Assay Detail
Binding
CHEMBL5050587
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Antagonist activity at human TLR8 expressed in Drosophila S2 by TR-FRET assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 14 | 7.94 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080083 | — | — | 1 | 8.70 |
| CHEMBL5079910 | — | — | 1 | 8.62 |
| CHEMBL5091113 | — | — | 1 | 8.52 |
| CHEMBL5090067 | — | — | 1 | 8.44 |
| CHEMBL5078689 | — | — | 1 | 8.33 |
| CHEMBL5085458 | — | — | 1 | 8.09 |
| CHEMBL5085289 | — | — | 1 | 8.08 |
| CHEMBL5077828 | — | — | 1 | 7.85 |
| CHEMBL5086681 | — | — | 1 | 7.66 |
| CHEMBL5077018 | — | — | 1 | 7.64 |
| CHEMBL5083541 | — | — | 1 | 7.48 |
| CHEMBL5081397 | — | — | 1 | 7.41 |
| CHEMBL5089903 | — | — | 1 | 7.29 |
| CHEMBL5089636 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080083 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5079910 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5091113 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5090067 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5078689 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5085458 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5085289 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5077828 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5086681 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5077018 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5083541 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5081397 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5089903 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5089636 | — | IC50 | = | 100.0 | nM | 7.00 |