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CRBN Fluorescence Polarization Assay from US Patent US20240132463: "SUBSTITUTED N-(2-(2,6-DIOXOPIPERIDIN-3-YL)-1,3-DIOXOISOINDOLIN-5-YL)ARYLSULFONAMIDE ANALOGS AS MODULATORS OF CEREBLON PROTEIN"
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Cereblon Binding Assay from US Patent US20240109877: "PYRIMIDINES FOR DEGRADING BRUTON'S TYROSINE KINASE"
Assay data:14 Active, 5 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Compound Activity by Fluorescent Polarization Assay from US Patent US11912682: "Isoindolinone compounds"
Assay data:126 Active, 103 Activity ≤ 1 µM, 155 Tested
Cereblon Binding Assay from US Patent US20240059711: "Cereblon Ligands and Uses Thereof"
Assay data:15 Active, 10 Activity ≤ 1 µM, 15 Tested
Cereblon Binding Assay from US Patent US20240059704: "Cereblon Ligands and Uses Thereof"
Assay data:5 Active, 2 Activity ≤ 1 µM, 5 Tested
In Vitro Assay: IC50 Measurements for Binding to CRBN/DDB1 from US Patent US20240059704: "Cereblon Ligands and Uses Thereof"
Assay data:4 Active, 1 Activity ≤ 1 µM, 4 Tested
Fluorescent Polarization Assay from US Patent US20240051936: "ISOINDOLINONE COMPOUNDS"
Assay data:40 Active, 30 Activity ≤ 1 µM, 66 Tested
Protac activity at CRBN/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 10 uM incubated for 6 hrs by Western blot analysis (Rvb = 0%)
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Protac activity at CRBN/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 1 uM incubated for 6 hrs by Western blot analysis (Rvb = 0%)
Protac activity at CRBN/AR in AR-positive human LNCaP cells assessed as induction of androgen receptor degradation at 0.1 uM incubated for 6 hrs by Western blot analysis (Rvb = 0%)
PROTAC activity at CRBN/BRD7 in human Ri-1 cells assessed as remaining BRD7 protein level at 1 uM incubated for 8 hrs by Western blot analysis relative to control
Assay data:1 Tested
PROTAC activity at CRBN/BRD9 in human Ri-1 cells assessed as remaining BRD9 protein level at 1 uM incubated for 8 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD7 in human Ri-1 cells assessed as remaining BRD7 protein level at 1 uM incubated for 2 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD9 in human Ri-1 cells assessed as remaining BRD9 protein level at 1 uM incubated for 2 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD7 in human HeLa cells assessed as remaining BRD7 protein level at 1 uM incubated for 16 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD7 in human HeLa cells assessed as remaining BRD7 protein level at 1 uM incubated for 4 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD9 in human HeLa cells assessed as remaining BRD9 protein level at 1 uM incubated for 16 hrs by Western blot analysis relative to control
PROTAC activity at CRBN/BRD9 in human HeLa cells assessed as remaining BRD9 protein level at 1 uM incubated for 4 hrs by Western blot analysis relative to control
Invivo PROTAC activity at CRBN/MDM2 in human RS4-11 cells xenografted in mouse assessed as fold change in cleaved PARP protein level in tumor at 25 mg/kg, iv administered as single dose and measured after 24 hrs by Western blot analysis (Rvb = 1 to 1.2 No_unit)
Invivo PROTAC activity at CRBN/MDM2 in human RS4-11 cells xenografted in mouse assessed as fold change in cleaved PARP protein level in tumor at 25 mg/kg, iv administered as single dose and measured after 6 hrs by Western blot analysis (Rvb = 1 to 1.2 No_unit)
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