Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 115 hits in this display
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 0.0300nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 0.630nMAssay Description:Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 0.640nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM332539((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(2-ethox...)
BDBM332539((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(2-ethox...)
BDBM332536((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(3-metho...)IC50: 0.760nMAssay Description:Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin pe...More data for this Ligand-Target Pair
BDBM332536((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(3-metho...)
IC50: 0.765nMAssay Description:The kinase analysis in vitro was performed using the HTRF kinEASE TK kit of Invitrogen Co., the procedure steps were carried out according to instruc...More data for this Ligand-Target Pair
IC50: 1.5nMAssay Description:Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin pe...More data for this Ligand-Target Pair
BDBM264129((R,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methox...)
BDBM264129((R,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methox...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 1.60nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM139994(US8901140, 9 | US9358227, 9)
BDBM139994(US8901140, 9 | US9358227, 9)
BDBM264128((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methoxyq...)IC50: 2.30nMAssay Description:To investigate whether a compound is able to inhibit the activity of EGFR and ErbB2 in cells, a mechanism-based assay using BT474 (EGFR overexpressio...More data for this Ligand-Target Pair
BDBM139992(US8901140, 7 | US9358227, 7)IC50: 4nMAssay Description:The following assay may be used to determine the activity of the compounds of the invention for inhibiting EGFR kinase activity. The half maximal inh...More data for this Ligand-Target Pair
BDBM139992(US8901140, 7 | US9358227, 7)
IC50: 4nMAssay Description:The following assay may be used to determine the activity of the compounds of the invention for inhibiting EGFR kinase activity. The half maximal inh...More data for this Ligand-Target Pair
BDBM264128((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methoxyq...)
IC50: 5nMAssay Description:To investigate whether a compound is able to inhibit the activity of EGFR and ErbB2 in cells, a mechanism-based assay using BT474 (EGFR overexpressio...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 6nMAssay Description:Inhibition of human GST-fused EGFR kinase domain expressed in baculovirus expression system measured after 30 mins by ELISAMore data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 6nMAssay Description:Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assess...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 6.90nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 6.90nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM139994(US8901140, 9 | US9358227, 9)
IC50: 9nMAssay Description:Irreversible inhibition of full length human ERBB1 autophosphorylation transfected in EGF-stimulated mouse NIH/3T3 cells incubated for 2 hrs followed...More data for this Ligand-Target Pair
IC50: 9.87nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 11.3nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112504(US8623883, No. 10)IC50: 12.1nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM264159((S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methox...)IC50: 14.2nMAssay Description:To investigate whether a compound is able to inhibit the activity of EGFR and ErbB2 in cells, a mechanism-based assay using BT474 (EGFR overexpressio...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 16.7nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 18.1nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM264159((S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-methox...)
IC50: 21.5nMAssay Description:To investigate whether a compound is able to inhibit the activity of EGFR and ErbB2 in cells, a mechanism-based assay using BT474 (EGFR overexpressio...More data for this Ligand-Target Pair
BDBM332536((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(3-metho...)
IC50: 39nMAssay Description:Inhibition of recombinant human His-tagged HER2 catalytic domain (676 to 1255 residues) expressed in baculovirus expression system using TK-biotin pe...More data for this Ligand-Target Pair
BDBM332536((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(3-metho...)
IC50: 39.3nMAssay Description:The kinase analysis in vitro was performed using the HTRF kinEASE TK kit of Invitrogen Co., the procedure steps were carried out according to instruc...More data for this Ligand-Target Pair
BDBM112504(US8623883, No. 10)
IC50: 41.3nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM332539((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(2-ethox...)
IC50: 42nMAssay Description:Inhibition of recombinant human His-tagged HER2 catalytic domain (676 to 1255 residues) expressed in baculovirus expression system using TK-biotin pe...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM332539((E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(2-ethox...)
IC50: 42.1nMAssay Description:The kinase analysis in vitro was performed using the HTRF kinEASE TK kit of Invitrogen Co., the procedure steps were carried out according to instruc...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 45.3nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 46nMAssay Description:Inhibition of human GST-fused HER2 kinase domain expressed in baculovirus expression system measured after 30 mins by ELISAMore data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 46nMAssay Description:Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assess...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 56nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 61nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
IC50: 61.5nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 77.5nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 83.7nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 84.0nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112504(US8623883, No. 10)
IC50: 86.0nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 88nMAssay Description:Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assesse...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 147nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 154nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 212nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 234nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 244nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
IC50: 247nMpH: 7.4 T: 2°CAssay Description:Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 978nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 1.17E+3nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 1.60E+3nMAssay Description: This assay quantifies the phosphorylation of EGFR at Tyr1068 and was used to measure the inhibitory effect of compounds on the transgenic EGFR del19...More data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
IC50: 7.40E+3nMAssay Description:Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic...More data for this Ligand-Target Pair
IC50: >1.00E+4nMAssay Description:Inhibition of EGFR phosphorylation in EGF-stimulated human KB cells preincubated for 1 hr followed by EGF stimulation measured after 6 mins by ELISAMore data for this Ligand-Target Pair
IC50: >1.00E+4nMAssay Description:Inhibition of EGFR phosphorylation in EGF-stimulated human KB cells preincubated for 1 hr followed by EGF stimulation measured after 6 mins by ELISAMore data for this Ligand-Target Pair
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
BDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
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