 cells assessed as reduction in MCL-2 expression level at 1 to 10 uM incubated for 24 hrs by western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at Androgen receptor in human LNCaP cells assessed as inhibition of Binding Function 3 (BF3) of AR measured by luciferase assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Activation of Androgen receptor-mediated transcription (unknown origin) in African green monkey CV-1 cells incubated for 40 hrs by Luciferase reporter gene assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at androgen receptor F876L mutant (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter assay
ANDROGEN/H Eurofins SafetyScreen44 (BI)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Antagonist activity at androgen receptor in DHT-treated human LNCaP cells assessed as disruption of ZMIZ1 interaction at 6 uM incubated for 6 hrs by rapid immunoprecipitation mass spectrometry
Antagonist activity at VP16-AR wild-type (unknown origin) transfected in human HepG2 cells cotransfected with ARE-LUC at upto 30 uM incubated for 48 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay relative to control
Assay data:9 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at AR in human LNCaP cells transfected with PSA assessed as inhibition of R1881-induced PSA luciferase activity pretreated with compound followed by R1881 addition at 50 uM and measured after 48 hrs by luciferase assay
Induction of full length androgen receptor degradation in human LNCaP cells assessed as reduction in AR protein level at 1 to 10 uM by Western blot analysis
Protac activity at CRBN/AR in human LNCaP cells assessed as AR degradation after 24 hrs by Western blotting analysis
Selective androgen receptor degradation activity at androgen receptor in human LNCaP cells assessed as down regulation of protein level at 10 uM after 24 hrs in presence of MG132 by Western blot analysis
Induction of androgen receptor T877A mutant degradation in human LNCaP cells at 10 uM measured after 24 hrs in presence of AR agonist R1881 by Western blot analysis relative to control
Assay data:8 Tested
Protac activity against VHL/AR in human VCAP cells assessed as induction of AR degradation incubated for 24 hrs by ELISA relative to untreated control
Assay data:2 Tested
Displacement of [3H]methyltrienolone from recombinant human AR after 1440 mins by scintillation counting analysis
Inhibition of AR F876L mutant (unknown origin) transfected in human PC3 cells assessed as receptor transactivation at 0.1 to 30 uM incubated for 24 hrs by dual luciferase reporter gene assay
Assay data:2 Active, 2 Tested
Protac activity against VHL/androgen receptor in human VCaP cells assessed as induction of androgen receptor protein degradation by Western blot analysis relative to control
Antagonist activity at AR (unknown origin) by cell based GAL4 reporter gene assay
Induction of AR/cIAP1 interaction in human 22Rv1 cells assessed as ubiquitin proteasome system mediated androgen receptor protein degradation at 30 uM after 6 hrs by Western blot analysis
Displacement of [3H]methyltrienolone from human androgen receptor at 10 uM after 1440 mins by scintillation counting method
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