Assay Detail
ADMET
CHEMBL4041419
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Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
15
Total Activities
15
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
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 4.92 | 5.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.83 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.74 |
| CHEMBL4103201 | — | — | 1 | 5.46 |
| CHEMBL1229592 | — | — | 1 | 5.40 |
| CHEMBL4090601 | — | — | 1 | 4.94 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 4.73 |
| CHEMBL4072299 | — | — | 1 | 4.70 |
| CHEMBL4069586 | — | — | 1 | 4.70 |
| CHEMBL4099713 | — | — | 1 | 4.66 |
| CHEMBL2180204 | — | — | 1 | 4.65 |
| CHEMBL4091966 | — | — | 1 | 4.63 |
| CHEMBL4094959 | — | — | 1 | 4.63 |
| CHEMBL4082783 | — | — | 1 | 4.57 |
| CHEMBL4062509 | — | — | 1 | 4.56 |
| CHEMBL4071151 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | EC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL3353410 | OSIMERTINIB | EC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL4103201 | — | EC50 | = | 3450.0 | nM | 5.46 |
| CHEMBL1229592 | — | EC50 | = | 3990.0 | nM | 5.40 |
| CHEMBL4090601 | — | EC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL939 | GEFITINIB | EC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL4072299 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4069586 | — | EC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL4099713 | — | EC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL2180204 | — | EC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL4091966 | — | EC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL4094959 | — | EC50 | = | 23300.0 | nM | 4.63 |
| CHEMBL4082783 | — | EC50 | = | 27100.0 | nM | 4.57 |
| CHEMBL4062509 | — | EC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL4071151 | — | EC50 | = | 28300.0 | nM | 4.55 |