Assay Detail
Binding
CHEMBL5148333
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Inhibition of wild type N-terminal GST tagged ALK cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cells incubated for 1 hr in presence of ATP
13
Total Activities
13
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
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel ALK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.95 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 8.92 |
| CHEMBL5179806 | — | — | 1 | 8.34 |
| CHEMBL5178030 | — | — | 1 | 8.19 |
| CHEMBL5209011 | — | — | 1 | 7.96 |
| CHEMBL5199005 | — | — | 1 | 7.80 |
| CHEMBL5169860 | — | — | 1 | 7.29 |
| CHEMBL5176307 | — | — | 1 | 7.12 |
| CHEMBL5175979 | — | — | 1 | - |
| CHEMBL5189267 | — | — | 1 | - |
| CHEMBL5199475 | — | — | 1 | - |
| CHEMBL5179387 | — | — | 1 | - |
| CHEMBL5178846 | — | — | 1 | - |
| CHEMBL5185272 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403108 | CERITINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5179806 | — | IC50 | = | 4.59 | nM | 8.34 |
| CHEMBL5178030 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5209011 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5199005 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5169860 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5176307 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5175979 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5189267 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5199475 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5179387 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5178846 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL5185272 | — | IC50 | > | 100.0 | nM | - |