Assay Detail
Binding
CHEMBL641516
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Binding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligand
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.42 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98464 | — | — | 1 | 9.44 |
| CHEMBL411692 | — | — | 1 | 9.33 |
| CHEMBL317580 | — | — | 1 | 9.23 |
| CHEMBL88147 | — | — | 1 | 9.19 |
| CHEMBL97748 | — | — | 1 | 8.45 |
| CHEMBL319539 | — | — | 1 | 8.17 |
| CHEMBL16687 | CGS-15943 | — | 1 | 7.86 |
| CHEMBL317373 | — | — | 1 | 7.84 |
| CHEMBL98570 | — | — | 1 | 7.66 |
| CHEMBL100382 | — | — | 1 | 7.63 |
| CHEMBL329284 | — | — | 1 | 7.49 |
| CHEMBL100195 | — | — | 1 | 7.48 |
| CHEMBL98828 | — | — | 1 | 7.47 |
| CHEMBL98512 | — | — | 1 | 7.37 |
| CHEMBL95229 | — | — | 1 | 7.35 |
| CHEMBL2112385 | — | — | 1 | 7.33 |
| CHEMBL94968 | — | — | 1 | 7.31 |
| CHEMBL318501 | — | — | 1 | 7.27 |
| CHEMBL97279 | — | — | 1 | 7.26 |
| CHEMBL97700 | — | — | 1 | 7.24 |
| CHEMBL97484 | — | — | 1 | 7.23 |
| CHEMBL95820 | — | — | 1 | 7.20 |
| CHEMBL95706 | — | — | 1 | 7.14 |
| CHEMBL95811 | — | — | 1 | 7.09 |
| CHEMBL97753 | — | — | 1 | 7.09 |
| CHEMBL2114300 | — | — | 1 | 7.08 |
| CHEMBL100426 | — | — | 1 | 6.71 |
| CHEMBL319976 | — | — | 1 | 6.67 |
| CHEMBL319941 | — | — | 1 | 6.46 |
| CHEMBL97961 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98464 | — | Ki | = | 0.362 | nM | 9.44 |
| CHEMBL411692 | — | Ki | = | 0.468 | nM | 9.33 |
| CHEMBL317580 | — | Ki | = | 0.586 | nM | 9.23 |
| CHEMBL88147 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL97748 | — | Ki | = | 3.56 | nM | 8.45 |
| CHEMBL319539 | — | Ki | = | 6.71 | nM | 8.17 |
| CHEMBL16687 | CGS-15943 | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL317373 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL98570 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL100382 | — | Ki | = | 23.6 | nM | 7.63 |
| CHEMBL329284 | — | Ki | = | 32.1 | nM | 7.49 |
| CHEMBL100195 | — | Ki | = | 32.9 | nM | 7.48 |
| CHEMBL98828 | — | Ki | = | 33.8 | nM | 7.47 |
| CHEMBL98512 | — | Ki | = | 42.5 | nM | 7.37 |
| CHEMBL95229 | — | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL2112385 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL94968 | — | Ki | = | 49.3 | nM | 7.31 |
| CHEMBL318501 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL97279 | — | Ki | = | 55.1 | nM | 7.26 |
| CHEMBL97700 | — | Ki | = | 57.9 | nM | 7.24 |
| CHEMBL97484 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL95820 | — | Ki | = | 62.9 | nM | 7.20 |
| CHEMBL95706 | — | Ki | = | 72.1 | nM | 7.14 |
| CHEMBL95811 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL97753 | — | Ki | = | 81.3 | nM | 7.09 |
| CHEMBL2114300 | — | Ki | = | 82.9 | nM | 7.08 |
| CHEMBL100426 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL319976 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL319941 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL97961 | — | Ki | = | 874.0 | nM | 6.06 |
| CHEMBL97307 | — | Ki | = | 882.0 | nM | 6.05 |
| CHEMBL2112381 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL2111571 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL89852 | — | Ki | = | 0.0314 | nM | - |
| CHEMBL330377 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL265096 | — | Ki | = | 0.00269 | nM | - |