Assay Detail
Functional
CHEMBL4197220
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double 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 | NCI-H1975 |
| 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 | 5.99 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.72 |
| CHEMBL4204139 | — | — | 1 | 6.52 |
| CHEMBL4209019 | — | — | 1 | 6.40 |
| CHEMBL4206166 | — | — | 1 | 6.38 |
| CHEMBL4204750 | — | — | 1 | 6.28 |
| CHEMBL4208673 | — | — | 1 | 6.26 |
| CHEMBL4203001 | — | — | 1 | 6.23 |
| CHEMBL4205781 | — | — | 1 | 6.17 |
| CHEMBL4217992 | — | — | 1 | 6.17 |
| CHEMBL4212884 | — | — | 1 | 6.10 |
| CHEMBL4213057 | — | — | 1 | 6.09 |
| CHEMBL4204983 | — | — | 1 | 6.05 |
| CHEMBL4215080 | — | — | 1 | 6.01 |
| CHEMBL4203016 | — | — | 1 | 5.99 |
| CHEMBL4210148 | — | — | 1 | 5.94 |
| CHEMBL4206288 | — | — | 1 | 5.89 |
| CHEMBL4215076 | — | — | 1 | 5.78 |
| CHEMBL4206716 | — | — | 1 | 5.69 |
| CHEMBL4207952 | — | — | 1 | 5.66 |
| CHEMBL4209801 | — | — | 1 | 5.61 |
| CHEMBL4207249 | — | — | 1 | 5.58 |
| CHEMBL4215582 | — | — | 1 | 5.14 |
| CHEMBL4210481 | — | — | 1 | 5.13 |
| CHEMBL4203541 | — | — | 1 | 4.91 |
| CHEMBL4210648 | — | — | 1 | - |
| CHEMBL4208877 | — | — | 1 | - |
| CHEMBL4215795 | — | — | 1 | - |
| CHEMBL4205095 | — | — | 1 | - |
| CHEMBL4207246 | — | — | 1 | - |
| CHEMBL4213724 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4204139 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4209019 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4206166 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4204750 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4208673 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4203001 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4205781 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4217992 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4212884 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4213057 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4204983 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4215080 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4203016 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4210148 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4206288 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL4215076 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL4206716 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4207952 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL4209801 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL4207249 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL4215582 | — | IC50 | = | 7160.0 | nM | 5.14 |
| CHEMBL4210481 | — | IC50 | = | 7350.0 | nM | 5.13 |
| CHEMBL4203541 | — | IC50 | = | 12450.0 | nM | 4.91 |
| CHEMBL4211799 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4206552 | — | IC50 | - | — | - | |
| CHEMBL4213899 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4218311 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4214664 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4213724 | — | IC50 | - | — | - | |
| CHEMBL4207246 | — | IC50 | - | — | - | |
| CHEMBL4205095 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4215795 | — | IC50 | - | — | - | |
| CHEMBL4208877 | — | IC50 | - | — | - | |
| CHEMBL4210648 | — | IC50 | - | — | - |