Assay Detail
Functional
CHEMBL4197219
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCC827 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.23 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.57 |
| CHEMBL4209019 | — | — | 1 | 7.36 |
| CHEMBL4206166 | — | — | 1 | 7.19 |
| CHEMBL4204139 | — | — | 1 | 7.10 |
| CHEMBL4217992 | — | — | 1 | 6.96 |
| CHEMBL4208673 | — | — | 1 | 6.89 |
| CHEMBL4206288 | — | — | 1 | 6.70 |
| CHEMBL4203001 | — | — | 1 | 6.62 |
| CHEMBL4203016 | — | — | 1 | 6.62 |
| CHEMBL4206716 | — | — | 1 | 6.57 |
| CHEMBL4215076 | — | — | 1 | 6.51 |
| CHEMBL4215080 | — | — | 1 | 6.46 |
| CHEMBL4210148 | — | — | 1 | 6.41 |
| CHEMBL4204983 | — | — | 1 | 6.35 |
| CHEMBL4212884 | — | — | 1 | 6.19 |
| CHEMBL4205781 | — | — | 1 | 6.05 |
| CHEMBL4205095 | — | — | 1 | 6.00 |
| CHEMBL4210481 | — | — | 1 | 5.94 |
| CHEMBL4209801 | — | — | 1 | 5.87 |
| CHEMBL4204750 | — | — | 1 | 5.86 |
| CHEMBL4215582 | — | — | 1 | 5.79 |
| CHEMBL4207249 | — | — | 1 | 5.78 |
| CHEMBL4203541 | — | — | 1 | 5.74 |
| CHEMBL4213057 | — | — | 1 | 5.72 |
| CHEMBL4213899 | — | — | 1 | 5.60 |
| CHEMBL4207952 | — | — | 1 | 5.44 |
| CHEMBL4208877 | — | — | 1 | 5.26 |
| CHEMBL4218311 | — | — | 1 | 5.16 |
| CHEMBL4211799 | — | — | 1 | 5.10 |
| CHEMBL4213724 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4209019 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4206166 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4204139 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4217992 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4208673 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4206288 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4203001 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4203016 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4206716 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4215076 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4215080 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4210148 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4204983 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4212884 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4205781 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4205095 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4210481 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4209801 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4204750 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL4215582 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4207249 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4203541 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL4213057 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL4213899 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4207952 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL4208877 | — | IC50 | = | 5430.0 | nM | 5.26 |
| CHEMBL4218311 | — | IC50 | = | 6910.0 | nM | 5.16 |
| CHEMBL4211799 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4213724 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4207246 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4210648 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4206552 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4214664 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4215795 | — | IC50 | > | 10000.0 | nM | - |