Assay Detail
Binding
CHEMBL4730145
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human EGFR T790M/L858R mutant expressed in baculovirus insect cell expression system in presence of ATP preincubated 5 mins measured for 30 mins by detection reagent based HTRF analysis
11
Total Activities
11
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
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.86 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 8.74 |
| CHEMBL4745868 | — | — | 1 | 8.59 |
| CHEMBL4776012 | — | — | 1 | 8.49 |
| CHEMBL4793105 | — | — | 1 | 8.41 |
| CHEMBL4740234 | — | — | 1 | 8.12 |
| CHEMBL4785849 | — | — | 1 | 7.89 |
| CHEMBL4746377 | — | — | 1 | 7.80 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.68 |
| CHEMBL4776073 | — | — | 1 | 7.33 |
| CHEMBL4789716 | — | — | 1 | 6.76 |
| CHEMBL4794857 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4745868 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4776012 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4793105 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4740234 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4785849 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4746377 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4776073 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4789716 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4794857 | — | IC50 | = | 213.0 | nM | 6.67 |