Assay ID | Title | Year | Journal | Article |
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. |
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. |
AID70176 | In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
AID70008 | In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
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. |
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. |
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. |
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. |
AID1228310 | AUC in 17-beta estradiol pellets supplemented nu/nu mouse xenografted with tamoxifen-resistant human MCF7 cells at 100 mg/kg/day, po administered for 4 weeks measured on day 28 | 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. |
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. |
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. |
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. |
AID102611 | In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |