| Assay ID | Title | Year | Journal | Article |
|---|
| AID598978 | Antagonist activity at P2X7 receptor in mouse LPS-stimulated peritoneal macrophages assessed as inhibition of ATP-induced IL1-beta release at 10 uM by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| AID598956 | Volume of distribution at steady state in rat | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598961 | Volume of distribution at steady state in dog | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| AID1636665 | Antagonist activity at human P2X7 receptor | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16
| Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion. |
| AID598979 | Trough plasma concentration in rheumatoid arthritis patient at 500 mg BID for 12 weeks | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598917 | Antagonist activity at P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced YOPRO-1 uptake | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598966 | Volume of distribution at steady state in monkey | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID616423 | Antagonist activity at P2X7R expressed in LPS-activated human monocytes assessed as inhibition of ATP-induced IL1-beta release in presence of low serum concentration | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
| Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X₇ receptor. |
| AID598958 | Cmax in rat at 5 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598953 | Fraction unbound in human plasma | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| AID598957 | Half life in rat | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598968 | Cmax in monkey | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598976 | Inhibition of human ERG at 1 uM | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598972 | Inhibition of human CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598918 | Antagonist activity at P2X7 receptor in human LPS-stimulated monocytes assessed as inhibition of ATP-induced IL1-beta release by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598960 | Plasma clearance in dog | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598971 | Inhibition of human CYP2C19 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| 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. |
| AID1239717 | Antagonist activity against human P2X7 receptor assessed as inhibition of IL-1beta production by cell based assay | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
| Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists. |
| AID598975 | Mutagenic activity in Salmonella Typhimurium by Ames assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| AID598955 | Plasma clearance in rat | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598962 | Half life in dog | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598959 | Oral bioavailability in rat at 5 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598964 | Oral bioavailability in dog | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598977 | Toxicity in rat at 500 mg/kg, po qd for 4 days | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID1358119 | Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake | | | |
| AID598967 | Half life in monkey | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598965 | Plasma clearance in monkey | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598920 | Antagonist activity at P2X7 receptor in human LPS-stimulated monocytes assessed as inhibition of ATP-induced IL1-beta release by ELISA in presence of human blood | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598974 | Inhibition of human CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598970 | Inhibition of human CYP1A2 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598963 | Cmax in dog | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| 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. |
| AID598973 | Inhibition of human CYP2D6 | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID598969 | Oral bioavailability in monkey | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| AID1346612 | Human P2X7 (P2X receptors) | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12
| Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |