Assay Detail
Binding
CHEMBL5511547
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant wildtype human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in Sf21 insect cells using Poly(Glu,Tyr) peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 50 mins in presence of ATP by ADP-Glo reagent based assay
32
Total Activities
16
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 and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.84 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5567575 | — | — | 2 | 9.00 |
| CHEMBL5561612 | — | — | 2 | 9.00 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 2 | 9.00 |
| CHEMBL5558799 | — | — | 2 | 8.70 |
| CHEMBL5559367 | — | — | 2 | 8.70 |
| CHEMBL5542205 | — | — | 2 | 8.22 |
| CHEMBL5567954 | — | — | 2 | 8.00 |
| CHEMBL5556548 | — | — | 2 | 7.68 |
| CHEMBL5562889 | — | — | 2 | 7.46 |
| CHEMBL5563422 | — | — | 2 | 7.44 |
| CHEMBL5567060 | — | — | 2 | 7.23 |
| CHEMBL5561729 | — | — | 2 | 7.02 |
| CHEMBL5566816 | — | — | 2 | 6.43 |
| CHEMBL5517919 | — | — | 2 | 5.82 |
| CHEMBL5562445 | — | — | 2 | - |
| CHEMBL4650281 | CLN-081 | 3.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5567575 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5561612 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5558799 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5559367 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5542205 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5567954 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5556548 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5562889 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5563422 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5567060 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5561729 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5566816 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5517919 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4650281 | CLN-081 | IC50 | < | 3.0 | nM | - |
| CHEMBL5562445 | — | IC50 | > | 794328234.72 | nM | - |
| CHEMBL5567060 | — | IC50 | > | 794328234.72 | nM | - |
| CHEMBL5561729 | — | IC50 | > | 794328234.72 | nM | - |
| CHEMBL5566816 | — | IC50 | > | 794328234.72 | nM | - |
| CHEMBL5562889 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5558799 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5567575 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5556548 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5567954 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5561612 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5559367 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5563422 | — | IC50 | > | 676082975.39 | nM | - |
| CHEMBL5517919 | — | IC50 | > | 933254300.8 | nM | - |
| CHEMBL5542205 | — | IC50 | > | 933254300.8 | nM | - |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | > | 933254300.8 | nM | - |
| CHEMBL4650281 | CLN-081 | IC50 | > | 933254300.8 | nM | - |
| CHEMBL5562445 | — | IC50 | > | 7400.0 | nM | - |