Assay Detail
Binding
CHEMBL4730144
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type EGFR (unknown origin) 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 | 7.18 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.92 |
| CHEMBL4745868 | — | — | 1 | 7.29 |
| CHEMBL4776012 | — | — | 1 | 7.28 |
| CHEMBL4793105 | — | — | 1 | 7.16 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.12 |
| CHEMBL4740234 | — | — | 1 | 6.89 |
| CHEMBL4785849 | — | — | 1 | 6.89 |
| CHEMBL4746377 | — | — | 1 | 6.59 |
| CHEMBL4776073 | — | — | 1 | 6.52 |
| CHEMBL4794857 | — | — | 1 | - |
| CHEMBL4789716 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4745868 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4776012 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4793105 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4740234 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4785849 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4746377 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL4776073 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4794857 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4789716 | — | IC50 | > | 1000.0 | nM | - |