Assay Detail
Functional
CHEMBL4041417
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC827 |
| 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 | 30 | 6.20 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229592 | — | — | 1 | 7.70 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.35 |
| CHEMBL4099713 | — | — | 1 | 7.16 |
| CHEMBL4100655 | — | — | 1 | 7.16 |
| CHEMBL4072299 | — | — | 1 | 7.16 |
| CHEMBL4062509 | — | — | 1 | 7.10 |
| CHEMBL4094959 | — | — | 1 | 7.05 |
| CHEMBL4060919 | — | — | 1 | 6.82 |
| CHEMBL2180203 | — | — | 1 | 6.80 |
| CHEMBL4099254 | — | — | 1 | 6.51 |
| CHEMBL4073960 | — | — | 1 | 6.37 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 6.35 |
| CHEMBL4095447 | — | — | 1 | 6.30 |
| CHEMBL4091966 | — | — | 1 | 6.23 |
| CHEMBL2180204 | — | — | 1 | 6.19 |
| CHEMBL4082783 | — | — | 1 | 5.94 |
| CHEMBL4073874 | — | — | 1 | 5.92 |
| CHEMBL4071151 | — | — | 1 | 5.69 |
| CHEMBL4075015 | — | — | 1 | 5.67 |
| CHEMBL4069586 | — | — | 1 | 5.50 |
| CHEMBL4101735 | — | — | 1 | 5.19 |
| CHEMBL4094527 | — | — | 1 | 5.00 |
| CHEMBL4084214 | — | — | 1 | 4.65 |
| CHEMBL4063701 | — | — | 1 | 4.63 |
| CHEMBL4103121 | — | — | 1 | 4.59 |
| CHEMBL4090601 | — | — | 1 | - |
| CHEMBL4103201 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229592 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3545308 | ROCILETINIB | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4099713 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4100655 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4072299 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4062509 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4094959 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4060919 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2180203 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4099254 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4073960 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1873475 | IBRUTINIB | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4095447 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4091966 | — | EC50 | = | 589.0 | nM | 6.23 |
| CHEMBL2180204 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4082783 | — | EC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4073874 | — | EC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL4071151 | — | EC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4075015 | — | EC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL4069586 | — | EC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4101735 | — | EC50 | = | 6390.0 | nM | 5.19 |
| CHEMBL4094527 | — | EC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4084214 | — | EC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL4063701 | — | EC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4103121 | — | EC50 | = | 25900.0 | nM | 4.59 |
| CHEMBL4090601 | — | EC50 | < | 14.0 | nM | - |
| CHEMBL4103201 | — | EC50 | < | 14.0 | nM | - |
| CHEMBL939 | GEFITINIB | EC50 | < | 14.0 | nM | - |
| CHEMBL1173655 | AFATINIB | EC50 | < | 14.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | EC50 | < | 14.0 | nM | - |