Assay Detail
Functional
CHEMBL5259681
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
17
Total Activities
17
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
Synthesis and evaluation of sulfonamide derivatives targeting EGFR<sup>790M/L858R</sup> mutations and ALK rearrangement as anticancer agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.54 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 10.72 |
| CHEMBL4449391 | — | — | 1 | 7.90 |
| CHEMBL5268803 | — | — | 1 | 7.87 |
| CHEMBL5284780 | — | — | 1 | 7.67 |
| CHEMBL5266571 | — | — | 1 | 7.21 |
| CHEMBL4565984 | — | — | 1 | 7.17 |
| CHEMBL5268146 | — | — | 1 | 7.09 |
| CHEMBL5270671 | — | — | 1 | 7.00 |
| CHEMBL5273295 | — | — | 1 | 6.77 |
| CHEMBL5290329 | — | — | 1 | 5.99 |
| CHEMBL5282957 | — | — | 1 | - |
| CHEMBL5279311 | — | — | 1 | - |
| CHEMBL5281327 | — | — | 1 | - |
| CHEMBL5281621 | — | — | 1 | - |
| CHEMBL5281520 | — | — | 1 | - |
| CHEMBL5289549 | — | — | 1 | - |
| CHEMBL5284889 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.019 | nM | 10.72 |
| CHEMBL4449391 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL5268803 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL5284780 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL5266571 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4565984 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5268146 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5270671 | — | IC50 | = | 100.5 | nM | 7.00 |
| CHEMBL5273295 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5290329 | — | IC50 | = | 1025.5 | nM | 5.99 |
| CHEMBL5282957 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5279311 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5281327 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5281621 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5281520 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5289549 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5284889 | — | IC50 | > | 10000.0 | nM | - |