Assay Detail
Binding
CHEMBL5050606
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Antagonist activity at human TLR7 expressed in human PBMC cells assessed as inhibition of ssRNA stimulated IFNalpha level preincubated for 30 mins followed by stimulation and measured after 20 hrs by AlphaLISA method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an <i>In Vivo</i> Efficacious TLR7/8 Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.33 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079910 | — | — | 1 | 10.00 |
| CHEMBL5090067 | — | — | 1 | 9.41 |
| CHEMBL5085458 | — | — | 1 | 9.17 |
| CHEMBL5085289 | — | — | 1 | 9.00 |
| CHEMBL5077018 | — | — | 1 | 8.96 |
| CHEMBL5086681 | — | — | 1 | 8.52 |
| CHEMBL5091113 | — | — | 1 | 8.15 |
| CHEMBL5078689 | — | — | 1 | 8.05 |
| CHEMBL5089636 | — | — | 1 | 7.96 |
| CHEMBL5081397 | — | — | 1 | 6.66 |
| CHEMBL5080083 | — | — | 1 | 5.77 |
| CHEMBL5077828 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079910 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5090067 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5085458 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5085289 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5077018 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5086681 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5091113 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5078689 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5089636 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5081397 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5080083 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5077828 | — | IC50 | > | 980.0 | nM | - |