Assay Detail
Functional
CHEMBL5115838
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Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay
26
Total Activities
26
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 proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.47 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 6.89 |
| CHEMBL5206775 | — | — | 1 | 6.66 |
| CHEMBL5175891 | — | — | 1 | 6.62 |
| CHEMBL5185559 | — | — | 1 | 6.28 |
| CHEMBL5201794 | — | — | 1 | 6.23 |
| CHEMBL5196498 | — | — | 1 | 6.02 |
| CHEMBL5200495 | — | — | 1 | 5.96 |
| CHEMBL5201418 | — | — | 1 | 5.82 |
| CHEMBL5176547 | — | — | 1 | 5.81 |
| CHEMBL5194534 | — | — | 1 | 5.55 |
| CHEMBL5198609 | — | — | 1 | 5.38 |
| CHEMBL5204954 | — | — | 1 | 5.33 |
| CHEMBL5194838 | — | — | 1 | 5.33 |
| CHEMBL5196377 | — | — | 1 | 5.30 |
| CHEMBL5197676 | — | — | 1 | 5.24 |
| CHEMBL5176846 | — | — | 1 | 5.13 |
| CHEMBL5179538 | — | — | 1 | 5.08 |
| CHEMBL5208802 | — | — | 1 | 5.07 |
| CHEMBL5186880 | — | — | 1 | 5.05 |
| CHEMBL5175976 | — | — | 1 | 5.03 |
| CHEMBL5193965 | — | — | 1 | 4.93 |
| CHEMBL5203490 | — | — | 1 | 4.89 |
| CHEMBL5207524 | — | — | 1 | 4.77 |
| CHEMBL5182398 | — | — | 1 | 4.77 |
| CHEMBL5208186 | — | — | 1 | 4.77 |
| CHEMBL5180910 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5206775 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5175891 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5185559 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5201794 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5196498 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5200495 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL5201418 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL5176547 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5194534 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL5198609 | — | IC50 | = | 4140.0 | nM | 5.38 |
| CHEMBL5204954 | — | IC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL5194838 | — | IC50 | = | 4720.0 | nM | 5.33 |
| CHEMBL5196377 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL5197676 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL5176846 | — | IC50 | = | 7350.0 | nM | 5.13 |
| CHEMBL5179538 | — | IC50 | = | 8360.0 | nM | 5.08 |
| CHEMBL5208802 | — | IC50 | = | 8550.0 | nM | 5.07 |
| CHEMBL5186880 | — | IC50 | = | 8890.0 | nM | 5.05 |
| CHEMBL5175976 | — | IC50 | = | 9310.0 | nM | 5.03 |
| CHEMBL5193965 | — | IC50 | = | 11670.0 | nM | 4.93 |
| CHEMBL5203490 | — | IC50 | = | 12830.0 | nM | 4.89 |
| CHEMBL5207524 | — | IC50 | = | 16970.0 | nM | 4.77 |
| CHEMBL5182398 | — | IC50 | = | 17060.0 | nM | 4.77 |
| CHEMBL5208186 | — | IC50 | = | 16990.0 | nM | 4.77 |
| CHEMBL5180910 | — | IC50 | = | 61980.0 | nM | 4.21 |