Assay Detail
Functional
CHEMBL4730200
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferation activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutation assessed as reduction in cell viability measured after 72 hrs by MTT assay
34
Total Activities
34
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
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 4.90 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 6.28 |
| CHEMBL4780534 | — | — | 1 | 5.66 |
| CHEMBL4754688 | — | — | 1 | 5.34 |
| CHEMBL4776833 | — | — | 1 | 5.02 |
| CHEMBL4743860 | — | — | 1 | 4.97 |
| CHEMBL4754481 | — | — | 1 | 4.97 |
| CHEMBL4753063 | — | — | 1 | 4.92 |
| CHEMBL4756906 | — | — | 1 | 4.91 |
| CHEMBL4799495 | — | — | 1 | 4.88 |
| CHEMBL4740516 | — | — | 1 | 4.87 |
| CHEMBL4746894 | — | — | 1 | 4.86 |
| CHEMBL4795151 | — | — | 1 | 4.86 |
| CHEMBL4750689 | — | — | 1 | 4.76 |
| CHEMBL4742383 | — | — | 1 | 4.76 |
| CHEMBL4781613 | — | — | 1 | 4.75 |
| CHEMBL4788876 | — | — | 1 | 4.72 |
| CHEMBL4798859 | — | — | 1 | 4.66 |
| CHEMBL4744312 | — | — | 1 | 4.60 |
| CHEMBL4757002 | — | — | 1 | 4.58 |
| CHEMBL4750398 | — | — | 1 | 4.55 |
| CHEMBL4798081 | — | — | 1 | 4.45 |
| CHEMBL4800351 | — | — | 1 | 4.44 |
| CHEMBL4787084 | — | — | 1 | - |
| CHEMBL4750261 | — | — | 1 | - |
| CHEMBL4799945 | — | — | 1 | - |
| CHEMBL4791980 | — | — | 1 | - |
| CHEMBL4790984 | — | — | 1 | - |
| CHEMBL4782114 | — | — | 1 | - |
| CHEMBL4787398 | — | — | 1 | - |
| CHEMBL4778794 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4780534 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL4754688 | — | IC50 | = | 4590.0 | nM | 5.34 |
| CHEMBL4776833 | — | IC50 | = | 9640.0 | nM | 5.02 |
| CHEMBL4743860 | — | IC50 | = | 10770.0 | nM | 4.97 |
| CHEMBL4754481 | — | IC50 | = | 10750.0 | nM | 4.97 |
| CHEMBL4753063 | — | IC50 | = | 11940.0 | nM | 4.92 |
| CHEMBL4756906 | — | IC50 | = | 12450.0 | nM | 4.91 |
| CHEMBL4799495 | — | IC50 | = | 13230.0 | nM | 4.88 |
| CHEMBL4740516 | — | IC50 | = | 13610.0 | nM | 4.87 |
| CHEMBL4746894 | — | IC50 | = | 13870.0 | nM | 4.86 |
| CHEMBL4795151 | — | IC50 | = | 13870.0 | nM | 4.86 |
| CHEMBL4750689 | — | IC50 | = | 17230.0 | nM | 4.76 |
| CHEMBL4742383 | — | IC50 | = | 17230.0 | nM | 4.76 |
| CHEMBL4781613 | — | IC50 | = | 17930.0 | nM | 4.75 |
| CHEMBL4788876 | — | IC50 | = | 18910.0 | nM | 4.72 |
| CHEMBL4798859 | — | IC50 | = | 21850.0 | nM | 4.66 |
| CHEMBL4744312 | — | IC50 | = | 25110.0 | nM | 4.60 |
| CHEMBL4757002 | — | IC50 | = | 26120.0 | nM | 4.58 |
| CHEMBL4750398 | — | IC50 | = | 28140.0 | nM | 4.55 |
| CHEMBL4798081 | — | IC50 | = | 35860.0 | nM | 4.45 |
| CHEMBL4800351 | — | IC50 | = | 36320.0 | nM | 4.44 |
| CHEMBL4787084 | — | IC50 | - | — | - | |
| CHEMBL4750261 | — | IC50 | - | — | - | |
| CHEMBL4799945 | — | IC50 | - | — | - | |
| CHEMBL4791980 | — | IC50 | - | — | - | |
| CHEMBL4790984 | — | IC50 | - | — | - | |
| CHEMBL4782114 | — | IC50 | - | — | - | |
| CHEMBL4787398 | — | IC50 | - | — | - | |
| CHEMBL4778794 | — | IC50 | - | — | - | |
| CHEMBL4750969 | — | IC50 | - | — | - | |
| CHEMBL4756475 | — | IC50 | - | — | - | |
| CHEMBL4744287 | — | IC50 | - | — | - | |
| CHEMBL4753109 | — | IC50 | - | — | - |