Assay Detail
Functional
CHEMBL4707743
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Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth 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 | U-87MG ATCC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 4.92 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4798480 | — | — | 1 | 5.62 |
| CHEMBL4798177 | — | — | 1 | 5.55 |
| CHEMBL4787536 | — | — | 1 | 5.46 |
| CHEMBL4743685 | — | — | 1 | 5.44 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.35 |
| CHEMBL4778502 | — | — | 1 | 5.35 |
| CHEMBL4783479 | — | — | 1 | 5.19 |
| CHEMBL4786701 | — | — | 1 | 5.16 |
| CHEMBL4780040 | — | — | 1 | 5.08 |
| CHEMBL4785096 | — | — | 1 | 5.06 |
| CHEMBL4753387 | — | — | 1 | 4.82 |
| CHEMBL4764241 | — | — | 1 | 4.72 |
| CHEMBL4788364 | — | — | 1 | 4.66 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 4.65 |
| CHEMBL4558324 | LAZERTINIB | 4.0 | 1 | 4.48 |
| CHEMBL4748209 | — | — | 1 | 4.29 |
| CHEMBL4757173 | — | — | 1 | 4.28 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 4.22 |
| CHEMBL4755027 | — | — | 1 | 4.17 |
| CHEMBL4793443 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4798480 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4798177 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4787536 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4743685 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4778502 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4783479 | — | IC50 | = | 6490.0 | nM | 5.19 |
| CHEMBL4786701 | — | IC50 | = | 6970.0 | nM | 5.16 |
| CHEMBL4780040 | — | IC50 | = | 8420.0 | nM | 5.08 |
| CHEMBL4785096 | — | IC50 | = | 8660.0 | nM | 5.06 |
| CHEMBL4753387 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL4764241 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4788364 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL939 | GEFITINIB | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL4558324 | LAZERTINIB | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL4748209 | — | IC50 | = | 51600.0 | nM | 4.29 |
| CHEMBL4757173 | — | IC50 | = | 53100.0 | nM | 4.28 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 60400.0 | nM | 4.22 |
| CHEMBL4755027 | — | IC50 | = | 68100.0 | nM | 4.17 |
| CHEMBL4793443 | — | IC50 | > | 100000.0 | nM | - |