Assay Detail
Functional
CHEMBL846887
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Hepatocyte |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.02 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50051 | — | — | 1 | 6.66 |
| CHEMBL48153 | — | — | 1 | 6.60 |
| CHEMBL49925 | — | — | 1 | 6.39 |
| CHEMBL297685 | — | — | 1 | 6.38 |
| CHEMBL296389 | — | — | 1 | 6.36 |
| CHEMBL301512 | — | — | 1 | 6.36 |
| CHEMBL51107 | — | — | 1 | 6.31 |
| CHEMBL300624 | — | — | 1 | 6.29 |
| CHEMBL51192 | — | — | 1 | 6.27 |
| CHEMBL299548 | — | — | 1 | 6.14 |
| CHEMBL48683 | — | — | 1 | 6.12 |
| CHEMBL51394 | — | — | 1 | 6.12 |
| CHEMBL50950 | — | — | 1 | 6.01 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 5.96 |
| CHEMBL48681 | — | — | 1 | 5.92 |
| CHEMBL51829 | — | — | 1 | 5.89 |
| CHEMBL297949 | — | — | 1 | 5.80 |
| CHEMBL52432 | — | — | 1 | 5.36 |
| CHEMBL48682 | — | — | 1 | 5.28 |
| CHEMBL51353 | — | — | 1 | 5.20 |
| CHEMBL440115 | FK453 | 1.0 | 1 | 5.09 |
| CHEMBL52276 | — | — | 1 | - |
| CHEMBL52735 | — | — | 1 | - |
| CHEMBL50839 | — | — | 1 | - |
| CHEMBL27508 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50051 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL48153 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL49925 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL297685 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL296389 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL301512 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL51107 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL300624 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL51192 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL299548 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL48683 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL51394 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL50950 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL48681 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL51829 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL297949 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL52432 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL48682 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL51353 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL440115 | FK453 | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL52276 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL52735 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL50839 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL27508 | — | IC50 | > | 10000.0 | nM | - |