Assay Detail
Binding
CHEMBL2406231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human wild-type ABL (Ser229 to Gln513)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay
16
Total Activities
16
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
Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.04 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.54 |
| CHEMBL2403874 | — | — | 1 | 8.05 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.70 |
| CHEMBL2403875 | — | — | 1 | 7.64 |
| CHEMBL2403816 | — | — | 1 | 7.40 |
| CHEMBL2403814 | — | — | 1 | 7.38 |
| CHEMBL2403820 | — | — | 1 | 7.21 |
| CHEMBL2403815 | — | — | 1 | 7.14 |
| CHEMBL2403818 | — | — | 1 | 6.95 |
| CHEMBL2403819 | — | — | 1 | 6.91 |
| CHEMBL2403813 | — | — | 1 | 6.80 |
| CHEMBL2403821 | — | — | 1 | 6.42 |
| CHEMBL510516 | — | — | 1 | 6.41 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.35 |
| CHEMBL2403817 | — | — | 1 | 5.89 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2403874 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL941 | IMATINIB | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL2403875 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2403816 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2403814 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2403820 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2403815 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2403818 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2403819 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2403813 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL2403821 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL510516 | — | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL522892 | DOVITINIB | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2403817 | — | IC50 | = | 1273.0 | nM | 5.89 |
| CHEMBL535 | SUNITINIB | IC50 | = | 1613.0 | nM | 5.79 |