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In Vitro Evaluation of EPAC2 Inhibition from US Patent US11124489: "EPAC antagonists"
Assay data:19 Active, 22 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Validation qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 4 (EPAC2)
Assay data:41 Active, 124 Activity ≤ 1 µM, 15613 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Validation qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 4 (EPAC2)
Assay data:265 Active, 171 Activity ≤ 1 µM, 15637 Tested
Confirmatory qHTS for antagonist of cAMP-regulated guanine nucleotide exchange factor 4 (EPAC2)
Assay data:691 Active, 129 Activity ≤ 1 µM, 5387 Tested
Confirmatory qHTS for agonist of cAMP-regulated guanine nucleotide exchange factor 4 (EPAC2)
Assay data:222 Active, 11 Activity ≤ 1 µM, 5387 Tested
Inhibition of 8Fluo-cAMP binding to DEP domain deficient mouse EPAC2 (280 to 988 residues) measured after 5 mins by fluorescence polarization assay
Assay data:5 Active, 2 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human GST-tagged EPAC2 expressed in Escherichia coli Rosetta 2(DE3) assessed as reduction in guanine nucleotide exchange activity using BODIPY-labeled GDP loaded Rap1A by fluorescence assay
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at mouse EPAC2 assessed as inhibition of EPAC2-mediated Rap1B (1 to 167 residues)-BODIPY GDP nucleotide exchange activity by 8-NBD-cAMP competition assay
Assay data:11 Active, 11 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at recombinant full length EPAC2 (unknown origin) assessed as inhibition of cAMP-mediated Rap1b-BODIPY GDP nucleotide exchange activity
Assay data:8 Active, 24 Tested
Inhibition of EPAC2 (unknown origin)
Assay data:1 Active, 1 Tested
Displacement of 8-NBD-cAMP from mouse EPAC2 by fluorescence assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Human Rap guanine nucleotide exchange factor 4 (Exchange protein activated by cyclic AMP (EPACs))
Non-competitive inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity at 1 uM in presence of C-terminal truncated Rap1B (1 to 167 residues)-BODIPY-GDP
Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 to 167 residues)-Mant-GDP by spectrofluorometric analysis
Inhibition of EPAC2 (unknown origin) assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1 to 167 residues)-BODIPY-GDP by microplate reader analysis
Assay data:4 Active, 1 Activity ≤ 1 µM, 5 Tested
Inhibition of 8-NBD-cAMP binding to EPAC2 (unknown origin) by microplate reader analysis
Assay data:27 Active, 7 Activity ≤ 1 µM, 31 Tested
Ratio of ESI-09 IC50 to compound IC50 for displacement of 8-NBD-cAMP from mouse recombinant EPAC2 by fluorescence assay
Assay data:10 Tested
Ratio of cAMP IC50 to compound IC50 for displacement of 8-NBD-cAMP from mouse recombinant EPAC2 by fluorescence assay
Assay data:36 Tested
Displacement of 8-NBD-cAMP from mouse recombinant EPAC2 by fluorescence assay
Assay data:20 Active, 1 Activity ≤ 1 µM, 49 Tested
Antagonist activity at EPAC2 (unknown origin) assessed as cAMP-induced guanine nucleotide exchange factor activity
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