Assay Detail
Binding
CHEMBL3705577
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: 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), NaH2PO4.2H2O (9.6 mM), HEPES (25 mM), sucrose (280 mM), glucose (5 mM), CaCl2 (0.5 mM), and probenecid (0.1425 g in 3 mL 1N NaOH was added for 500 mL solution)] in 384-well plates.293-rat P2X7 stable cells were incubated in HHPB (pH 7.4) [consisting of Hank's BSS (1×); HEPES (pH 7.4) (20 mM) (Sigma); probenecid (0.710g/5 mL 1N NaOH) (Sigma); and BSA (0.05%) (Roche) which was added after the pH had been adjusted] in 384-well plates. Fluo-4 NW dye mix (Molecular Probes, Inc., Eugene, Oreg., USA) was prepared in buffer (see manufacturer's instructions). Cell plates were removed from the 37° C. incubator, the media discarded and then 30 μL of dye was added to each well. Plates were placed in the 37° C., non-CO2 incubator for 30 minutes and then room temperature for 30 minutes.
244
Total Activities
180
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | P2X7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Benzamides
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 244 | 7.53 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3679059 | — | — | 3 | 10.05 |
| CHEMBL3679011 | — | — | 1 | 9.55 |
| CHEMBL3679036 | — | — | 3 | 9.51 |
| CHEMBL3679043 | — | — | 1 | 9.27 |
| CHEMBL3679042 | — | — | 1 | 9.15 |
| CHEMBL3679084 | — | — | 3 | 9.15 |
| CHEMBL3639778 | — | — | 1 | 9.12 |
| CHEMBL3679051 | — | — | 1 | 9.12 |
| CHEMBL3679094 | — | — | 3 | 9.09 |
| CHEMBL3679022 | — | — | 1 | 9.08 |
| CHEMBL3679063 | — | — | 3 | 9.07 |
| CHEMBL3679029 | — | — | 1 | 9.02 |
| CHEMBL3679104 | — | — | 1 | 9.02 |
| CHEMBL3679005 | — | — | 1 | 9.00 |
| CHEMBL3679134 | — | — | 2 | 8.96 |
| CHEMBL3679013 | — | — | 1 | 8.92 |
| CHEMBL3679035 | — | — | 1 | 8.92 |
| CHEMBL3679026 | — | — | 1 | 8.92 |
| CHEMBL3679028 | — | — | 1 | 8.89 |
| CHEMBL3679078 | — | — | 1 | 8.85 |
| CHEMBL3679098 | — | — | 2 | 8.85 |
| CHEMBL3679048 | — | — | 3 | 8.82 |
| CHEMBL3679039 | — | — | 1 | 8.80 |
| CHEMBL3679053 | — | — | 1 | 8.80 |
| CHEMBL3679090 | — | — | 1 | 8.80 |
| CHEMBL3679115 | — | — | 2 | 8.80 |
| CHEMBL3679139 | — | — | 2 | 8.74 |
| CHEMBL3679149 | — | — | 2 | 8.72 |
| CHEMBL3679152 | — | — | 1 | 8.72 |
| CHEMBL3679075 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3679059 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3679011 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL3679036 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3679043 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL3679036 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL3679084 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3679042 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3679051 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3639778 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3679094 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL3679022 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL3679063 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL3679063 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL3679084 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL3679029 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL3679104 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3679005 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3679134 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3679134 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3679035 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3679026 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3679084 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3679013 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3679028 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3679098 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3679078 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3679048 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3679053 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3679090 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3679039 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3679115 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3679139 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3679152 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3679149 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3679075 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3679135 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3679059 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3679067 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3679129 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3679037 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3679021 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3679110 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3679001 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3679138 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3679032 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3679036 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3679072 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3679129 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3679087 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3679080 | — | IC50 | = | 3.2 | nM | 8.49 |