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Inhibition of HSP90 in human Hs-578T cells assessed as degradation of CDK4 at 5 uM incubated for 24 hrs by Western blot analysis
Assay data:3 Active, 3 Tested
SummaryRelated BioAssays by Target
Inhibition of HSP90alpha (unknown origin)
Assay data:7 Active, 5 Activity ≤ 1 µM, 8 Tested
Displacement of 2-[4-(2-Chloro-5-hydroxy-4-methoxy-phenyl)-5-cyano-7Hpyrrolo[2,3-d]pyrimidin-2-ylsulfanyl]-N-(2,2,2-trifluoroethyl)-acetamide spy ligand from N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cells assessed as inhibition constant by real-time in-cell 19F NMR spectroscopy
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Displacement of 2-[4-(2-Chloro-5-hydroxy-4-methoxy-phenyl)-5-cyano-7Hpyrrolo[2,3-d]pyrimidin-2-ylsulfanyl]-N-(2,2,2-trifluoroethyl)-acetamide spy ligand from N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cells assessed as ratio of dissociation constants of spy ligand (Kd) to test compound (Kd) by real-time in-cell 19F NMR spectroscopy
Assay data:3 Tested
Binding affinity to N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cells measured for 2 hrs by 19F in-cell NMR spectroscopy
Assay data:1 Active, 1 Tested
Binding affinity to N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cell lysate by 1H-15N NMR spectroscopy
Assay data:4 Active, 4 Tested
Binding affinity to N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cell lysate by 19F NMR spectroscopy
Binding affinity to N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cells by 19F in-cell NMR spectroscopy
Inhibition of N-terminal human Hsp90-alpha ATP binding domain (2 to 236 residues) overexpressed in HEK293T cell lysate by fluorescence polarization assay
Assay data:7 Active, 1 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
Inhibition of recombinant human HSP90 expressed in Escherichia coli BL21 assessed as increase in DTT induced insulin aggregation by measuring increase in absorbance at 100 uM pre-incubated for 1 hrs followed by DTT addition by microplate reader analysis
Inhibition of recombinant human HSP90 ATPase activity expressed in Escherichia coli BL21 incubated for 3 hrs in presence of ATP by malachite green dye based microplate reader analysis
Inhibition of HSP90 in human HeLa cells assessed as reduction in ERK phosphorylation at 30 to 100 uM measured after 12 hrs by Western blot analysis
Inhibition of HSP90 in human HeLa cells assessed as reduction in p70s6k phosphorylation at 30 to 100 uM measured after 12 hrs by Western blot analysis
Inhibition of HSP90 in human HeLa cells assessed as reduction in AKT phosphorylation at 30 to 100 uM measured after 12 hrs by Western blot analysis
Inhibition of HSP90 in human HeLa cells assessed as reduction in CDK4 protein expression at 30 to 100 uM measured after 24 hrs by Western blot analysis
Binding affinity to recombinant human HSP90alpha assessed as gibbs free energy change by isothermal titration calorimetry assay
Assay data:4 Tested
Binding affinity to recombinant human HSP90alpha assessed as change in entropy by isothermal titration calorimetry assay
Binding affinity to recombinant human HSP90alpha assessed as change in enthalpy by isothermal titration calorimetry assay
Binding affinity to recombinant human HSP90alpha assessed as association constant by isothermal titration calorimetry assay
Binding affinity to recombinant human HSP90alpha assessed as dissociation constant by isothermal titration calorimetry assay
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