Assay Detail
Binding
CHEMBL5153035
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Inhibition of EGFR (unknown origin) Del19 mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay
27
Total Activities
27
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
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.94 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206110 | — | — | 1 | 9.52 |
| CHEMBL4537790 | — | — | 1 | 9.52 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.30 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.05 |
| CHEMBL5180914 | — | — | 1 | 8.89 |
| CHEMBL5206697 | — | — | 1 | 7.94 |
| CHEMBL5169346 | — | — | 1 | 7.79 |
| CHEMBL5195531 | — | — | 1 | 7.71 |
| CHEMBL5186794 | — | — | 1 | 7.60 |
| CHEMBL5194285 | — | — | 1 | 7.37 |
| CHEMBL5184313 | — | — | 1 | 7.25 |
| CHEMBL5192038 | — | — | 1 | 6.94 |
| CHEMBL5182465 | — | — | 1 | 6.92 |
| CHEMBL5185330 | — | — | 1 | 6.81 |
| CHEMBL5208312 | — | — | 1 | 6.63 |
| CHEMBL5176295 | — | — | 1 | 6.31 |
| CHEMBL5199106 | — | — | 1 | 6.31 |
| CHEMBL5205073 | — | — | 1 | 6.29 |
| CHEMBL5190513 | — | — | 1 | 5.99 |
| CHEMBL5204446 | — | — | 1 | 5.73 |
| CHEMBL5180070 | — | — | 1 | 5.52 |
| CHEMBL5190227 | — | — | 1 | 5.20 |
| CHEMBL5183329 | — | — | 1 | 4.47 |
| CHEMBL5196064 | — | — | 1 | 4.20 |
| CHEMBL5173596 | — | — | 1 | 4.15 |
| CHEMBL5176258 | — | — | 1 | - |
| CHEMBL5191366 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206110 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4537790 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL939 | GEFITINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5180914 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5206697 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5169346 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL5195531 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL5186794 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL5194285 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL5184313 | — | IC50 | = | 56.8 | nM | 7.25 |
| CHEMBL5192038 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5182465 | — | IC50 | = | 119.1 | nM | 6.92 |
| CHEMBL5185330 | — | IC50 | = | 154.6 | nM | 6.81 |
| CHEMBL5208312 | — | IC50 | = | 235.5 | nM | 6.63 |
| CHEMBL5176295 | — | IC50 | = | 490.6 | nM | 6.31 |
| CHEMBL5199106 | — | IC50 | = | 492.9 | nM | 6.31 |
| CHEMBL5205073 | — | IC50 | = | 509.3 | nM | 6.29 |
| CHEMBL5190513 | — | IC50 | = | 1026.7 | nM | 5.99 |
| CHEMBL5204446 | — | IC50 | = | 1874.3 | nM | 5.73 |
| CHEMBL5180070 | — | IC50 | = | 3034.0 | nM | 5.52 |
| CHEMBL5190227 | — | IC50 | = | 6302.0 | nM | 5.20 |
| CHEMBL5183329 | — | IC50 | = | 33860.0 | nM | 4.47 |
| CHEMBL5196064 | — | IC50 | = | 63506.7 | nM | 4.20 |
| CHEMBL5173596 | — | IC50 | = | 70396.7 | nM | 4.15 |
| CHEMBL5176258 | — | IC50 | - | — | - | |
| CHEMBL5191366 | — | IC50 | > | 100000.0 | nM | - |