Assay Detail
Binding
CHEMBL680028
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Inhibition of autophosphorylation of cytoplasmic domain of epidermal growth factor receptor
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 |
Publication
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.10 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL285063 | — | — | 1 | 8.70 |
| CHEMBL94061 | — | — | 1 | 7.96 |
| CHEMBL29197 | — | — | 1 | 7.16 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 7.10 |
| CHEMBL116853 | — | — | 1 | 7.05 |
| CHEMBL115187 | — | — | 1 | 6.89 |
| CHEMBL157128 | — | — | 1 | 6.82 |
| CHEMBL111038 | — | — | 1 | 6.72 |
| CHEMBL113900 | — | — | 1 | 6.60 |
| CHEMBL30973 | — | — | 1 | 6.51 |
| CHEMBL414631 | — | — | 1 | 6.48 |
| CHEMBL327023 | — | — | 1 | 6.26 |
| CHEMBL117326 | — | — | 1 | 6.25 |
| CHEMBL281300 | — | — | 1 | 6.23 |
| CHEMBL323630 | — | — | 1 | 6.19 |
| CHEMBL263788 | — | — | 1 | 6.10 |
| CHEMBL326280 | — | — | 1 | 6.10 |
| CHEMBL324718 | — | — | 1 | 6.09 |
| CHEMBL116525 | — | — | 1 | 6.04 |
| CHEMBL115440 | — | — | 1 | 6.03 |
| CHEMBL283682 | — | — | 1 | 6.03 |
| CHEMBL114593 | — | — | 1 | 6.02 |
| CHEMBL114728 | — | — | 1 | 5.80 |
| CHEMBL326811 | — | — | 1 | 5.79 |
| CHEMBL424252 | — | — | 1 | 5.72 |
| CHEMBL118000 | — | — | 1 | 5.64 |
| CHEMBL114490 | — | — | 1 | 5.63 |
| CHEMBL421047 | — | — | 1 | 5.58 |
| CHEMBL114392 | — | — | 1 | 5.57 |
| CHEMBL116857 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL285063 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL94061 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL29197 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL607707 | PELITINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL116853 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL115187 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL157128 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL111038 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL113900 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL30973 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL414631 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL327023 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL117326 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL281300 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL323630 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL263788 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL326280 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL324718 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL116525 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL115440 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL283682 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL114593 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL114728 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL326811 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL424252 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL118000 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL114490 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL421047 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL114392 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL116857 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL332497 | — | IC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL325156 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL113901 | — | IC50 | = | 5220.0 | nM | 5.28 |
| CHEMBL113985 | — | IC50 | = | 5390.0 | nM | 5.27 |
| CHEMBL113902 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL116012 | — | IC50 | = | 10320.0 | nM | 4.99 |
| CHEMBL114073 | — | IC50 | = | 10590.0 | nM | 4.97 |
| CHEMBL113996 | — | IC50 | = | 13570.0 | nM | 4.87 |