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In Vitro Evaluation of EPAC1 Inhibition from US Patent US11124489: "EPAC antagonists"
Assay data:24 Active, 53 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as induction of perturbation of allosteric network sites by CHESCA method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as binding to R279 Guanidinium residue by guanidinium HSQC NMR spectroscopy
Assay data:2 Active, 2 Tested
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) by STD and guanidinium HSQC NMR analysis
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as induction Intermolecular NOEs peaks in PBC and BBR residues by 15N-NOESY-HSQC NMR spectroscopy
Assay data:4 Active, 4 Tested
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as induction of conformational changes in compound by NOESY NMR spectroscopy
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as compound binding to base binding region incubated for 30 mins by CHESPA method
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as compound binding to phosphate binding cassette region incubated for 30 mins by CHESPA method
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues)expressed in Escherichia coli BL21 (DE3) assessed as compound binding to cAMP-binding sites incubated for 30 mins by CHESPA method
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by 1H,15N-HSQC NMR spectroscopy
Binding affinity to GST-tagged human EPAC1 L273W mutant expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by 8-NBD-cAMP based competitive fluorescence assay
Binding affinity to GST-tagged human EPAC1 CNBD (149 to 318 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by 8-NBD-cAMP based competitive fluorescence assay
Validation qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 3 (EPAC1)
Assay data:160 Active, 22 Activity ≤ 1 µM, 15634 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Validation qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 3 (EPAC1)
Assay data:115 Active, 91 Activity ≤ 1 µM, 15634 Tested
Confirmatory qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 3 (EPAC1)
Assay data:143 Active, 10 Activity ≤ 1 µM, 5387 Tested
Confirmatory qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 3 (EPAC1)
Assay data:748 Active, 66 Activity ≤ 1 µM, 5387 Tested
Inhibition of 8Fluo-cAMP binding to recombinant human His-tagged EPAC1 (157 to 881 residues) expressed in Escherichia coli measured after 5 mins by fluorescence polarization assay
Assay data:5 Active, 1 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human EPAC1 cAMP binding domain (149 to 318 residues) assessed as change in chemical shift at 100 uM in presence of human serum albumin by [15N-1H]HSQC spectroscopic analysis relative to compound alone
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to human EPAC1 cAMP binding domain (149 to 318 residues) assessed as increase in peak intensity at 100 uM in presence of human serum albumin by [15N-1H]HSQC spectroscopic analysis relative to control
Binding affinity to human EPAC1 cAMP binding domain (149 to 318 residues) assessed as increase in peak intensity in presence of human serum albumin by [15N-1H]HSQC spectroscopic analysis relative to control
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