Assay Detail
Binding
CHEMBL4727488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at TLR8 in human THP-1 cells assessed as inhibition of resiquimod-induced TNFalpha production
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.86 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790219 | — | — | 1 | 9.00 |
| CHEMBL4762866 | — | — | 1 | 8.70 |
| CHEMBL4748638 | — | — | 1 | 8.52 |
| CHEMBL4783510 | — | — | 1 | 8.30 |
| CHEMBL4761527 | — | — | 1 | 8.00 |
| CHEMBL4740820 | — | — | 1 | 7.75 |
| CHEMBL4782200 | — | — | 1 | 7.70 |
| CHEMBL4755173 | — | — | 1 | 7.58 |
| CHEMBL4792072 | — | — | 1 | 7.40 |
| CHEMBL4776103 | — | — | 1 | 7.22 |
| CHEMBL4745239 | — | — | 1 | 7.12 |
| CHEMBL4796453 | — | — | 1 | 7.06 |
| CHEMBL4634860 | — | — | 1 | - |
| CHEMBL4740968 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790219 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4762866 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4748638 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4783510 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4761527 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4740820 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4782200 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4755173 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4792072 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4776103 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4745239 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4796453 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4634860 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4740968 | — | IC50 | < | 1.0 | nM | - |