| Assay ID | Title | Year | Journal | Article |
|---|
| AID1228215 | Drug metabolism in beagle dog liver microsomes assessed as GW-7604 formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID91598 | Maximum stimulation of alkaline phosphatase activity expressed as a percent of the maximum induced by 10 nM estradiol | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
| 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats. |
| 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. |
| 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. |
| 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. |
| AID1205573 | Clearance in Alderley Park Han Wistar rat at 0.5 mg/kg, iv | 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. |
| AID1205577 | Oral bioavailability in Alderley Park Han Wistar rat at 1 mg/kg using 5% DMSO, 95% of a 30% aqueous cyclodextrin solution | 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. |
| AID1535227 | Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS at 2 to 10 uM 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. |
| AID70324 | Antagonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives. |
| AID1205574 | Volume of distribution at steady state in CD-1 mouse at 0.5 mg/kg, iv | 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. |
| 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. |
| AID1228223 | Drug metabolism in beagle dog liver microsomes assessed as (E)-3-(4-((Z)-2-(3-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| AID1228225 | Drug metabolism in CD-1 mouse liver microsomes assessed as (E)-3-(4-((Z)-2-(4-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| 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. |
| 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. |
| 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 |
| 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. |
| AID1228228 | Drug metabolism in human liver microsomes assessed as (E)-3-(4-((Z)-2-(4-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS an | 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. |
| AID1228209 | Metabolic stability in CD-1 mouse liver microsomes assessed as compound remaining at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID1205566 | Free plasma concentration in human 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. |
| AID1205567 | Free plasma concentration in mouse 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. |
| 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. |
| AID1228212 | Metabolic stability in human liver microsomes assessed as compound remaining at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID70321 | Displacement of [3H]17-beta-estradiol from human Estrogen receptor alpha | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives. |
| 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. |
| AID1228210 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| 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 |
| AID1228222 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as (E)-3-(4-((Z)-2-(3-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs b | 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. |
| AID1228229 | AUC in mouse 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. |
| 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. |
| AID1205576 | Oral bioavailability in CD-1 mouse at 50 mg/kg using 0.5% polysorbate suspension | 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. |
| AID1228306 | Antitumor activity against tamoxifen-resistant human MCF7 cells xenografted in nu/nu mouse supplemented with 17-beta estradiol pellets assessed as tumor volume at 100 mg/kg/day, po administered for 4 weeks measured twice weekly during compound dosing rela | 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. |
| AID1228221 | Drug metabolism in CD-1 mouse liver microsomes assessed as (E)-3-(4-((Z)-2-(3-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| AID1205572 | Clearance in CD-1 mouse at 0.5 mg/kg, iv | 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. |
| 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. |
| AID1228220 | Drug metabolism in human liver microsomes assessed as (E)-3-(4-((E)-1-(3-hydroxyphenyl)-2-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS an | 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. |
| AID1228217 | Drug metabolism in CD-1 mouse liver microsomes assessed as (E)-3-(4-((E)-1-(3-hydroxyphenyl)-2-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| AID1205575 | Volume of distribution at steady state in Alderley Park Han Wistar rat at 0.5 mg/kg, iv | 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. |
| 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 |
| AID1228224 | Drug metabolism in human liver microsomes assessed as (E)-3-(4-((Z)-2-(3-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS an | 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. |
| AID70645 | Displacement of [3H]17-beta-estradiol from human Estrogen receptor beta | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives. |
| AID1205558 | Inhibition of cell proliferation in human MCF7 cells after 7 days 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. |
| 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. |
| AID1228211 | Metabolic stability in beagle dog liver microsomes assessed as compound remaining at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID91597 | Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11
| 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid: a non-steroidal estrogen with functional selectivity for bone over uterus in rats. |
| AID1228219 | Drug metabolism in beagle dog liver microsomes assessed as (E)-3-(4-((E)-1-(3-hydroxyphenyl)-2-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| AID1205559 | Octanol-buffer partition coefficient, log D of the compound at ratio of 1:100 at pH 7.4 by shake-flask method | 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. |
| AID70189 | Agonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha; Not active means no effect at < 1000 nM | 2000 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
| Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives. |
| 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. |
| 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. |
| 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. |
| 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 |
| AID1228214 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as GW-7604 formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID1228218 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as (E)-3-(4-((E)-1-(3-hydroxyphenyl)-2-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs b | 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. |
| 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 |
| 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. |
| AID1228227 | Drug metabolism in beagle dog liver microsomes assessed as (E)-3-(4-((Z)-2-(4-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/ | 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. |
| AID1228216 | Drug metabolism in human liver microsomes assessed as GW-7604 formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| AID1228213 | Drug metabolism in CD-1 mouse liver microsomes assessed as GW-7604 formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs by LC/MS/MS 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. |
| 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. |
| AID1228226 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as (E)-3-(4-((Z)-2-(4-hydroxyphenyl)-1-phenylbut-1-enyl)phenyl)acrylic acid formation at 4 uM preincubated for 10 mins followed by addition of NADPH regenerating system measured after 4 hrs b | 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. |
| 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 |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |