Assay ID | Title | Year | Journal | Article |
AID1724950 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg administered via gavage | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724955 | AUC in CD1 mouse at 5 mg/kg, iv | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724946 | Clearance in Sprague-Dawley rat plasma at 5 mg/kg, iv administered as bolus dose | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724954 | Clearance in CD1 mouse plasma at 5 mg/kg, iv | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1599455 | Inhibition of Bcl-xL (unknown origin) | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | The chemical biology of apoptosis: Revisited after 17 years. |
AID1293719 | Binding affinity to Bcl-2 (unknown origin) by FRET assay | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
AID1293724 | Cytotoxicity against human Bcl-XL dependant MOLT4 cells by cell based assay | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
AID1724959 | Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth inhibition at 25 mg/kg/day, po qd for 14 days relative to control | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724944 | Half life in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724951 | Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724952 | Half life in CD1 mouse at 5 mg/kg, iv | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724949 | AUC in Sprague-Dawley rat at 5 mg/kg, po administered via gavage | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724961 | Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth inhibition at 25 mg/kg/day, po qd for 14 days co-administered with 30 mg/kg irinotecan relative to control | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724948 | Cmax in Sprague-Dawley rat at 5 mg/kg, po administered via gavage | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724947 | AUC in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724958 | Oral bioavailability in CD1 mouse at 5 mg/kg | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724940 | Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724945 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv administered as bolus dose | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724953 | Volume of distribution at steady state in CD1 mouse at 5 mg/kg, iv | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1293725 | Cytotoxicity against human Bcl-2 dependant RS4:11 cells by cell based assay | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
AID1724962 | Antitumor activity against human COLO205 cells xenografted in SCID/beige mouse assessed as tumor growth delay at 25 mg/kg/day, po qd for 14 days co-administered with 30 mg/kg irinotecan relative to control | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724943 | Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs in presence of 10% human serum by CellTiter-Glo luminescent assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724956 | Cmax in CD1 mouse at 5 mg/kg, po | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724942 | Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide) F-Bak(GQVGRQLAIIGDK(6-FAM)INR-amide) binding to BCL2 (unknown origin) incubated for 1 hr by TR-FRET assay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1724957 | AUC in CD1 mouse at 5 mg/kg, po | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X |
AID1293720 | Binding affinity to Bcl-XL (unknown origin) by FRET assay | 2016 | Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
| Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |