Assay Detail
Functional
CHEMBL862521
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.76 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204638 | — | — | 1 | 9.30 |
| CHEMBL203599 | — | — | 1 | 9.00 |
| CHEMBL205059 | — | — | 1 | 8.70 |
| CHEMBL437890 | — | — | 1 | 8.46 |
| CHEMBL203661 | — | — | 1 | 8.30 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 8.13 |
| CHEMBL373207 | — | — | 1 | 8.12 |
| CHEMBL204085 | — | — | 1 | 8.12 |
| CHEMBL202424 | — | — | 1 | 7.70 |
| CHEMBL202556 | — | — | 1 | 7.66 |
| CHEMBL382073 | — | — | 1 | 7.64 |
| CHEMBL203644 | — | — | 1 | 7.62 |
| CHEMBL202398 | — | — | 1 | 7.50 |
| CHEMBL383499 | — | — | 1 | 7.44 |
| CHEMBL202411 | — | — | 1 | 7.37 |
| CHEMBL380669 | — | — | 1 | 7.19 |
| CHEMBL202425 | — | — | 1 | 6.94 |
| CHEMBL203645 | — | — | 1 | 6.77 |
| CHEMBL202621 | — | — | 1 | 6.76 |
| CHEMBL202421 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204638 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL203599 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL205059 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL437890 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL203661 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL373207 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL204085 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL202424 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL202556 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL382073 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL203644 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL202398 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL383499 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL202411 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL380669 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL202425 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL203645 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL202621 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL202421 | — | IC50 | = | 320.0 | nM | 6.50 |