Assay Detail
Binding
CHEMBL5037241
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Antagonist activity at human TLR7 expressed in HEK-blue-HTLR7 cells assessed as inhibition of CL264-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 | 5.15 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5078399 | — | — | 1 | 5.92 |
| CHEMBL5088130 | — | — | 1 | 5.58 |
| CHEMBL5089951 | — | — | 1 | 5.57 |
| CHEMBL4541672 | — | — | 1 | 5.32 |
| CHEMBL5087172 | — | — | 1 | 5.31 |
| CHEMBL5075899 | — | — | 1 | 5.31 |
| CHEMBL5089259 | — | — | 1 | 5.28 |
| CHEMBL5086543 | — | — | 1 | 5.14 |
| CHEMBL5087425 | — | — | 1 | 5.12 |
| CHEMBL5091450 | — | — | 1 | 5.11 |
| CHEMBL5078384 | — | — | 1 | 5.09 |
| CHEMBL5077767 | — | — | 1 | 5.08 |
| CHEMBL5078099 | — | — | 1 | 5.07 |
| CHEMBL5094930 | — | — | 1 | 5.03 |
| CHEMBL5080514 | — | — | 1 | 5.01 |
| CHEMBL5088615 | — | — | 1 | 4.99 |
| CHEMBL5087096 | — | — | 1 | 4.93 |
| CHEMBL5076481 | — | — | 1 | 4.88 |
| CHEMBL5074861 | — | — | 1 | 4.87 |
| CHEMBL5079289 | — | — | 1 | 4.79 |
| CHEMBL5091556 | — | — | 1 | 4.75 |
| CHEMBL5082124 | — | — | 1 | - |
| CHEMBL5092134 | — | — | 1 | - |
| CHEMBL5083691 | — | — | 1 | - |
| CHEMBL5094133 | — | — | 1 | - |
| CHEMBL5084358 | — | — | 1 | - |
| CHEMBL5083487 | — | — | 1 | - |
| CHEMBL5091278 | — | — | 1 | - |
| CHEMBL5092610 | — | — | 1 | - |
| CHEMBL5074229 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5078399 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5088130 | — | IC50 | = | 2660.0 | nM | 5.58 |
| CHEMBL5089951 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4541672 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL5087172 | — | IC50 | = | 4880.0 | nM | 5.31 |
| CHEMBL5075899 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL5089259 | — | IC50 | = | 5220.0 | nM | 5.28 |
| CHEMBL5086543 | — | IC50 | = | 7290.0 | nM | 5.14 |
| CHEMBL5087425 | — | IC50 | = | 7590.0 | nM | 5.12 |
| CHEMBL5091450 | — | IC50 | = | 7740.0 | nM | 5.11 |
| CHEMBL5078384 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL5077767 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL5078099 | — | IC50 | = | 8490.0 | nM | 5.07 |
| CHEMBL5094930 | — | IC50 | = | 9250.0 | nM | 5.03 |
| CHEMBL5080514 | — | IC50 | = | 9790.0 | nM | 5.01 |
| CHEMBL5088615 | — | IC50 | = | 10140.0 | nM | 4.99 |
| CHEMBL5087096 | — | IC50 | = | 11630.0 | nM | 4.93 |
| CHEMBL5076481 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL5074861 | — | IC50 | = | 13630.0 | nM | 4.87 |
| CHEMBL5079289 | — | IC50 | = | 16220.0 | nM | 4.79 |
| CHEMBL5091556 | — | IC50 | = | 17840.0 | nM | 4.75 |
| CHEMBL5082124 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5092134 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5083691 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5094133 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5084358 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5083487 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5091278 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5092610 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5074229 | — | IC50 | > | 30000.0 | nM | - |