| Assay ID | Title | Year | Journal | Article |
|---|
| AID1152438 | Toxicity in N-methylnitrosurea-induced mammary cancer Sprague-Dawley rat model assessed as liver weight at 200 mg/kg administered through diet for 7 days | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1062026 | Agonist activity at human RARalpha expressed in HEK293 cells assessed as transcriptional activation at 10'-6 M after 48 hrs by luciferase reporter gene assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1250638 | Anticancer activity in methylnitrosourea-induced mammary cancer model of Sprague-Dawley rat assessed as decrease of tumor size at 200 mg/kg treated with diet for 4 weeks relative to control | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers. |
| AID1152429 | Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1896518 | Prevention of UVB-induced carcinogenesis in Ptch+/- / SHK-1 mouse assessed as reduction in tumor number at 20 mg/kg measured after twice a week of UVB irradiation for 34 weeks | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers. |
| AID1062020 | Antitumor activity against Sprague-Dawley rat mammary tumor cells assessed as increase in apoptotic index at 200 mg/kg, po after 7 days by TUNEL assay relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1062024 | Inhibition of KLF4-ER-mediated rat RK3E cell transformation after 3 weeks | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1062028 | Binding affinity to human RXRalpha ligand binding domain by fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1152431 | Agonist activity at human RXR-alpha-ligand binding domain homodimers assessed as coactivator recruitment by measuring GRIP1 binding to receptor by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1062023 | Toxicity in Sprague-Dawley rat assessed as increase in body weight at 200 mg/kg, po after 7 days relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1152437 | Toxicity in N-methylnitrosurea-induced mammary cancer Sprague-Dawley rat model assessed as body weight at 200 mg/kg administered through diet for 7 days | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1062025 | Toxicity in 50 days old Sprague-Dawley rat assessed as increase in serum triglyceride level at 200 mg/kg, po administered with diet after 7 days relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1062027 | Agonist activity at RXRalpha in rat RK3E cells assessed as transcriptional activation by luciferase reporter gene assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1062021 | Antitumor activity against BRDU-labeled Sprague-Dawley rat mammary tumor cells assessed as reduction in proliferation index at 200 mg/kg, po after 7 days relative to control | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Methyl-substituted conformationally constrained rexinoid agonists for the retinoid X receptors demonstrate improved efficacy for cancer therapy and prevention. |
| AID1152432 | Agonist activity at RXR-alpha in rat R3KE cells infected with oncogene KLF4-ER assessed as inhibition of KLF4-mediated oncogenic transformation | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1896476 | Binding affinity to human RXRalpha LBD (T225 to T462 residues) by fluorescence quenching assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers. |
| AID1250622 | Binding affinity to human RXRalpha LBD after 15 mins by isothermal titration calorimetry assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers. |
| AID1152436 | Anticancer activity against N-methylnitrosurea-induced mammary cancer in Sprague-Dawley rat assessed as decrease in proliferation index at 200 mg/kg administered through diet for 7 days by BrdU incorporation assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1250630 | Metabolic stability in methylnitrosourea-induced mammary cancer model of Sprague-Dawley rat assessed as compound level in serum at 200 mg/kg treated with diet for 3 months | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers. |
| AID1152434 | Induction of hyperlipidemia in N-methylnitrosurea-induced mammary cancer Sprague-Dawley rat model assessed as increase in serum triglyceride level at 200 mg/kg administered through diet for 7 days | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1152430 | Agonist activity at Gal4-fused human RAR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity at 1 uM treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1152428 | Binding affinity to human RXR-alpha-ligand binding domain homodimers by fluorescence quenching method | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity. |
| AID1896477 | Agonist activity at human GAL4-fused RXRalpha LBD (T225 to T462 residues) expressed in HEK293 cells incubated for 24 hrs by Dual-Glo luciferase assay | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
| Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2014 | The Journal of biological chemistry, Jan-10, Volume: 289, Issue:2
| Defining the communication between agonist and coactivator binding in the retinoid X receptor α ligand binding domain. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |