Assay Detail
Functional
CHEMBL950401
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Antiproliferative activity against human BT474 cells overexpressing ErbB2 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 | BT-474 |
| 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 | 7.10 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL500381 | — | — | 1 | 7.75 |
| CHEMBL466586 | — | — | 1 | 7.55 |
| CHEMBL507329 | GW869810X | — | 1 | 7.52 |
| CHEMBL517123 | GSK-182497A | — | 1 | 7.52 |
| CHEMBL512076 | GSK-192082A | — | 1 | 7.52 |
| CHEMBL500640 | — | — | 1 | 7.47 |
| CHEMBL497804 | — | — | 1 | 7.41 |
| CHEMBL525805 | — | — | 1 | 7.40 |
| CHEMBL501705 | — | — | 1 | 7.38 |
| CHEMBL497184 | — | — | 1 | 7.35 |
| CHEMBL500115 | — | — | 1 | 7.07 |
| CHEMBL496174 | — | — | 1 | 7.03 |
| CHEMBL523573 | — | — | 1 | 6.96 |
| CHEMBL495979 | — | — | 1 | 6.69 |
| CHEMBL495733 | — | — | 1 | 6.19 |
| CHEMBL495734 | — | — | 1 | 6.17 |
| CHEMBL497803 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL500381 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL466586 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL507329 | GW869810X | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL517123 | GSK-182497A | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL512076 | GSK-192082A | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL500640 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL497804 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL525805 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL501705 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL497184 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL500115 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL496174 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL523573 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL495979 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL495733 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL495734 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL497803 | — | IC50 | = | 1700.0 | nM | 5.77 |