Assay Detail
Binding
CHEMBL4622222
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 2-((1E,3E,5E)-5-(3,3-Dimethyl-1-(6-((4-(((3-methyl-5-(1H-pyrazolo[3,4-b]pyridin-4-yl)pyridin-2-yl)oxy)methyl)bicyclo[2.2.2]octan-1-yl)amino)-6-oxohexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-1-ethyl-3,3-dimethyl-5-sulfo-3H-indol-1-ium trifluoroacetate from biotinylated human TLR8 extracellular domain (27 to 827 residues) expressed in Drosophila S2 cells after 30 mins by europium-labeled streptavidin based TR-FRET assay
27
Total Activities
27
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
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 | 27 | 5.93 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4634860 | — | — | 1 | 7.17 |
| CHEMBL4642652 | — | — | 1 | 7.16 |
| CHEMBL4647012 | — | — | 1 | 6.85 |
| CHEMBL4637821 | — | — | 1 | 6.66 |
| CHEMBL4632846 | — | — | 1 | 6.57 |
| CHEMBL4647559 | — | — | 1 | 6.55 |
| CHEMBL4644098 | — | — | 1 | 6.50 |
| CHEMBL4634366 | — | — | 1 | 6.40 |
| CHEMBL4649727 | — | — | 1 | 6.22 |
| CHEMBL4633872 | — | — | 1 | 6.10 |
| CHEMBL4647201 | — | — | 1 | 5.89 |
| CHEMBL4633436 | — | — | 1 | 5.85 |
| CHEMBL4635744 | — | — | 1 | 5.85 |
| CHEMBL4646609 | — | — | 1 | 5.80 |
| CHEMBL4643502 | — | — | 1 | 5.77 |
| CHEMBL4632520 | — | — | 1 | 5.72 |
| CHEMBL4640935 | — | — | 1 | 5.70 |
| CHEMBL4635717 | — | — | 1 | 5.68 |
| CHEMBL4646719 | — | — | 1 | 5.62 |
| CHEMBL4648996 | — | — | 1 | 5.57 |
| CHEMBL4633423 | — | — | 1 | 5.50 |
| CHEMBL4641604 | — | — | 1 | 5.43 |
| CHEMBL4635547 | — | — | 1 | 5.38 |
| CHEMBL4639145 | — | — | 1 | 5.12 |
| CHEMBL4642538 | — | — | 1 | 4.72 |
| CHEMBL4647602 | — | — | 1 | 4.31 |
| CHEMBL4641633 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4634860 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4642652 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4647012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4637821 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4632846 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4647559 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4644098 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4634366 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4649727 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4633872 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4647201 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4633436 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4635744 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4646609 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4643502 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4632520 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4640935 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4635717 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4646719 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4648996 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4633423 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4641604 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4635547 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4639145 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4642538 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4647602 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4641633 | — | IC50 | < | 20.0 | nM | - |