Assay Detail
Binding
CHEMBL4730563
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Inhibition of EGFRvIII mutant in human U87 cells assessed as phosphorylation after 1 hr by immunoblotting analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U87 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.32 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4743220 | — | — | 1 | 8.35 |
| CHEMBL4744655 | — | — | 1 | 8.21 |
| CHEMBL4791756 | — | — | 1 | 7.97 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.90 |
| CHEMBL4783428 | — | — | 1 | 7.79 |
| CHEMBL4740063 | — | — | 1 | 7.66 |
| CHEMBL4786961 | — | — | 1 | 7.56 |
| CHEMBL4762453 | — | — | 1 | 7.51 |
| CHEMBL4750375 | — | — | 1 | 7.49 |
| CHEMBL4794223 | — | — | 1 | 7.44 |
| CHEMBL4744207 | — | — | 1 | 7.40 |
| CHEMBL1198370 | — | — | 1 | 7.37 |
| CHEMBL4759031 | — | — | 1 | 7.35 |
| CHEMBL4743464 | — | — | 1 | 7.26 |
| CHEMBL4793453 | — | — | 1 | 7.24 |
| CHEMBL4759650 | — | — | 1 | 7.12 |
| CHEMBL4778159 | — | — | 1 | 7.08 |
| CHEMBL4453068 | — | — | 1 | 6.72 |
| CHEMBL4786797 | — | — | 1 | 5.64 |
| CHEMBL4793944 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4743220 | — | IC50 | = | 4.48 | nM | 8.35 |
| CHEMBL4744655 | — | IC50 | = | 6.21 | nM | 8.21 |
| CHEMBL4791756 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4783428 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL4740063 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4786961 | — | IC50 | = | 27.6 | nM | 7.56 |
| CHEMBL4762453 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL4750375 | — | IC50 | = | 32.2 | nM | 7.49 |
| CHEMBL4794223 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL4744207 | — | IC50 | = | 40.1 | nM | 7.40 |
| CHEMBL1198370 | — | IC50 | = | 43.1 | nM | 7.37 |
| CHEMBL4759031 | — | IC50 | = | 44.8 | nM | 7.35 |
| CHEMBL4743464 | — | IC50 | = | 54.8 | nM | 7.26 |
| CHEMBL4793453 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL4759650 | — | IC50 | = | 75.4 | nM | 7.12 |
| CHEMBL4778159 | — | IC50 | = | 83.5 | nM | 7.08 |
| CHEMBL4453068 | — | IC50 | = | 188.4 | nM | 6.72 |
| CHEMBL4786797 | — | IC50 | = | 2312.0 | nM | 5.64 |
| CHEMBL4793944 | — | IC50 | = | 3846.0 | nM | 5.42 |