Assay Detail
Binding
CHEMBL2186853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Bcr-Abl T315I mutant using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assay
38
Total Activities
38
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
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.55 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178268 | — | — | 1 | 9.03 |
| CHEMBL1214141 | — | — | 1 | 9.01 |
| CHEMBL2178277 | — | — | 1 | 9.01 |
| CHEMBL2177645 | — | — | 1 | 8.95 |
| CHEMBL2177642 | — | — | 1 | 8.91 |
| CHEMBL2178278 | — | — | 1 | 8.71 |
| CHEMBL2177646 | — | — | 1 | 8.66 |
| CHEMBL2177648 | — | — | 1 | 8.29 |
| CHEMBL2178274 | — | — | 1 | 8.10 |
| CHEMBL2178276 | — | — | 1 | 8.01 |
| CHEMBL2178273 | — | — | 1 | 7.97 |
| CHEMBL2177633 | — | — | 1 | 7.97 |
| CHEMBL2178270 | — | — | 1 | 7.94 |
| CHEMBL2178272 | — | — | 1 | 7.90 |
| CHEMBL2177649 | — | — | 1 | 7.85 |
| CHEMBL2177632 | — | — | 1 | 7.84 |
| CHEMBL2178269 | — | — | 1 | 7.75 |
| CHEMBL2178271 | — | — | 1 | 7.73 |
| CHEMBL2177634 | — | — | 1 | 7.60 |
| CHEMBL2177635 | — | — | 1 | 7.53 |
| CHEMBL2177647 | — | — | 1 | 7.50 |
| CHEMBL2178267 | — | — | 1 | 7.48 |
| CHEMBL2178279 | — | — | 1 | 7.42 |
| CHEMBL2178275 | — | — | 1 | 7.41 |
| CHEMBL2177636 | — | — | 1 | 7.05 |
| CHEMBL2177629 | — | — | 1 | 7.04 |
| CHEMBL2177630 | — | — | 1 | 7.02 |
| CHEMBL2177631 | — | — | 1 | 6.91 |
| CHEMBL2178281 | — | — | 1 | 6.89 |
| CHEMBL2177641 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178268 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL1214141 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL2178277 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL2177645 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL2177642 | — | IC50 | = | 1.22 | nM | 8.91 |
| CHEMBL2178278 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL2177646 | — | IC50 | = | 2.18 | nM | 8.66 |
| CHEMBL2177648 | — | IC50 | = | 5.09 | nM | 8.29 |
| CHEMBL2178274 | — | IC50 | = | 7.93 | nM | 8.10 |
| CHEMBL2178276 | — | IC50 | = | 9.83 | nM | 8.01 |
| CHEMBL2177633 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL2178273 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL2178270 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL2178272 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL2177649 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2177632 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL2178269 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2178271 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL2177634 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL2177635 | — | IC50 | = | 29.6 | nM | 7.53 |
| CHEMBL2177647 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL2178267 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL2178279 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2178275 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL2177636 | — | IC50 | = | 89.4 | nM | 7.05 |
| CHEMBL2177629 | — | IC50 | = | 92.2 | nM | 7.04 |
| CHEMBL2177630 | — | IC50 | = | 95.7 | nM | 7.02 |
| CHEMBL2177631 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL2178281 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2177641 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL2177644 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2177650 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL2177643 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL2177638 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL2177637 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL2177639 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL2178280 | — | IC50 | = | 659.0 | nM | 6.18 |
| CHEMBL2177640 | — | IC50 | = | 2130.0 | nM | 5.67 |