Assay Detail
Functional
CHEMBL4156074
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Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies and pharmacological characterization of N5-heteroarylalkyl-substituted-2-(2-furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine-based derivatives as inverse agonists at human A2A adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.04 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162638 | — | — | 1 | 8.38 |
| CHEMBL4159215 | — | — | 1 | 8.05 |
| CHEMBL4172818 | — | — | 1 | 7.88 |
| CHEMBL4167557 | — | — | 1 | 7.85 |
| CHEMBL4175676 | — | — | 1 | 7.48 |
| CHEMBL113142 | ZM-241385 | — | 1 | 7.29 |
| CHEMBL4161758 | — | — | 1 | 7.12 |
| CHEMBL4172399 | — | — | 1 | 7.09 |
| CHEMBL4172715 | — | — | 1 | 7.04 |
| CHEMBL4167813 | — | — | 1 | 7.02 |
| CHEMBL4167125 | — | — | 1 | 6.96 |
| CHEMBL4172264 | — | — | 1 | 6.95 |
| CHEMBL4165484 | — | — | 1 | 6.92 |
| CHEMBL4168980 | — | — | 1 | 6.41 |
| CHEMBL4168016 | — | — | 1 | 6.26 |
| CHEMBL4175878 | — | — | 1 | 5.56 |
| CHEMBL4162037 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162638 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL4159215 | — | IC50 | = | 8.96 | nM | 8.05 |
| CHEMBL4172818 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4167557 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4175676 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL113142 | ZM-241385 | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4161758 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4172399 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4172715 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4167813 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4167125 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4172264 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4165484 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4168980 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL4168016 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL4175878 | — | IC50 | = | 2773.0 | nM | 5.56 |
| CHEMBL4162037 | — | IC50 | = | 4571.0 | nM | 5.34 |