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Protac activity at CRBN/GSPT1 in human MOLT-4 cells assessed as induction of GSPT1 degradation assessed as maximum degradation after 24 hrs relative to control
Assay data:14 Tested
SummaryPubMed CitationRelated BioAssays by Target
Protac activity at CRBN/IKZF1 in human MOLT-4 cells assessed as induction of IKZF1 degradation after 24 hrs
Assay data:4 Active, 3 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Protac activity at CRBN/IKZF1 in human MOLT-4 cells assessed as induction of IKZF1 degradation assessed as maximum degradation after 24 hrs relative to control
Displacement of fluorescent tracer from NanoLuc-tagged CRBN (unknown origin) by NanoBRET assay
Assay data:14 Active, 10 Activity ≤ 1 µM, 14 Tested
Metabolic stability in human hepatocytes assessed as intrinsic clearance and measured upto 60 mins in presence of NADPH by LC-MS/MS analysis
Assay data:3 Tested
SummaryPubMed Citation
Microsomal stability in human liver microsomes assessed as intrinsic clearance and measured upto 60 mins in presence of NADPH by LC-MS/MS analysis
Metabolic stability in human plasma assessed as half life and measured upto 240 mins by LC-MS/MS analysis
Protac activity at CRBN/HiBiT-tagged IKZF1 in human MOLT-4 cells assessed as IKZF1 degradation by measuring luminescence by luminescence based HiBiT assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 5 Tested
Drug accumulation in human MOLT-4 cells assessed as intracellular bioavailability by LC-MS analysis
Assay data:5 Tested
Drug accumulation in human MOLT-4 cells assessed as intracellular drug accumulation incubated for 4 hrs by LC-MS analysis
Drug accumulation in human MOLT-4 cells assessed as intracellular unbound fraction incubated for 4 hrs by LC-MS analysis
Stability in human plasma assessed as half life at 1 uM by LC-MS/MS analysis
Metabolic stability in human liver microsome assessed as half-life at 1 uM in presence of NADPH incubated up to 60 mins by LC-MS/MS analysis
Kinetic solubility of compound in PBS at 200 uM incubated for 30 mins by LC-MS/MS analysis
Efflux ratio of apparent permeability of compound across basolateral to apical side over apical to basolateral side in human Caco-2 cells at 10 uM incubated for 90 mins by LC-MS/MS analysis
Apparent permeability in in human Caco-2 cells at 10 uM incubated for 90 mins by LC-MS/MS analysis
Distribution coefficient, logD of compound at 1 mg/ml measured at pH 7.4 by chromatography based LC-UV analysis
Inhibition of angiogenesis (new microvessel growth) in rat aortic ring model at 200 uM in Endothelial basal medium (EBM) and Dimethylsulfoxide (DMSO)
Assay data:1 Tested
Inhibition of angiogenesis (new microvessel growth) in rat aortic ring model at 100 uM in Endothelial basal medium (EBM) and Dimethylsulfoxide (DMSO)
Inhibition of microvessel outgrowth in the rat aortic ring assay
Assay data:39 Tested
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