Assay Detail
Binding
CHEMBL2186859
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type Bcr-Abl 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 |
| Confidence | 6 — Multiple protein complex / RNA |
| 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 | 8.67 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178270 | — | — | 1 | 9.48 |
| CHEMBL2178277 | — | — | 1 | 9.44 |
| CHEMBL2178271 | — | — | 1 | 9.39 |
| CHEMBL2178276 | — | — | 1 | 9.38 |
| CHEMBL2177649 | — | — | 1 | 9.35 |
| CHEMBL2178268 | — | — | 1 | 9.35 |
| CHEMBL2177648 | — | — | 1 | 9.28 |
| CHEMBL2178269 | — | — | 1 | 9.28 |
| CHEMBL2177632 | — | — | 1 | 9.28 |
| CHEMBL2177646 | — | — | 1 | 9.28 |
| CHEMBL2177634 | — | — | 1 | 9.27 |
| CHEMBL2177645 | — | — | 1 | 9.22 |
| CHEMBL2177642 | — | — | 1 | 9.16 |
| CHEMBL2178278 | — | — | 1 | 9.15 |
| CHEMBL2177647 | — | — | 1 | 9.14 |
| CHEMBL2177633 | — | — | 1 | 9.11 |
| CHEMBL2178279 | — | — | 1 | 9.01 |
| CHEMBL2177636 | — | — | 1 | 9.00 |
| CHEMBL2178275 | — | — | 1 | 9.00 |
| CHEMBL2178273 | — | — | 1 | 8.99 |
| CHEMBL2177635 | — | — | 1 | 8.93 |
| CHEMBL1214141 | — | — | 1 | 8.90 |
| CHEMBL2178267 | — | — | 1 | 8.85 |
| CHEMBL2178272 | — | — | 1 | 8.78 |
| CHEMBL2178274 | — | — | 1 | 8.71 |
| CHEMBL2177631 | — | — | 1 | 8.65 |
| CHEMBL2177650 | — | — | 1 | 8.59 |
| CHEMBL2177629 | — | — | 1 | 8.57 |
| CHEMBL2177630 | — | — | 1 | 8.46 |
| CHEMBL2177637 | — | — | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178270 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL2178277 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL2178271 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL2178276 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2177649 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL2178268 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL2177648 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2178269 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2177632 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2177646 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL2177634 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL2177645 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2177642 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL2178278 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2177647 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL2177633 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL2178279 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL2177636 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL2178275 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL2178273 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL2177635 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL1214141 | — | IC50 | = | 1.25 | nM | 8.90 |
| CHEMBL2178267 | — | IC50 | = | 1.42 | nM | 8.85 |
| CHEMBL2178272 | — | IC50 | = | 1.66 | nM | 8.78 |
| CHEMBL2178274 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL2177631 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL2177650 | — | IC50 | = | 2.56 | nM | 8.59 |
| CHEMBL2177629 | — | IC50 | = | 2.67 | nM | 8.57 |
| CHEMBL2177630 | — | IC50 | = | 3.44 | nM | 8.46 |
| CHEMBL2177637 | — | IC50 | = | 5.96 | nM | 8.22 |
| CHEMBL2177638 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL2178280 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2177644 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL2177639 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL2177641 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL2178281 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2177643 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL2177640 | — | IC50 | = | 1629.0 | nM | 5.79 |