Assay Detail
Binding
CHEMBL861551
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ErbB2
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.12 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.05 |
| CHEMBL206029 | — | — | 1 | 8.05 |
| CHEMBL381604 | GW799251X | — | 1 | 7.92 |
| CHEMBL205798 | GW703087X | — | 1 | 7.89 |
| CHEMBL204570 | — | — | 1 | 7.89 |
| CHEMBL206782 | — | — | 1 | 7.54 |
| CHEMBL207410 | GW772405X | — | 1 | 7.50 |
| CHEMBL381080 | — | — | 1 | 7.50 |
| CHEMBL205966 | GW659893X | — | 1 | 7.44 |
| CHEMBL206003 | — | — | 1 | 7.42 |
| CHEMBL205235 | — | — | 1 | 7.36 |
| CHEMBL208358 | — | — | 1 | 7.35 |
| CHEMBL204467 | — | — | 1 | 7.33 |
| CHEMBL207247 | GW807930X | — | 1 | 7.28 |
| CHEMBL205045 | — | — | 1 | 7.26 |
| CHEMBL205765 | GW794726X | — | 1 | 7.23 |
| CHEMBL207869 | — | — | 1 | 7.22 |
| CHEMBL205284 | — | — | 1 | 7.18 |
| CHEMBL380078 | — | — | 1 | 7.16 |
| CHEMBL204625 | — | — | 1 | 7.04 |
| CHEMBL438440 | — | — | 1 | 6.85 |
| CHEMBL205047 | — | — | 1 | 6.80 |
| CHEMBL379093 | GW651576X | — | 1 | 6.11 |
| CHEMBL438075 | — | — | 1 | 5.74 |
| CHEMBL205870 | — | — | 1 | 5.42 |
| CHEMBL205652 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL206029 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL381604 | GW799251X | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL205798 | GW703087X | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL204570 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL206782 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL207410 | GW772405X | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL381080 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL205966 | GW659893X | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL206003 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL205235 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL208358 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL204467 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL207247 | GW807930X | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL205045 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL205765 | GW794726X | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL207869 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL205284 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL380078 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL204625 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL438440 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL205047 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL379093 | GW651576X | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL438075 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL205870 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL205652 | — | IC50 | = | 21000.0 | nM | 4.68 |