Assay Detail
Binding
CHEMBL3707790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR Assay: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose supplemented with 10% Fetal Bovine Serum (FBS) and appropriate selection marker. Cells were seeded at a density of 25000 cells/well (96-well clear bottom black walled plates) in 100 ul volume/well. On the day of the experiment, cell plates were washed with assay buffer, containing (in mM): 130 NaCl, 2 KCl, 1 CaCl2, 1 MgCl2, 10 HEPES, 5 glucose; pH 7.40 and 300 mOs. After the wash, cells were loaded with the Calcium-4 dye (Molecular Device) and incubated in the dark for 60 minutes. Test compounds were prepared at 250x the test concentration in neat DMSO. Intermediate 96-well compound plates were prepared by transferring 1.2 uL of the compound into 300 uL of assay buffer. A further 3x dilution occurred when transferring 50 uL/well of the compound plate to 100 uL/well in the cell plate.
112
Total Activities
110
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | 1321-N1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
P2X7 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 112 | 6.67 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3674090 | — | — | 1 | 8.62 |
| CHEMBL3674082 | — | — | 1 | 8.60 |
| CHEMBL3674081 | — | — | 1 | 8.25 |
| CHEMBL3674094 | — | — | 1 | 8.11 |
| CHEMBL3674070 | — | — | 1 | 8.10 |
| CHEMBL3674129 | — | — | 1 | 8.07 |
| CHEMBL3674087 | — | — | 1 | 8.06 |
| CHEMBL3674126 | — | — | 1 | 8.04 |
| CHEMBL3674139 | — | — | 1 | 8.01 |
| CHEMBL3674093 | — | — | 1 | 8.00 |
| CHEMBL3674051 | — | — | 1 | 8.00 |
| CHEMBL3674085 | — | — | 1 | 8.00 |
| CHEMBL3674077 | — | — | 1 | 7.99 |
| CHEMBL3674075 | — | — | 1 | 7.91 |
| CHEMBL3674089 | — | — | 1 | 7.91 |
| CHEMBL3674116 | — | — | 1 | 7.90 |
| CHEMBL3674097 | — | — | 1 | 7.89 |
| CHEMBL3674137 | — | — | 1 | 7.89 |
| CHEMBL3674119 | — | — | 1 | 7.89 |
| CHEMBL3674083 | — | — | 1 | 7.88 |
| CHEMBL3674103 | — | — | 1 | 7.88 |
| CHEMBL3674128 | — | — | 1 | 7.85 |
| CHEMBL3674086 | — | — | 1 | 7.84 |
| CHEMBL3674115 | — | — | 1 | 7.83 |
| CHEMBL3674102 | — | — | 1 | 7.83 |
| CHEMBL3674105 | — | — | 1 | 7.82 |
| CHEMBL3674100 | — | — | 1 | 7.82 |
| CHEMBL3674125 | — | — | 1 | 7.80 |
| CHEMBL3674107 | — | — | 1 | 7.80 |
| CHEMBL3674092 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3674090 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3674082 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3674081 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3674094 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3674070 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3674129 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3674087 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3674126 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3674139 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3674085 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3674093 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3674051 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3674077 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL3674075 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3674089 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3674116 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL3674119 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3674137 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL3674097 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL3674103 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL3674083 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL3674128 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL3674086 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL3674115 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL3674102 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL3674100 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL3674105 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3674125 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3674107 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL3674092 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL3674099 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3674096 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3674131 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3674118 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3674121 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL3674066 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL3674132 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL3674056 | — | IC50 | = | 67.9 | nM | 7.17 |
| CHEMBL3674056 | — | IC50 | = | 67.9 | nM | 7.17 |
| CHEMBL3674050 | — | IC50 | = | 76.2 | nM | 7.12 |
| CHEMBL3674112 | — | IC50 | = | 101.4 | nM | 6.99 |
| CHEMBL3674074 | — | IC50 | = | 117.2 | nM | 6.93 |
| CHEMBL3674095 | — | IC50 | = | 126.2 | nM | 6.90 |
| CHEMBL3674134 | — | IC50 | = | 127.9 | nM | 6.89 |
| CHEMBL3674135 | — | IC50 | = | 127.9 | nM | 6.89 |
| CHEMBL3674108 | — | IC50 | = | 131.8 | nM | 6.88 |
| CHEMBL3674069 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3674068 | — | IC50 | = | 158.5 | nM | 6.80 |
| CHEMBL3674076 | — | IC50 | = | 161.1 | nM | 6.79 |
| CHEMBL3674127 | — | IC50 | = | 166.0 | nM | 6.78 |