| Assay ID | Title | Year | Journal | Article |
|---|
| AID1205556 | Antagonist activity at ER alpha in human MCF7 cells assessed as inhibition of estradiol-induced PR expression treated for 24 hrs after incubation with estradiol for 30 mins by laser scanning imaging cytometer analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1690958 | Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assay relative to E2 | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1205557 | Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1690977 | Antiproliferative activity against human MCF7 cells assessed as cell mass at 10 uM measured after 72 hrs by crystal violet staining based assay relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1690957 | Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta by LanthaScreen TR-FRET assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID239820 | Mean fluorescence intensity corrected to basal for GW-5638 selective peptide binding to human estrogen receptor alpha | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
| AID1443550 | Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer. |
| AID1690963 | Antagonist activity at recombinant human GST-tagged ERbeta assessed as inhibition of E2-induced increase in fluorescein-labelled coactivator PGC1 peptide recruitment at 1 uM measured after 10 mins by LanthaScreen TR-FRET assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1228230 | AUC in mouse assessed as GW-7604 at 100 mg/kg, po | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1690969 | Antagonist activity at ERalpha (unknown origin) expressed in human U2OS cells assessed as inhibition of E2-induced transactivation measured after 21 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1228235 | Cytotoxicity against human MCF7 cells assessed as cell viability at 0.000005 to 10 uM after 5 days by CellTiter-Glo assay relative to fulvestrant | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1251784 | Antiproliferative activity against human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1251780 | Binding affinity to ERalpha receptor (unknown origin) | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1690989 | Cytotoxicity against African green monkey COS7 cells assessed as reduction in cell metabolic activity up to 10 uM measured after 72 hrs by modified MTT based EZ4U assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1205555 | Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1690964 | Antagonist activity at recombinant human GST-tagged ERbeta assessed as inhibition of E2-induced increase in fluorescein-labelled coactivator PGC1 peptide recruitment at 5 uM measured after 30 mins by LanthaScreen TR-FRET assay relative to control | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID244507 | Ishikawa cell alkaline phosphatase activity as percent maximal induction relative to 17 alpha-estradiol | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
| AID1535225 | Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay relative to fulvestrant | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
| Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft. |
| AID1228205 | Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1690956 | Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1251783 | Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1228236 | Displacement of [3H]-E2 from estrogen receptor-alpha (unknown origin) by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1251782 | Agonist activity at progesterone receptor in human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1205554 | Binding affinity to ER alpha (unknown origin) by LanthaScreen TR-FRET competitive binding assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1443552 | Induction of ERalpha degradation in human MCF7 cells assessed as remaining ERalpha protein level at 10 uM after 18 to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer. |
| AID1690986 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell metabolic activity up to 10 uM measured after 72 hrs by modified MTT based EZ4U assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1205568 | Free plasma concentration in rat by LC-UV-MS analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1690974 | Selective estrogen receptor alpha degrader activity in human MCF7 cells assessed as down regulation of ERalpha expression at 1 uM measured after 4 hrs in presence of protease inhibitor MG-132 by Western blot analysis | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1228206 | Induction of estrogen receptor-alpha degradation in human MCF7 cells at 5.12 x 10'-12 to 10'-5 M after 4 hrs by in-cell western assay relative to control | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID239927 | Binding affinity for human estrogen receptor alpha | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
| AID1690971 | Selective estrogen receptor alpha degrader activity in human MCF7 cells assessed as residual ERalpha level at 1 uM measured after 24 hrs by Western blot analysis (Rvb = 100%) | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1443551 | Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer. |
| AID1205563 | Thermodynamic solubility of the compound in 0.1 M aqueous phosphate buffer at 25 degC at pH 7.4 after 24 hrs | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1251781 | Antagonist activity at ERalpha receptor in human MCF7 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1228231 | Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID239921 | Binding affinity for human estrogen receptor beta | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
| AID1205571 | Intrinsic clearance in rat hepatocytes measured per 10'6 cells | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1228239 | Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228208 | Induction of estrogen receptor-alpha degradation in human MCF7 cells at 5.12 x 10'-12 to 10'-5 M after 4 hrs by in-cell western assay relative to fulvestrant | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1665630 | Brain to serum concentration ratio, Kp of the compound in C57BL/6 mouse at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID1443553 | Induction of ERalpha degradation in human MCF7 cells after 18 to 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer. |
| AID1690972 | Selective estrogen receptor alpha degrader activity in human MCF7 cells assessed as down regulation of ERalpha expression at 1 uM measured after 24 hrs by Western blot analysis relative to fulvestrant | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1599423 | Inhibition of Fluormone-ES2 binding affinity to ERalpha (unknown origin) after 2 hrs by fluorescent polarization based competition binding assay | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Estrogen signaling: An emanating therapeutic target for breast cancer treatment. |
| AID1228237 | Displacement of [3H]-E2 from estrogen receptor-beta (unknown origin) by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12
| Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1535226 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
| Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft. |
| AID249539 | pIC50 for 1 nM estradiol-induced Ishikawa cell proliferation | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling. |
| AID1251812 | Agonist activity at progesterone receptor (unknown origin) at 100 uM | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregu |
| AID1535224 | Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
| Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft. |
| AID1690959 | Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta by LanthaScreen TR-FRET assay relative to E2 | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1205564 | Inhibition of hERG channel by electrophysiology | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators. |
| AID1665608 | AUC (0.5 to 6 hrs) in C57BL/6 mouse brain at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID1665619 | AUC (0.5 to 6 hrs) in C57BL/6 mouse serum at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID1690960 | Selectivity ratio of IC50 for displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha to IC50 for displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| AID1690970 | Antagonist activity at ERbeta (unknown origin) expressed in human U2OS cells assessed as inhibition of E2-induced transactivation measured after 21 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |