| Assay ID | Title | Year | Journal | Article |
|---|
| AID1240280 | Protein binding in human plasma | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240287 | Time duration showing fAUC above cellular EC50 against EZH2 in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240290 | Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 50 to 200 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240272 | Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240289 | Inhibition of EZH2 in human KARPAS422 cells xenografted CB17 SCID mouse assessed as reduction in H3K27me3 levels at 200 mg/kg, sc BID for 17 days measured at 1 to 12 hrs post last dose by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240279 | Protein binding in dog plasma | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240286 | Half life in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240274 | Intrinsic clearance in rat liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240288 | AUC in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240292 | Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 100 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240275 | Intrinsic clearance in dog liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240277 | Protein binding in mouse plasma | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240282 | Volume of distribution at steady state in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240284 | AUC in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1734648 | Inhibition of wild-type EZH2 in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins followed by addition of [3H]-SAM measured after 2 hrs by Topcount scintillation proximity assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl |
| AID1240271 | Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240285 | Cmax in CB17 SCID mouse at 200 mg/kg, sc by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240291 | Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 50 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240293 | Antitumor activity against human KARPAS422 cells xenografted in CB17 SCID mouse assessed as reduction tumor volume at 200 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240295 | Toxicity in human KARPAS422 cells xenografted CB17 SCID mouse assessed as body weight loss at 50 to 200 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240294 | Toxicity in human KARPAS422 cells xenografted CB17 SCID mouse assessed as drug tolerability at 50 to 200 mg/kg, sc BID for 28 days | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240273 | Intrinsic clearance in mouse liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1734649 | Inhibition of EZH2 Y641F mutant in PRC2 complex (unknown origin) using RKQLATKAARK(Me3)SAPATGGVKKP-NH2 peptide substrate preincubated for 30 mins followed by addition of [3H]-SAM measured after 2 hrs by Topcount scintillation proximity assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl |
| AID1240270 | Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240276 | Intrinsic clearance in human liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1240281 | Half life in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1734650 | Inhibition of EZH2 in human HeLa cells assessed as inhibition of trimethylation of H3K27 after 72 hrs by AlphaLISA assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl |
| AID1240283 | Clearance in CB17 SCID mouse at 1 mg/kg, iv by LC-MS method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1854352 | Inhibition of SARS-CoV-2 PLpro | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Chalcone-amide, a privileged backbone for the design and development of selective SARS-CoV/SARS-CoV-2 papain-like protease inhibitors. |
| AID1240278 | Protein binding in rat plasma | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Discovery, design, and synthesis of indole-based EZH2 inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| 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] |