Assay Detail
Binding
CHEMBL4727486
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Antagonist activity at TLR7 in human PBMC assessed as inhibition of ssRNA40-induced IFNalpha production
15
Total Activities
15
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
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.23 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740968 | — | — | 1 | 8.52 |
| CHEMBL4748638 | — | — | 1 | 8.22 |
| CHEMBL4783510 | — | — | 1 | 7.60 |
| CHEMBL4740820 | — | — | 1 | 7.35 |
| CHEMBL4792072 | — | — | 1 | 7.34 |
| CHEMBL4755173 | — | — | 1 | 7.28 |
| CHEMBL4782200 | — | — | 1 | 7.15 |
| CHEMBL4796453 | — | — | 1 | 7.02 |
| CHEMBL4776103 | — | — | 1 | 6.77 |
| CHEMBL4745239 | — | — | 1 | 6.70 |
| CHEMBL4743698 | — | — | 1 | 6.51 |
| CHEMBL4761527 | — | — | 1 | 6.30 |
| CHEMBL4790219 | — | — | 1 | - |
| CHEMBL4634860 | — | — | 1 | - |
| CHEMBL4762866 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740968 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4748638 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4783510 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4740820 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4792072 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4755173 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4782200 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4796453 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4776103 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4745239 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4743698 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4761527 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4790219 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4634860 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4762866 | — | IC50 | < | 1.0 | nM | - |