Assay Detail
Binding
CHEMBL4622225
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Antagonist activity at TLR8 in human PBMC assessed as inhibition of DOTAP-ssRNA40 induced TNFalpha production preincubated for 30 mins followed by ssRNA40 addition measured after 20 hrs by HTRF assay
26
Total Activities
26
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
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.37 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642652 | — | — | 1 | 8.96 |
| CHEMBL4641633 | — | — | 1 | 8.82 |
| CHEMBL4644098 | — | — | 1 | 8.57 |
| CHEMBL4649727 | — | — | 1 | 8.35 |
| CHEMBL4634366 | — | — | 1 | 8.05 |
| CHEMBL4647201 | — | — | 1 | 7.96 |
| CHEMBL4633872 | — | — | 1 | 7.89 |
| CHEMBL4647559 | — | — | 1 | 7.82 |
| CHEMBL4632520 | — | — | 1 | 7.75 |
| CHEMBL4635717 | — | — | 1 | 7.52 |
| CHEMBL4635547 | — | — | 1 | 7.52 |
| CHEMBL4632846 | — | — | 1 | 7.48 |
| CHEMBL4643502 | — | — | 1 | 7.48 |
| CHEMBL4640935 | — | — | 1 | 7.46 |
| CHEMBL4641604 | — | — | 1 | 7.41 |
| CHEMBL4637821 | — | — | 1 | 7.35 |
| CHEMBL4633423 | — | — | 1 | 7.33 |
| CHEMBL4642538 | — | — | 1 | 7.12 |
| CHEMBL4646719 | — | — | 1 | 7.04 |
| CHEMBL4648996 | — | — | 1 | 7.03 |
| CHEMBL4647012 | — | — | 1 | 6.85 |
| CHEMBL4635744 | — | — | 1 | 6.52 |
| CHEMBL4639145 | — | — | 1 | 6.50 |
| CHEMBL4647602 | — | — | 1 | 5.92 |
| CHEMBL4646609 | — | — | 1 | 5.82 |
| CHEMBL4633436 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642652 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4641633 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4644098 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4649727 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4634366 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4647201 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4633872 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4647559 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4632520 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4635717 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4635547 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4632846 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4643502 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4640935 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4641604 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4637821 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4633423 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4642538 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4646719 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4648996 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4647012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4635744 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4639145 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4647602 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4646609 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4633436 | — | IC50 | = | 8000.0 | nM | 5.10 |