Assay Detail
Binding
CHEMBL3889239
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Radioligand Binding Assay: human or rat P2X7-1321 N1 cells were collected and frozen @−80° C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 μl: 10 μl compound (10×)+(b) 40 μl tracer (2.5×)+50 μl membrane (2×). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2009, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4° C. The assay was terminated by filtration (GF/B filters pre-soaked with 0.3% PEI) and washed with washing buffer (Tris-HCl 50 mM).
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
P2X7 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 7.83 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3919664 | — | — | 1 | 8.92 |
| CHEMBL4112493 | — | — | 1 | 8.80 |
| CHEMBL3911720 | — | — | 1 | 8.70 |
| CHEMBL3954936 | — | — | 1 | 8.66 |
| CHEMBL4068397 | — | — | 1 | 8.66 |
| CHEMBL3904992 | — | — | 1 | 8.60 |
| CHEMBL4113200 | — | — | 1 | 8.60 |
| CHEMBL4095741 | — | — | 1 | 8.51 |
| CHEMBL3983427 | — | — | 1 | 8.49 |
| CHEMBL3951380 | — | — | 1 | 8.30 |
| CHEMBL4079239 | JNJ-54175446 | 2.0 | 1 | 8.26 |
| CHEMBL3937843 | — | — | 1 | 8.21 |
| CHEMBL3895947 | — | — | 1 | 8.11 |
| CHEMBL4113942 | — | — | 1 | 7.85 |
| CHEMBL3924464 | — | — | 1 | 7.79 |
| CHEMBL3904743 | — | — | 1 | 7.72 |
| CHEMBL3938984 | — | — | 1 | 7.58 |
| CHEMBL3901310 | — | — | 1 | 6.87 |
| CHEMBL3984318 | — | — | 1 | 6.13 |
| CHEMBL3910103 | — | — | 1 | 6.10 |
| CHEMBL3923509 | — | — | 1 | 5.70 |
| CHEMBL4074304 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3919664 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4112493 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3911720 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3954936 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4068397 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3904992 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4113200 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4095741 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3983427 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3951380 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL4079239 | JNJ-54175446 | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3937843 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL3895947 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL4113942 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL3924464 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL3904743 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL3938984 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL3901310 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL3984318 | — | Ki | = | 741.3 | nM | 6.13 |
| CHEMBL3910103 | — | Ki | = | 794.3 | nM | 6.10 |
| CHEMBL3923509 | — | Ki | = | 1995.3 | nM | 5.70 |
| CHEMBL4074304 | — | Ki | = | 2238.7 | nM | 5.65 |