Assay Detail
ADMET
CHEMBL4770078
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Antiproliferative activity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 1 — Organism |
| 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 | 14 | 6.27 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.15 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.10 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 7.55 |
| CHEMBL4780855 | — | — | 1 | 5.54 |
| CHEMBL4781497 | — | — | 1 | 5.46 |
| CHEMBL4785528 | — | — | 1 | 5.27 |
| CHEMBL4791953 | — | — | 1 | 5.09 |
| CHEMBL4779681 | — | — | 1 | 4.98 |
| CHEMBL4782898 | — | — | 1 | - |
| CHEMBL4800533 | — | — | 1 | - |
| CHEMBL4791108 | — | — | 1 | - |
| CHEMBL4798996 | — | — | 1 | - |
| CHEMBL4794102 | — | — | 1 | - |
| CHEMBL4776694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4780855 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL4781497 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL4785528 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL4791953 | — | IC50 | = | 8080.0 | nM | 5.09 |
| CHEMBL4779681 | — | IC50 | = | 10370.0 | nM | 4.98 |
| CHEMBL4782898 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4800533 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4791108 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4798996 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4794102 | — | IC50 | - | — | - | |
| CHEMBL4776694 | — | IC50 | - | — | - |