Assay Detail
Functional
CHEMBL4628611
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Calu-3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.61 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441563 | — | — | 1 | 7.43 |
| CHEMBL4643111 | — | — | 1 | 6.85 |
| CHEMBL4635100 | — | — | 1 | 6.75 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 6.67 |
| CHEMBL4648271 | — | — | 1 | 6.56 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.03 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.01 |
| CHEMBL4648924 | — | — | 1 | - |
| CHEMBL4642158 | — | — | 1 | - |
| CHEMBL4634817 | — | — | 1 | - |
| CHEMBL4643903 | — | — | 1 | - |
| CHEMBL4638194 | — | — | 1 | - |
| CHEMBL4636996 | — | — | 1 | - |
| CHEMBL4646638 | — | — | 1 | - |
| CHEMBL4641942 | — | — | 1 | - |
| CHEMBL4639556 | — | — | 1 | - |
| CHEMBL4632500 | — | — | 1 | - |
| CHEMBL2441567 | — | — | 1 | - |
| CHEMBL4634127 | — | — | 1 | - |
| CHEMBL4634499 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441563 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4643111 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4635100 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL554 | LAPATINIB | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4648271 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 926.0 | nM | 6.03 |
| CHEMBL939 | GEFITINIB | IC50 | = | 985.0 | nM | 6.01 |
| CHEMBL4648924 | — | IC50 | - | — | - | |
| CHEMBL4642158 | — | IC50 | - | — | - | |
| CHEMBL4634817 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638194 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636996 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646638 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641942 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639556 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632500 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2441567 | — | IC50 | - | — | - | |
| CHEMBL4634127 | — | IC50 | - | — | - | |
| CHEMBL4634499 | — | IC50 | - | — | - |