Report error Found 15862 Enz. Inhib. hit(s) with Target = 'P2X purinoceptor 7'
Affinity DataEC50: 158nMAssay Description:Antagonist activity at P2X7 receptor in human whole blood assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed ...More data for this Ligand-Target Pair
Affinity DataEC50: 1.66E+4nMAssay Description:Agonist activity at human P2X7R expressing HEK293 cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed b...More data for this Ligand-Target Pair
Affinity DataEC50: 9.14E+3nMAssay Description:Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as BzATP EC50 at 0.2 uM incubated for 30 mins by Fura-2 AM ...More data for this Ligand-Target Pair
Affinity DataEC50: 400nMAssay Description:The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataEC50: 2.19E+3nMAssay Description:Negative allosteric modulation activity at human P2X7 receptor expressed in human 1321N1 cells assessed as ATP induced calcium response by measuring ...More data for this Ligand-Target Pair
Affinity DataEC50: 9.44E+3nMAssay Description:Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as BzATP EC50 at 0.1 uM incubated for 30 mins by Fura-2 AM ...More data for this Ligand-Target Pair
Affinity DataKd: 710nMAssay Description:Binding affinity to human wild type P2X7R assessed as dissociation constant by microscale thermophoresis analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 6.08E+3nMAssay Description:Negative allosteric modulation activity at human P2X7 receptor expressed in human 1321N1 cells assessed as ATP induced calcium response by measuring ...More data for this Ligand-Target Pair
Affinity DataKd: 3.60nMAssay Description:Maximum binding affinity towards P2X purinoceptor 7 expressed in HEK 293 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 7.80E+5nMAssay Description:Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataEC50: 6.62E+3nMAssay Description:Negative allosteric modulation activity at human P2X7 receptor expressed in human 1321N1 cells assessed as ATP induced calcium response by measuring ...More data for this Ligand-Target Pair
Affinity DataEC50: 34nMAssay Description:Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataEC50: >1.00E+5nMAssay Description:Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataEC50: <1.00E+5nMAssay Description:Agonist activity at human P2X7R expressing HEK293 cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed b...More data for this Ligand-Target Pair
Affinity DataEC50: 158nMAssay Description:Antagonist activity at P2X7 receptor in human whole blood assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed ...More data for this Ligand-Target Pair
Affinity DataKd: 3.60nMAssay Description:Equilibrium constant for P2X purinoceptor 7 expressed in HEK 293 cells at 1 uMMore data for this Ligand-Target Pair
Affinity DataEC50: 8.31E+3nMAssay Description:Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as BzATP EC50 at 0.05 uM incubated for 30 mins by Fura-2 AM...More data for this Ligand-Target Pair
Affinity DataEC50: 5.20E+4nMAssay Description:Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataEC50: <1.00E+5nMAssay Description:Agonist activity at human P2X7R expressed in HEK293 cells assessed as reduction in YO-PRO-1 iodide dye uptake preincubated for 30 mins followed by YO...More data for this Ligand-Target Pair
Affinity DataEC50: 9.20E+4nMAssay Description:Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataEC50: 2.24E+4nMAssay Description:Agonist activity at human P2X7R expressed in HEK293 cells assessed as reduction in YO-PRO-1 iodide dye uptake preincubated for 30 mins followed by YO...More data for this Ligand-Target Pair
Affinity DataEC50: 6.20E+4nMAssay Description:The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 7 (P2X7)More data for this Ligand-Target Pair
Affinity DataIC50: 0.0100nMAssay Description:Inhibition of P2X7 receptor (unknown origin) assessed as inhibition of IL1beta productionMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0501nMAssay Description:Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptakeMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0600nMAssay Description:Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta rel...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0794nMAssay Description:Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptakeMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0900nMAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0900nMpH: 7.4 T: 2°CAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.110nMAssay Description:Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptakeMore data for this Ligand-Target Pair
Affinity DataIC50: 0.110nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluo...More data for this Ligand-Target Pair
Affinity DataIC50: 0.150nMAssay Description:Inhibition of P2X7 (unknown origin) assessed as reduction in IL-1 beta releaseMore data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMpH: 7.4Assay Description:Ca2+ Flux: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of Bz-ATP-induced Ca2+ flux after 30 mins by FLIPR assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptakeMore data for this Ligand-Target Pair
Affinity DataIC50: 0.230nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluo...More data for this Ligand-Target Pair
Affinity DataIC50: 0.280nMAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.280nMAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.280nMpH: 7.4 T: 2°CAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMpH: 7.4Assay Description:Ca2+ Flux: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMpH: 7.4Assay Description:1321N1 cells expressing the recombinant human or rat P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose...More data for this Ligand-Target Pair
Affinity DataIC50: 0.310nMAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.310nMpH: 7.4 T: 2°CAssay Description:Fluorescent Imaging Plate Reader (FLIPR) assay: Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), N...More data for this Ligand-Target Pair
Affinity DataIC50: 0.316nMAssay Description:Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptakeMore data for this Ligand-Target Pair
Affinity DataIC50: 0.320nMAssay Description:Antagonist activity at human P2X7 receptor in LPS/IFN-gamma-differentiated human THP-1 cells assessed as suppression of BzATP-stimulated IL-1beta rel...More data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMAssay Description:Cell culture: 293 HEK cells, stably transfected with plasmids capable of expressing human P2X7 receptor, were cultured by standard methods. Cells wer...More data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMpH: 7.4 T: 2°CAssay Description:Briefly, 293-human or mouse P2X7 stable cells were incubated in sucrose buffer, pH 7.4 [KCl (5 mM), NaH2PO42H2O (9.6 mM), HEPES (25 mM), sucrose (280...More data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMAssay Description:Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium mobilization monitored for 5 min...More data for this Ligand-Target Pair
