Assay Detail
Binding
CHEMBL5734595
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biological Assay: HEK-Blue-cells (Invivogen) overexpressing human TLR7, TLR8 or TLR9 receptors were used for screening inhibitors of these receptors using an inducible SEAP (secreted embryonic alkaline phosphatase) reporter gene under the control of the IFN-β minimal promoter fused to five NF-κB and AP-1-binding sites. Briefly, cells are seeded into Greiner 384 well plates (15000 cells per well for TLR7, 20,000 for TLR8 and 25,000 for TLR9) and then treated with test compounds in DMSO to yield a final dose response concentration range of 0.05 nM-50 μM. After a 30 minute compound pre-treatment at room temperature, the cells are then stimulated with a TLR7 ligand (gardiquimod at a final concentration of 7.5 μM), TLR8 ligand (R848 at a final concentration of 15.9 μM) or TLR9 ligand (ODN2006 at a final concentration of 5 nM) to activate NF-κB and AP-1 which induce the production of SEAP. After a 22 hour incubation at 37° C., 5% CO2, SEAP levels are determined with the addition of HEK-Blue Detection reagent (Invivogen), a cell culture medium that allows for detection of SEAP, according to manufacturer's specifications.
2934
Total Activities
953
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
[1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 978 | 7.87 | 9.30 |
| kon | 978 | - | - |
| k_off | 978 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5988319 | — | — | 3 | 9.30 |
| CHEMBL5883015 | — | — | 3 | 9.30 |
| CHEMBL5961198 | — | — | 3 | 9.30 |
| CHEMBL5764996 | — | — | 3 | 9.30 |
| CHEMBL5809363 | — | — | 3 | 9.30 |
| CHEMBL5821604 | — | — | 3 | 9.22 |
| CHEMBL5893710 | — | — | 3 | 9.15 |
| CHEMBL5940991 | — | — | 3 | 9.15 |
| CHEMBL5840490 | — | — | 3 | 9.15 |
| CHEMBL5931240 | — | — | 3 | 9.15 |
| CHEMBL5759798 | — | — | 3 | 9.15 |
| CHEMBL5964117 | — | — | 3 | 9.15 |
| CHEMBL5846293 | — | — | 3 | 9.15 |
| CHEMBL5949257 | — | — | 3 | 9.10 |
| CHEMBL5819919 | — | — | 3 | 9.10 |
| CHEMBL5743961 | — | — | 3 | 9.10 |
| CHEMBL5745390 | — | — | 3 | 9.10 |
| CHEMBL5963140 | — | — | 3 | 9.10 |
| CHEMBL5761494 | — | — | 3 | 9.10 |
| CHEMBL5899235 | — | — | 3 | 9.10 |
| CHEMBL5938401 | — | — | 3 | 9.05 |
| CHEMBL5925306 | — | — | 3 | 9.05 |
| CHEMBL6035407 | — | — | 3 | 9.05 |
| CHEMBL5928140 | — | — | 3 | 9.00 |
| CHEMBL6060887 | — | — | 6 | 9.00 |
| CHEMBL6011519 | — | — | 3 | 9.00 |
| CHEMBL5997772 | — | — | 3 | 8.96 |
| CHEMBL6008446 | — | — | 3 | 8.96 |
| CHEMBL6063549 | — | — | 3 | 8.96 |
| CHEMBL5865529 | — | — | 3 | 8.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5988319 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5764996 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5809363 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5883015 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5961198 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5821604 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5840490 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5846293 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5759798 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5964117 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5893710 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5940991 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5931240 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5761494 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5743961 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5819919 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5963140 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5949257 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5899235 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5745390 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL6035407 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5938401 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5925306 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL6060887 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6011519 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5928140 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6008446 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6012337 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5997772 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6063549 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5774703 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5865529 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5743765 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5778522 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6037193 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6033730 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5771567 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5918821 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5962043 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5990321 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL6046180 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5847442 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5925353 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5792267 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5805073 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5987075 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5797671 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL6036977 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4650329 | AFIMETORAN | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5810324 | — | IC50 | = | 1.4 | nM | 8.85 |