Assay Detail
Binding
CHEMBL5736166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR and cAMP Inhibition Assay: hADORA1/CHO (hA1 expressing) cells (Genscript) were plated at 1×104 cells/well into 384-well polystyrene plates one day before starting the experiment. On the day of experiment, the supernatant was discard and replaced with 40 L of dye (FLIPR calcium 5 Assay Kit) per well and the plates were incubated for 60 mins at 37° C. plus 5% CO2. Then testing compounds were added at different concentrations for FLIPR inhibition assay. After a 400 s incubation with compound, 10 M adenosine was added into the cells, and the signal was captured by FLIPR.hA2a/CHO, hA2b/CHO and mA2a/CHO (Genscript) were plated at 5×103 cells/well into 384-well polystyrene plates at the day of experiment. Compounds were pre-incubated with cells for 30 min at 37° C., 5% CO2. Then 10 M adenosine was added to the cells and incubated for 30 min at 37° C., 5% CO2. Detection reagent (CISBIO) was added and the plates were incubated for 60 min at room temperature. The signal was captured by Envision.
318
Total Activities
106
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
Triazolo-pyrimidine compounds and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 106 | 6.65 | 8.36 |
| kon | 106 | - | - |
| k_off | 106 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5827075 | — | — | 3 | 8.36 |
| CHEMBL5999728 | — | — | 3 | 8.33 |
| CHEMBL5928153 | — | — | 3 | 8.32 |
| CHEMBL5867675 | — | — | 3 | 7.92 |
| CHEMBL5986561 | — | — | 3 | 7.92 |
| CHEMBL6007478 | — | — | 3 | 7.91 |
| CHEMBL5800386 | — | — | 3 | 7.85 |
| CHEMBL5917926 | — | — | 3 | 7.85 |
| CHEMBL6057843 | — | — | 3 | 7.79 |
| CHEMBL5880072 | — | — | 3 | 7.77 |
| CHEMBL5841873 | — | — | 3 | 7.72 |
| CHEMBL6057896 | — | — | 3 | 7.68 |
| CHEMBL5747460 | — | — | 3 | 7.63 |
| CHEMBL5765395 | — | — | 3 | 7.42 |
| CHEMBL5833725 | — | — | 3 | 7.42 |
| CHEMBL5829088 | — | — | 3 | 7.42 |
| CHEMBL5825227 | — | — | 3 | 7.39 |
| CHEMBL6003948 | — | — | 3 | 7.35 |
| CHEMBL5913092 | — | — | 3 | 7.35 |
| CHEMBL5974806 | — | — | 3 | 7.33 |
| CHEMBL5795044 | — | — | 3 | 7.32 |
| CHEMBL5882133 | — | — | 3 | 7.32 |
| CHEMBL5940119 | — | — | 3 | 7.32 |
| CHEMBL6030840 | — | — | 3 | 7.29 |
| CHEMBL5756623 | — | — | 3 | 7.25 |
| CHEMBL5966778 | — | — | 3 | 7.24 |
| CHEMBL5919017 | — | — | 3 | 7.19 |
| CHEMBL6043653 | — | — | 3 | 7.17 |
| CHEMBL6022992 | — | — | 3 | 7.14 |
| CHEMBL5875672 | — | — | 3 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5827075 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5999728 | — | IC50 | = | 4.69 | nM | 8.33 |
| CHEMBL5928153 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5986561 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5867675 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6007478 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL5917926 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5800386 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL6057843 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL5880072 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5841873 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL6057896 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5747460 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL5829088 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5765395 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5833725 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5825227 | — | IC50 | = | 40.9 | nM | 7.39 |
| CHEMBL5913092 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL6003948 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5974806 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5882133 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5795044 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5940119 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL6030840 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5756623 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5966778 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5919017 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL6043653 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL6022992 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5875672 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5836704 | — | IC50 | = | 71.6 | nM | 7.14 |
| CHEMBL6063197 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5847956 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL6055525 | — | IC50 | = | 80.5 | nM | 7.09 |
| CHEMBL5990931 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5810207 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5956015 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5817464 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL6016827 | — | IC50 | = | 93.5 | nM | 7.03 |
| CHEMBL6062538 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5787943 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5957422 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL6041892 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5896698 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL6044836 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5993458 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5857008 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL5988628 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5813457 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL5774791 | — | IC50 | = | 142.0 | nM | 6.85 |