Assay Detail
Binding
CHEMBL1935839
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Inhibition of Her-2 by time-resolved fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.08 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.05 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.05 |
| CHEMBL1934623 | — | — | 1 | 7.75 |
| CHEMBL1934632 | — | — | 1 | 7.52 |
| CHEMBL1934624 | — | — | 1 | 7.39 |
| CHEMBL1934625 | — | — | 1 | 7.39 |
| CHEMBL1934626 | — | — | 1 | 7.21 |
| CHEMBL1933083 | — | — | 1 | 7.14 |
| CHEMBL1934633 | — | — | 1 | 7.07 |
| CHEMBL1934629 | — | — | 1 | 6.96 |
| CHEMBL1934631 | — | — | 1 | 6.92 |
| CHEMBL1934630 | — | — | 1 | 6.89 |
| CHEMBL1934627 | — | — | 1 | 6.85 |
| CHEMBL1934628 | — | — | 1 | 6.75 |
| CHEMBL1934622 | — | — | 1 | 6.66 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.62 |
| CHEMBL1934621 | — | — | 1 | 6.12 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1934623 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1934632 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1934624 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1934625 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1934626 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1933083 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1934633 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1934629 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1934631 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1934630 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1934627 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1934628 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1934622 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL939 | GEFITINIB | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1934621 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 760.0 | nM | 6.12 |