Assay Detail
Binding
CHEMBL5260455
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Inhibition of wild type EGFR (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 25 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 | 9.22 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 10.60 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 10.54 |
| CHEMBL5284924 | — | — | 1 | 10.28 |
| CHEMBL5289859 | — | — | 1 | 9.80 |
| CHEMBL5285052 | — | — | 1 | 9.55 |
| CHEMBL5287229 | — | — | 1 | 9.46 |
| CHEMBL5280082 | — | — | 1 | 9.40 |
| CHEMBL5288276 | — | — | 1 | 9.07 |
| CHEMBL5275642 | — | — | 1 | 9.00 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 8.80 |
| CHEMBL5278657 | — | — | 1 | 8.28 |
| CHEMBL5269375 | — | — | 1 | 7.64 |
| CHEMBL5285308 | — | — | 1 | 7.47 |
| CHEMBL5270693 | — | — | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 0.029 | nM | 10.54 |
| CHEMBL5284924 | — | IC50 | = | 0.053 | nM | 10.28 |
| CHEMBL5289859 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5285052 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5287229 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5280082 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5288276 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL5275642 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5278657 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5269375 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5285308 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5270693 | — | IC50 | = | 0.008 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.24 | nM | - |