Assay Detail
Binding
CHEMBL5037240
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Antagonist activity at human TLR9 expressed in HEK-blue-HTLR7 cells assessed as inhibition of CpGB-induced NFkappaB activation measured after overnight incubation by SEAP-based spectrophotometry assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Systematic Optimization of Potent and Orally Bioavailable Purine Scaffold as a Dual Inhibitor of Toll-Like Receptors 7 and 9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.66 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5094930 | — | — | 1 | 8.15 |
| CHEMBL5078399 | — | — | 1 | 7.40 |
| CHEMBL5086543 | — | — | 1 | 7.22 |
| CHEMBL5088130 | — | — | 1 | 7.10 |
| CHEMBL5091556 | — | — | 1 | 7.05 |
| CHEMBL5074861 | — | — | 1 | 7.00 |
| CHEMBL5092134 | — | — | 1 | 6.92 |
| CHEMBL5087172 | — | — | 1 | 6.92 |
| CHEMBL5087425 | — | — | 1 | 6.85 |
| CHEMBL5078384 | — | — | 1 | 6.82 |
| CHEMBL5075899 | — | — | 1 | 6.72 |
| CHEMBL5089259 | — | — | 1 | 6.70 |
| CHEMBL5087096 | — | — | 1 | 6.62 |
| CHEMBL5082124 | — | — | 1 | 6.60 |
| CHEMBL5079289 | — | — | 1 | 6.58 |
| CHEMBL5076481 | — | — | 1 | 6.55 |
| CHEMBL5091450 | — | — | 1 | 6.47 |
| CHEMBL5089951 | — | — | 1 | 6.36 |
| CHEMBL5088615 | — | — | 1 | 6.33 |
| CHEMBL5078099 | — | — | 1 | 6.30 |
| CHEMBL4541672 | — | — | 1 | 5.92 |
| CHEMBL5077767 | — | — | 1 | 5.47 |
| CHEMBL5080514 | — | — | 1 | 5.06 |
| CHEMBL5083487 | — | — | 1 | - |
| CHEMBL5094133 | — | — | 1 | - |
| CHEMBL5083691 | — | — | 1 | - |
| CHEMBL5074229 | — | — | 1 | - |
| CHEMBL5092610 | — | — | 1 | - |
| CHEMBL5091278 | — | — | 1 | - |
| CHEMBL5084358 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5094930 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5078399 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5086543 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5088130 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5091556 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5074861 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5092134 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5087172 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5087425 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5078384 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5075899 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5089259 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5087096 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5082124 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5079289 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5076481 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5091450 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5089951 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5088615 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5078099 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4541672 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5077767 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5080514 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL5083487 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5094133 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5083691 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5074229 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5092610 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5091278 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5084358 | — | IC50 | > | 30000.0 | nM | - |