Assay Detail
Binding
CHEMBL3707872
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Luciferase-Based Assay: Recombinant human c-Src or Yes (28 ng/well, Panvera/Invitrogen, Madison Wis.), ATP (3 μM), a tyrosine kinase substrate (PTK2, 250 μM, Promega Corp., Madison Wis.), and test agents (at concentrations ranging from about 1 nM/l to about 100 μM/l), in the presence of Src kinase reaction buffer (Upstate USA, Lake Placid N.Y.). After reacting for about 90 minutes at room temperature, residual ATP was determined using a luciferase-based assay (KinaseGlo, Promega Corp.) as a measure of kinase activity.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Benzotriazine inhibitors of kinases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.11 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 9.30 |
| CHEMBL3651257 | — | — | 1 | 9.15 |
| CHEMBL3651296 | — | — | 1 | 8.92 |
| CHEMBL3651228 | — | — | 1 | 8.91 |
| CHEMBL249821 | — | — | 1 | 8.89 |
| CHEMBL3651297 | — | — | 1 | 8.59 |
| CHEMBL231218 | — | — | 1 | 8.51 |
| CHEMBL218549 | — | — | 1 | 8.43 |
| CHEMBL3648061 | — | — | 1 | 8.14 |
| CHEMBL230614 | — | — | 1 | 8.11 |
| CHEMBL230686 | — | — | 1 | 7.99 |
| CHEMBL3648058 | — | — | 1 | 7.74 |
| CHEMBL268825 | — | — | 1 | 7.66 |
| CHEMBL230685 | — | — | 1 | 6.96 |
| CHEMBL3651299 | — | — | 1 | 6.33 |
| CHEMBL218042 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3651257 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3651296 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3651228 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL249821 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL3651297 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL231218 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL218549 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3648061 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL230614 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL230686 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL3648058 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL268825 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL230685 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3651299 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL218042 | — | IC50 | = | 822.0 | nM | 6.08 |