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Inhibition of mTOR FKBP12(h) at 10.0 M in the Eurofins Kinase panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of recombinant human EmGFP fused FKBP12/GST-tagged human mTOR (1360 to 2549 residues) FRB domain incubated for 1 hrs by LanthaScreen based TR-FRET assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of FKBP12 (unknown origin) measured for 6 hrs relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of FKBP12 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to FKBP12 (unknown origin)
Assay data:10 Active, 1 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 11 Tested
Protac activity at CRBN/FKBP12 in human Jurkat cells
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Induction of degradation of FKBP12 (unknown origin)
SPR Assay to Characterize Ternary Complex Formation with FKBP12 from US Patent US11603377: "MTORC1 modulators and uses thereof"
Assay data:45 Active, 63 Activity ≤ 1 µM, 63 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
SPR Assay to Determine Binding Affinity to FKBP12 from US Patent US11603377: "MTORC1 modulators and uses thereof"
Assay data:50 Active, 64 Activity ≤ 1 nM, 64 Activity ≤ 1 µM, 64 Tested
Binding affinity to FKBP12 (unknown origin) assessed as inhibition constant
Assay data:7 Active, 6 Activity ≤ 1 µM, 7 Tested
Inhibition of human full length recombinant mTOR/FKBP12 in presence of [gamma-33P]ATP incubated for 40 mins by radiometric scintillation counting analysis
PROTAC activity at CRBN/FKBP12 in human Jurkat cells assessed as induction of FKBP12 degradation incubated for 12 hrs by Western blot analysis
NanoBRET assay (FKBP12-NLuc) (FKBP1B)
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMRelated BioAssays by Target
NanoBRET assay (FKBP12-NLuc) (FKBP1A)
NanoBRET assay (FKBP51-NLuc) (FKBP1A)
Competitive fluorescence polarization binding assay (FKBP1A)
Competitive fluorescence polarization binding assay (FKBP1B)
mTOR/FKBP12(h) Kinase panel
SPR Protocol to Measure Binding of a Compound to FKBP12 from US Patent US11059830: "Compounds that participate in cooperative binding and uses thereof"
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
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