Assay Detail
Binding
CHEMBL5260457
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 20 mins by HTRF assay
15
Total Activities
15
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 | 15 | 8.68 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5270693 | — | — | 1 | 10.70 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 10.23 |
| CHEMBL5284924 | — | — | 1 | 10.19 |
| CHEMBL5285052 | — | — | 1 | 9.82 |
| CHEMBL5289859 | — | — | 1 | 9.49 |
| CHEMBL5280082 | — | — | 1 | 9.38 |
| CHEMBL5287229 | — | — | 1 | 9.25 |
| CHEMBL5275642 | — | — | 1 | 8.80 |
| CHEMBL5288276 | — | — | 1 | 8.52 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 7.96 |
| CHEMBL5278657 | — | — | 1 | 7.77 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 7.60 |
| CHEMBL5269375 | — | — | 1 | 7.14 |
| CHEMBL5285308 | — | — | 1 | 6.90 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5270693 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL5284924 | — | IC50 | = | 0.064 | nM | 10.19 |
| CHEMBL5285052 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL5289859 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5280082 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5287229 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5275642 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5288276 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5278657 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5269375 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5285308 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 354.0 | nM | 6.45 |