Assay Detail
Binding
CHEMBL643011
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Binding affinity was determined in radioligand binding assay at rat striatal Adenosine A2A receptor vs [3H]-CGS- 21680
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 7.83 | 8.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL97700 | — | — | 1 | 8.95 |
| CHEMBL97753 | — | — | 1 | 8.94 |
| CHEMBL95811 | — | — | 1 | 8.86 |
| CHEMBL98570 | — | — | 1 | 8.44 |
| CHEMBL2114300 | — | — | 1 | 8.18 |
| CHEMBL97748 | — | — | 1 | 8.16 |
| CHEMBL97484 | — | — | 1 | 8.13 |
| CHEMBL319539 | — | — | 1 | 8.12 |
| CHEMBL97961 | — | — | 1 | 8.12 |
| CHEMBL329284 | — | — | 1 | 8.03 |
| CHEMBL97307 | — | — | 1 | 8.02 |
| CHEMBL95820 | — | — | 1 | 8.00 |
| CHEMBL319976 | — | — | 1 | 7.99 |
| CHEMBL88147 | — | — | 1 | 7.99 |
| CHEMBL94968 | — | — | 1 | 7.98 |
| CHEMBL318501 | — | — | 1 | 7.96 |
| CHEMBL98464 | — | — | 1 | 7.96 |
| CHEMBL317580 | — | — | 1 | 7.92 |
| CHEMBL95229 | — | — | 1 | 7.78 |
| CHEMBL330377 | — | — | 1 | 7.76 |
| CHEMBL2112385 | — | — | 1 | 7.73 |
| CHEMBL100195 | — | — | 1 | 7.70 |
| CHEMBL411692 | — | — | 1 | 7.70 |
| CHEMBL317373 | — | — | 1 | 7.55 |
| CHEMBL100382 | — | — | 1 | 7.55 |
| CHEMBL97279 | — | — | 1 | 7.54 |
| CHEMBL2112381 | — | — | 1 | 7.53 |
| CHEMBL98828 | — | — | 1 | 7.47 |
| CHEMBL319941 | — | — | 1 | 7.25 |
| CHEMBL95706 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL97700 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL97753 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL95811 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL98570 | — | Ki | = | 3.64 | nM | 8.44 |
| CHEMBL2114300 | — | Ki | = | 6.65 | nM | 8.18 |
| CHEMBL97748 | — | Ki | = | 6.97 | nM | 8.16 |
| CHEMBL97484 | — | Ki | = | 7.43 | nM | 8.13 |
| CHEMBL319539 | — | Ki | = | 7.58 | nM | 8.12 |
| CHEMBL97961 | — | Ki | = | 7.58 | nM | 8.12 |
| CHEMBL329284 | — | Ki | = | 9.43 | nM | 8.03 |
| CHEMBL97307 | — | Ki | = | 9.67 | nM | 8.02 |
| CHEMBL95820 | — | Ki | = | 9.93 | nM | 8.00 |
| CHEMBL319976 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL88147 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL94968 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL318501 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL98464 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL317580 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL95229 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL330377 | — | Ki | = | 17.2 | nM | 7.76 |
| CHEMBL2112385 | — | Ki | = | 18.8 | nM | 7.73 |
| CHEMBL100195 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL411692 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL317373 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL100382 | — | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL97279 | — | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL2112381 | — | Ki | = | 29.7 | nM | 7.53 |
| CHEMBL98828 | — | Ki | = | 33.7 | nM | 7.47 |
| CHEMBL319941 | — | Ki | = | 55.9 | nM | 7.25 |
| CHEMBL95706 | — | Ki | = | 59.8 | nM | 7.22 |
| CHEMBL2111571 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL98512 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL100426 | — | Ki | = | 453.0 | nM | 6.34 |
| CHEMBL89852 | — | Ki | > | 100.0 | nM | - |
| CHEMBL16687 | CGS-15943 | Ki | = | 3.3 | nM | - |
| CHEMBL265096 | — | Ki | > | 100.0 | nM | - |