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Cytotoxicity activity against human HepG2 cells assessed by CellTiter-Glo luminescent cell viability assay.
Assay data:1241 Active, 184 Activity ≤ 1 µM, 1545 Tested
Summary
Inhibition of BRDT (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryRelated BioAssays by Target
Anticancer activity against human MV4-11 cells assessed as cell growth inhibition
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Antiproliferative activity against human SU-DHL-4 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
Assay data:2 Active, 3 Tested
Binding affinity to BRD4 BD2 (unknown origin) assessed as dissociation constant by ITC analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antitumor activity against human CAPAN-1 cells xenografted in mouse assessed as tumor growth inhibition at 15 mg/kg, po bid administered for 21 days
Assay data:3 Tested
Anticancer activity against human CAPAN-1 cells
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant by ITC analysis
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay
Assay data:21 Active, 1 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 21 Tested
Inhibition of BRD4 BD2 (unknown origin) at 1 uM by TR-FRET assay
Assay data:8 Tested
Inhibition of BRD4 BD1 (unknown origin) at 1 uM by TR-FRET assay
Assay data:27 Tested
Protac activity at CRBN/BRD4 in human MV4-11 cells assessed as induction of BRD4 protein degradation by measuring residual activity at 10 uM measured after 6 hrs by Western blot analysis (Rvb = 100%)
Assay data:2 Tested
Protac activity at CRBN/BRD4 in human MV4-11 cells assessed as induction of BRD4 protein degradation by measuring residual activity at 1 uM measured after 6 hrs by Western blot analysis (Rvb = 100%)
Assay data:1 Tested
Protac activity at CRBN/BRD4 in human MM1.S cells assessed as induction of BRD4 protein degradation by measuring residual activity at 10 uM measured after 6 hrs by Western blot analysis (Rvb = 100%)
Protac activity at CRBN/BRD4 in human MM1.S cells assessed as induction of BRD4 protein degradation by measuring residual activity at 1 uM measured after 6 hrs by Western blot analysis (Rvb = 100%)
Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Assay data:12 Active, 12 Activity ≤ 1 µM, 12 Tested
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
Binding affinity to SMARCA2A (unknown origin) assessed as change in melting temperature at 200 uM incubated for 30 to 60 mins by SYPRO orange dye based thermal shift assay
Binding affinity to PCAF (unknown origin) assessed as change in melting temperature at 200 uM incubated for 30 to 60 mins by SYPRO orange dye based thermal shift assay
Binding affinity to BAZ2B (unknown origin) assessed as change in melting temperature at 200 uM incubated for 30 to 60 mins by SYPRO orange dye based thermal shift assay
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