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Binding affinity to ERRB3 (unknown origin) assessed as strong interaction at 100 nM
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of HER3 (unknown origin)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of human GST-fused EGFR T790M/C797S double mutant expressed in Sf9 insect cells by HTRF assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
ERBB3 DiscoveRx kinase panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
TR-FRET Assay for ERBB Kinases from US Patent US10994015: "EGFR proteolysis targeting chimeric molecules and associated methods of use"
Assay data:93 Active, 6 Activity ≤ 1 nM, 70 Activity ≤ 1 µM, 108 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
KinomeScan assay: inhibition of ERBB3
Assay data:108 Tested
Inhibition of HER2/HER3 dimerization in human Calu-3 cells incubated for 48 hrs by proximity ligation assay
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of HER2/HER3 dimerization in human A549 cells incubated for 48 hrs by proximity ligation assay
Inhibition of human ERBB3 assessed as percent of control at 2000 nM by KINOMEscan assay relative to control
Inhibition of DNA-tagged human ERBB3 assessed as percent of control at 50000 nM by qPCR analysis relative to control
Inhibition of human ERBB3 assessed as percent of control at 1000 nM by KINOMEscan assay relative to control
Inhibition of human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by kinome scan method relative to control
Inhibition of recombinant human wild type partial length HER3 (684 to 987 residues) expressed in mammalian expression system by competitive binding assay
Inhibition of HER3 (unknown origin) at 10 uM using peptide as substrate incubated for 10 mins by caliper assay relative to control
Binding affinity to wild-type human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system assessed as residual binding level at 10 uM by Kinomescan method relative to control
Inhibition of wild-type human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system at 1 uM by Kinomescan method relative to control
Inhibition of wild-type human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system at 10 uM by Kinomescan method relative to control
Binding affinity to wild-type human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system assessed as residual binding level at 1 uM by Kinomescan method relative to control
Inhibition of wild-type human partial length ERBB3 (G684 to A987 residues) expressed in mammalian expression system assessed as residual activity at 10 uM by Kinomescan method relative to control
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