Assay Detail
Functional
CHEMBL950400
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Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HN5 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.80 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495734 | — | — | 1 | 7.43 |
| CHEMBL500381 | — | — | 1 | 7.28 |
| CHEMBL466586 | — | — | 1 | 7.24 |
| CHEMBL512076 | GSK-192082A | — | 1 | 7.02 |
| CHEMBL497184 | — | — | 1 | 7.00 |
| CHEMBL517123 | GSK-182497A | — | 1 | 7.00 |
| CHEMBL525805 | — | — | 1 | 6.95 |
| CHEMBL501705 | — | — | 1 | 6.90 |
| CHEMBL507329 | GW869810X | — | 1 | 6.80 |
| CHEMBL497804 | — | — | 1 | 6.80 |
| CHEMBL523573 | — | — | 1 | 6.72 |
| CHEMBL500640 | — | — | 1 | 6.70 |
| CHEMBL496174 | — | — | 1 | 6.62 |
| CHEMBL500115 | — | — | 1 | 6.42 |
| CHEMBL495979 | — | — | 1 | 6.27 |
| CHEMBL495733 | — | — | 1 | 6.26 |
| CHEMBL497803 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495734 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL500381 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL466586 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL512076 | GSK-192082A | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL497184 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL517123 | GSK-182497A | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL525805 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL501705 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL507329 | GW869810X | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL497804 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL523573 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL500640 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL496174 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL500115 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL495979 | — | IC50 | = | 536.0 | nM | 6.27 |
| CHEMBL495733 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL497803 | — | IC50 | = | 590.0 | nM | 6.23 |