Assay Detail
Binding
CHEMBL5736726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: All test compounds were prepared as a stock solution of 10 mM in 100% DMSO.Inhibition binding assays were performed using 2.5 μg of membranes prepared from HEK293 cells transiently transfected with human adenosine A2a receptor or 10 μg of membranes prepared from CHO cells stably transfected with human adenosine A1 receptor. Membranes were incubated in 50 mM Tris-HCl (HEK293-hA2a; pH 7.4) or 20 mM HEPES, 100 mM NaCl, 10 mM MgCl2 (CHO-hA1; pH 7.4) in the presence of varying concentrations of test compound and 1 nM [3H]ZM241385 (HEK293-hA2a) or [3H]DPCPX (CHO-hA1) at 25° C. for 1 h. The assay was then terminated by rapid filtration onto GF/B grade Unifilter plates using a TomTec cell harvester, followed by 5×0.5 ml washes with double distilled H2O. Nonspecific binding was defined in the presence of 1 μM CGS15943 (HEK293-hA2a) or 1 μM DPCPX (CHO-hA1). Bound radioactivity was determined by liquid scintillation counting (Trilux Microbeta® Counter) and inhibition curves were analysed using a four-parameter logistic equation.
159
Total Activities
51
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
1,2,4-triazine-4-amine derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 7.43 | 9.84 |
| kon | 53 | - | - |
| k_off | 53 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2024114 | — | — | 3 | 9.84 |
| CHEMBL6028641 | — | — | 3 | 9.35 |
| CHEMBL5840492 | — | — | 3 | 8.74 |
| CHEMBL5826653 | — | — | 3 | 8.69 |
| CHEMBL5757899 | — | — | 3 | 8.54 |
| CHEMBL5863037 | — | — | 3 | 8.52 |
| CHEMBL5934455 | — | — | 3 | 8.46 |
| CHEMBL5992104 | — | — | 3 | 8.45 |
| CHEMBL5747068 | — | — | 3 | 8.20 |
| CHEMBL5807956 | — | — | 3 | 8.07 |
| CHEMBL5865636 | — | — | 3 | 8.05 |
| CHEMBL6055126 | — | — | 3 | 8.03 |
| CHEMBL2021950 | — | — | 3 | 7.83 |
| CHEMBL6023938 | — | — | 3 | 7.81 |
| CHEMBL5956914 | — | — | 3 | 7.76 |
| CHEMBL5844679 | — | — | 3 | 7.68 |
| CHEMBL5799083 | — | — | 3 | 7.62 |
| CHEMBL5992670 | — | — | 3 | 7.62 |
| CHEMBL2024119 | — | — | 3 | 7.60 |
| CHEMBL5802809 | — | — | 3 | 7.52 |
| CHEMBL6037066 | — | — | 3 | 7.49 |
| CHEMBL5942988 | — | — | 3 | 7.43 |
| CHEMBL6001450 | — | — | 3 | 7.40 |
| CHEMBL2024112 | — | — | 3 | 7.36 |
| CHEMBL5860515 | — | — | 3 | 7.36 |
| CHEMBL5876807 | — | — | 3 | 7.33 |
| CHEMBL2024115 | — | — | 6 | 7.29 |
| CHEMBL5998181 | — | — | 3 | 7.26 |
| CHEMBL2024111 | — | — | 3 | 7.25 |
| CHEMBL5947862 | — | — | 3 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2024114 | — | Ki | = | 0.145 | nM | 9.84 |
| CHEMBL6028641 | — | Ki | = | 0.447 | nM | 9.35 |
| CHEMBL5840492 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL5826653 | — | Ki | = | 2.04 | nM | 8.69 |
| CHEMBL5757899 | — | Ki | = | 2.88 | nM | 8.54 |
| CHEMBL5863037 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL5934455 | — | Ki | = | 3.47 | nM | 8.46 |
| CHEMBL5992104 | — | Ki | = | 3.55 | nM | 8.45 |
| CHEMBL5747068 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL5807956 | — | Ki | = | 8.51 | nM | 8.07 |
| CHEMBL5865636 | — | Ki | = | 8.91 | nM | 8.05 |
| CHEMBL6055126 | — | Ki | = | 9.33 | nM | 8.03 |
| CHEMBL2021950 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL6023938 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL5956914 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL5844679 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL5799083 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL5992670 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2024119 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5802809 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL6037066 | — | Ki | = | 32.4 | nM | 7.49 |
| CHEMBL5942988 | — | Ki | = | 37.2 | nM | 7.43 |
| CHEMBL6001450 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL5860515 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL2024112 | — | Ki | = | 43.7 | nM | 7.36 |
| CHEMBL5876807 | — | Ki | = | 46.8 | nM | 7.33 |
| CHEMBL2024115 | — | Ki | = | 51.3 | nM | 7.29 |
| CHEMBL5998181 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2024115 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2024111 | — | Ki | = | 56.2 | nM | 7.25 |
| CHEMBL5947862 | — | Ki | = | 67.6 | nM | 7.17 |
| CHEMBL5844887 | — | Ki | = | 70.8 | nM | 7.15 |
| CHEMBL6040157 | — | Ki | = | 75.9 | nM | 7.12 |
| CHEMBL5753430 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL5907501 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5751291 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL2024118 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2024120 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL5859757 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL5749831 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL5801947 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL2024120 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL5872977 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL2024117 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL6008883 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL4594442 | IMARADENANT | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL6032966 | — | Ki | = | 977.0 | nM | 6.01 |
| CHEMBL6062145 | — | Ki | = | 1072.0 | nM | 5.97 |
| CHEMBL5863927 | — | Ki | = | 4266.0 | nM | 5.37 |
| CHEMBL6062244 | — | Ki | = | 5623.0 | nM | 5.25 |