| Assay ID | Title | Year | Journal | Article |
|---|
| AID1801138 | In vivo Deuterated 1-Butanol PLD Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\ | 2015 | ACS chemical biology, Feb-20, Volume: 10, Issue:2
| Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. |
| AID1801141 | Exogenous PldA Assay from Article 10.1021/cb500828m: \\Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.\\ | 2015 | ACS chemical biology, Feb-20, Volume: 10, Issue:2
| Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID729447 | Cytotoxicity against human U87MG cells assessed as cell viability up to 10 uM by WST-1 assay in presence of 10% FBS relative to control | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729461 | Inhibition of human KOP receptor at 10 uM by radioligand binding assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729455 | Inhibition of CYP2D6 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729449 | AUC in balck6 mouse lung at 10 mg/kg, ip up to 6 hrs by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729467 | Inhibition of GFP-tagged PLD2 in human HEK293 cells assessed as deuterated 1-butanol incorporation pretreated for 5 mins prior to substrate addition measured after 30 mins by mass spectrometry | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729446 | Ratio of AUC in balck6 mouse brain to AUC in balck6 mouse plasma at 10 mg/kg, ip up to 6 hrs | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729462 | Solubility of the compound in PBS buffer | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729441 | Agonist activity at human MOP receptor | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729456 | Inhibition of CYP1A2 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID1532920 | Inhibition of PLD1 (unknown origin) | | | |
| AID729453 | Inhibition of CYP2C9 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729452 | Fraction unbound in human plasma after 4 hrs by equilibrium dialysis method | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729443 | Inhibition of PLD2 in human U87MG cells assessed as decrease in cell migration after 48 hrs by transwell invasion assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729459 | Inhibition of human ERG | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729451 | Fraction unbound in rat plasma after 4 hrs by equilibrium dialysis method | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729450 | AUC in balck6 mouse brain at 10 mg/kg, ip up to 6 hrs by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID1532921 | Inhibition of PLD2 (unknown origin) | | | |
| AID729463 | Inhibition of human ERG at 10 uM by radioligand binding assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729457 | Clearance in rat liver microsomes at 1 uM incubated for 5 mins prior to NADPH addition measured after 3 to 45 mins by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729468 | Inhibition of PLD1 in human Calu-1 cells assessed as deuterated 1-butanol incorporation pretreated for 5 mins prior to substrate addition measured after 30 mins by mass spectrometry | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729470 | Selectivity ratio of IC50 for human PLD1 to IC50 for human PLD2 | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729448 | AUC in balck6 mouse plasma at 10 mg/kg, ip up to 6 hrs by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729458 | Clearance in human liver microsomes at 1 uM incubated for 5 mins prior to NADPH addition measured after 3 to 45 mins by LC/MS/MS analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729454 | Inhibition of CYP3A4 (unknown origin) | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID1532923 | Selectivity ratio of IC50 for PDL1 (unknown origin) to IC50 for PDL2 (unknown origin) | | | |
| AID729464 | Stability of the compound in PBS buffer up to 48 hrs | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729460 | Inhibition of human MOP receptor at 10 uM by radioligand binding assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| AID729442 | Agonist activity at human KOP receptor | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |