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p53 small molecule agonists, cell-based qHTS assay with human liver microsomes: qHTS cell viability counter screen
Assay data:300 Active, 138 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same Project
Agonist activity at human PGR in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:55 Active, 39 Activity ≤ 1 µM, 930 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity towards human NR3C1 in an in vitro cell free assay measured by filtration, radioactivity method
Assay data:83 Active, 2 Activity ≤ 1 nM, 58 Activity ≤ 1 µM, 1095 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
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
Agonist activity at human Androgen receptor measured by CALUX bioassay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to human Androgen receptor
Assay data:22 Active, 8 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
Modulation of Androgen receptor (unknown origin)
Assay data:20 Active, 8 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 21 Tested
Binding affinity to androgen receptor (unknown origin) at 10 uM by fluorescence polarization competitive binding assay
Assay data:4 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Competitive Radioligand Displacement Assay from Article 10.1016/j.bmcl.2008.09.002: "Effect of B-ring substitution pattern on binding mode of propionamide selective androgen receptor modulators."
Assay data:8 Active, 2 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
Competitive Radioligand Displacement Assay from Article 10.1016/j.bmc.2006.06.019: "Arylisothiocyanato selective androgen receptor modulators (SARMs) for prostate cancer."
Assay data:19 Active, 2 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 19 Tested
Competitive Radioligand Displacement Assay and AR-Mediated Transcription Activation Assay from Article 10.1006/bbrc.1998.8209: "Discovery of nonsteroidal androgens."
Assay data:7 Active, 3 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1016/j.bmcl.2007.01.007: "Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones."
Assay data:40 Active, 1 Activity ≤ 1 nM, 40 Activity ≤ 1 µM, 40 Tested
AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm060792t: "Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator."
Assay data:12 Active, 1 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm070231h: "Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators."
Assay data:11 Active, 1 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 12 Tested
AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm061329j: "Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones."
Assay data:34 Active, 1 Activity ≤ 1 nM, 34 Activity ≤ 1 µM, 34 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Receptor Binding and Transactivation Assay from Article 10.1021/jm061101w: "Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold."
Assay data:12 Active, 2 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Displacement of fluormone-AL green from GST-tagged androgen receptor LBD (unknown origin) measured after 4 hrs by fluorescence polarization assay
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method
Assay data:25 Active, 1 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 43 Tested
Cytochrome P450 Family 3 Subfamily A Member 4 (CYP3A4) small molecule antagonists: luciferase reporter qHTS assay
Assay data:1792 Active, 248 Activity ≤ 1 µM, 9667 Tested
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