Assay Detail
Binding
CHEMBL5147462
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ALK L1196M mutant (unknown origin) using biotinylated substrate incubated for 1 hr in the presence of ATP at Km concentration by HTRF assay
14
Total Activities
14
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 and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.22 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171152 | — | — | 1 | 8.82 |
| CHEMBL5095068 | IRUPLINALKIB | 2.0 | 1 | 8.77 |
| CHEMBL5172847 | — | — | 1 | 8.46 |
| CHEMBL5178402 | — | — | 1 | 8.42 |
| CHEMBL5195006 | — | — | 1 | 8.41 |
| CHEMBL5200942 | — | — | 1 | 8.41 |
| CHEMBL5179104 | — | — | 1 | 8.38 |
| CHEMBL5176751 | — | — | 1 | 8.34 |
| CHEMBL5185835 | — | — | 1 | 8.28 |
| CHEMBL5170703 | — | — | 1 | 8.21 |
| CHEMBL5172119 | — | — | 1 | 8.03 |
| CHEMBL5184310 | — | — | 1 | 7.91 |
| CHEMBL5173297 | — | — | 1 | 7.35 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171152 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5095068 | IRUPLINALKIB | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5172847 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5178402 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5195006 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5200942 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5179104 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5176751 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5185835 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5170703 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5172119 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5184310 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL5173297 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 52.0 | nM | 7.28 |