| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID1194467 | Intrinsic clearance in mouse liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321417 | Fraction unbound in human plasma after 4 hrs by LC-MS/MS based equilibrium dialysis method | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194465 | Inhibition of human CHT Leu530Ala and Val531Ala mutant expressed in HEK293 cells assessed as remaining transporter activity in presence of 10 uM [3H]choline by [3H]choline uptake assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321426 | Drug uptake in cannulated Sprague-Dawley rat brain at 1 mg/kg, iv administered twice at 24 hrs interval followed by 0.75 min of isoflurane treatment post 15 min second dose measured after 0.25 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321413 | Inhibition of [3H]choline uptake at human choline transporter expressed in HEK293 cells preincubated for 15 mins followed by [3H]choline addition measured after 10 to 15 mins by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321422 | Inhibition of human CYP3A4 | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194472 | Inhibition of human CYP3A4 | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194462 | Inhibition of human CHT Leu530Ala and Val531Ala mutant expressed in HEK293 cells assessed as remaining transporter activity at 5 uM in presence of 100 nM [3H]choline by [3H]choline uptake assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194469 | Inhibition of human CYP1A2 | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194470 | Inhibition of human CYP2C9 | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321415 | Intrinsic clearance in human liver microsomes at 1 uM preincubated with microsomes followed by NADPH addition measured up to 45 mins by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321421 | Inhibition of human CYP2D6 | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194463 | Inhibition of human CHT Leu530Ala and Val531Ala mutant expressed in HEK293 cells assessed as remaining transporter activity at 5 uM in presence of 10 uM [3H]choline by [3H]choline uptake assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321427 | Ratio of drug level in cannulated Sprague-Dawley rat brain to plasma at 1 mg/kg, iv | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321420 | Inhibition of human CYP2C9 | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194471 | Inhibition of human CYP2D6 | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321419 | Inhibition of human CYP1A2 | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321416 | Fraction unbound in rat plasma after 4 hrs by LC-MS/MS based equilibrium dialysis method | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321418 | Fraction unbound in rat brain after 4 hrs by LC-MS/MS based equilibrium dialysis method | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321412 | Half life in cannulated Sprague-Dawley rat plasma at 1 mg/kg, iv by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194468 | Fraction unbound in mouse plasma by equilibrium dialysis method | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194474 | Drug level in mouse brain at 1 mg/kg, ip administered as cassette dosing | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321414 | Intrinsic clearance in rat liver microsomes at 1 uM preincubated with microsomes followed by NADPH addition measured up to 45 mins by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194466 | Inhibition of DAT (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321425 | Plasma concentration in cannulated Sprague-Dawley rat at 1 mg/kg, iv after 0.25 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1321411 | Plasma clearance in cannulated Sprague-Dawley rat at 1 mg/kg, iv up to 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| AID1194475 | Ratio of drug level in brain to plasma in mouse at 1 mg/kg, ip administered as cassette dosing | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194473 | Plasma concentration in mouse at 1 mg/kg, ip administered as cassette dosing | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194464 | Inhibition of human CHT Leu530Ala and Val531Ala mutant expressed in HEK293 cells assessed as remaining transporter activity in presence of 100 nM [3H]choline by [3H]choline uptake assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1194476 | Hepatic clearance in mouse liver microsomes | 2015 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 25, Issue:8
| Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter. |
| AID1321424 | Volume of distribution at steady state in cannulated Sprague-Dawley rat at 1 mg/kg, iv up to 24 hrs by LC-MS/MS analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |