Assay Detail
Binding
CHEMBL1787641
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Inhibition of human ABL T315I mutant using [EAIYAAPFAKKK] peptide substrate after 2 hrs 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 | 6.86 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784635 | — | — | 1 | 7.75 |
| CHEMBL1784634 | — | — | 1 | 7.60 |
| CHEMBL1784641 | — | — | 1 | 7.57 |
| CHEMBL1236871 | — | — | 1 | 7.44 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.40 |
| CHEMBL1784637 | — | — | 1 | 7.22 |
| CHEMBL1784628 | — | — | 1 | 6.98 |
| CHEMBL1784639 | — | — | 1 | 6.97 |
| CHEMBL1784627 | — | — | 1 | 6.92 |
| CHEMBL1784625 | — | — | 1 | 6.91 |
| CHEMBL1784640 | — | — | 1 | 6.86 |
| CHEMBL1784638 | — | — | 1 | 6.85 |
| CHEMBL1784636 | — | — | 1 | 6.52 |
| CHEMBL1784629 | — | — | 1 | 6.49 |
| CHEMBL1784633 | — | — | 1 | 6.44 |
| CHEMBL1784626 | — | — | 1 | 6.36 |
| CHEMBL1784630 | — | — | 1 | 6.34 |
| CHEMBL1784632 | — | — | 1 | 6.26 |
| CHEMBL1784631 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784635 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1784634 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1784641 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1236871 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1784637 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL1784628 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL1784639 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL1784627 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL1784625 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL1784640 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL1784638 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1784636 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL1784629 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL1784633 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL1784626 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL1784630 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL1784632 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1784631 | — | IC50 | = | 3717.0 | nM | 5.43 |