Assay Detail
Binding
CHEMBL4382297
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Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay
15
Total Activities
15
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 a potent dual ALK and EGFR T790M inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.23 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4565984 | — | — | 1 | 7.82 |
| CHEMBL4449391 | — | — | 1 | 7.77 |
| CHEMBL4448107 | — | — | 1 | 7.77 |
| CHEMBL4473365 | — | — | 1 | 7.75 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.70 |
| CHEMBL4540442 | — | — | 1 | 7.51 |
| CHEMBL4467561 | — | — | 1 | 7.42 |
| CHEMBL4520341 | — | — | 1 | 7.40 |
| CHEMBL4581316 | — | — | 1 | 7.39 |
| CHEMBL4531697 | — | — | 1 | 7.04 |
| CHEMBL4516287 | — | — | 1 | 6.99 |
| CHEMBL4558227 | — | — | 1 | 6.91 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.75 |
| CHEMBL4465103 | — | — | 1 | 6.16 |
| CHEMBL1229592 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4565984 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4449391 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4448107 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4473365 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4540442 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4467561 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4520341 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4581316 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4531697 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4516287 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL4558227 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4465103 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL1229592 | — | IC50 | = | 990.0 | nM | 6.00 |