Assay Detail
Binding
CHEMBL5238071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) C1156Y mutant expressed in baculovirus-infected Sf21 cells using LANCE Ultra ULight-PolyGT substrate incubated for 2 hrs by TR-FRET assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.62 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.19 |
| CHEMBL5268953 | — | — | 1 | 7.79 |
| CHEMBL5286542 | — | — | 1 | 7.78 |
| CHEMBL5268149 | — | — | 1 | 7.77 |
| CHEMBL5283671 | — | — | 1 | 7.71 |
| CHEMBL5286011 | — | — | 1 | 7.69 |
| CHEMBL5271682 | — | — | 1 | 7.67 |
| CHEMBL5266396 | — | — | 1 | 7.46 |
| CHEMBL5269028 | — | — | 1 | 7.39 |
| CHEMBL5283829 | — | — | 1 | 7.29 |
| CHEMBL5291435 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5268953 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL5286542 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL5268149 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL5283671 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL5286011 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL5271682 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL5266396 | — | IC50 | = | 34.6 | nM | 7.46 |
| CHEMBL5269028 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL5283829 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL5291435 | — | IC50 | = | 77.2 | nM | 7.11 |