Assay Detail
Binding
CHEMBL3743579
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Antagonist activity at P2X7R in human whole blood assessed as inhibition of LPS-induced IL-1beta production incubated for 30 mins followed by ATP addition for 30 mins by ELISA assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Series of Dihydropyridinone P2X7 Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.60 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3739648 | — | — | 1 | 8.22 |
| CHEMBL3740684 | — | — | 1 | 7.89 |
| CHEMBL3739741 | — | — | 1 | 7.77 |
| CHEMBL3740645 | — | — | 1 | 7.77 |
| CHEMBL3740130 | — | — | 1 | 7.70 |
| CHEMBL3741681 | — | — | 1 | 7.68 |
| CHEMBL3741076 | — | — | 1 | 7.57 |
| CHEMBL3740255 | — | — | 1 | 7.48 |
| CHEMBL3741276 | — | — | 1 | 7.33 |
| CHEMBL3741992 | — | — | 1 | 7.22 |
| CHEMBL3740237 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3739648 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3740684 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3739741 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3740645 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3740130 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3741681 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3741076 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3740255 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3741276 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3741992 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3740237 | — | IC50 | = | 107.0 | nM | 6.97 |