Assay Detail
Binding
CHEMBL4375049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA
26
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR<sup>L858R/T790M/C797S</sup>).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.13 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 8.52 |
| CHEMBL4294743 | — | — | 1 | 8.24 |
| CHEMBL4459978 | — | — | 2 | 7.56 |
| CHEMBL4474196 | — | — | 2 | 7.56 |
| CHEMBL4462965 | — | — | 2 | 7.43 |
| CHEMBL4218431 | — | — | 1 | 7.41 |
| CHEMBL4529308 | — | — | 2 | 7.25 |
| CHEMBL4446258 | — | — | 2 | 7.19 |
| CHEMBL4214567 | — | — | 1 | 7.14 |
| CHEMBL4443062 | — | — | 1 | 7.14 |
| CHEMBL4443413 | — | — | 2 | 7.09 |
| CHEMBL4450934 | — | — | 2 | 7.05 |
| CHEMBL4453276 | — | — | 2 | 6.64 |
| CHEMBL4461479 | — | — | 2 | - |
| CHEMBL4461253 | — | — | 1 | - |
| CHEMBL4468949 | — | — | 1 | - |
| CHEMBL4553136 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4294743 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4474196 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL4459978 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL4462965 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL4218431 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL4529308 | — | IC50 | = | 56.1 | nM | 7.25 |
| CHEMBL4446258 | — | IC50 | = | 65.1 | nM | 7.19 |
| CHEMBL4443062 | — | IC50 | = | 73.1 | nM | 7.14 |
| CHEMBL4214567 | — | IC50 | = | 73.1 | nM | 7.14 |
| CHEMBL4443413 | — | IC50 | = | 81.7 | nM | 7.09 |
| CHEMBL4450934 | — | IC50 | = | 88.6 | nM | 7.05 |
| CHEMBL4462965 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4450934 | — | IC50 | = | 224.1 | nM | 6.65 |
| CHEMBL4453276 | — | IC50 | = | 227.9 | nM | 6.64 |
| CHEMBL4529308 | — | IC50 | = | 498.1 | nM | 6.30 |
| CHEMBL4459978 | — | IC50 | = | 518.8 | nM | 6.29 |
| CHEMBL4453276 | — | IC50 | = | 587.6 | nM | 6.23 |
| CHEMBL4461479 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4474196 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4443413 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4446258 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4461479 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4461253 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4468949 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4553136 | — | IC50 | > | 1000.0 | nM | - |