Assay Detail
Binding
CHEMBL3707547
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding: Human or rat P2X7-1321N1 cells were collected and frozen @-80.degree. C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 .mu.l:10 .mu.l compound (10.times.)+(b) 40 .mu.l tracer (2.5.times.)+50 .mu.l membrane (2.times.). 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.degree. 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 |
| Cell Type | P2X7-1321N1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocines as P2X7 modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 8.13 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3697516 | — | — | 1 | 8.89 |
| CHEMBL3697527 | — | — | 1 | 8.49 |
| CHEMBL3697519 | — | — | 1 | 8.47 |
| CHEMBL3697511 | — | — | 1 | 8.40 |
| CHEMBL6067665 | — | — | 1 | 8.40 |
| CHEMBL3697539 | — | — | 1 | 8.40 |
| CHEMBL3697523 | — | — | 1 | 8.30 |
| CHEMBL3697542 | — | — | 1 | 8.20 |
| CHEMBL3697536 | — | — | 1 | 8.20 |
| CHEMBL3697537 | — | — | 1 | 8.20 |
| CHEMBL3697541 | — | — | 1 | 8.10 |
| CHEMBL3697531 | — | — | 1 | 8.10 |
| CHEMBL3697543 | — | — | 1 | 8.10 |
| CHEMBL3697544 | — | — | 1 | 8.10 |
| CHEMBL3697532 | — | — | 1 | 8.10 |
| CHEMBL3697540 | — | — | 1 | 8.00 |
| CHEMBL3697534 | — | — | 1 | 7.90 |
| CHEMBL3697533 | — | — | 1 | 7.86 |
| CHEMBL3697545 | — | — | 1 | 7.80 |
| CHEMBL3697538 | — | — | 1 | 7.80 |
| CHEMBL3697535 | — | — | 1 | 7.50 |
| CHEMBL3697530 | — | — | 1 | 7.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3697516 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3697527 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3697519 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3697511 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL6067665 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3697539 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3697523 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3697542 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3697536 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3697537 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3697541 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3697531 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3697543 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3697544 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3697532 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3697540 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3697534 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL3697533 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL3697545 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL3697538 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL3697535 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL3697530 | — | Ki | = | 35.5 | nM | 7.45 |