Assay Detail
Binding
CHEMBL1787640
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Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate after 1 hr by TR-FRET assay
19
Total Activities
19
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
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.60 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784634 | — | — | 1 | 8.44 |
| CHEMBL1236871 | — | — | 1 | 8.44 |
| CHEMBL1784639 | — | — | 1 | 8.37 |
| CHEMBL1784638 | — | — | 1 | 8.32 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.07 |
| CHEMBL1784641 | — | — | 1 | 7.92 |
| CHEMBL1784637 | — | — | 1 | 7.76 |
| CHEMBL1784635 | — | — | 1 | 7.76 |
| CHEMBL1784627 | — | — | 1 | 7.75 |
| CHEMBL1784640 | — | — | 1 | 7.54 |
| CHEMBL1784628 | — | — | 1 | 7.54 |
| CHEMBL1784625 | — | — | 1 | 7.39 |
| CHEMBL1784629 | — | — | 1 | 7.31 |
| CHEMBL1784630 | — | — | 1 | 7.30 |
| CHEMBL1784636 | — | — | 1 | 7.26 |
| CHEMBL1784626 | — | — | 1 | 7.20 |
| CHEMBL1784633 | — | — | 1 | 7.14 |
| CHEMBL1784632 | — | — | 1 | 6.89 |
| CHEMBL1784631 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784634 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1236871 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1784639 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1784638 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL1784641 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1784637 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL1784635 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL1784627 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1784640 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1784628 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL1784625 | — | IC50 | = | 40.3 | nM | 7.39 |
| CHEMBL1784629 | — | IC50 | = | 48.7 | nM | 7.31 |
| CHEMBL1784630 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL1784636 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1784626 | — | IC50 | = | 62.7 | nM | 7.20 |
| CHEMBL1784633 | — | IC50 | = | 72.6 | nM | 7.14 |
| CHEMBL1784632 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1784631 | — | IC50 | = | 1000.0 | nM | 6.00 |