Target & Activity
| Target | Activity | Value |
|---|---|---|
| CaMKII | Ki | 0.9 μM |
Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| HEK293 | IC50 | 0.158 μM | Antagonist activity at recombinant human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced intracellular ethidium bromide uptake after 2 hrs by fluorescence assay | [PMID: 25597334] |
| HEK293 | IC50 | 0.25 μM | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium ion uptake after 2 hrs | [PMID: 26547056] |
| HEK293 | IC50 | 158 nM | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced accumulation of ethidium+ after 120 mins by fluorescence assay | [PMID: 24246730] |
| HEK293 | IC50 | 280 nM | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence analysis | [PMID: 22400713] |
| HEK293 | IC50 | 96 μM | Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced ethidium bromide uptake after 2 hrs by fluorescence assay | [PMID: 28126517] |
| THP-1 | IC50 | 0.129 μM | Antagonist activity at P2X7 receptor expressed in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta production after 4 hrs by ELISA | [PMID: 26547056] |
| THP-1 | IC50 | 0.143 μM | Antagonist activity at P2X7 receptor in LPS/IFN-gamma-differentiated human THP1 cells assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP induction measured after 30 mins by ELISA | [PMID: 25597334] |
| THP-1 | IC50 | 120 nM | Antagonist activity at human P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced IL8 release pretreated for 30 mins before bzATP challenge measured after 30 mins by ELISA | [PMID: 22400713] |
| THP-1 | IC50 | 188 nM | Inhibition of BzATP-stimulated IL1-beta release in human THP1 cells by ELISA | [PMID: 18078749] |
| THP-1 | IC50 | 81 nM | Inhibition of Bz-ATP-induced IL1-beta release in LPS/IFN-gamma-differentiated human THP1 cells by ELISA | [PMID: 19110420] |
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