Assay Detail
Binding
CHEMBL923929
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Inhibition of Abl-T315I mutant
26
Total Activities
26
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
The design and preliminary structure-activity relationship studies of benzotriazines as potent inhibitors of Abl and Abl-T315I enzymes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.90 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250019 | — | — | 1 | 8.92 |
| CHEMBL249821 | — | — | 1 | 8.47 |
| CHEMBL250625 | — | — | 1 | 8.33 |
| CHEMBL250214 | — | — | 1 | 7.82 |
| CHEMBL399268 | — | — | 1 | 7.80 |
| CHEMBL399246 | — | — | 1 | 7.68 |
| CHEMBL250213 | — | — | 1 | 7.58 |
| CHEMBL400403 | — | — | 1 | 7.32 |
| CHEMBL400303 | — | — | 1 | 7.30 |
| CHEMBL440963 | — | — | 1 | 7.29 |
| CHEMBL400402 | — | — | 1 | 7.26 |
| CHEMBL250021 | — | — | 1 | 7.18 |
| CHEMBL398279 | — | — | 1 | 7.12 |
| CHEMBL250623 | — | — | 1 | 6.85 |
| CHEMBL250423 | — | — | 1 | 6.82 |
| CHEMBL398845 | — | — | 1 | 6.79 |
| CHEMBL250821 | — | — | 1 | 6.24 |
| CHEMBL249820 | — | — | 1 | 6.16 |
| CHEMBL249819 | — | — | 1 | 6.09 |
| CHEMBL250218 | — | — | 1 | 6.02 |
| CHEMBL231220 | — | — | 1 | 5.79 |
| CHEMBL251015 | — | — | 1 | 5.75 |
| CHEMBL268825 | — | — | 1 | 5.63 |
| CHEMBL436137 | — | — | 1 | 5.37 |
| CHEMBL230686 | — | — | 1 | 4.99 |
| CHEMBL231524 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250019 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL249821 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL250625 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL250214 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL399268 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL399246 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL250213 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL400403 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL400303 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL440963 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL400402 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL250021 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL398279 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL250623 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL250423 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL398845 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL250821 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL249820 | — | Ki | = | 687.0 | nM | 6.16 |
| CHEMBL249819 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL250218 | — | Ki | = | 956.0 | nM | 6.02 |
| CHEMBL231220 | — | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL251015 | — | Ki | = | 1770.0 | nM | 5.75 |
| CHEMBL268825 | — | Ki | = | 2340.0 | nM | 5.63 |
| CHEMBL436137 | — | Ki | = | 4240.0 | nM | 5.37 |
| CHEMBL230686 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL231524 | — | Ki | > | 2500.0 | nM | - |