Assay Detail
Functional
CHEMBL4628608
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant 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 | NCI-H1975 |
| 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 | 5.63 | 5.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4634127 | — | — | 1 | 5.91 |
| CHEMBL4648271 | — | — | 1 | 5.83 |
| CHEMBL4636996 | — | — | 1 | 5.83 |
| CHEMBL4635100 | — | — | 1 | 5.78 |
| CHEMBL4638194 | — | — | 1 | 5.78 |
| CHEMBL4642158 | — | — | 1 | 5.75 |
| CHEMBL4634499 | — | — | 1 | 5.70 |
| CHEMBL4648924 | — | — | 1 | 5.64 |
| CHEMBL4643111 | — | — | 1 | 5.64 |
| CHEMBL2441567 | — | — | 1 | 5.59 |
| CHEMBL2441563 | — | — | 1 | 5.36 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.26 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 5.13 |
| CHEMBL4646638 | — | — | 1 | - |
| CHEMBL4641942 | — | — | 1 | - |
| CHEMBL4639556 | — | — | 1 | - |
| CHEMBL4643903 | — | — | 1 | - |
| CHEMBL4634817 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL4632500 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4634127 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4648271 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4636996 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4635100 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL4638194 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4642158 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL4634499 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4648924 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL4643111 | — | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL2441567 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2441563 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 5510.0 | nM | 5.26 |
| CHEMBL554 | LAPATINIB | IC50 | = | 7370.0 | nM | 5.13 |
| CHEMBL4646638 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641942 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639556 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643903 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634817 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632500 | — | IC50 | > | 10000.0 | nM | - |