Assay Detail
Binding
CHEMBL3737993
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Inhibition of Abl T315I mutant (unknown origin) after 30 mins by phosphocellulose paper disk assay using 0.1 mM EAIYAAPFAKKK peptide substrate
17
Total Activities
17
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
Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.71 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3736320 | — | — | 1 | 9.10 |
| CHEMBL3735207 | — | — | 1 | 8.89 |
| CHEMBL1171086 | — | — | 1 | 8.80 |
| CHEMBL1213120 | — | — | 1 | 8.10 |
| CHEMBL3735312 | — | — | 1 | 7.77 |
| CHEMBL3736466 | — | — | 1 | 7.70 |
| CHEMBL2058540 | — | — | 1 | 6.41 |
| CHEMBL2058538 | — | — | 1 | 6.21 |
| CHEMBL3736306 | — | — | 1 | 6.04 |
| CHEMBL3735576 | — | — | 1 | 5.99 |
| CHEMBL3735795 | — | — | 1 | 5.83 |
| CHEMBL3735491 | — | — | 1 | 5.72 |
| CHEMBL3736026 | — | — | 1 | 5.70 |
| CHEMBL3734967 | — | — | 1 | 5.57 |
| CHEMBL3734907 | — | — | 1 | 5.45 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 4.13 |
| CHEMBL3735380 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3736320 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3735207 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1171086 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1213120 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3735312 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3736466 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2058540 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2058538 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3736306 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3735576 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL3735795 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL3735491 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3736026 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL3734967 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3734907 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL941 | IMATINIB | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL3735380 | — | IC50 | > | 100000.0 | nM | - |