Assay Detail
Binding
CHEMBL5162303
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Inhibition of wild type human N-terminal GST tagged EGFR (669 to 1210 residues) expressed in Sf21 insect cells incubated for 30 mins in presence of ATP by HTRF analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.18 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 9.24 |
| CHEMBL3647420 | PYROTINIB | 3.0 | 1 | 9.01 |
| CHEMBL5190132 | — | — | 1 | 8.99 |
| CHEMBL5176920 | — | — | 1 | 8.96 |
| CHEMBL5179954 | — | — | 1 | 8.92 |
| CHEMBL5184610 | — | — | 1 | 8.87 |
| CHEMBL5175489 | — | — | 1 | 8.83 |
| CHEMBL5175873 | — | — | 1 | 8.67 |
| CHEMBL5192750 | — | — | 1 | 8.64 |
| CHEMBL5201973 | — | — | 1 | 8.63 |
| CHEMBL5193451 | — | — | 1 | 8.55 |
| CHEMBL5209046 | — | — | 1 | 8.50 |
| CHEMBL5178703 | — | — | 1 | 8.09 |
| CHEMBL5183924 | — | — | 1 | 8.02 |
| CHEMBL5202846 | — | — | 1 | 7.93 |
| CHEMBL5180725 | — | — | 1 | 7.68 |
| CHEMBL5180965 | — | — | 1 | 7.64 |
| CHEMBL5181694 | — | — | 1 | 7.59 |
| CHEMBL5176854 | — | — | 1 | 7.49 |
| CHEMBL5170965 | — | — | 1 | 7.06 |
| CHEMBL5203179 | — | — | 1 | 6.96 |
| CHEMBL5200783 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL3647420 | PYROTINIB | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5190132 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL5176920 | — | IC50 | = | 1.11 | nM | 8.96 |
| CHEMBL5179954 | — | IC50 | = | 1.19 | nM | 8.92 |
| CHEMBL5184610 | — | IC50 | = | 1.36 | nM | 8.87 |
| CHEMBL5175489 | — | IC50 | = | 1.47 | nM | 8.83 |
| CHEMBL5175873 | — | IC50 | = | 2.13 | nM | 8.67 |
| CHEMBL5192750 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL5201973 | — | IC50 | = | 2.32 | nM | 8.63 |
| CHEMBL5193451 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5209046 | — | IC50 | = | 3.13 | nM | 8.50 |
| CHEMBL5178703 | — | IC50 | = | 8.13 | nM | 8.09 |
| CHEMBL5183924 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5202846 | — | IC50 | = | 11.82 | nM | 7.93 |
| CHEMBL5180725 | — | IC50 | = | 20.72 | nM | 7.68 |
| CHEMBL5180965 | — | IC50 | = | 22.75 | nM | 7.64 |
| CHEMBL5181694 | — | IC50 | = | 25.92 | nM | 7.59 |
| CHEMBL5176854 | — | IC50 | = | 32.14 | nM | 7.49 |
| CHEMBL5170965 | — | IC50 | = | 86.33 | nM | 7.06 |
| CHEMBL5203179 | — | IC50 | = | 110.32 | nM | 6.96 |
| CHEMBL5200783 | — | IC50 | = | 1833.8 | nM | 5.74 |