Assay Detail
Binding
CHEMBL2439213
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Inhibition of HER-2 (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometry
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.88 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2437226 | — | — | 1 | 8.41 |
| CHEMBL3436359 | — | — | 1 | 8.17 |
| CHEMBL2437227 | — | — | 1 | 8.07 |
| CHEMBL2437224 | — | — | 1 | 8.07 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 7.99 |
| CHEMBL3436356 | — | — | 1 | 7.91 |
| CHEMBL3436354 | — | — | 1 | 7.88 |
| CHEMBL3436357 | — | — | 1 | 7.84 |
| CHEMBL2437225 | — | — | 1 | 7.80 |
| CHEMBL2437223 | — | — | 1 | 7.74 |
| CHEMBL3436358 | — | — | 1 | 7.70 |
| CHEMBL3436355 | — | — | 1 | 7.62 |
| CHEMBL3436360 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2437226 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3436359 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2437227 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL2437224 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL3436356 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL3436354 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL3436357 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL2437225 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL2437223 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL3436358 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL3436355 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL3436360 | — | IC50 | = | 53.3 | nM | 7.27 |