Assay Detail
Binding
CHEMBL4146209
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant ALK L1196M mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.63 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4168868 | — | — | 1 | 8.46 |
| CHEMBL4172048 | — | — | 1 | 8.30 |
| CHEMBL4177038 | — | — | 1 | 7.85 |
| CHEMBL4174031 | — | — | 1 | 7.09 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4168868 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4172048 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4177038 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4174031 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 355.0 | nM | 6.45 |