| Assay ID | Title | Year | Journal | Article |
|---|
| AID1251815 | Degradation activity of ERalpha receptor in human MCF7 cells at 0.01 to 300 nM after 48 hrs by Western blot analysis | 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 |
| AID1512599 | Lipophilicity, log D of the compound at pH 7.4 by shake flask method | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| 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 |
| AID1512600 | Stability of the compound assessed as parent compound remaining in buffer at pH 7.4 measured after 3 days by 1H-NMR analysis | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| 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 |
| AID1512618 | Induction of ERalpha degradation in human MCF7 cells assessed as downregulation of ER alpha receptor expression measured after 18 to 22 hrs by immunofluorescence assay relative to fulvestrant | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| 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 |
| 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 |
| AID1251786 | Thermodynamic solubility of the compound in 0.1 M phosphate buffer at pH 7.4 after 24 hrs | 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 |
| AID1251804 | Clearance in Alderley Park beagle dog at 2.5 umol/kg, iv and 5 umol/kg, po | 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 |
| AID1512607 | Induction of ERalpha degradation in human MCF7 cells assessed as downregulation of ER alpha receptor expression measured after 18 to 22 hrs by immunofluorescence assay | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| AID1512604 | Intrinsic clearance in rat hepatocytes assessed per 10'6 cells | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| AID1512605 | Intrinsic clearance in human hepatocytes assessed per 10'6 cells | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| AID1512603 | Fraction unbound in human plasma by equilibrium dialysis method | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| AID1251809 | Volume of distribution at steady state in SCID mouse at 2.3 umol/kg, iv and 5.6 umol/kg, po | 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 |
| AID1251816 | Antitumor activity against human MCF7 cells xenografted in mouse assessed as tumor growth inhibition administered orally daily once | 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 |
| AID1512606 | Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus infected insect cells measured after 20 mins by TR-FRET Lanthascreen assay | 2019 | ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
| Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry. |
| AID1251803 | Volume of distribution at steady state in Alderley Park beagle dog at 2.5 umol/kg, iv and 5 umol/kg, po | 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 |
| AID1251785 | Lipophilicity, log D of the compound at pH 7.4 | 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 |
| AID1251810 | Clearance in SCID mouse at 2.3 umol/kg, iv and 5.6 umol/kg, po | 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 |
| AID1251808 | Oral bioavailability in Han Wistar rat at 4.5 umol/kg | 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 |
| AID1698772 | Induction of estrogen receptor degradation in human MCF7 cells | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD). |
| AID1251817 | Antitumor activity against human MCF7 cells xenografted in mouse assessed as tumor regression at 5 mg/kg, po qd | 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 |
| AID1251806 | Volume of distribution at steady state in Han Wistar rat at 2.2 umol/kg, iv and 4.5 umol/kg, po | 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 |
| AID1251788 | Fraction unbound in human 10% plasma by equilibrium dialysis | 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 |
| AID1251814 | Agonist activity at progesterone receptor in human MCF7 cells in presence of 0.25 uM tamoxifen | 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 |
| AID1251793 | Binding affinity to glucocorticoid 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 |
| AID1251805 | Oral bioavailability in Alderley Park beagle dog at 5 umol/kg | 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 |
| AID1251807 | Clearance in Han Wistar rat at 2.2 umol/kg, iv and 4.5 umol/kg, po | 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 |
| AID1251790 | Intrinsic clearance in human cryopreserved hepatocytes assessed per 10'6 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 |
| 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 |
| AID1698771 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD). |
| AID1251811 | Oral bioavailability in SCID mouse at 5.6 umol/kg | 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 |
| AID1698770 | Binding affinity to estrogen receptor (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
| Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD). |
| AID1251813 | Antagonist activity at ERalpha receptor in human MCF7 cells in presence of 0.25 uM tamoxifen | 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 |
| AID1251792 | Binding affinity to progesterone 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 |
| AID1251789 | Intrinsic clearance in rat cryopreserved hepatocytes assessed per 10'6 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 |
| AID1251787 | Fraction unbound in Han Wistar rat 10% plasma by equilibrium dialysis | 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 |
| AID1251791 | Binding affinity to androgen 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 |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |