| Assay ID | Title | Year | Journal | Article |
|---|
| AID1666460 | Cytotoxicity against human MDA-MB-231 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831763 | Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID1666444 | Cytotoxicity against human OVCAR4 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666410 | Cytotoxicity against human EKVX cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666413 | Cytotoxicity against human HOP62 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666423 | Cytotoxicity against human HCT15 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501693 | Volume of distribution at steady state in rat at 1 mg/kg, iv for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID501703 | Drug level in plasma of rat chronic constriction injury model at 20 mg/kg, po bid for 8 days measured on last day | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666441 | Cytotoxicity against human UACC62 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666426 | Cytotoxicity against human SW620 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501694 | Tmax in rat at 3 mg/kg, po for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666379 | Antagonist activity at P2X7R in human THP1 cells assessed as inhibition of LPS and BzATP-induced ROS production at 10'-5 mol/L pretreated with compound followed by LPS/BzATP addition and measured up to 5 hrs by kinetic chemiluminescence based fluorometric | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501695 | Cmax in rat at 3 mg/kg, po for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID501704 | Antiallodynic activity in rat chronic constriction injury model assessed as nerve injury-induced allodynia at 30 mg/kg, po bid measured post dose on day 1 of 8 days treatment | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID528205 | Half life in rat at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666431 | Cytotoxicity against human SNB75 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831770 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID1666451 | Cytotoxicity against human ACHN cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666435 | Cytotoxicity against human M14 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528206 | Oral bioavailability in rat at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1831764 | Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID1831766 | Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID528209 | Half life in dog at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID501683 | Inhibition of CYP1A2 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666442 | Cytotoxicity against human IGROV1 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666415 | Cytotoxicity against human NCI-H226 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831767 | Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID501681 | Inhibition of human P2X7 receptor by ethidium bromide release assay | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666462 | Cytotoxicity against human BT549 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666449 | Cytotoxicity against human 786-0 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528207 | Clearance in dog blood at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666447 | Cytotoxicity against human NCI/ADR-RES cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666427 | Cytotoxicity against human SF268 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666459 | Cytotoxicity against human MCF7 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501696 | AUC in rat at 3 mg/kg, po for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666464 | Cytotoxicity against human MDA-MB-468 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501690 | Lipophilicity, log D of the compound at pH 7.4 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666384 | Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation at 10 uM preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based fl | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501684 | Inhibition of CYP2C9 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666432 | Cytotoxicity against human U251 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666421 | Cytotoxicity against human HCC2998 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501699 | Drug level in rat brain at 50 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1831771 | Apparent permeability across basolateral to apical side in MDCK-MDR1 cells by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID501692 | Half life in rat at 1 mg/kg, iv for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666395 | Solubility of compound in saline at 1mg/ml | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666381 | Antagonist activity at P2X7 receptor in human THP-1 cells assessed as inhibition of LPS and BzATP-induced IL-1beta production at 10'-5 mol/L pretreated with compound followed by LPS/BzATP addition and measured after 2 to 6 hrs by ELISA | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1543109 | Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay | | | |
| AID1666450 | Cytotoxicity against human A498 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666434 | Cytotoxicity against human MALME-3M cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831772 | Efflux ratio of permeability across basolateral to apical side over apical to basolateral side in MDCK2-MDR1 cells | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID1666398 | Drug metabolism in mouse measured after 40 mins | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831769 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID1666430 | Cytotoxicity against human SNB19 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666452 | Growth inhibition of human Caki1 cells assessed as growth percentage at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666457 | Cytotoxicity against human PC3 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528210 | Oral bioavailability in dog at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666420 | Cytotoxicity against human COLO205 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666428 | Cytotoxicity against human SF295 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1831762 | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. |
| AID501701 | Antiallodynic activity in rat chronic constriction injury model assessed as nerve injury-induced allodynia at 20 mg/kg, po bid measured post dose on day 1 of 8 days treatment | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666408 | Cytotoxicity against human RPMI8226 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501706 | Solubility of the compound | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID528211 | Clearance in monkey blood at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID501700 | Drug level in rat plasma at 50 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666446 | Cytotoxicity against human OVCAR8 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666458 | Cytotoxicity against human DU145 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528213 | Half life in monkey at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666456 | Cytotoxicity against human UO31 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666445 | Cytotoxicity against human OVCAR5 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666412 | Cytotoxicity against human HL-60(TB) cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666437 | Cytotoxicity against human SK-MEL-2 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666406 | Cytotoxicity against human A549/ATCC cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666422 | Cytotoxicity against human HCT116 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666418 | Cytotoxicity against human NCI-H460 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528203 | Clearance in rat blood at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666382 | Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666454 | Cytotoxicity against human SN12C cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666409 | Cytotoxicity against human MOLT4 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528225 | Antagonist activity at rat recombinant P2X7 receptor | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1543108 | Competitive displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay | | | |
| AID1666424 | Cytotoxicity against human HT-29 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666417 | Cytotoxicity against human NCI-H322M cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666440 | Cytotoxicity against human UACC257 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666443 | Cytotoxicity against human OVCAR3 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501691 | Blood clearance in rat at 1 mg/kg, iv for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID501686 | Inhibition of CYP2D6 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666405 | Cytotoxicity against human CCRF-CEM cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666433 | Cytotoxicity against human LOXIMVI cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666463 | Cytotoxicity against human T47D cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501687 | Inhibition of CYP3A4 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666438 | Cytotoxicity against human SK-MEL-28 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666453 | Cytotoxicity against human RXF393 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528212 | Volume of distribution at steady state in monkey at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID528215 | Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells by ethidium accumulation assay | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666419 | Cytotoxicity against human NCI-H522 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528214 | Oral bioavailability in monkey at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID501702 | Drug level in brain of rat chronic constriction injury model at 20 mg/kg, po bid for 8 days measured on last day | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666439 | Cytotoxicity against human SK-MEL-5 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666414 | Cytotoxicity against human HOP92 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501689 | Inhibition of rat P2X7 receptor by ethidium bromide release assay | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID501697 | Oral bioavailability in rat at 3 mg/kg for 1 hrs | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID528208 | Volume of distribution at steady state in dog at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID1666383 | Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666429 | Cytotoxicity against human SF539 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501685 | Inhibition of CYP2C19 | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666448 | Cytotoxicity against human SKOV3 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666455 | Cytotoxicity against human TK10 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666397 | Metabolic stability in human liver microsomes assessed as half life at 0.2 mg/ml incubated for 60 mins by UPLC/MS-MS analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666461 | Cytotoxicity against human Hs 578T cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666416 | Cytotoxicity against human NCI-H23 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666411 | Cytotoxicity against human K562 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666425 | Cytotoxicity against human KM12 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666396 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 0.2 mg/ml incubated for 60 mins by UPLC/MS-MS analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666380 | Antagonist activity at P2X7 receptor in human THP-1 cells assessed as inhibition of LPS and BzATP-induced IL-1beta production at 10'-6 mol/L pretreated with compound followed by LPS/BzATP addition and measured after 2 to 6 hrs by ELISA | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666466 | Metabolic stability in human hepatocytes | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID1666407 | Cytotoxicity against human SR cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID501688 | Intrinsic clearance in human liver microsome | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| AID1666436 | Cytotoxicity against human MDA-MB-435 cells assessed as effect on cell growth at 10 uM incubated for 48 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
| Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
| AID528204 | Volume of distribution at steady state in rat at 1 mg/kg, iv and 3 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
| Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
| AID501705 | Plasma protein binding in human | 2010 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 20, Issue:17
| Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |