Assay Detail
Binding
CHEMBL4388527
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of probe binding to EGFR L858R mutant (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assay
25
Total Activities
25
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
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.53 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.85 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.74 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.70 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 8.57 |
| CHEMBL4582933 | — | — | 1 | 8.24 |
| CHEMBL4457885 | — | — | 1 | 8.19 |
| CHEMBL4517633 | — | — | 1 | 8.05 |
| CHEMBL4457447 | — | — | 1 | 7.96 |
| CHEMBL4456266 | — | — | 1 | 7.75 |
| CHEMBL4519305 | — | — | 1 | 7.70 |
| CHEMBL4531250 | — | — | 1 | 7.57 |
| CHEMBL4547475 | — | — | 1 | 7.48 |
| CHEMBL4446124 | — | — | 1 | 7.44 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.42 |
| CHEMBL4519470 | — | — | 1 | 7.32 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.10 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.08 |
| CHEMBL4441244 | — | — | 1 | 6.70 |
| CHEMBL4576802 | — | — | 1 | 6.66 |
| CHEMBL4451538 | — | — | 1 | 6.52 |
| CHEMBL4463005 | — | — | 1 | 6.38 |
| CHEMBL4593016 | — | — | 1 | 6.38 |
| CHEMBL4546553 | — | — | 1 | 6.31 |
| CHEMBL4551202 | — | — | 1 | - |
| CHEMBL4560998 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL554 | LAPATINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL31965 | CANERTINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4582933 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4457885 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4517633 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4457447 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4456266 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4519305 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4531250 | — | IC50 | = | 26.8 | nM | 7.57 |
| CHEMBL4547475 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4446124 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4519470 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL939 | GEFITINIB | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4441244 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL4576802 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL4451538 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4463005 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4593016 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4546553 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL4551202 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4560998 | — | IC50 | > | 10000.0 | nM | - |