Assay Detail
Functional
CHEMBL4708519
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.38 | 7.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.13 |
| CHEMBL4800491 | — | — | 1 | 6.68 |
| CHEMBL4787616 | — | — | 1 | 6.38 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 6.28 |
| CHEMBL4789286 | — | — | 1 | 6.16 |
| CHEMBL4762165 | — | — | 1 | 5.67 |
| CHEMBL4779676 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 73.4 | nM | 7.13 |
| CHEMBL4800491 | — | IC50 | = | 206.6 | nM | 6.68 |
| CHEMBL4787616 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 520.5 | nM | 6.28 |
| CHEMBL4789286 | — | IC50 | = | 699.2 | nM | 6.16 |
| CHEMBL4762165 | — | IC50 | = | 2139.0 | nM | 5.67 |
| CHEMBL4779676 | — | IC50 | - | — | - |