Assay Detail
Binding
CHEMBL5734690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TLR7 Agonist Activity Assay: Engineered human embryonic kidney blue cells (HEK-Blue TLR cells; Invivogen) possessing a human TLR7-secreted embryonic alkaline phosphatase (SEAP) reporter transgene were suspended in a non-selective, culture medium (DMEM high-glucose (Invitrogen), supplemented with 10% fetal bovine serum (Sigma)). HEK-Blue TLR7 cells were added to each well of a 384-well tissue-culture plate (15,000 cells per well) and incubated 16-18 h at 37° C., 5% CO2. Compounds (100 nl) were dispensed into wells containing the HEK-Blue TLR cells and the treated cells were incubated at 37° C., 5% CO2. After 18 h treatment ten microliters of freshly-prepared Quanti-Blue reagent (Invivogen) was added to each well, incubated for 30 min (37° C., 5% CO2) and SEAP levels measured using an Envision plate reader (OD=620 nm). The half maximal effective concentration values (EC50; compound concentration which induced a response halfway between the assay baseline and maximum) were calculated.
231
Total Activities
73
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 77 | 8.26 | 9.46 |
| kon | 77 | - | - |
| k_off | 77 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5787885 | — | — | 3 | 9.46 |
| CHEMBL5885144 | — | — | 3 | 9.43 |
| CHEMBL5757520 | — | — | 3 | 9.35 |
| CHEMBL6040035 | — | — | 3 | 9.34 |
| CHEMBL5993886 | — | — | 3 | 9.27 |
| CHEMBL5790478 | — | — | 3 | 9.21 |
| CHEMBL5863568 | — | — | 3 | 9.15 |
| CHEMBL5977638 | — | — | 6 | 9.08 |
| CHEMBL6046238 | — | — | 3 | 9.06 |
| CHEMBL5849962 | — | — | 3 | 9.05 |
| CHEMBL5935960 | — | — | 3 | 9.04 |
| CHEMBL5803401 | — | — | 3 | 9.04 |
| CHEMBL6040007 | — | — | 3 | 9.02 |
| CHEMBL5948820 | — | — | 3 | 8.96 |
| CHEMBL5769037 | — | — | 3 | 8.95 |
| CHEMBL5745822 | — | — | 3 | 8.95 |
| CHEMBL5788562 | — | — | 3 | 8.94 |
| CHEMBL5778223 | — | — | 3 | 8.92 |
| CHEMBL5961499 | — | — | 3 | 8.92 |
| CHEMBL5772844 | — | — | 3 | 8.92 |
| CHEMBL5967615 | — | — | 3 | 8.91 |
| CHEMBL5926850 | — | — | 3 | 8.89 |
| CHEMBL6041191 | — | — | 3 | 8.89 |
| CHEMBL5992328 | — | — | 3 | 8.89 |
| CHEMBL5980725 | — | — | 3 | 8.89 |
| CHEMBL5985963 | — | — | 3 | 8.86 |
| CHEMBL5949769 | — | — | 3 | 8.85 |
| CHEMBL5757665 | — | — | 3 | 8.81 |
| CHEMBL5865451 | — | — | 3 | 8.80 |
| CHEMBL5801959 | — | — | 3 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5787885 | — | EC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5885144 | — | EC50 | = | 0.374 | nM | 9.43 |
| CHEMBL5757520 | — | EC50 | = | 0.45 | nM | 9.35 |
| CHEMBL6040035 | — | EC50 | = | 0.46 | nM | 9.34 |
| CHEMBL5993886 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL5790478 | — | EC50 | = | 0.62 | nM | 9.21 |
| CHEMBL5863568 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5977638 | — | EC50 | = | 0.83 | nM | 9.08 |
| CHEMBL6046238 | — | EC50 | = | 0.871 | nM | 9.06 |
| CHEMBL5849962 | — | EC50 | = | 0.89 | nM | 9.05 |
| CHEMBL5935960 | — | EC50 | = | 0.91 | nM | 9.04 |
| CHEMBL5803401 | — | EC50 | = | 0.91 | nM | 9.04 |
| CHEMBL6040007 | — | EC50 | = | 0.96 | nM | 9.02 |
| CHEMBL5977638 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5948820 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5745822 | — | EC50 | = | 1.12 | nM | 8.95 |
| CHEMBL5769037 | — | EC50 | = | 1.12 | nM | 8.95 |
| CHEMBL5788562 | — | EC50 | = | 1.14 | nM | 8.94 |
| CHEMBL5778223 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5961499 | — | EC50 | = | 1.19 | nM | 8.92 |
| CHEMBL5772844 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5967615 | — | EC50 | = | 1.23 | nM | 8.91 |
| CHEMBL6041191 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5992328 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5980725 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5926850 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5985963 | — | EC50 | = | 1.38 | nM | 8.86 |
| CHEMBL5949769 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5757665 | — | EC50 | = | 1.56 | nM | 8.81 |
| CHEMBL5865451 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5801959 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5849169 | — | EC50 | = | 1.71 | nM | 8.77 |
| CHEMBL5872235 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5813554 | — | EC50 | = | 1.77 | nM | 8.75 |
| CHEMBL5823588 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6064906 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5943152 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5778189 | — | EC50 | = | 1.82 | nM | 8.74 |
| CHEMBL6049946 | — | EC50 | = | 2.07 | nM | 8.68 |
| CHEMBL5936570 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5747710 | — | EC50 | = | 2.22 | nM | 8.65 |
| CHEMBL5757312 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5947975 | — | EC50 | = | 2.51 | nM | 8.60 |
| CHEMBL6057462 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5986883 | — | EC50 | = | 2.82 | nM | 8.55 |
| CHEMBL5817643 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5849169 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5950488 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5793963 | — | EC50 | = | 3.57 | nM | 8.45 |
| CHEMBL5888658 | — | EC50 | = | 3.9 | nM | 8.41 |