Assay Detail
Functional
CHEMBL4770077
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability measured after 72 hrs by MTT assay
14
Total Activities
14
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 new thieno[3,2-d]pyrimidine derivatives targeting EGFR NSCLCs by the conformation constrained strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.01 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781497 | — | — | 1 | 5.38 |
| CHEMBL4800533 | — | — | 1 | 5.16 |
| CHEMBL3786343 | OLMUTINIB | 4.0 | 1 | 5.02 |
| CHEMBL4791108 | — | — | 1 | 5.00 |
| CHEMBL4785528 | — | — | 1 | 5.00 |
| CHEMBL4791953 | — | — | 1 | 4.97 |
| CHEMBL4780855 | — | — | 1 | 4.97 |
| CHEMBL4779681 | — | — | 1 | 4.96 |
| CHEMBL4782898 | — | — | 1 | 4.84 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 4.75 |
| CHEMBL4798996 | — | — | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL4794102 | — | — | 1 | - |
| CHEMBL4776694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781497 | — | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL4800533 | — | IC50 | = | 6950.0 | nM | 5.16 |
| CHEMBL3786343 | OLMUTINIB | IC50 | = | 9610.0 | nM | 5.02 |
| CHEMBL4791108 | — | IC50 | = | 10050.0 | nM | 5.00 |
| CHEMBL4785528 | — | IC50 | = | 10050.0 | nM | 5.00 |
| CHEMBL4791953 | — | IC50 | = | 10760.0 | nM | 4.97 |
| CHEMBL4780855 | — | IC50 | = | 10780.0 | nM | 4.97 |
| CHEMBL4779681 | — | IC50 | = | 10890.0 | nM | 4.96 |
| CHEMBL4782898 | — | IC50 | = | 14510.0 | nM | 4.84 |
| CHEMBL939 | GEFITINIB | IC50 | = | 17790.0 | nM | 4.75 |
| CHEMBL4798996 | — | IC50 | - | — | - | |
| CHEMBL553 | ERLOTINIB | IC50 | > | 20000.0 | nM | - |
| CHEMBL4794102 | — | IC50 | - | — | - | |
| CHEMBL4776694 | — | IC50 | - | — | - |