Assay Detail
Binding
CHEMBL2050143
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Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.11 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29197 | — | — | 1 | 6.64 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.92 |
| CHEMBL2047253 | — | — | 1 | 4.93 |
| CHEMBL2047242 | — | — | 1 | 4.71 |
| CHEMBL2047248 | — | — | 1 | 4.62 |
| CHEMBL2047247 | — | — | 1 | 4.58 |
| CHEMBL2047245 | — | — | 1 | 4.37 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL2047252 | — | — | 1 | - |
| CHEMBL2047251 | — | — | 1 | - |
| CHEMBL2047250 | — | — | 1 | - |
| CHEMBL2047249 | — | — | 1 | - |
| CHEMBL2047241 | — | — | 1 | - |
| CHEMBL2047246 | — | — | 1 | - |
| CHEMBL2047244 | — | — | 1 | - |
| CHEMBL2047243 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29197 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2047253 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL2047242 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL2047248 | — | IC50 | = | 24100.0 | nM | 4.62 |
| CHEMBL2047247 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL2047245 | — | IC50 | = | 42600.0 | nM | 4.37 |
| CHEMBL535 | SUNITINIB | IC50 | = | 172100.0 | nM | - |
| CHEMBL2047252 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047251 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047250 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2047249 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2047241 | — | IC50 | = | 276100.0 | nM | - |
| CHEMBL2047246 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL2047244 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL2047243 | — | IC50 | > | 200000.0 | nM | - |