| Assay ID | Title | Year | Journal | Article |
|---|
| AID1230875 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 10 mg/kg, po measured at 6 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230879 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 10 mg/kg, po measured at 3 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230861 | Apparent permeability across basolateral to apical side in human Caco2 cells | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230857 | Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230888 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 1 mg/kg, po measured at 1 hr relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230881 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 10 mg/kg, po measured at 10 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230856 | Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230872 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 10 mg/kg, po measured at 24 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230912 | Inhibition of recombinant human cFMS at 3 uM relative to control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230928 | Mutagenicity in Salmonella typhi in absence of S9 fractions | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230917 | Inhibition of ATM (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230887 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 1 mg/kg, po measured at 24 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230863 | Clearance in rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230854 | Inhibition of mTOR (unknown origin) by HTR-FRET substrate phosphorylation assay | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230910 | Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor volume reduction at 1 mg/kg administered as bid with 10 hrs separation between morning and evening doses for 21 days measured on day 21 post last dose relative to | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230923 | Inhibition of CYP450 (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230918 | Selectivity ratio of IC50 for PI3Kalpha (unknown origin) to IC50 for mTOR (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230914 | Inhibition of human DNA PK | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230874 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 10 mg/kg, po measured at 3 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230894 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 1 mg/kg, po measured at 3 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230859 | Metabolic stability in human liver S9 fraction assessed as compound remaining measured at 60 mins | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230925 | Inhibition of PDE3 (unknown origin) at 10 uM relative to control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230927 | Mutagenicity in Salmonella typhi in presence of S9 fractions | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230880 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 10 mg/kg, po measured at 6 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230865 | Oral bioavailability in rat at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230898 | Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor volume reduction administered as bid with 10 hrs separation between morning and evening doses for 21 days measured on day 21 post last dose | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230890 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 1 mg/kg, po measured at 6 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230903 | Toxicity in CB17 SCID mouse xenografted with human PC3 cells assessed as body weight loss at 1 mg/kg, administered as qd for 21 days | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230869 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 10 mg/kg, po measured at 3 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230889 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 1 mg/kg, po measured at 3 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230919 | Selectivity ratio of IC50 for ATM (unknown origin) to IC50 for mTOR (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230922 | Oral bioavailability in dog at 0.3 mg/kg | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230897 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 1 mg/kg, po measured at 24 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230895 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 1 mg/kg, po measured at 6 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230920 | Selectivity ratio of IC50 for ATR (unknown origin) to IC50 for mTOR (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230916 | Inhibition of ATR (unknown origin) at 30 uM relative to control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1872239 | Inhibition of mTOR (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Recent advances in DDR (DNA damage response) inhibitors for cancer therapy. |
| AID1230908 | Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor volume reduction at 0.25 mg/kg administered as bid with 10 hrs separation between morning and evening doses for 21 days measured on day 21 post last dose relative | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230858 | Metabolic stability in rat liver S9 fraction assessed as compound remaining measured at 60 mins | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230851 | Cmax in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230911 | Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor volume reduction at 1 mg/kg administered as qd for 21 days measured on day 21 post last dose relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230868 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 10 mg/kg, po measured at 1 hr relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230853 | AUC (0 to infinity) in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230913 | Inhibition of recombinant human cFMS | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230883 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 1 mg/kg, po measured at 1 hr relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230892 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 1 mg/kg, po measured at 24 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230864 | Mean residence time in rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230926 | Inhibition of PDE3 (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230901 | Toxicity in CB17 SCID mouse xenografted with human PC3 cells assessed as body weight loss at 0.25 to 1 mg/kg, administered as bid with 10 hrs separation between morning and evening doses for 21 days | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230873 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 10 mg/kg, po measured at 1 hr relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230886 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 1 mg/kg, po measured at 10 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230891 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 1 mg/kg, po measured at 10 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230878 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 10 mg/kg, po measured at 1 hr by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230893 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 1 mg/kg, po measured at 1 hr by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230909 | Antitumor activity against human PC3 cells xenografted in CB17 SCID mouse assessed as tumor volume reduction at 0.5 mg/kg administered as bid with 10 hrs separation between morning and evening doses for 21 days measured on day 21 post last dose relative t | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230915 | Inhibition of PI3Kalpha (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230860 | Apparent permeability across apical to basolateral side in human Caco2 cells | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230885 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 1 mg/kg, po measured at 6 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230884 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 1 mg/kg, po measured at 3 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230876 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 10 mg/kg, po measured at 10 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230882 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 10 mg/kg, po measured at 24 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230866 | Ratio of Cmax in rat at 5 mg/kg, po to IC50 for mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230862 | Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230867 | Ratio of AUC (0 to infinity) in rat at 5 mg/kg, po to IC50 for mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230871 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 10 mg/kg, po measured at 10 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230870 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of S6 phosphorylation at 10 mg/kg, po measured at 6 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230921 | Oral bioavailability in mouse at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230896 | Plasma concentration in CB17 SCID mouse xenografted with human PC3 cells at 1 mg/kg, po measured at 10 hrs by LC/MS-MS analysis | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230850 | Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKT phosphorylation at S473 after 1 hr | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1872250 | Inhibition of DNA-PK (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Recent advances in DDR (DNA damage response) inhibitors for cancer therapy. |
| AID1230877 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in CB17 SCID mouse assessed as inhibition of Akt phosphorylation at S473 at 10 mg/kg, po measured at 24 hrs relative to vehicle-treated control | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| AID1230924 | Inhibition of human ERG | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115. |
| 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] |