Assay Detail
Binding
CHEMBL5260458
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 10 mins by HTRF assay
12
Total Activities
12
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
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.68 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5270693 | — | — | 1 | 9.19 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 8.89 |
| CHEMBL5285052 | — | — | 1 | 8.21 |
| CHEMBL5284924 | — | — | 1 | 8.06 |
| CHEMBL5287229 | — | — | 1 | 7.92 |
| CHEMBL5289859 | — | — | 1 | 7.82 |
| CHEMBL5280082 | — | — | 1 | 7.72 |
| CHEMBL5275642 | — | — | 1 | 7.46 |
| CHEMBL5288276 | — | — | 1 | 7.11 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.82 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.50 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5270693 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5285052 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5284924 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5287229 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5289859 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5280082 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5275642 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5288276 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 364.0 | nM | 6.44 |