Assay Detail
Functional
CHEMBL882189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against the P2X7 ion channel
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 24 | 7.53 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441479 | — | — | 1 | 8.80 |
| CHEMBL129982 | — | — | 1 | 8.40 |
| CHEMBL131774 | — | — | 1 | 8.30 |
| CHEMBL131162 | — | — | 1 | 8.30 |
| CHEMBL341226 | — | — | 1 | 8.30 |
| CHEMBL134194 | — | — | 1 | 8.20 |
| CHEMBL340983 | — | — | 1 | 8.20 |
| CHEMBL336619 | — | — | 1 | 8.10 |
| CHEMBL424451 | — | — | 1 | 8.00 |
| CHEMBL405790 | — | — | 1 | 8.00 |
| CHEMBL130840 | — | — | 1 | 8.00 |
| CHEMBL130590 | — | — | 1 | 7.90 |
| CHEMBL128101 | — | — | 1 | 7.80 |
| CHEMBL131883 | — | — | 1 | 7.40 |
| CHEMBL335466 | — | — | 1 | 7.40 |
| CHEMBL338236 | — | — | 1 | 7.20 |
| CHEMBL131241 | — | — | 1 | 7.20 |
| CHEMBL338579 | — | — | 1 | 7.10 |
| CHEMBL100539 | — | — | 1 | 7.10 |
| CHEMBL337873 | — | — | 1 | 6.90 |
| CHEMBL338637 | — | — | 1 | 6.50 |
| CHEMBL337419 | — | — | 1 | 6.40 |
| CHEMBL340015 | — | — | 1 | 5.90 |
| CHEMBL336517 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441479 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL129982 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL131774 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL131162 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL341226 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL134194 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL340983 | — | Kd | = | 6.31 | nM | 8.20 |
| CHEMBL336619 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL424451 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL405790 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL130840 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL130590 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL128101 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL131883 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL335466 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL338236 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL131241 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL338579 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL100539 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL337873 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL338637 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL337419 | — | Kd | = | 398.11 | nM | 6.40 |
| CHEMBL340015 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL336517 | — | Kd | = | 3981.07 | nM | 5.40 |