Assay Detail
Binding
CHEMBL3762137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin)
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 | Autocuration |
Publication
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 9.05 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.52 |
| CHEMBL3758502 | — | — | 1 | 9.30 |
| CHEMBL3758602 | — | — | 1 | 8.89 |
| CHEMBL3758739 | — | — | 1 | 8.47 |
| CHEMBL3759096 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3758502 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3758602 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3758739 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3759096 | — | Ki | < | 0.5 | nM | - |