Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
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. |
AID1218824 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218828 | Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 9 | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID712527 | Antagonist activity at human CXCR3 expressed in HEK293T cells co-expressing Galphaqi5 assessed as inhibition of CXCL10-induced [3H]-inositolphosphates levels | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
| CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors. |
AID290643 | Half life in cynomolgus monkey at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218843 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290639 | Clearance in dog at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID642275 | Drug level in C57BL/6 mouse blood at 10 mg/kg, sc after 1 hr | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of potent and specific CXCR3 antagonists. |
AID1218848 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290628 | Displacement of [125I ]IP10 from CXCR3 receptor expressed in PBMC | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218847 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290645 | Bioavailability in cynomolgus monkey at 5 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID642273 | Receptor occupancy of CXCR3 in mouse whole blood assessed as inhibition of ITAC binding by fluorescence quenching based FACS analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of potent and specific CXCR3 antagonists. |
AID1218827 | Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290642 | Half life in dog at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID641650 | Displacement of [125I]-IP-10 from CXCR3 | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of potent and specific CXCR3 antagonists. |
AID1218853 | Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218845 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218851 | Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID348586 | Binding affinity to human muscarinic M3 receptor | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. |
AID1218849 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290635 | Inhibition of ITAC-induced CXCR3 mediated cell migration | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218823 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218826 | Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 3 | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID712528 | Displacement of [125I]-CXCL11 from human CXCR3 expressed in HEK293 cells | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
| CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors. |
AID290646 | Inhibition of cell migration in mouse assessed as reduction of bleomycin-induced cellular infiltration into lungs at 3 mg/kg, sc | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID290636 | Inhibition of MIG-induced CXCR3 mediated cell migration | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID468582 | Drug level in bleomycin-induced mouse blood at 1 mg/mL, sc | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID468581 | Drug level in bleomycin-induced mouse blood at 3 mg/mL, sc | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID348583 | Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. |
AID1218854 | Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290638 | Inhibition of cell migration in subcutaneously dosed mouse assessed as reduction of bleomycin-induced cellular infiltration into lungs | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID712529 | Displacement of [125I]-CXCL10 from human CXCR3 expressed in HEK293 cells | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
| CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors. |
AID1218844 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID707874 | Binding affinity to CXCR3 | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
AID290641 | Half life in rat at 0.5 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID313790 | Antagonist activity at CXCR3 assessed as IP-10-mediated cell migration | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. |
AID641651 | Displacement of [125I]-IP-10 from CXCR3 in presence of 100% human serum | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of potent and specific CXCR3 antagonists. |
AID1218846 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID468550 | Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218825 | Ratio of IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition to IC50 for CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218817 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218850 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID313785 | Displacement of [125I]IP-10 from CXCR3 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. |
AID642276 | Drug level in C57BL/6 mouse blood at 1 mg/kg, sc after 1 hr | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery of potent and specific CXCR3 antagonists. |
AID449699 | Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMC | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Imidazo-pyrazine derivatives as potent CXCR3 antagonists. |
AID348585 | Binding affinity to human muscarinic M2 receptor | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. |
AID1218818 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218822 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218820 | Time dependent inhibition of CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218852 | Ratio of IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins to IC50 for CYP3A4 in human liver microsomes using testosterone as substrate preincubated for 30 mins in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290630 | Clearance in rat at 0.5 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID290640 | Clearance in cynomolgus monkey at 1 mg/kg, iv | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID707908 | Lipophilicity, log P of the compound | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
AID468547 | Displacement of [125I]-1P10 from human CXCR3 expressed in PBMC after 2 hrs in RPMI buffer by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218819 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 90 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID313791 | Antagonist activity at CXCR3 assessed as ITAC-mediated cell migration | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. |
AID313786 | Displacement of [125I]ITAC from CXCR3 receptor | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. |
AID290644 | Bioavailability in dog at 2.5 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID290634 | Inhibition of IP10-induced CXCR3 mediated cell migration | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID290637 | Antagonist activity at human CXCR3 assessed as inhibition of ITAC-induced calcium mobilization | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID468580 | Drug level in bleomycin-induced mouse blood at 10 mg/mL, sc | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID313792 | Antagonist activity at CXCR3 assessed as MIG-mediated cell migration | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
| Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists. |
AID1218856 | Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of testosterone to 6beta-hydroxytestosterone at 0.3 to 75 uM by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID290633 | Displacement of [125I] ITAC from the CXCR3 receptor | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID290631 | Bioavailability in rat at 2 mg/kg, po | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. |
AID1218821 | Time dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by 10-fold dilution and substrate addition by LC-MS/MS analysis in presence of NADPH | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID1218855 | Time dependent inhibition of CYP3A4 in human liver microsomes assessed as conversion of midazolam to 1'-hydroxymidazolam at 0.3 to 75 uM by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7
| Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. |
AID348584 | Binding affinity to human muscarinic M1 receptor | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
| Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |