Assay Detail
Binding
CHEMBL3706047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR Assay: Ca.sup.2+flux: 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 .mu.l volume/well. On the day of the experiment, cell plates were washed with assay buffer, containing (in mM): 130 NaCl, 2 KCl, 1 CaCl.sub.2, 1 MgCl.sub.2, 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 250.times. the test concentration in neat DMSO. Intermediate 96-well compound plates were prepared by transferring 1.2 .mu.L of the compound into 300 .mu.L of assay buffer. A further 3.times. dilution occurred when transferring 50 .mu.L/well of the compound plate to 100 .mu.L/well in the cell plate.
45
Total Activities
45
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
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 |
|---|---|---|---|
| IC50 | 45 | 7.59 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3697521 | — | — | 1 | 8.96 |
| CHEMBL3697548 | — | — | 1 | 8.77 |
| CHEMBL3697551 | — | — | 1 | 8.59 |
| CHEMBL3697543 | — | — | 1 | 8.51 |
| CHEMBL3697509 | — | — | 1 | 8.42 |
| CHEMBL3697539 | — | — | 1 | 8.30 |
| CHEMBL3697544 | — | — | 1 | 8.21 |
| CHEMBL3697531 | — | — | 1 | 8.20 |
| CHEMBL3697534 | — | — | 1 | 8.11 |
| CHEMBL3697515 | — | — | 1 | 8.11 |
| CHEMBL3697511 | — | — | 1 | 8.02 |
| CHEMBL3697516 | — | — | 1 | 8.01 |
| CHEMBL6067665 | — | — | 1 | 8.00 |
| CHEMBL3697520 | — | — | 1 | 8.00 |
| CHEMBL3697542 | — | — | 1 | 7.99 |
| CHEMBL3697540 | — | — | 1 | 7.98 |
| CHEMBL3697530 | — | — | 1 | 7.90 |
| CHEMBL3697535 | — | — | 1 | 7.88 |
| CHEMBL3697538 | — | — | 1 | 7.88 |
| CHEMBL3697519 | — | — | 1 | 7.88 |
| CHEMBL3697527 | — | — | 1 | 7.87 |
| CHEMBL3697541 | — | — | 1 | 7.84 |
| CHEMBL3697550 | — | — | 1 | 7.83 |
| CHEMBL3697536 | — | — | 1 | 7.82 |
| CHEMBL3697545 | — | — | 1 | 7.77 |
| CHEMBL3697552 | — | — | 1 | 7.71 |
| CHEMBL3697533 | — | — | 1 | 7.70 |
| CHEMBL3697532 | — | — | 1 | 7.70 |
| CHEMBL3697537 | — | — | 1 | 7.69 |
| CHEMBL3697546 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3697521 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3697548 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3697551 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3697543 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3697509 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3697539 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3697544 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3697531 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3697534 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3697515 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3697511 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3697516 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL6067665 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3697520 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3697542 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL3697540 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3697530 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL3697535 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL3697538 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3697519 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL3697527 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL3697541 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL3697550 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL3697536 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3697545 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL3697552 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL3697533 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3697532 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3697537 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL3697546 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL3697528 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL3697523 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL3697529 | — | IC50 | = | 51.1 | nM | 7.29 |
| CHEMBL3697513 | — | IC50 | = | 63.4 | nM | 7.20 |
| CHEMBL3697512 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL3697522 | — | IC50 | = | 94.8 | nM | 7.02 |
| CHEMBL3697547 | — | IC50 | = | 97.7 | nM | 7.01 |
| CHEMBL3697549 | — | IC50 | = | 100.5 | nM | 7.00 |
| CHEMBL3697526 | — | IC50 | = | 118.3 | nM | 6.93 |
| CHEMBL3697517 | — | IC50 | = | 481.9 | nM | 6.32 |
| CHEMBL3639963 | — | IC50 | = | 1905.5 | nM | 5.72 |
| CHEMBL3697514 | — | IC50 | = | 2296.2 | nM | 5.64 |
| CHEMBL3697524 | — | IC50 | = | 3698.3 | nM | 5.43 |
| CHEMBL3697518 | — | IC50 | = | 5688.5 | nM | 5.25 |
| CHEMBL3697510 | — | IC50 | > | 10000.0 | nM | - |