Assay Detail
Functional
CHEMBL1009320
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HN5 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.09 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.00 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 7.82 |
| CHEMBL504034 | — | — | 1 | 7.52 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.30 |
| CHEMBL466586 | — | — | 1 | 7.22 |
| CHEMBL512076 | GSK-192082A | — | 1 | 7.02 |
| CHEMBL461426 | — | — | 1 | 7.00 |
| CHEMBL517123 | GSK-182497A | — | 1 | 7.00 |
| CHEMBL451513 | — | — | 1 | 6.92 |
| CHEMBL507329 | GW869810X | — | 1 | 6.80 |
| CHEMBL517585 | — | — | 1 | 6.62 |
| CHEMBL505626 | — | — | 1 | 6.60 |
| CHEMBL499534 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL504034 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL31965 | CANERTINIB | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL466586 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL512076 | GSK-192082A | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL461426 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL517123 | GSK-182497A | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL451513 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL507329 | GW869810X | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL517585 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL505626 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL499534 | — | EC50 | = | 400.0 | nM | 6.40 |