Assay Detail
Functional
CHEMBL5707348
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
6
Total Activities
6
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
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.16 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1643989 | — | — | 1 | 8.05 |
| CHEMBL1643976 | — | — | 1 | 7.54 |
| CHEMBL1229592 | — | — | 1 | 7.33 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.82 |
| CHEMBL91867 | — | — | 1 | 6.07 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1643989 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1643976 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1229592 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL180022 | NERATINIB | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL91867 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL939 | GEFITINIB | IC50 | > | 33000.0 | nM | - |