Assay Detail
Binding
CHEMBL5153037
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Inhibition of EGFR (unknown origin) L858R/T790M 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 | 6.60 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537790 | — | — | 1 | 10.70 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.10 |
| CHEMBL5206110 | — | — | 1 | 6.99 |
| CHEMBL5194285 | — | — | 1 | 6.90 |
| CHEMBL5169346 | — | — | 1 | 6.49 |
| CHEMBL5180914 | — | — | 1 | 6.44 |
| CHEMBL5206697 | — | — | 1 | 6.21 |
| CHEMBL5190513 | — | — | 1 | 6.17 |
| CHEMBL5184313 | — | — | 1 | 6.16 |
| CHEMBL5204446 | — | — | 1 | 5.95 |
| CHEMBL5185330 | — | — | 1 | 5.77 |
| CHEMBL5186794 | — | — | 1 | 5.47 |
| CHEMBL5192038 | — | — | 1 | 5.26 |
| CHEMBL5208312 | — | — | 1 | 4.74 |
| CHEMBL5176258 | — | — | 1 | - |
| CHEMBL5205073 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL5173596 | — | — | 1 | - |
| CHEMBL5190227 | — | — | 1 | - |
| CHEMBL5199106 | — | — | 1 | - |
| CHEMBL5183329 | — | — | 1 | - |
| CHEMBL5191366 | — | — | 1 | - |
| CHEMBL5176295 | — | — | 1 | - |
| CHEMBL5182465 | — | — | 1 | - |
| CHEMBL5195531 | — | — | 1 | - |
| CHEMBL5196064 | — | — | 1 | - |
| CHEMBL5180070 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537790 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5206110 | — | IC50 | = | 102.8 | nM | 6.99 |
| CHEMBL5194285 | — | IC50 | = | 126.4 | nM | 6.90 |
| CHEMBL5169346 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL5180914 | — | IC50 | = | 361.1 | nM | 6.44 |
| CHEMBL5206697 | — | IC50 | = | 609.0 | nM | 6.21 |
| CHEMBL5190513 | — | IC50 | = | 676.7 | nM | 6.17 |
| CHEMBL5184313 | — | IC50 | = | 698.3 | nM | 6.16 |
| CHEMBL5204446 | — | IC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL5185330 | — | IC50 | = | 1681.0 | nM | 5.77 |
| CHEMBL5186794 | — | IC50 | = | 3358.0 | nM | 5.47 |
| CHEMBL5192038 | — | IC50 | = | 5450.0 | nM | 5.26 |
| CHEMBL5208312 | — | IC50 | = | 18066.7 | nM | 4.74 |
| CHEMBL5176258 | — | IC50 | - | — | - | |
| CHEMBL5205073 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | > | 100.0 | nM | - |
| CHEMBL5173596 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5190227 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5199106 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5183329 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5191366 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5176295 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5182465 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5195531 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5196064 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5180070 | — | IC50 | > | 100000.0 | nM | - |