Assay Detail
Binding
CHEMBL676070
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Inhibition of human epidermal growth factor receptor (HER-2) using enzyme assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.22 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329856 | — | — | 1 | 7.85 |
| CHEMBL94062 | — | — | 1 | 7.80 |
| CHEMBL91009 | — | — | 1 | 7.48 |
| CHEMBL328704 | — | — | 1 | 7.42 |
| CHEMBL93386 | — | — | 1 | 7.28 |
| CHEMBL90595 | — | — | 1 | 7.14 |
| CHEMBL414220 | — | — | 1 | 7.07 |
| CHEMBL91811 | — | — | 1 | 6.95 |
| CHEMBL327838 | — | — | 1 | 6.94 |
| CHEMBL285063 | — | — | 1 | 6.94 |
| CHEMBL93784 | — | — | 1 | 6.93 |
| CHEMBL328977 | — | — | 1 | 6.91 |
| CHEMBL93049 | — | — | 1 | 6.91 |
| CHEMBL92961 | — | — | 1 | 6.79 |
| CHEMBL328245 | — | — | 1 | 6.75 |
| CHEMBL92356 | — | — | 1 | 6.74 |
| CHEMBL94061 | — | — | 1 | 6.52 |
| CHEMBL91867 | — | — | 1 | 6.42 |
| CHEMBL93783 | — | — | 1 | 6.38 |
| CHEMBL94066 | — | — | 1 | 6.34 |
| CHEMBL442754 | — | — | 1 | 6.20 |
| CHEMBL419501 | — | — | 1 | 6.13 |
| CHEMBL91925 | — | — | 1 | 5.93 |
| CHEMBL92731 | — | — | 1 | 5.84 |
| CHEMBL94068 | — | — | 1 | 5.81 |
| CHEMBL94109 | — | — | 1 | 5.80 |
| CHEMBL2112370 | — | — | 1 | 5.72 |
| CHEMBL316127 | — | — | 1 | 5.56 |
| CHEMBL93537 | — | — | 1 | 5.55 |
| CHEMBL2112369 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329856 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL94062 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL91009 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL328704 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL93386 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL90595 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL414220 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL91811 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL327838 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL285063 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL93784 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL328977 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL93049 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL92961 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL328245 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL92356 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL94061 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL91867 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL93783 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL94066 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL442754 | — | IC50 | = | 634.0 | nM | 6.20 |
| CHEMBL419501 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL91925 | — | IC50 | = | 1164.0 | nM | 5.93 |
| CHEMBL92731 | — | IC50 | = | 1428.0 | nM | 5.84 |
| CHEMBL94068 | — | IC50 | = | 1559.0 | nM | 5.81 |
| CHEMBL94109 | — | IC50 | = | 1592.0 | nM | 5.80 |
| CHEMBL2112370 | — | IC50 | = | 1912.0 | nM | 5.72 |
| CHEMBL316127 | — | IC50 | = | 2776.0 | nM | 5.56 |
| CHEMBL93537 | — | IC50 | = | 2808.0 | nM | 5.55 |
| CHEMBL2112369 | — | IC50 | = | 2921.0 | nM | 5.53 |
| CHEMBL94123 | — | IC50 | = | 4182.0 | nM | 5.38 |
| CHEMBL92902 | — | IC50 | = | 5042.0 | nM | 5.30 |
| CHEMBL92882 | — | IC50 | = | 8832.0 | nM | 5.05 |
| CHEMBL92086 | — | IC50 | = | 15238.0 | nM | 4.82 |
| CHEMBL93754 | — | IC50 | = | 15624.0 | nM | 4.81 |
| CHEMBL329642 | — | IC50 | = | 21657.0 | nM | 4.66 |
| CHEMBL91748 | — | IC50 | = | 25710.0 | nM | 4.59 |
| CHEMBL93464 | — | IC50 | = | 91325.0 | nM | 4.04 |