Assay Detail
Binding
CHEMBL5511546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6His-tagged TEV-GS fused EGFR D770_N771insNPG mutant (G696 to G1210 reisudes) (unknown origin) expressed in Sf21 cells using Poly(Glu,Tyr) peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of ATP by ADP-Glo reagent based assay
33
Total Activities
17
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 | 33 | 7.45 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5562889 | — | — | 2 | 8.52 |
| CHEMBL5566816 | — | — | 2 | 8.22 |
| CHEMBL5568120 | — | — | 1 | 7.75 |
| CHEMBL5567060 | — | — | 2 | 7.66 |
| CHEMBL5517919 | — | — | 2 | 7.52 |
| CHEMBL5563422 | — | — | 2 | 7.11 |
| CHEMBL5561729 | — | — | 2 | 7.06 |
| CHEMBL5567954 | — | — | 2 | 7.04 |
| CHEMBL5562445 | — | — | 2 | 6.82 |
| CHEMBL5556548 | — | — | 2 | 6.77 |
| CHEMBL5561612 | — | — | 2 | - |
| CHEMBL5559367 | — | — | 2 | - |
| CHEMBL5567575 | — | — | 2 | - |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 2 | - |
| CHEMBL4650281 | CLN-081 | 3.0 | 2 | - |
| CHEMBL5558799 | — | — | 2 | - |
| CHEMBL5542205 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5562889 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5566816 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5568120 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5567060 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5517919 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5563422 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5561729 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5567954 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5562445 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5556548 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5566816 | — | IC50 | > | 831763771.1 | nM | - |
| CHEMBL5561729 | — | IC50 | > | 831763771.1 | nM | - |
| CHEMBL5567060 | — | IC50 | > | 831763771.1 | nM | - |
| CHEMBL5562445 | — | IC50 | > | 831763771.1 | nM | - |
| CHEMBL5542205 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4650281 | CLN-081 | IC50 | < | 3.0 | nM | - |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | < | 3.0 | nM | - |
| CHEMBL5559367 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5561612 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5567575 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5558799 | — | IC50 | < | 2.0 | nM | - |
| CHEMBL5562889 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL4650319 | MOBOCERTINIB | IC50 | > | 851138038.2 | nM | - |
| CHEMBL5542205 | — | IC50 | > | 851138038.2 | nM | - |
| CHEMBL5517919 | — | IC50 | > | 851138038.2 | nM | - |
| CHEMBL5563422 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL5559367 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL5561612 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL5567954 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL5556548 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL5567575 | — | IC50 | > | 524807460.25 | nM | - |
| CHEMBL4650281 | CLN-081 | IC50 | > | 851138038.2 | nM | - |
| CHEMBL5558799 | — | IC50 | > | 524807460.25 | nM | - |