Assay Detail
Binding
CHEMBL887078
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Inhibition of Tie2 autophosphorylation in EA.hy926 cells after 2.5 hrs
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.74 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL245746 | — | — | 1 | 8.30 |
| CHEMBL245947 | — | — | 1 | 7.96 |
| CHEMBL397090 | — | — | 1 | 7.89 |
| CHEMBL246152 | — | — | 1 | 7.82 |
| CHEMBL246355 | — | — | 1 | 7.64 |
| CHEMBL246356 | — | — | 1 | 7.48 |
| CHEMBL245948 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL245746 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL245947 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL397090 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL246152 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL246355 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL246356 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL245948 | — | IC50 | = | 85.0 | nM | 7.07 |