Assay Detail
Binding
CHEMBL4770070
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Inhibition of N-terminal GST-fused human EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate incubated for 20 mins by Mobility shift assay
21
Total Activities
21
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
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR NSCLCs by the conformation constrained strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.19 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.22 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 9.05 |
| CHEMBL4779681 | — | — | 1 | 6.96 |
| CHEMBL4791953 | — | — | 1 | 6.70 |
| CHEMBL4780855 | — | — | 1 | 6.64 |
| CHEMBL4785528 | — | — | 1 | 6.62 |
| CHEMBL4781497 | — | — | 1 | 6.60 |
| CHEMBL4800533 | — | — | 1 | 6.48 |
| CHEMBL4791108 | — | — | 1 | 6.48 |
| CHEMBL4783370 | — | — | 1 | - |
| CHEMBL4793630 | — | — | 1 | - |
| CHEMBL4794102 | — | — | 1 | - |
| CHEMBL4776694 | — | — | 1 | - |
| CHEMBL4800612 | — | — | 1 | - |
| CHEMBL4782898 | — | — | 1 | - |
| CHEMBL4784264 | — | — | 1 | - |
| CHEMBL4796150 | — | — | 1 | - |
| CHEMBL4798996 | — | — | 1 | - |
| CHEMBL4778698 | — | — | 1 | - |
| CHEMBL4783097 | — | — | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4779681 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4791953 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4780855 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4785528 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4781497 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4800533 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4791108 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4783370 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4793630 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4794102 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4776694 | — | IC50 | - | — | - | |
| CHEMBL4800612 | — | IC50 | - | — | - | |
| CHEMBL4782898 | — | IC50 | - | — | - | |
| CHEMBL4784264 | — | IC50 | - | — | - | |
| CHEMBL4796150 | — | IC50 | - | — | - | |
| CHEMBL4798996 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4778698 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4783097 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | IC50 | - | — | - |