Assay Detail
Binding
CHEMBL4398796
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant expressed in baculovirus expression system using poly (Glu,Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR<sup>L858R/T790M/C797S</sup>.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 13 | - | - |
| IC50 | 7 | 7.59 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4443483 | — | — | 1 | 8.66 |
| CHEMBL4465497 | — | — | 1 | 8.10 |
| CHEMBL4516635 | — | — | 1 | 8.03 |
| CHEMBL4593609 | — | — | 1 | 7.72 |
| CHEMBL4471235 | — | — | 1 | 7.43 |
| CHEMBL4538066 | — | — | 1 | 6.75 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.43 |
| CHEMBL4578962 | — | — | 1 | - |
| CHEMBL4585477 | — | — | 1 | - |
| CHEMBL4565609 | — | — | 1 | - |
| CHEMBL4533998 | — | — | 1 | - |
| CHEMBL4475098 | — | — | 1 | - |
| CHEMBL4518608 | — | — | 1 | - |
| CHEMBL4451766 | — | — | 1 | - |
| CHEMBL4456618 | — | — | 1 | - |
| CHEMBL4456115 | — | — | 1 | - |
| CHEMBL4447201 | — | — | 1 | - |
| CHEMBL4563177 | — | — | 1 | - |
| CHEMBL4467422 | — | — | 1 | - |
| CHEMBL4540305 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4443483 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4465497 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4516635 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4593609 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL4471235 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL4538066 | — | IC50 | = | 179.6 | nM | 6.75 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 369.2 | nM | 6.43 |
| CHEMBL4578962 | — | Inhibition | - | % | - | |
| CHEMBL4585477 | — | Inhibition | - | % | - | |
| CHEMBL4565609 | — | Inhibition | - | % | - | |
| CHEMBL4533998 | — | Inhibition | - | % | - | |
| CHEMBL4475098 | — | Inhibition | - | % | - | |
| CHEMBL4518608 | — | Inhibition | - | % | - | |
| CHEMBL4451766 | — | Inhibition | - | % | - | |
| CHEMBL4456618 | — | Inhibition | - | % | - | |
| CHEMBL4456115 | — | Inhibition | - | % | - | |
| CHEMBL4447201 | — | Inhibition | - | % | - | |
| CHEMBL4563177 | — | Inhibition | - | % | - | |
| CHEMBL4467422 | — | Inhibition | - | % | - | |
| CHEMBL4540305 | — | Inhibition | - | % | - |