Assay Detail
Binding
CHEMBL1105451
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in HEK293 cells after 60 mins by rapid filtration assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.31 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090577 | — | — | 1 | 10.52 |
| CHEMBL1093271 | — | — | 1 | 10.02 |
| CHEMBL1090578 | — | — | 1 | 9.72 |
| CHEMBL1093018 | — | — | 1 | 9.40 |
| CHEMBL1093479 | — | — | 1 | 8.58 |
| CHEMBL1090576 | — | — | 1 | 8.49 |
| CHEMBL1093203 | — | — | 1 | 8.21 |
| CHEMBL1092271 | — | — | 1 | 7.72 |
| CHEMBL1090575 | — | — | 1 | 7.32 |
| CHEMBL1092270 | — | — | 1 | 6.83 |
| CHEMBL1093270 | — | — | 1 | 6.64 |
| CHEMBL17127 | SCH-58261 | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090577 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL1093271 | — | Ki | = | 0.096 | nM | 10.02 |
| CHEMBL1090578 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL1093018 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1093479 | — | Ki | = | 2.62 | nM | 8.58 |
| CHEMBL1090576 | — | Ki | = | 3.21 | nM | 8.49 |
| CHEMBL1093203 | — | Ki | = | 6.13 | nM | 8.21 |
| CHEMBL1092271 | — | Ki | = | 19.01 | nM | 7.72 |
| CHEMBL1090575 | — | Ki | = | 47.96 | nM | 7.32 |
| CHEMBL1092270 | — | Ki | = | 147.9 | nM | 6.83 |
| CHEMBL1093270 | — | Ki | = | 228.4 | nM | 6.64 |
| CHEMBL17127 | SCH-58261 | Ki | = | 594.1 | nM | 6.23 |